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  Subjects -> PHARMACY AND PHARMACOLOGY (Total: 557 journals)
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Journal Cover Saudi Pharmaceutical Journal
  [SJR: 0.417]   [H-I: 14]   [0 followers]  Follow
    
  This is an Open Access Journal Open Access journal
   ISSN (Print) 1319-0164
   Published by Elsevier Homepage  [2970 journals]
  • New acyclic secondary metabolites from the biologically active fraction of
           Albizia lebbeck Flowers

    • Abstract: Publication date: Available online 24 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Shaza M. Al-Massarani, Ali A. El Gamal, Mohamed Farag, Mansour S. Al-Said, Maged S. Abdel-Kader, Omer A. Basudan, Saleh I. Alqasoumi
      The total extract of Albizia lebbeck flowers was examined in vivo for its possible hepatoprotective activity in comparison with the standard drug silymarin at two doses. The higher dose expressed promising activity especially in reducing the levels of AST, ALT and bilirubin. Fractionation via liquid- liquid partition and reexamination of the fractions revealed that the n-butanol fraction was the best in improving liver biochemical parameters followed by the n-hexane fraction. However, serum lipid parameters were best improved with CHCl3 fraction. The promising biological activity results initiated an intensive chromatographic purification of Albizia lebbeck flowers fractions. Two compounds, identified from natural source for the first time, the acyclic farnesyl sesquiterpene glycoside1-O-[6-O-α-L- arabinopyranosyl-β-D-glucopyranoside]–(2E,6E-) -farnesol (6) and the squalene derivative2,3-dihydroxy-2,3-dihydrosqualene (9), in addition to eight compounds reported here for the first time from the genus Albizia; two benzyl glycosides, benzyl 1-O-β-D- glucopyranoside (1) and benzyl 6-O-α-L-arabinopyranosyl β-D-