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  Subjects -> PHARMACY AND PHARMACOLOGY (Total: 570 journals)
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Journal Cover Saudi Pharmaceutical Journal
  [SJR: 0.552]   [H-I: 20]   [0 followers]  Follow
    
  This is an Open Access Journal Open Access journal
   ISSN (Print) 1319-0164
   Published by Elsevier Homepage  [3039 journals]
  • Drug release behavior of polymeric matrix filled in capsule

    • Authors: Thawatchai Phaechamud; Wanwilai Darunkaisorn
      Pages: 627 - 634
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Thawatchai Phaechamud, Wanwilai Darunkaisorn
      A single unit sustainable drug release system was developed using hydroxypropyl methylcellulose (HPMC)-based matrices filled in capsule as the drug delivery device. Release behavior of propranolol HCl from these capsules was investigated and least square fitting was performed for the dissolution data with the different mathematical expressions. Effect of diluent, polymer, pH and hydrodynamic force on the drug release from the developed systems was investigated. The utilization of HPMC as a matrix former extended the drug release longer than 8h. HPMC viscosity grades affected the drug release, that is, increasing the amount of fillers such as lactose and dibasic calcium phosphate enhanced the drug release rate of HPMC matrices. The hydrodynamic force, type and amount of incorporated polymer apparently influenced the drug release. The physiochemical properties of polymers and interaction between HPMC and other polymers were important factors for prolongation of the drug release. The release mechanism from HPMC-based matrices in capsules was the non-Fickian transport in which the sustainable drug release of HPMC capsules could be achieved by the addition of polymeric matrix.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.04.003
       
  • Effect of amlodipine, lisinopril and allopurinol on acetaminophen-induced
           hepatotoxicity in rats

    • Authors: Nesreen E.M. Mohammed; Basim A.S. Messiha; Ali A. Abo-Saif
      Pages: 635 - 644
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Nesreen E.M. Mohammed, Basim A.S. Messiha, Ali A. Abo-Saif
      Background Exposure to chemotherapeutic agents such as acetaminophen may lead to serious liver injury. Calcium deregulation, angiotensin II production and xanthine oxidase activity are suggested to play mechanistic roles in such injury. Objective This study evaluates the possible protective effects of the calcium channel blocker amlodipine, the angiotensin converting enzyme inhibitor lisinopril, and the xanthine oxidase inhibitor allopurinol against experimental acetaminophen-induced hepatotoxicity, aiming to understand its underlying hepatotoxic mechanisms. Material and methods Animals were allocated into a normal control group, a acetaminophen hepatotoxicity control group (receiving a single oral dose of acetaminophen; 750mg/kg/day), and four treatment groups receive N-acetylcysteine (300mg/kg/day; a reference standard), amlodipine (10mg/kg/day), lisinopril (20mg/kg/day) and allopurinol (50mg/kg/day) orally for 14 consecutive days prior to acetaminophen administration. Evaluation of hepatotoxicity was performed by the assessment of hepatocyte integrity markers (serum transaminases), oxidative stress markers (hepatic malondialdehyde, glutathione and catalase), and inflammatory markers (hepatic myeloperoxidase and nitrate/nitrite), in addition to a histopathological study. Results Rats pre-treated with amlodipine, lisinopril or allopurinol showed significantly lower serum transaminases, significantly lower hepatic malondialdehyde, myeloperoxidase and nitrate/nitrite, as well as significantly higher hepatic glutathione and catalase levels, compared with acetaminophen control rats. Serum transaminases were normalized in the lisinopril treatment group, while hepatic myeloperoxidase was normalized in the all treatment groups. Histopathological evaluation strongly supported the results of biochemical estimations. Conclusion Amlodipine, lisinopril or allopurinol can protect against acetaminophen-induced hepatotoxicity, showing mechanistic roles of calcium channels, angiotensin converting enzyme and xanthine oxidase enzyme in the pathogenesis of hepatotoxicity induced by acetaminophen.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.04.004
       
  • Prevalence and genotyping of Toxoplasma gondii among Saudi pregnant women
           in Saudi Arabia

    • Authors: Jawahir Alghamdi; Maha Hussein Elamin; Samia Alhabib
      Pages: 645 - 651
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Jawahir Alghamdi, Maha Hussein Elamin, Samia Alhabib
      Introduction: Toxoplasma gondii (T. gondii) is an intracellular protozoan that can infect all mammals, who serve as intermediate host. It causes congenital, neurological, eyes complications and mild or asymptomatic infections in humans. Purpose of this study: To investigate not only the prevalence of T. gondii, but also to find out its genotyping using multiple sequential molecular methods to predict exactly the precise genotyping of T. gondii among Saudi pregnant women. Methods: A cross-sectional study was conducted using multi-stage methods. Initial stage involved enrolment of 250 Saudi pregnant women from multi-centre healthcare and community based settings in the capital of Saudi Arabia Riyadh. The second stage was embracement of the laboratory investigation that included Enzyme immunoassay (ELISA), DNA extraction, PCR, nested-PCR assay, and genotyping of the seropositive cases. Results: 203 women agreed to take part in our study with a response rate of 81.2% (203/250). Using ELISA, we found that the prevalence of Toxoplasma gondii IgG and IgM antibodies was 32.5% and 6.4%, respectively. We found that 29 samples (80.6%) were of genotype II; however 7 samples (19.4%) were of genotype III. Conclusion: Defining the population structure of T. gondii from Saudi Arabia has important implications for transmission, immunogenicity, pathogenesis, and in planning preventive strategies. Relationship between such variation in structure and disease manifestation in pregnant women is still difficult to assess due to the role of host immune status and genetic background on the control of infection, and of other parasitic features such as the infecting dose or parasite stage. Our finding of the genotyping of T. gondii might facilitate and inform future studies on comparative genomics and identification of genes that control important biological phenotypes including pathogenesis and transmission among Saudi women.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.05.001
       
  • Knowledge, attitudes and practices of the general public toward sun
           exposure and protection: A national survey in Saudi Arabia

    • Authors: Khalid M. AlGhamdi; Aeed S. AlAklabi; Abdulla Z. AlQahtani
      Pages: 652 - 657
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Khalid M. AlGhamdi, Aeed S. AlAklabi, Abdulla Z. AlQahtani
      Background: Many international studies have been conducted to assess the knowledge, attitudes and practices (KAP) of the public toward sun exposure and sun-protection measures. However, there are scarce data on these factors from the Middle East. Objectives: This study aimed to explore the KAP of the public toward sun exposure and sun-protection measures among Saudis. Methods: A cross-sectional survey using a specially designed questionnaire was conducted on a stratified random sample of the general population in the five geographical regions of Saudi Arabia (central, eastern, northern, southern, and western). Data were collected between October 2010 and March 2011. Multiple logistic regressions were applied to relate the use of sunscreen and skin cancer awareness with various socio-demographic variables. Results: The questionnaire was distributed to 2900 Saudis. A total of 2622 questionnaires were completed, returned, and included in the data analysis, corresponding to a response rate of 90.4%. The mean (SD) age of respondents was 27.8±9.7years. Fifty percent (1301/1601) of the respondents were males. Fifty-five percent (1406/2544) were aware of the association between sun exposure and skin cancer. Female, young and student respondents were more likely to be aware of the connection between sun exposure and skin cancer (p <0.001). Likewise, respondents from the middle social class and those with higher education levels were more likely to be informed (p <0.02). The prevalence of regular sunscreen use among study participants was only 23.7%, and female and employed respondents were more likely to use sunscreen (p <0.001). Protective clothes were the most commonly used sun protection measure as reported by more than 90% of our participants. Conclusion: This study has shown that sun awareness and protection are generally inadequate in the Saudi population and suggests the need for health education programs.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.04.002
       
  • Evaluation of antimicrobial activity of glycinate and carbonate
           derivatives of cholesterol: Synthesis and characterization

    • Authors: Rajendran Sribalan; Vediappen Padmini; Andiappan Lavanya; Kandasamy Ponnuvel
      Pages: 658 - 668
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Rajendran Sribalan, Vediappen Padmini, Andiappan Lavanya, Kandasamy Ponnuvel
      A series of glycinate and carbonate derivatives of cholesterol (4a–t) were synthesized, characterized and assessed for their in vitro antimicrobial activity. Our results revealed that the compounds exerted inhibitory activities against gram-negative bacteria and fungi.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.05.003
       
  • Bridging theory and practice: Mixed methods approach to instruction of law
           and ethics within the pharmaceutical sciences

    • Authors: Kyle John Wilby; Ziad Ghantous Nasr
      Pages: 669 - 673
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Kyle John Wilby, Ziad Ghantous Nasr
      Background: Professional responsibilities are guided by laws and ethics that must be introduced and mastered within pharmaceutical sciences training. Instructional design to teaching typically introduces concepts in a traditional didactic approach and requires student memorization prior to application within practice settings. Additionally, many centers rely on best practices from abroad, due to lack of locally published laws and guidance documents. Objectives: The aim of this paper was to summarize and critically evaluate a professional skills laboratory designed to enhance learning through diversity in instructional methods relating to pharmacy law and best practices regarding narcotics, controlled medications, and benzodiazepines. Setting: This study took place within the Professional Skills Laboratory at the College of Pharmacy at Qatar University. Method: A total of 25 students participated in a redesigned laboratory session administered by a faculty member, clinical lecturer, teaching assistant, and a professional skills laboratory technician. The laboratory consisted of eight independent stations that students rotated during the 3-h session. Stations were highly interactive in nature and were designed using non-traditional approaches such as charades, role-plays, and reflective drawings. All stations attempted to have students relate learned concepts to practice within Qatar. Main outcome measures: Student perceptions of the laboratory were measured on a post-questionnaire and were summarized descriptively. Using reflection and consensus techniques, two faculty members completed a SWOC (Strengths, Weaknesses, Opportunities, and Challenges) analysis in preparation for future cycles. Results: 100% (25/25) of students somewhat or strongly agreed that their knowledge regarding laws and best practices increased and that their learning experience was enhanced by a mixed-methods approach. A total of 96% (24/25) of students stated that the mixed-methods instructional approach should be continued in the future. The SWOC analysis identified the mixed methods approach and student feedback as strengths and opportunities, while resource shortages and lack of impact assessment were identified as weaknesses and challenges. Conclusion: Creative redesign of instructional methods pertaining to law and best practices was effective to achieve positive student perceptions regarding instructional methods and learning. Future cycles should include rigorous assessment methods to evaluate impact on student learning and practice.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.06.001
       
  • Effect of tramadol on metamizol pharmacokinetics and pharmacodynamics
           after single and repeated administrations in arthritic rats

    • Authors: Luis Alfonso Moreno-Rocha; Francisco Javier López-Muñoz; José Raúl Medina-López; Adriana Miriam Domínguez-Ramírez
      Pages: 674 - 684
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Luis Alfonso Moreno-Rocha, Francisco Javier López-Muñoz, José Raúl Medina-López, Adriana Miriam Domínguez-Ramírez
      Combined administration of certain doses of opioid compounds with a non-steroidal anti-inflammatory drug can produce additive or supra-additive effects while reducing unwanted effects. We have recently reported that co-administration of metamizol with tramadol produces antinociceptive effect potentiation, after acute treatment. However, none information about the effect produced by the combination after chronic or repeated dose administration exists. The aims of this study were to investigate whether the antinociceptive synergism produced by the combination of metamizol and tramadol (177.8+17.8mg/kg, s.c. respectively) is maintained after repeated treatment and whether the effects observed are primarily due to pharmacodynamic interactions or may be related to pharmacokinetics changes. Administration of metamizol plus tramadol acute treatment significantly enhanced the antinociceptive effect of the drugs given alone (P <0.05). Nevertheless, this effect decreased about 53% after the chronic treatment (3 doses per day, for 4days). No pharmacokinetic interaction between metamizol and tramadol was found under acute treatment (P >0.05). The mechanism involved in the synergism of the antinociceptive effect observed with the combination of metamizol and tramadol in single dose cannot be attributed to a pharmacokinetic interaction, and other pharmacodynamic interactions have to be considered. On the other hand, when metamizol and tramadol were co-administered under repeated administrations, a pharmacokinetic interaction and tolerance development occurred. Differences found in metamizol active metabolites’ pharmacokinetics (P <0.05) were related to the development of tolerance produced by the combination after repeated doses. This work shows an additional preclinical support for the combination therapy. The clinical utility of this combination in a suitable dose range should be evaluated in future studies.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.06.005
       
  • Contribution of community pharmacists in educating the asthma patients

    • Authors: Hamoud Saud Alotaibi; Thippeswamy Boreddy Shivanandappa; Sivagurunathan Nagarethinam
      Pages: 685 - 688
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Hamoud Saud Alotaibi, Thippeswamy Boreddy Shivanandappa, Sivagurunathan Nagarethinam
      Background: In asthma, the preventive measures taken by patients play an important role in improving life span and quality of life. This can be done more efficiently by community pharmacist by providing patient counseling and improving knowledge of patient about disease, risk factors, medication management and preventive measures to control asthma. Objectives: The objective of the study was to evaluate the contribution of community pharmacists in improvement of life span and quality of life of asthma patients. Method: The study was performed from Mid September to Mid-November 2014 in Dawadmi, Riyadh province, KSA. Data were collected by using a structured face to face questionnaire with randomly selected different community pharmacies. The questionnaire composed of different closed questions about the action plan of pharmacists in asthma management and factors that affect the counseling of asthma patients by the pharmacists. Results: It is noteworthy to observe that, in general, pharmacists are sufficiently knowledgeable and competent to counsel their asthma patients effectively.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.06.002
       
  • A pragmatic approach to the analysis of a combination formulation

    • Authors: Noshin Mubtasim; Eva Rahman Kabir; Ashis Kumar Podder; Subrata Bhadra
      Pages: 689 - 697
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Noshin Mubtasim, Eva Rahman Kabir, Ashis Kumar Podder, Subrata Bhadra
      The aim of the paper was to formulate a combined oral dosage form of rosuvastatin calcium and amlodipine besylate and to develop and validate an analytical method to be adopted for both routine quality control assay and in vitro dissolution studies of the formulation. The proposed combination formulation has shown compatibility with the chosen excipients, verified through FT-IR study. A novel gradient RP-HPLC method was developed and validated according to the ICH guideline which was found to be suitable for the simultaneous estimation of rosuvastatin calcium and amlodipine besylate from the formulation. The retention time of 2.7 and 6.08min allows the analysis of large amount of samples with less mobile phase which makes the method economic. The dissolution profiles of both the drugs in different dissolution medium were encouraging which makes the combination formulation of rosuvastatin calcium and amlodipine besylate superior and effective in achieving patient compliance.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.06.004
       
  • Olanzapine induced biochemical and histopathological changes after its
           chronic administration in rats

    • Authors: Rehmat Shah; Fazal Subhan; Gowhar Ali; Ihsan Ullah; Sami Ullah; Muhammad Shahid; Nisar Ahmad; Khwaja Fawad
      Pages: 698 - 704
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Rehmat Shah, Fazal Subhan, Gowhar Ali, Ihsan Ullah, Sami Ullah, Muhammad Shahid, Nisar Ahmad, Khwaja Fawad
      Objective: Olanzapine is a second generation antipsychotic acting mainly as a dopamine D2 and serotonine 5-HT2 receptors antagonist prescribed in the treatment of schizophrenia and various other psychiatric illnesses. Even though olanzapine is widely used in psychiatry, its effects on the architecture of pancreas, liver and kidneys are little known. The histology of pancreas especially has never been studied. For these reasons, the current study was designed to elucidate the toxic effects of chronic administration of olanzapine on pancreas, liver and kidneys and the enzymes released by these tissues in an escalating dose manner. Methods: Fourteen male rats were divided into two groups equally, the olanzapine group and the controls. Olanzapine was administered in a dose of 5mg/kg/d for the first eight weeks, 10mg/kg/d for next four weeks and 15mg/kg/d through the last two week period of 14weeks experiment. The controls received acidified saline only. Both the groups received restricted diet (20g/12h). The body weight and level of random blood sugar (RBS) were measured on a weekly basis. The levels of lipase, amylase, alanine transaminase (ALT) and aspartate transaminase (AST) were determined terminally. At the end of the experiment, the tissues were dissected out for histopathological evaluation. Results: Significant loss in body weight, change in the level of random blood sugar (∗∗ P <0.05, ∗∗∗ P <0.001) and significant rise in amylase and lipase levels (∗ P <0.05, ∗∗∗ P <0.001) were observed. However, the same treatment has shown no significant change in the levels of alanine and aspartate transaminases (P >0.05). The pancreas has shown derangement of beta cells and fibrotic growth. A mild to moderate focal increase in glomerular cellularity, cellular proliferation and glomerular capsules with negligible basement membranes were observed in the kidneys. No changes were observed in the architecture of the liver. Conclusion: The findings of this study indicated that the incidence of adverse effects associated with olanzapine could be prevented/alleviated/delayed by allowing restricted diet.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.06.006
       
  • Quinoline based furanones and their nitrogen analogues: Docking, synthesis
           and biological evaluation

    • Authors: Sukhbir Lal Khokra; Jyoti; Chetan; Pawan Kaushik; M.M. Alam; M.S. Zaman; Aftab Ahmad; Shah Alam Khan; Asif Husain
      Pages: 705 - 717
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Sukhbir Lal Khokra, Jyoti, Chetan, Pawan Kaushik, M.M. Alam, M.S. Zaman, Aftab Ahmad, Shah Alam Khan, Asif Husain
      A small library of twenty-four quinoline based butenolides also known as furanones and their nitrogen analogues was prepared by using two different aroylpropionic acids, viz. 3-(2-naphthoyl)propionic acid (3) and 3-(biphenyl-4-yl)propionic acid (4), as starting materials. The 3-aroylpropionic acids were reacted with different 6-substituted-2-chloroquinolin-3-carbaldehydes (2a–d) to obtain the corresponding furan-2(3H)-ones (5a–h). The purified and characterized furanones were then converted into their corresponding 2(3H)-pyrrolones (6a–h) and N-benzyl-pyrrol-2(3H)-ones (7a–h). The antimicrobial activities of the title compounds were evaluated against two strains of each Gram +ve (Staphylococcus aureus and Bacillus subtilis), Gram −ve bacteria (Escherichia coli and Pseudomonas aeruginosa) and against fungal strains of Aspergillus niger and Aspergillus flavus. In vivo anti-inflammatory potential of the title compounds was investigated by standard method. Majority of the compounds showed significant antibacterial activity against both the Gram +ve strains. Eight most potent anti-inflammatory compounds (5b, 5d, 5h, 6b, 7b, 7d, 7f, 7h) which exhibited >53% inhibition in edema, were also screened for their in vivo analgesic activity. All the tested compounds were found to have significant reduction in ulcerogenic action but only three compounds (5d, 5h and 7h) showed comparable analgesic activity to standard drug, diclofenac. The results were also validated using in silico approach and maximum mol doc score was obtained for compounds 7a–h. On comparing the in vivo and in silico anti-inflammatory results of synthesized compounds, N-benzyl pyrrolones (7a–h) emerged as the potent anti-inflammatory agents. It was also observed that compounds that possess electron withdrawing group such as Cl or NO2 are more biologically active.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.05.002
       
  • How to improve suspected ADR reporting among pharmacists in the GCC'

    • Authors: Kerry Wilbur
      Pages: 718 - 719
      Abstract: Publication date: November 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 6
      Author(s): Kerry Wilbur


      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2015.04.005
       
  • Investigation for the quality factors on the tablets containing medicated
           pellets

    • Authors: Xueying Tan; Jingbo Hu
      Pages: 507 - 514
      Abstract: Publication date: September 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 5
      Author(s): Xueying Tan, Jingbo Hu
      Sustained and controlled pellets are considered as one of the ideal dosage forms. Due to the large coverage area of pellets, loaded drugs can be absorbed completely in the body and bioavailability is improved correspondingly. Coated pellets-containing tablet is a special oral formulation consisting of various pellets with different release rate. Desired rate of drug release rate can be achieved by adjusting the proportion of pellets. However, this formulation faces strict requirements in the process of preparation. Several factors will influence release behavior of tablets, including pellet cores, coating, and tabletting. Therefore, these factors will be investigated sufficiently in this review to provide valuable information for manufacturing process.

      PubDate: 2016-10-11T19:04:04Z
      DOI: 10.1016/j.jsps.2015.01.020
       
  • Oral antimicrobial peptides: Types and role in the oral cavity

    • Authors: Zohaib Khurshid; Mustafa Naseem; Zeeshan Sheikh; Shariq Najeeb; Sana Shahab; Muhammad Sohail Zafar
      Pages: 515 - 524
      Abstract: Publication date: September 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 5
      Author(s): Zohaib Khurshid, Mustafa Naseem, Zeeshan Sheikh, Shariq Najeeb, Sana Shahab, Muhammad Sohail Zafar
      Antimicrobial peptides (AMPs) are a wide-ranging class of host-defense molecules that act early to contest against microbial invasion and challenge. These are small cationic peptides that play an important in the development of innate immunity. In the oral cavity, the AMPs are produced by the salivary glands and the oral epithelium and serve defensive purposes. The aim of this review was to discuss the types and functions of oral AMPs and their role in combating microorganisms and infections in the oral cavity.

      PubDate: 2016-10-11T19:04:04Z
      DOI: 10.1016/j.jsps.2015.02.015
       
  • A review of polymers as multifunctional excipients in drug dosage form
           technology

    • Authors: Bożena Karolewicz
      Pages: 525 - 536
      Abstract: Publication date: September 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 5
      Author(s): Bożena Karolewicz
      In the article, groups of multifunctional polymers used in drug dosage form technology were classified and evaluated. These compounds, in addition to their basic function as excipients, may have additional properties, e.g. stimuli sensitivity, enzyme inhibition, intestinal epithelium penetration enhancement, efflux pump inhibition, taste-masking, pharmacological activity and the ability to interact with enzymes responsible for drug metabolism. While classifying specific groups of multifunctional polymers, special emphasis was placed on the advantages of using them when designing new drug. Such advantages include, i.a., increasing substance bioavailability, improving substance stability during formulation and the possibility of obtaining forms of controlled or localized release to a specific site in the organism.

      PubDate: 2016-10-11T19:04:04Z
      DOI: 10.1016/j.jsps.2015.02.025
       
  • Orally disintegrating films: A modern expansion in drug delivery system

    • Authors: Muhammad Irfan; Sumeira Rabel; Quratulain Bukhtar; Muhammad Imran Qadir; Farhat Jabeen; Ahmed Khan
      Pages: 537 - 546
      Abstract: Publication date: September 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 5
      Author(s): Muhammad Irfan, Sumeira Rabel, Quratulain Bukhtar, Muhammad Imran Qadir, Farhat Jabeen, Ahmed Khan
      Over the past few decades, tendency toward innovative drug delivery systems has majorly increased attempts to ensure efficacy, safety and patient acceptability. As discovery and development of new chemical agents is a complex, expensive and time consuming process, so recent trends are shifting toward designing and developing innovative drug delivery systems for existing drugs. Out of those, drug delivery system being very eminent among pediatrics and geriatrics is orally disintegrating films (ODFs). These fast disintegrating films have superiority over fast disintegrating tablets as the latter are associated with the risks of choking and friability. This drug delivery system has numerous advantages over conventional fast disintegrating tablets as they can be used for dysphasic and schizophrenic patients and are taken without water due to their ability to disintegrate within a few seconds releasing medication in mouth. Various approaches are employed for formulating ODFs and among which solvent casting and spraying methods are frequently used. Generally, hydrophilic polymers along with other excipients are used for preparing ODFs which allow films to disintegrate quickly releasing incorporated active pharmaceutical ingredient (API) within seconds. Orally disintegrating films have potential for business and market exploitation because of their myriad of benefits over orally disintegrating tablets. This present review attempts to focus on benefits, composition, approaches for formulation and evaluation of ODFs. Additionally, the market prospect of this innovative dosage form is also targeted.

      PubDate: 2016-10-11T19:04:04Z
      DOI: 10.1016/j.jsps.2015.02.024
       
  • Diabetes mellitus and oxidative stress—A concise review

    • Authors: Ullah Asmat; Khan Abad; Khan Ismail
      Pages: 547 - 553
      Abstract: Publication date: September 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 5
      Author(s): Ullah Asmat, Khan Abad, Khan Ismail
      Human body is continuously exposed to different types of agents that results in the production of reactive species called as free radicals (ROS/RNS) which by the transfer of their free unpaired electron causes the oxidation of cellular machinery. In order to encounter the deleterious effects of such species, body has got endogenous antioxidant systems or it obtains exogenous antioxidants from diet that neutralizes such species and keeps the homeostasis of body. Any imbalance between the RS and antioxidants leads to produce a condition known as “oxidative stress” that results in the development of pathological condition among which one is diabetes. Most of the studies reveal the inference of oxidative stress in diabetes pathogenesis by the alteration in enzymatic systems, lipid peroxidation, impaired Glutathione metabolism and decreased Vitamin C levels. Lipids, proteins, DNA damage, Glutathione, catalane and superoxide dismutase are various biomarkers of oxidative stress in diabetes mellitus. Oxidative stress induced complications of diabetes may include stroke, neuropathy, retinopathy and nephropathy. The basic aim of this review was to summarize the basics of oxidative stress in diabetes mellitus.

      PubDate: 2016-10-11T19:04:04Z
      DOI: 10.1016/j.jsps.2015.03.013
       
  • HIV pharmaceutical care in primary healthcare: improvement in CD4 count
           and reduction in drug-related problems

    • Authors: Caroline de Godoi Rezende Costa Molino; Renata Cavalcanti Carnevale; Aline Teotonio Rodrigues; Patricia Moriel; Priscila Gava Mazzola
      Abstract: Publication date: Available online 15 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Caroline de Godoi Rezende Costa Molino, Renata Cavalcanti Carnevale, Aline Teotonio Rodrigues, Patricia Moriel, Priscila Gava Mazzola
      Background Highly active antiretroviral therapy (HAART) is complex and many factors contribute to a patient’s response to initial therapy including adherence, drug effectiveness, and tolerance. Close HAART follow-up is needed, particularly when there are concurrent therapies such as prophylactic antibiotics and medications for the treatment of comorbidities. Objective To assess the effectiveness of pharmacist intervention in reducing drug related problems in HIV/AIDS outpatients (intervention group) and in improving clinical parameters in the intervention group compared to the control group. Methods We conducted a prospective controlled intervention study with patients paired by gender and initial T CD4+ lymphocyte (CD4) count. HIV-infected patients of a public outpatient service were enrolled for the study by consecutive and convenience sampling. Patients selected for the study were divided into a control group and an intervention group. Both groups were followed for one year; however, only the intervention group received pharmaceutical care. The primary outcome was the drug related problem (DRP) analysis for the intervention group. Secondary outcomes were CD4 count and viral load evaluation for both groups. Results There was a total of 143 patients enrolled in this study, with 53 (37.06%) patients in the control group and 90 (62.94%) patients in the intervention group. A total of 202 pharmacist interventions with 193 pharmacist-patient and 9 pharmacist-physician interventions were proposed. After one year of pharmaceutical care, a reduction of 38.43% between the initial and final DRPs was found (p=0.0001). The most common DRPs found were related to medication safety. The intervention group showed a mean increase of 84% for the CD4 count in comparison to that observed in the control group. The viral load was not significantly different between the final and initial mean values for both groups. Conclusion Pharmacist appointments enabled identification, prevention, and solving of drug related problems, especially those related to drug safety. Also, pharmacist interventions improved adherence and increased HAART effectiveness as suggested by the higher elevation in the CD4 count seen in the intervention group in comparison to the control group.

      PubDate: 2016-11-21T16:20:14Z
      DOI: 10.1016/j.jsps.2016.11.004
       
  • Analysis of inorganic and organic constituents of myrrh resin by GC-MS and
           ICP-MS: An emphasis on medicinal assets

    • Authors: Syed Rizwan Ahamad; Abdul Rahman Al-Ghadeer; Raisuddin Ali; Wajhul Qamar; Suliman Aljarboa
      Abstract: Publication date: Available online 20 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Syed Rizwan Ahamad, Abdul Rahman Al-Ghadeer, Raisuddin Ali, Wajhul Qamar, Suliman Aljarboa
      The aim of the present investigation was to explore the constituents of the Arabian myrrh resin obtained from Commiphora myrrha. The organic and inorganic composition of the myrrh gum resin has been investigated using gas chromatography-mass spectrometry (GC-MS) and inductively coupled plasma-mass spectrometry (ICP-MS). Analysis executed by ICP-MS reveals the presence of various inorganic elements in significant amount in the myrrh resin. The elements which were found to be present in large amounts include calcium, magnesium, aluminum, phosphorus, chlorine, chromium, bromine and scandium. The important organic constituents identified in the myrrh ethanolic extract include limonene, curzerene, germacrene B, isocericenine, myrcenol, beta selinene, spathulenol etc. The present work complements other myrrh associated investigations done in the past and provides additional data for the future researches.

      PubDate: 2016-11-21T16:20:14Z
      DOI: 10.1016/j.jsps.2016.10.011
       
  • DEVELOPMENT AND EVALUATION OF KETOPROFEN SUSTAINED RELEASE MATRIX TABLET
           USING HIBISCUS ROSA-SINENSISLEAVES MUCILAGE

    • Authors: M. Kaleemullah; K. Jiyauddin; E. Thiban; S. Rasha; A.D. Samer; S. Budiasih; O.E. Gamal; A. Fadli; Y. Eddy
      Abstract: Publication date: Available online 10 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): M. Kaleemullah, K. Jiyauddin, E. Thiban, S. Rasha, A.D. Samer, S. Budiasih, O.E. Gamal, A. Fadli, Y. Eddy
      Currently, the use of natural gums and mucilage is of increasing importance in pharmaceutical formulations as valuable drug excipient. Natural plant-based materials are economic, free of side effects, biocompatible and biodegradable. Therefore, Ketoprofen matrix tablets were formulated by employing Hibiscus rosa-sinensis leaves mucilage as natural polymer and HPMC (K100M) as a synthetic polymer to sustain the drug release from matrix system. Direct compression method was used to develop sustained released matrix tablets. The formulated matrix tablets were evaluated in terms of physical appearance, weight variation, thickness, diameter, hardness, friability and in vitro drug release. The difference between the natural and synthetic polymers were investigated concurrently. Matrix tablets developed from each formulation passed all standard physical evaluation tests. The dissolution studies of formulated tablets revealed sustained drug release up to 24 hours compared to the reference drug Apo Keto® SR tablets. The dissolution data later were fitted into kinetic models such as zero order equation, first order equation, Higuchi equation, Hixson Crowell equation and Korsmeyer-Peppas equation to study the release of drugs from each formulation. The best formulations were selected based on the similarity factor (f2) value of 50% and more. Through the research, it is found that by increasing the polymers concentration, the rate of drug release decreased for both natural and synthetic polymers. The best formulation was found to be F3 which contained 40% Hibiscus rosa-sinensis mucilage polymer and showed comparable dissolution profile to the reference drug with f2 value of 78.03%. The release kinetics of this formulation has shown to follow non-Fickian type which involved both diffusion and erosion mechanism. Additionally, the statistical results indicated that there was no significant difference (p>0.05) between the F3 and reference drug in term of MDT and T50% with p-values of 1.00 and 0.995 respectively.

      PubDate: 2016-11-14T15:26:45Z
      DOI: 10.1016/j.jsps.2016.10.006
       
  • Shortage of psychotropic medications in community pharmacies in Saudi
           Arabia: Causes and solutions

    • Authors: Yazed Sulaiman Al-Ruthia; Wael Mansy; Mohammad Barasin; Yazeed Mohammad Ghawaa; Mohammed AlSultan; Mohammad A. Alsenaidy; Solaiman Alhawas; Sultan AlGhadeer
      Abstract: Publication date: Available online 12 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Yazed Sulaiman Al-Ruthia, Wael Mansy, Mohammad Barasin, Yazeed Mohammad Ghawaa, Mohammed AlSultan, Mohammad A. Alsenaidy, Solaiman Alhawas, Sultan AlGhadeer
      Background Patients with mental disorders, such as depression and anxiety, who seek medical care in private psychiatric clinics in Riyadh, Saudi Arabia, have recently expressed concerns to doctors about difficulty in filling psychotropic medications, such as Amitriptyline and Aripiprazole, at retail community pharmacies. Objectives The aim of this study was to investigate if there is a shortage of some commonly prescribed psychotropic medications in retail community pharmacies in Saudi Arabia, and if so, to explore the possible reasons behind the shortage of these medications. Methods The availability of 28 commonly prescribed psychotropic medications was checked in multiple retail community pharmacies in 4 different regions of Saudi Arabia. Further, potential reasons behind the shortage of some psychotropic medications in retail community pharmacies were also explored. Results Amitriptyline, Amoxapine, Aripiprazole, Bupropion, Buspirone, Duloxetine, Haloperidol, Hydroxyzine, Lithium, Prochlorperazine, Procyclidine, Promethazine, Thioridazine, Trazodone, and Trifluoperazine were unavailable in over half of the 248 community pharmacies surveyed. Four possible reasons behind the shortage of these medications were reported by 31 pharmacists working in different retail community pharmacies’ purchasing departments, with a majority (58.06%) reporting the primary reason for a shortage of these medications that they are slow-moving items with low profit margins. Conclusions The findings of this study should expedite the reform process in both the Ministry of Health and the Saudi Food and Drug Authority (SFDA) to publish and enforce an essential list of medications for retail community pharmacies, which should include the most commonly prescribed psychotropic medications.

      PubDate: 2016-11-14T15:26:45Z
      DOI: 10.1016/j.jsps.2016.10.013
       
  • Using an integrated information system to reduce interruptions and the
           number of non-relevant contacts in the inpatient pharmacy at tertiary
           hospital

    • Authors: Saleh Binobaid; Mohammed Almeziny; Ip-Shing Fan
      Abstract: Publication date: Available online 12 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Saleh Binobaid, Mohammed Almeziny, Ip-Shing Fan
      Patient care is provided by a multidisciplinary team of healthcare professionals intended for high-quality and safe patient care. Accordingly, the team must work synergistically and communicate efficiently. In many hospitals, nursing and pharmacy communication relies mainly on telephone calls. In fact, numerous studies have reported telephone calls as a source of interruption for both pharmacy and nursing operations, therefore, the workload increases and the chance of errors raises. This report describes the implementation of an integrated information system that possibly can reduce telephone calls through providing real-time tracking capabilities and sorting prescriptions urgency. thus significantly improving traceability of all prescriptions inside pharmacy. The research design is based on a quasi-experiment using pre-post testing using the continuous improvement approach. The improvement project is performed using a six-step method. A survey was conducted in Prince Sultan Military Medical City (PSMMC) to measure the volume and types of telephone calls before and after implementation to evaluate the impact of the new system. Beforehand of the system implementation, during the two-week measurement period, all pharmacies received 4,466 calls and the majority were follow-up calls. Subsequently of the integrated system roll out, there was a significant reduction (p > 0.001) in the volume of telephone calls to 2,630 calls, besides the calls nature turned out to be to more professional inquiries (p > 0.001). As a result, avoidable interruptions and workload were decreased.

      PubDate: 2016-11-14T15:26:45Z
      DOI: 10.1016/j.jsps.2016.11.005
       
  • A case of severe erythema nodosum induced by methimazole :

    • Authors: Selma Emre; Didem Ozdemir; Sibel Orhun; Goknur Kalkan; Sertac Sener
      Abstract: Publication date: Available online 12 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Selma Emre, Didem Ozdemir, Sibel Orhun, Goknur Kalkan, Sertac Sener
      Erythema nodosum (EN), is the most common variant of septal panniculitis and is possibly a delayed hypersensitivity reaction triggered by a wide range of antigenic stimuli. Hypersensitivity reactions due to medications have been recognized as a cause of 3 to 10 percent of EN cases. Case reports of EN associated with the anti-thyroid drugs are quite rarely reported in the literature even if there is a common use of anti-thyroid drugs. We report an EN case due to methimazole. The patients complaints arose immediately fifteen days after the beginning ofmethimazole treatment. To the best of our knowledge, this case report is the first of an erythema nodosum induced by methimazole.

      PubDate: 2016-11-14T15:26:45Z
      DOI: 10.1016/j.jsps.2016.11.003
       
  • LC-ESI-MS/MS profiling of phenolics from Eleutherococcus spp.
           inflorescences, structure-activity relationship as antioxidants,
           inhibitors of hyaluronidase and acetylcholinesterase

    • Authors: Daniel Załuski; Marta Olech; Rafał Kuźniewski; Robert Verpoorte; Renata Nowak; Helena D. Smolarz
      Abstract: Publication date: Available online 12 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Daniel Załuski, Marta Olech, Rafał Kuźniewski, Robert Verpoorte, Renata Nowak, Helena D. Smolarz
      Nature is a source of many plant-based molecules used as pro- or drugs. Eleutherococcus species’ are native to Asia and the North Russia, and are traditionally used to treat various diseases. In turn, neither secondary metabolites of the species cultivated in the West Europe nor the bioactivity are known. No differences in the phenols and flavonoids content in the inflorescences were found. The richest in polyphenols was E. giraldii (5.18 mg/g), while in flavonoids E. gracilistylus (1.80 mg/g). Using LC-ESI-MS/MS, protocatechuic and trans-caffeic acids have been identified as the most abundant compounds in E. gracilistylus, E. giraldii, E. senticosus (833.4; 855.6; 614.7 and 280.8; 156.0; 167.6 μg/g DE). It was observed that all species were able to chelate Fe2+ with the EC50 value of 0.2, 0.6, 0.3 mg/mL for E. gracilistylus, E. giraldii, E. senticosus, respectively. E. gracilistylus exhibited the strongest antiperoxidation and anti-DPPH∗ activity (EC50 3.2 and 0.48 mg/mL). The weak inhibitory potential has been observed in case of AChE inhibition at the level of 16.17 and 12.2% for E. gracilistylus, E. giraldii. We report for the first time that the extracts inhibited Hyal activity in the range from 16.4 to 60.7%. To our best knowledge, no information was available on this activity of the inflorescences and this provide a background to study inflorescences in more detail. Considering the SAR, an antioxidant activity may be correlated with a high amount of protocatechuic and trans-caffeic acids and their chemical structure.

      PubDate: 2016-11-14T15:26:45Z
      DOI: 10.1016/j.jsps.2016.11.002
       
  • Isolation, biological evaluation and validated HPTLC-quantification of the
           marker constituent of the edible Saudi plant Sisymbrium irio L.

    • Authors: Shaza M. Al-Massarani; Ali A. El Gamal; Perwez Alam; Ebtesam S. Al-Sheddi; Mai M. Al-Oqail; Nida N. Farshori
      Abstract: Publication date: Available online 12 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Shaza M. Al-Massarani, Ali A. El Gamal, Perwez Alam, Ebtesam S. Al-Sheddi, Mai M. Al-Oqail, Nida N. Farshori
      Phytochemical investigation and chromatographic purification of the n-hexane fraction of the aerial parts of the edible Saudi plant Sisymbrium irio led to the isolation of β- sitosterol (1), stigmasterol (2) and β -sitosterol-β-D-glucoside (3). The cytotoxic effects of the n-hexane, dichloromethane, ethyl acetate and n-butanol fractions were tested against three cancer cell lines viz., MCF-7, HCT-116 and HepG2, using the crystal violet staining (CVS) method, while the antibacterial activity against a number of pathogenic bacterial strains, was also estimated using the broth microdilution assay. The n-hexane fraction showed potent cytotoxic activities against all tested human cancer cell lines (IC50: 11.7-13.4 μg/mL), while the dichloromethane fraction was particularly potent against HCT-116 cells (IC50: 5.42 μg/mL). On the other hand, the n-hexane and EtOAc fractions demonstrated significant inhibitory activities against the Gram positive bacteria S. pyogenes and C. perfringens; and the Gram negative bacterium S.enteritidis. Our results warrant the therapeutic potential of S. irio as nutritional supplement to reduce the risk of contemporary diseases. Additionally, a validated high performance thin-layer chromatography (HPTLC) method was developed for the quantitative analysis of biomarker β-sitosterol glucoside (isolated in high quantity) from the n-hexane fraction. The system was found to furnish a compact, sharp, symmetrical and high resolution band for β-sitosterol glucoside (Rf = 0.43±0.002). The limit of detection (LOD) & limit of quantification (LOQ) for β-sitosterol glucoside was found to be 21.84 & 66.18 ng band-1, respectively. β-sitosterol glucoside was found to be present only in n-hexane fraction (2.10 μg/mg of dried fraction) while it was absent in the other fractions of S.irio which validated the high cytotoxic and antibacterial activity of n-hexane fraction of S.irio.

      PubDate: 2016-11-14T15:26:45Z
      DOI: 10.1016/j.jsps.2016.10.012
       
  • Chemical constituents of Helichrysum italicum (Roth) G. Don essential oil
           and their antimicrobial activity against Gram-positive and Gram-negative
           bacteria, filamentous fungi and Candida albicans

    • Authors: Bouzid Djihane; Nouioua Wafa; Soltani Elkhamssa; De Haro Juan Pedro; Angeles Esteban Maria; Zerroug Mouhamed Mihoub
      Abstract: Publication date: Available online 12 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Bouzid Djihane, Nouioua Wafa, Soltani Elkhamssa, De Haro Juan Pedro, Angeles Esteban Maria, Zerroug Mouhamed Mihoub
      The aerial parts of Helichrysum italicum (Roth) G. Don were subjected to hydrodistillation to obtain essential oils which had been analyzed by gas chromatography and gas chromatography coupled with mass spectrometry and tested for antimicrobial activity against 12 bacteria, two yeasts and four fungi by agar diffusion method. The essential oil yielded 0.44% (v/w) and 67 compounds accounting for 99.24% of the oil were identified with a high content of oxygenated sesquiterpenes (61.42%). The most oxygenated sesquiterpenes compounds were α-Cedrene (13.61%), α-Curcumene (11.41%), Geranyl acetate (10.05%), Limonene (6.07%), Nerol (5.04%), Neryl acetate (4.91%) and α-Pinene (3.78%). The antimicrobial activity of the essential oil was assayed by using the disc diffusion method on Echerchia coli ATCC 25922, Staphylococcus aureus ATCC 6538, Micrococcus luteus ATCC 4698, Klebsiella pneumonia ATCC 4352, Enterococcus cereus ATCC 2035, Bacillus cereus ATCC 10876, Staphylococcus epidermidis ATCC 12228, Bacillus subtilis ATCC 9372, Pseudomonas aeruginosa ATCC 27853, Enterococcus faecalis ATCC 49452, Proteus mirabilis ATCC 35659, Listeria monocytogenes ATCC 15313 and yeasts Candida albicans ATCC 10231, Saccharomyces cerevisiae ATCC 9763 and fungi, Fusarium solani var. coeruleum, Aspergillus niger, Alternaria alternata, Ascochyta rabiei. Helichrysum italicum inhibited the growth of all the tested microorganisms except three bacteria, Echerchia coli ATCC 25922, Klebsiella pneumonia ATCC 4352 and Listeria monocytogenes ATCC 15313. The most sensitive bacterium was Enterococcus cereus ATCC 2035 with minimum inhibitory and bactericidal concentrations of 0.79 μg.ml-1. A minimum fungistatic and fungicide concentration of 6.325 μg.ml-1 and 12.65 μg.ml-1 respectively were obtained with Candida albicans ATCC 10231 and Saccharomyces cerevisiae ATCC 9763. However the four fungi were more resistant with fungistatic minimum concentration ranging from 6.325 μg.ml-1 to 50.6 μg.ml-1 and a fungicide minimum concentration of 50.6 μg.ml-1. This antimicrobial activity could be attributed to the essential oil chemical composition. Thus this study represents a first step in the study of the chemical composition of H. italicum (Roth) G. Don collected from north Algeria and its antimicrobial properties.

      PubDate: 2016-11-14T15:26:45Z
      DOI: 10.1016/j.jsps.2016.11.001
       
  • Comparative study of antioxidant activity and validated RP-HPTLC analysis
           of rutin in the leaves of different Acacia species grown in Saudi Arabia

    • Authors: Perwez Alam; Mohammed F. Alajmi; Ahmed H. Arbab; Mohammad K. Parvez; Nasir A. Siddiqui; Saleh I. Alqasoumi; Adnan J. Al-Rehaily; Mohammed S. Al-Dosary; Omer A. Basudan
      Abstract: Publication date: Available online 5 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Perwez Alam, Mohammed F. Alajmi, Ahmed H. Arbab, Mohammad K. Parvez, Nasir A. Siddiqui, Saleh I. Alqasoumi, Adnan J. Al-Rehaily, Mohammed S. Al-Dosary, Omer A. Basudan
      The present study assessed the comparative antioxidant potential of the ethanol extract (EE) of leaves of four Acacia species (A. salicina, AS; A. laeta, AL; A. hamulosa AH; and A. tortilis, AT) grown in Saudi Arabia, including RP-HPTLC quantification of antioxidant biomarker rutin. In vitro DPPH radical scavenging and β-carotene-linoleic acid bleaching assays showed the promising antioxidant activities of Acacia extracts: ASEE (IC50: 60.39 and 324.65 μg/ml) >ALEE (IC50: 217.06 and 423.36 μg/ml) >ATEE (IC50: 250.13 and 747.50 μg/ml) >AHEE (IC50: 255.83 and 417.28 μg/ml). This was comparable to rutin tested at 500μg/ml. Further, a RP- HPTLC densitometric method was developed (acetonitrile: water; 6:4; v/v) using glass-backed RP-18 silica gel F254 plate, and scanned at UVmax 254 nm. The method was validated as per the ICH guidelines. Analysis of the validated RP-HPTLC displayed an intense peak (Rf = 0.65±0.004) of rutin that was estimated (μg/mg dry weight) to be highest in ASEE (10.42), followed by ALEE (2.67), AHEE (1.36) and ATEE (0.31). Taken together, presence of rutin strongly supported the high antioxidant property of the tested Acacia species, especially A. salicina. The developed RP-HPTLC method therefore, affirms its application in the quality control of commercialized herbal drugs or formulation containing rutin.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2016.10.010
       
  • Rhanterium epapposum Oliv. Essential Oil: Chemical composition and
           antimicrobial, insect-repellent and anticholinesterase Activities

    • Authors: Betul Demirci; Hasan Soliman Yusufoglu; Nurhayat Tabanca; Halide Edip Temel; Ulrich R. Bernier; Natasha M. Agramonte; Saleh Ibrahim Alqasoumi; Adnan Jathlan Al-Rehaily; Kemal Husnu Can Başer; Fatih Demirci
      Abstract: Publication date: Available online 1 November 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Betul Demirci, Hasan Soliman Yusufoglu, Nurhayat Tabanca, Halide Edip Temel, Ulrich R. Bernier, Natasha M. Agramonte, Saleh Ibrahim Alqasoumi, Adnan Jathlan Al-Rehaily, Kemal Husnu Can Başer, Fatih Demirci
      The essential oil (EO) of the aerial parts of Rhanterium epapposum Oliv. (Asteraceae), was obtained by hydrodistillation. The oil was subsequently analyzed both by GC-FID and GC-MS, simultaneously. Forty-five components representing 99.2% of the oil composition were identified. The most abundant compounds were camphene (38.5%), myrcene (17.5%), limonene (10.1%) and α-pinene (8.7%). Referring to the ethnobotanical utilization, an insecticidal assay was performed, where the oil repelled the yellow fever mosquito Aedes aegypti L. at a minimum effective dose (MED of 0.035 ± 0.010 mg/cm2) compared to the positive control DEET (MED of 0.015 ± 0.004 mg/cm2). Additionally, the in vitro antimicrobial activity against a panel of pathogens was determined using a microdilution method. The acetyl- and butyrylcholine esterase inhibitory activities were measured using the colorimetric Ellman method. The bioassay results showed that the oil was rather moderate in antimicrobial and cholinesterase inhibitions when compared to the standard compounds.

      PubDate: 2016-11-07T14:05:27Z
      DOI: 10.1016/j.jsps.2016.10.009
       
  • Comparative assessment of saliva and plasma for drug bioavailability and
           bioequivalence studies in humans

    • Authors: Nasir M. Idkaidek
      Abstract: Publication date: Available online 17 October 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Nasir M. Idkaidek
      Aims: To study the pharmacokinetics of selected drugs in plasma and saliva matrixes in healthy human volunteers, and to suggest using non-invasive saliva sampling instead of plasma as a surrogate in bioavailability and bioequivalence (BA/BE) studies. Methods: Four different pilot BA/BE studies were done in 12–18 healthy humans. Saliva and plasma samples were collected for 3–5 half life values of metformin, tolterodine, rosuvastatin, and paracetamol after oral dosing. Saliva and plasma samples were assayed using LC-MSMS, and then pharmacokinetic parameters were calculated by non-compartmental analysis using Kinetica program. Effective intestinal permeability (P eff) values were also optimized to predict the actual average plasma profile of each drug by Nelder-Mead algorithm of the Parameter Estimation module using SimCYP program. Results: All studied drugs showed salivary excretion with strong correlation coefficients between saliva and plasma concentrations. The optimized P eff ranged 1.44–68.3×10−4 cm/s for the drugs under investigation. Saliva/plasma concentrations ratios ranged 0.17–1.5. Inter and intra individual variability of primary pharmacokinetic parameters in saliva matrix was either close to or higher than plasma matrix. This requires larger sample size in saliva studies for some drugs. Conclusion: Our results suggest that there is a potential in BA/BE studies for saliva to be considered as a surrogate for plasma concentration, which goes along with drug regulations. The use of saliva instead of plasma in such studies makes them non-invasive, easy and with a lower clinical burden.

      PubDate: 2016-10-31T07:36:09Z
      DOI: 10.1016/j.jsps.2016.10.002
       
  • Curcumin modulates myotoxicity associated with sub-chronic use of
           atorvastatin in rats: A histopathological and biochemical analysis

    • Authors: Said Said Elshama; Ayman El-Meghawry El-Kenawy; Hosam-Eldin Hussein Osman
      Abstract: Publication date: Available online 17 October 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Said Said Elshama, Ayman El-Meghawry El-Kenawy, Hosam-Eldin Hussein Osman
      Atorvastatin is considered to be one of the most commonly used of all statins antihyperlipidemic drugs despite the fact that there is much controversy about its safety. Its therapeutic use becomes severely limited by the hazards of inducing myotoxicity. Curcumin is one of the safe spices that have chemoprotection and cytoprotection effects against endogenous and exogenous noxious stimuli. This study investigates the effect of curcumin on atorvastatin sub-chronic use - induced myotoxicity in rats by the assessment of serum creatinine phosphokinase, lactic acid dehydrogenase, myoglobin, troponin, potassium, creatinine and histopathological changes of skeletal, smooth and cardiac muscles by light and electron microscope examination. Eighty adult albino rats were divided into four groups: each group consists of twenty rats. The control group received water, the second group received atorvastatin, third group received curcumin and the fourth group received curcumin with atorvastatin for 90days by gastric gavage. The prolonged use of atorvastatin induced significant abnormalities of all myotoxicity biomarkers associated with histopathological and ultrastructural changes in the different types of the muscles. Co-administration of curcumin with sub-chronic use of atorvastatin led to an improvement in myotoxicity manifestations.

      PubDate: 2016-10-31T07:36:09Z
      DOI: 10.1016/j.jsps.2016.10.003
       
  • Pharmacy Malpractice: The rate and prevalence of dispensing high-risk
           prescription-only medications at community pharmacies in Saudi Arabia

    • Authors: Thamir M Alshammari; Salman A Alhindi; Ahmed M Alrashdi; Imaan Benmerzouga; Mohamad Aljofan
      Abstract: Publication date: Available online 17 October 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Thamir M Alshammari, Salman A Alhindi, Ahmed M Alrashdi, Imaan Benmerzouga, Mohamad Aljofan
      Objective To assess the compliance of community pharmacies with the regulations that prohibit the dispensing of prescription-only medications in the absence of a physician prescription in Saudi Arabia. Method A cross-sectional study was conducted in the period between October 2014 and January 2015. A list of 10 prescription-only medications were selected to be studied. 150 community pharmacies were visited across 6 major regions in Saudi Arabia to assess the prevalence of non-compliance among community pharmacies. Pharmacies were selected in random and researchers (disguised as patients) requested to purchase prescription-only medications in the absence of a prescription. Not all medications were purchased at once. Data was recorded per pharmacy, where pharmacies that approved dispense of the selected drug was scored as non-compliant and the pharmacies that rejected dispense of the selected drug was scored as compliant. Compliance rate was calculated per region per drug. Pharmacies based in governmental hospitals were visited in parallel. A total of 20 were visited. Data and statistical analysis were performed using Statistical Analyses Software (SAS 9.3). Results A total of 150 pharmacies were visited over a period of 3 months. On average, the percent approved dispense of prescription-only drugs across 6 regions in Saudi Arabia is 63% and the percent rejected dispense is 37% representing a significant non-compliance rate regarding to the selected list of medications in this study. The frequency of dispense per medication across 6 major regions in Saudi Arabia is as follow: Isosorbide dinitrate (86%), Enoxaparin (82%), nitroglycerin (74%), Propranolol (73%), Verapamil (70%), Warfarin (65%), Methyldopa (64%), Ciprofloxacin (57%) and Codeine (4%). Conclusions Non-compliance of community pharmacies with the law of pharmaceutical practice is at an alarming rate in the Kingdom of Saudi Arabia and authoritative figures must intervene to impede and combat such activities.

      PubDate: 2016-10-31T07:36:09Z
      DOI: 10.1016/j.jsps.2016.10.001
       
  • In-Home Vaccination Service: One-Shot or a Sustainable Prevention?

    • Authors: Tariq M. Alhawassi; Bander S. Balkhi
      Abstract: Publication date: Available online 17 October 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Tariq M. Alhawassi, Bander S. Balkhi


      PubDate: 2016-10-31T07:36:09Z
      DOI: 10.1016/j.jsps.2016.10.007
       
  • Hybrid polymeric matrices for oral modified release Desvenlafaxine
           succinate tablets

    • Authors: Wael Samy; Ayman Elnoby; Hanan M. El-Gowelli; Nazik Elgindy
      Abstract: Publication date: Available online 17 October 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Wael Samy, Ayman Elnoby, Hanan M. El-Gowelli, Nazik Elgindy
      Purpose Desvenlafaxine succinate (DSV) is a water soluble anti-depressant drug, which is rapidly absorbed after oral administration exaggerating its side effects. The current work aims to prepare controllable release DSV matrix to reduce DSV side effects related to its initial burst. Methods Fifteen DSV matrix formulations were prepared using different polymers, polymer/drug ratios and matrix excipients and characterized using Differential Scanning Calorimetry (DSC), infra-red (IR) spectroscopy, water uptake and in-vitro DSV release. The release kinetics were calculated to determine the drug release mechanism. Ex-vivo DSV absorption via rat intestinal mucosal cells and the calculation of the apparent permeability coefficient (Papp) were performed using everted sac technique. Results Maltodextrin was the best matrix excipient (F7 and F10) showing acceptable decrease in the initial burst compared to the innovator. The addition of negatively charged polymers sodium carboxy methyl cellulose (SCMC) or sodium alginate resulted in an interaction that was proved by DSC and IR findings. This interaction slowed DSV release. F10 showed an excellent absorption of more than 80% of DSV after 4 hours and the highest similarity factor with the innovator (84.7). Conclusion A controllable release pattern of DSV was achieved using Methocel, Maltodextrin and SCMC. The obtained results could be used as a platform to control the release of cationic water soluble drugs that suffer from side effects associated with their initial burst after oral administration.

      PubDate: 2016-10-31T07:36:09Z
      DOI: 10.1016/j.jsps.2016.10.005
       
  • Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic
           delivery of diclofenac

    • Authors: Ehab Mostafa Elzayat; Ali Abdelzaher Abdel-Rahman; Sayed Mohamed Ahmed; Fars Kaed Alanazi; Walid Abdulazim Habib; Hisham Suliman Abou-Auda; Adel Sakr
      Abstract: Publication date: Available online 17 October 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Ehab Mostafa Elzayat, Ali Abdelzaher Abdel-Rahman, Sayed Mohamed Ahmed, Fars Kaed Alanazi, Walid Abdulazim Habib, Hisham Suliman Abou-Auda, Adel Sakr
      The rapid availability of the drug at the site of action followed by maintaining its effect for a long period of time is of great clinical importance. Thus, the purpose of the present study was to prepare and evaluate multi-layered matrix tablets of diclofenac using Eudragit RL/RS blend to achieve both immediate and sustained therapeutic effects. Diclofenac potassium (25mg) was incorporated in an outer immediate release layer to provide immediate pain relief whereas; diclofenac sodium (75mg) was incorporated in the inner core to provide extended drug release. Wet granulation was employed to prepare the inner core of the tablets which were further layered with an immediate release drug layer in the perforated pan coater. The in-vitro and in-vivo performance of the developed formulation were compared with the marketed products Voltaren® SR 75mg and Cataflam® 25mg. The in-vitro drug release of the prepared formulation showed similarity (f2 = 66.19) to the marketed product. The pharmacokinetic study showed no significant difference (p>0.05) in AUC0-24 and Cmax between the test and reference formulations. The AUC0-24 values were 105.36±83.3 and 92.87±55.53 μg.h/ml whereas; the Cmax values were 11.25±6.87 and 12.97±8.45 μg/ml, for the test and reference, respectively. The multi-layered tablets proved to be bioequivalent with the commercially available tablets and in agreement with the observed in-vitro drug release results. Stable physical characteristics and drug release profiles were observed in both long term and accelerated conditions stability studies.

      PubDate: 2016-10-31T07:36:09Z
      DOI: 10.1016/j.jsps.2016.10.004
       
  • Prophylactic and Curative Anti-ulcerogenic activity and the possible
           mechanisms of action of some desert plants

    • Authors: Reham M. El-Meligy; Amani S. Awaad; Gamal A. Soliman; Sanaa A. Kenawy; Saleh I. Alqasoumi
      Abstract: Publication date: Available online 19 October 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Reham M. El-Meligy, Amani S. Awaad, Gamal A. Soliman, Sanaa A. Kenawy, Saleh I. Alqasoumi
      The present study was aimed to evaluate the anti-ulcerogenic activities and the possible mechanisms of action of seven desert plants from different families. Conyza dioscoridis (L.) Desf. (Asteraceae), Euphorbia hirta L. (Euphorpiaceae), Origanum syriacum L., Salvia lanigera L. (Lamiaceae), Sisymbrium irio L., Solanum nigrum Linn. (Solanaceae) and Solenostemma arghel (Del.) Hayne. (Asclepiadaceae), were tested using prophylactic and curative models of absolute ethanol-induced ulcer, at three doses (125, 250 & 500 mg/kg) of each extract. The investigated extracts possessed dose dependent anti-ulcerogenic activities in both models, with LD50 higher than 5 g/kg. The most effective extracts were C. dioscoridis and S. irio with percent protection of control ulcer; 91.1% and 85.4% respectively. The antisecretory activity of both C. dioscoridis and S. irio appears to be mainly related to the suppression of gastrin release. The in-vitro potential radical (DPPH) scavenging activities of the investigated extracts were well supported with the reduction in gastric MDA (50.6% and 43.3%) and enhancing the level of reduced GSH (2.84, 2.59 mg/g tissue) for C. dioscoridis and S. irio respectively. In addition, suppression of the inflammatory mediator TNF-α may be one of the possible mechanisms of action. The alcohol extracts of C. dioscoridis and S. irio showed no alteration on liver and kidney functions. Phytochemical screening of the investigated extracts revealed the presence of flavonoids, tannins and sterols which could be related to the activities.

      PubDate: 2016-10-31T07:36:09Z
      DOI: 10.1016/j.jsps.2016.10.008
       
  • The Prevalence Extent of Complementary and Alternative Medicine (CAM) Use
           Among Saudis

    • Authors: Norah A Alrowais; Nada A Alyousefi
      Abstract: Publication date: Available online 1 October 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Norah A Alrowais, Nada A Alyousefi
      INTRODUCTION There is worldwide interest in the use of CAM. StudyingCAM in Saudipopulation is important as it will reflect the influence of psychosocial, cultural and religious factors on health beliefs and behaviors. The objective of this study is to present an updated review on the use of CAM practices in Saudi Arabia including commonly used types, common conditions for which it has been used and who uses CAM. METHODS This review used data from national surveys conducted in Saudi Arabia and published between 2000 and 2015. The literature search was performed considering standards adopted such as Moose guidelines for observational studies. Two authors independently reviewed each article. The search yielded 73 articles, and a total of 36 articles were included. Further careful data extraction was carried out by two independents reviewers. RESULTS Most of the reviewed studies were cross-sectional in design and were published between 2014 and 2015, and mostly in Riyadh region. Substantial difference in the findings for the patterns of CAM use was revealed. The most commonly employed practice was of spiritual type such as prayer, reciting Quran alone or on water. Other types include: herbs (8-76%), honey (14-73%) and dietary products (6-82%). Cupping (Alhijamah) was least used (4-45%). Acupuncture was more practiced among professionals. CONCLUSION The utilization of CAM is widely practiced in Saudi Arabia. There is need for efforts to promote research in the field of CAM to address each practice individually. Population surveys should be encouraged supported by mass media to raise knowledge and awarness about the practice of different CAM modalities. The national center of CAM should play a major role in these efforts.

      PubDate: 2016-10-04T17:23:34Z
      DOI: 10.1016/j.jsps.2016.09.009
       
  • Volatile constituents and biological activities of the leaf and root of
           Echinacea species from South Africa

    • Authors: M. Nyalambisa; I.A. Oyemitan; R. Matewu; O.O. Oyedeji; O.S. Oluwafemi; S.P. Songca; B.N. Nkeh-Chungag; A.O. Oyedeji
      Abstract: Publication date: Available online 30 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): M. Nyalambisa, I.A. Oyemitan, R. Matewu, O.O. Oyedeji, O.S. Oluwafemi, S.P. Songca, B.N. Nkeh-Chungag, A.O. Oyedeji
      Echinacea is used ethnomedicinally for the treatment of various diseases such as coughs, respiratory infections, bronchitis among other uses in Eastern Cape region of South Africa. This study evaluated the volatile components of the essential oil of the plant, its toxicity, anti-inflammatory and analgesic activities in rodents. Dried leaf and root of the plant were separately processed by hydrodistillation for 4 h and their essential oils ((EOs) collected. Extracted oils were subjected to GC/GC-MS analysis. The essential oil was further evaluated for acute toxicity, anti-inflammatory and analgesic activities. The toxicity profile of the essential oil was evaluated in mice through the oral route (p.o.), anti-inflammatory activity was evaluated on the carrageenan-induced edema model in rats at the doses of 100-200 mg/kg, while its analgesic effect was evaluated on the acetic acid-induced writhings model in mice at doses of 100-200 mg/kg. GC/GC-MS analysis of EOs showed that the number of compounds identified in the leaf and root oils were 25 and 31 for respectively. The chemical compositions of the oils varied and the major compounds identified in the oils include germacrene D, naphthalene, caryophyllene oxide, α-phellandrene and α-cadinol. The essential root oil did not cause mortality at the highest dose of 5000 mg/kg, hence its LD50 was estimated to be ⩾ 5000 mg/kg, p.o. The anti-inflammatory test results showed that the essential root oil caused significant (P < 0.05-0.01) reduction in oedema size compared to the negative control group on the carrageenan-induced oedema and the results for the analgesic test showed that the essential root oil caused significant (p < 0.05) reduction in number of writhings at 1000 mg/kg compared to the negative control group. It is concluded that root and leaf of this Echinacea species contain volatile oils which varied in their yield and chemical compositions. The essential root oil is non-toxic orally and it demonstrated significant anti-inflammatory and analgesic activities in laboratory animals.

      PubDate: 2016-10-04T17:23:34Z
      DOI: 10.1016/j.jsps.2016.09.010
       
  • The impact of formulation attributes and process parameters on black seed
           oil loaded liposomes and their performance in animal models of analgesia

    • Authors: Zerin T. Rushmi; Nasrin Akter; Rabeya J. Mow; Merina Afroz; Mohsin Kazi; Marcel de Matas; Mahbubur Rahman; Mohammad H. Shariare
      Abstract: Publication date: Available online 1 October 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Zerin T. Rushmi, Nasrin Akter, Rabeya J. Mow, Merina Afroz, Mohsin Kazi, Marcel de Matas, Mahbubur Rahman, Mohammad H. Shariare
      This study aimed to formulate black seed oil (Nigella sativa) loaded liposomes using the ethanol injection method to enhance oral bioavailability and improve therapeutic activity in small animal studies of analgesia. The impact of formulation attributes and process parameters on the liposomal system was evaluated with key quality attributes being particle size, morphology, and entrapment efficiency. The particle size and entrapment efficiency of the liposome preparation was found to be between the range of 50 - 900 nm and 34% to 87% respectively. Particle size distribution data suggested that increasing the percentage of oil, up to a certain concentration, reduced the size of the liposomes significantly from 520±81.2nm to 51.48 ± 1.31nm. Stirring and injection rate were shown to have marked impact on the average particle size of liposome. It was observed that entrapment efficiency of liposomes was greatly influenced by the amount of cholesterol and type of cryoprotectant used during formulation. The stability study indicated that the liposomal preparation was stable at ambient conditions for one month. In vivo studies showed that the liposomal preparation demonstrated significant analgesic activity in mice.
      Graphical abstract image

      PubDate: 2016-10-04T17:23:34Z
      DOI: 10.1016/j.jsps.2016.09.011
       
  • High-performance thin-layer chromatography based concurrent estimation of
           biomarkers ent-phyllanthidine and rutin in the dried aerial parts of
           Flueggea virosa

    • Authors: Nasir A. Siddiqui; Ramzi A. Mothana; Adnan J. Al-Rehaily; Perwez Alam; Mohammed Yusuf; Sarfaraz Ahmad; Abdulrahman Alatar
      Abstract: Publication date: Available online 30 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Nasir A. Siddiqui, Ramzi A. Mothana, Adnan J. Al-Rehaily, Perwez Alam, Mohammed Yusuf, Sarfaraz Ahmad, Abdulrahman Alatar
      The biomarkers are needed to be defined for standardization purposes so that safe and effective herbal formulations can be catered to the society. There is an urgent need for statistical support of herbal drugs because most of the herbal products are still used in the non- standardized form. This study is based on the development of a simple and sensitive RP-HPTLC method for concurrent estimation of two biomarkers ent-phyllanthidine and rutin in the methanol extract of aerial parts of Flueggea virosa. The developed method was found to be simple and sensitive. Separation and quantification were performed with acetonitrile: water (4:6 v/v) used as the mobile phase on glass-backed RP-HPTLC plate. Detection of absorption maxima and quantification was done at 310nm of UV region. The developed chromatographic system was found to give a sharp band for ent-phyllanthidine and rutin at Rf 0.73±0.01 and 0.68±0.01, respectively. The linearity ranges for ent- phyllanthidine, and rutin were found to be 200-1600ngband-1 and 100- 1400ngband-1, respectively with correlation coefficients (r2 values) of 0.998 and 0.997, respectively. The percentage of ent-phyllanthidine and rutin was found to be 9.121±0.02% and 1.018±0.04% (w/w), respectively. The resolution of bands and separation of constituents in FVME exhibited the perfect optimization of the developed method. The validation statistics supports the proposed method for standardizing crude drugs as well as formulations of a natural product containing ent-phyllanthidine and rutin.

      PubDate: 2016-10-04T17:23:34Z
      DOI: 10.1016/j.jsps.2016.09.006
       
  • Plant growth and diosgenin enhancement effect of silver nanoparticles in
           Fenugreek (Trigonella foenum-graecum L.)

    • Authors: B. Jasim; Roshmi Thomas; Jyothis Mathew; E.K. Radhakrishnan
      Abstract: Publication date: Available online 30 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): B. Jasim, Roshmi Thomas, Jyothis Mathew, E.K. Radhakrishnan
      Various methods have been used to enhance production of chemically diverse phyto-chemicals especially medicinal natural products. With the advancement in nanotechnology, nanoparticles have been reported to have varying impact in plant growth and inducibility of phyto-chemical composition. Major objective of the study was to study the secondary metabolite modulatory effect of silver nanoparticles. In the current study, fenugreek seedlings when treated with biosynthesized silver nanoparticles (Ag-NPs) was found to have significant impact on its growth parameters like leaf number, root length, shoot length and wet weight. On HPLC based analysis, Ag-NPs treated seedlings showed an enhancement in the production of major phyto-chemical diosgenin to a level of 214.06±17.07 μg/mL. An untreated control gave an yield of only 164.44±7.67 μg/mL of diosgenin, the observed phyto-chemical enhancement effect induced by Ag-NP is very significant. Most remarkably, the Ag-NP used in the study was found to play dual role of enhancement of both plant growth and diosgenin synthesis. Hence the study is of immense application as it open up development of new methods based on nanoelicitors to enhance the biosynthesis of medicinal natural products in plants.

      PubDate: 2016-10-04T17:23:34Z
      DOI: 10.1016/j.jsps.2016.09.012
       
  • Investigation of the in vitro performance difference of drug-Soluplus®
           and drug-PEG 6000 dispersions when prepared using spray drying or
           lyophilization

    • Authors: Mohammad A. Altamimi; Steven H. Neau
      Abstract: Publication date: Available online 30 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Mohammad A. Altamimi, Steven H. Neau
      Purpose To evaluate the physicochemical and in vitro characteristics of solid dispersions using BCS II model drugs with Soluplus® and one of its component homopolymers, PEG 6000. Methods Nifedipine (NIF) and sulfamethoxazole (SMX) of 99.3 and 99.5% purity, respectively, were selected as BCS II model drugs, such that an improved dissolution rate and concentration in the gastrointestinal tract should increase oral bioavailability. Soluplus® is an amorphous, tri-block, graft co-polymer with polyvinyl caprolactam, polyvinyl acetate, and polyethylene glycol (PCL:PVAc:PEG6000) in the ratio 57:30:13. PEG 6000 (BASF) is a waxy material with melting point of about 60 °C. Solid dispersions were prepared using lyophilization or spray drying techniques. Dissolution study, crystallinity content, and analysis for new chemical bond formation have been used to evaluate the dispersed martials. Results Although each polymer improved the drug dissolution rate, dissolution from Soluplus® was slower. Enhanced dissolution rates were observed with NIF solid dispersions, but the dissolution profiles were quite different due to the selected technique, polymer, and dissolution medium. For SMX, there was similarity across the dissolution profiles despite the medium, polymer, or applied technique. Each polymer was able to maintain an elevated drug concentration over the three hour duration of the dissolution profile, i.e., supersaturation was supported by the polymer. DSC thermograms revealed no melting endotherm, suggesting that the drug is amorphous or molecularly dispersed. Conclusion NIF and SMX solid dispersions were successfully prepared by spray drying and lyophilization using Soluplus® or PEG 6000. Each polymer enhanced the drug dissolution rate; NIF dissolution rate was improved to a greater extent. Dispersions with PEG 6000 had a faster dissolution rate due to its hydrophilic nature. DSC analysis showed that no crystalline material exists in the dispersions.

      PubDate: 2016-10-04T17:23:34Z
      DOI: 10.1016/j.jsps.2016.09.013
       
  • Pharmacovigilance System in Saudi Arabia

    • Authors: Thamir M. Alshammari; Mohammed Alshakka; Hisham Aljadhey
      Abstract: Publication date: Available online 30 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Thamir M. Alshammari, Mohammed Alshakka, Hisham Aljadhey
      Pharmacovigilance plays an important role in ensuring that patients are receiving safe drugs In Saudi Arabia, Saudi Food and Drug Authority, health institutions, marketing authorization holders and healthcare professional are involved in pharmacovigilance activities regardless to the level of the involvement. Although pharmacovigilance is well established in developed nations, it is considered a new concept in Saudi Arabia. It is a collective effort from various stakeholders to make pharmacovigilance successful towards promoting safe and effective use of medicines among the population. However, the practice of pharmacovigilance still needs more attention especially from marketing authorization holders and healthcare professionals. The aim of this review is to describe the current situation of pharmacovigilance in Saudi Arabia and the activities that have been conducted by the stakeholders.

      PubDate: 2016-10-04T17:23:34Z
      DOI: 10.1016/j.jsps.2016.09.008
       
  • Enantioselective analysis of fluoxetine in pharmaceutical formulations by
           capillary zone electrophoresis

    • Authors: Melania Cârcu-Dobrin; Monica Budău; Gabriel Hancu; Laszlo Gagyi; Aura Rusu; Hajnal Kelemen
      Abstract: Publication date: Available online 30 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Melania Cârcu-Dobrin, Monica Budău, Gabriel Hancu, Laszlo Gagyi, Aura Rusu, Hajnal Kelemen
      Fluoxetine is an antidepressant, a selective serotonin reuptake inhibitor (SSRI) used primarily in the treatment of major depression, panic disorder and obsessive compulsive disorder. Chiral separation of racemic fluoxetine is necessary due to its enantioseletive metabolism. In order to develop a suitable method for chiral separation of fluoxetine, cyclodextrin (CD) modified capillary electrophoresis (CE) was employed. A large number of native and derivatized, neutral and ionized CD derivatives were screened to find the optimal chiral selector. As a result of this process, heptakis(2,3,6-tri-O-methyl)-β-CD (TRIMEB) was selected for enantiomeric discrimination. A factorial analysis study was performed by orthogonal experimental design in which several factors are varied at the same time to optimize the separation method. The optimized method (50 mM phosphate buffer, pH = 5.0, 10 mM TRIMEB, 15 °C, + 20 kV, 50 mbar/1 second, detection at 230 nm) was successful for baseline separation of fluoxetine enantiomers within 5 minutes. Our method was validated according to ICH guidelines and proved to be sensitive, linear, accurate and precise for the chiral separation of fluoxetine.

      PubDate: 2016-10-04T17:23:34Z
      DOI: 10.1016/j.jsps.2016.09.007
       
  • Effect of nitazoxanide on albendazole pharmacokinetics in cerebrospinal
           fluid and plasma in rats

    • Authors: Ruiz-Olmedo María Isabel; González-Hernández Iliana; Palomares-Alonso Francisca; Franco-Pérez Javier; González F María de Lourdes; Jung-Cook Helgi
      Abstract: Publication date: Available online 30 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Ruiz-Olmedo María Isabel, González-Hernández Iliana, Palomares-Alonso Francisca, Franco-Pérez Javier, González F María de Lourdes, Jung-Cook Helgi
      Background Although albendazole is the drug-of-choice for the treatment of neurocysticercosis, its efficacy is limited due to its low bioavailability. An alternative for optimizing pharmacological treatment is through drug combinations. In vitro studies have shown that nitazoxanide and tizoxanide (the active metabolite of nitazoxanide) exhibit cysticidal activity and that the combination of tizoxanide with albendazole sulfoxide (the active metabolite of albendazole) produced an additive effect. Objectives 1) To assess the concentration profile of tizoxanide in plasma and in cerebrospinal fluid; 2) to evaluate the influence of nitazoxanide on the pharmacokinetics of albendazole in plasma and in cerebrospinal fluid. Methods Two different studies were conducted. In study 1, 10 male Sprague-Dawley rats received a single oral dose of 7.5 mg/kg of nitazoxanide and serial blood and cerebrospinal fluid samples were collected over a period of 4 h. In study 2, 38 healthy male Sprague-Dawley rats were randomly divided into two groups: one of these received a single dose of albendazole (15 mg/kg) and, in the other group, albendazole (15 mg/kg) was co-administered with nitazoxanide (7.5 mg/kg). Plasma and cerebrospinal fluid samples were collected from 0–16 h after administration. Albendazole sulfoxide and tizoxanide levels were assayed by using HPLC or LC/MS techniques. Results In study 1, tizoxanide reached a maximum plasma concentration of 244.42 ± 31.98 ng/mL at 0.25 h; however, in cerebrospinal fluid, this could be detected only at 0.5 h, and levels were below the quantification limit (10 ng/mL). These data indicate low permeation of tizoxanide into the blood brain barrier. In study 2, Cmax, the area under the curve, and the mean residence time of albendazole sulfoxide in plasma and cerebrospinal fluid were not affected by co-administration with nitazoxanide. Conclusion The results of the present study indicate that in rats at the applied doses, tizoxanide does not permeate into the cerebrospinal fluid. Furthermore, nitazoxanide does not appear to alter significantly the pharmacokinetics of albendazole in plasma or in cerebrospinal fluid.

      PubDate: 2016-10-04T17:23:34Z
      DOI: 10.1016/j.jsps.2016.09.005
       
  • CYP2C9, CYPC19 and CYP2D6 Gene Profiles and Gene Susceptibility to Drug
           Response and Toxicity in Turkish Population

    • Authors: Merve Arici; Gül Özhan
      Abstract: Publication date: Available online 17 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): ARICI Merve, ÖZHAN Gül
      Pharmacogenetics is a vast field covering drug discovery research, the genetic basis of pharmacokinetics and dynamics, genetic testing and clinical management in diseases. Pharmacogenetic approach usually focuses on variations of drug transporters, drug targets, drug metabolizing enzymes and other biomarker genes. Cytochrome P450 (CYP) enzymes, an essential source of variability in drug-response, play role not only phase I-dependent metabolism of xenobiotics but also metabolism of endogenous compounds such as steroids, vitamins and fatty acids. CYP2C9, CYP2C19 and CYP2D6 enzymes being highly polymorphic are responsible for metabolism of a variety of drug groups. In the study, it was determined the genotype and allele frequency of CYP2C9∗2, CYP2C19∗3, CYP2C19∗2, CYP2C19∗3, CYP2C19∗17, CYP2D6∗9 and CYP2D6∗41, very common and functional single-nucleotide polymorphisms (SNPs), in healthy volunteers. The genotype distributions were consistent with the Hardy-Weinberg equilibrium in the population (p>0.05). It is believed that the determination of polymorphisms in the enzymes may be beneficial in order to prevention or reduction of adverse effects and death.The recessive allele frequencies of CYP2C9∗2, CYP2C19∗3, CYP2C19∗2, CYP2C19∗3, CYP2C19∗17, CYP2D6∗9 and CYP2D6∗41 were 11, 13, 12, 13, 25, 4 and 15%, respectively. According to the obtained results, the carriers of CYP2D6∗9 variant allele should be received higher doses of the drugs metabolizing with this enzyme in Turkish population, while the carriers of other variant alleles do not generally have any requirement of dose regimen.

      PubDate: 2016-09-19T15:43:29Z
      DOI: 10.1016/j.jsps.2016.09.003
       
  • Utilization of Gel Electrophoreses for the Quantitative Estimation of
           Digestive Enzyme Papain

    • Authors: Magdy M. Muharram; Maged S. Abdel-Kader
      Abstract: Publication date: Available online 14 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Magdy M. Muharram, Maged S. Abdel-Kader
      SDS-PAGE densitometric method for analysis of papain in Pharmaceutical formulations was developed and validated for the first time. Standard and samples were mixed with SDS sample buffer and denatured at 95˚C for 5 minutes and the gel was run at 20mA and 200V for 30-40 minutes in SDS-PAGE buffer. Gels were stained in Coomassie blue solution and distained by 5% methanol and 10% acetic acid. Distained gels were imaged and analyzed using the ChemiDoc™ XRS+ System. Bands of papain appeared at R f value 0.78 ± 0.03 corresponding to molecular weight 23406 Da between proteins with molecular weight 31000 and 21500 Da of the broad range protein standard. The generated calibration curve was used for quantitative estimation of papain in pharmaceutical formulations. The developed method was validated for precision, accuracy, specificity and robustness as described by the ICH guidelines. The proposed method gives an alternative approach for enzymes and proteins analysis.

      PubDate: 2016-09-19T15:43:29Z
      DOI: 10.1016/j.jsps.2016.09.002
       
  • Effect of Aster tataricus on production of inflammatory mediators in LPS
           stimulated rat astrocytoma cell line (C6) and THP-1 cells

    • Authors: Hong-tao Zhang; Miao Tian; Qiao-wei He; Nan Chi; Chun-ming Xiu; Yun-bo Wang
      Abstract: Publication date: Available online 14 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Hong-tao Zhang, Miao Tian, Qiao-wei He, Nan Chi, Chun-ming Xiu, Yun-bo Wang
      Neuroinflamation is the commonest cause of neurodegenerative diseases such as Alzheimers disease. Present investigation evaluates the inhibitory effect of ethanolic root extract of Aster tataricus (AS) on inflammatory mediators production in lipopolysaccharide (LPS) stimulated C6 cells. C6 cells were treated with AS (20 and 40 mg/kg) and nimesulide (NSL, 1.5 μg/ml) for 1 day. Thereafter various parameters such production of ROS, release of nitrite, MDA, glutathione level and NF-κB translocation were estimated in C6 cell lines. Effect of AS was estimated on the expressions of tumor necrosis factor α (TNF-α) of human monocytic leukemia cell line (THP-1). It was observed that AS (20 and 40 mg/ml) treated group shows significant (p<0.01) decrease in production of ROS, Nitrite release and MDA level in LPS activated C6 cell lines compared to negative control group. Moreover, treatment with it decreases glutathione level and inhibits the translocation of NF-κB in LPS activated C6 cell lines compared to negative control group. There were significant (p<0.01) decrease in expression of TNF-α in AS treated group compared to negative control group in THP-1 cell lines. Present investigation concludes the anti neuroinflammatory effect of ethanolic extract of AS root by decreasing oxidative stress and attenuates the cytokine.

      PubDate: 2016-09-19T15:43:29Z
      DOI: 10.1016/j.jsps.2016.09.001
       
  • Comparison of physicochemical properties of suppositories containing
           starch hydrolysates

    • Authors: Piotr Belniak; Katarzyna Świąder; Michał Szumiło; Aleksandra Hyla; Ewa Poleszak
      Abstract: Publication date: Available online 17 September 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Piotr Belniak, Katarzyna Świąder, Michał Szumiło, Aleksandra Hyla, Ewa Poleszak
      The purpose of this work was to determine the effect of starch hydrolysates (SH) on the physicochemical properties of suppositories. The study was conducted with suppositories with acetaminophen (AAP) a typical antipyretic analgesic, as model drug on lipophilic (cocoa butter) and hydrophilic base (polyethylene glycol 1500+400). The suppositories with and without the addition of SH were examined for physicochemical tests according to European Pharmacopoeia 8th edition (Ph. Eur.): the uniformity of mass of single-dose preparation test, the softening time determination of lipophilic suppositories test, the disintegration of suppositories test, and dissolution test with flow-through apparatus. The results confirm the possibility of using starch hydrolysates as a cheap and safe addition to modify physicochemical properties of suppositories.

      PubDate: 2016-09-19T15:43:29Z
      DOI: 10.1016/j.jsps.2016.09.004
       
 
 
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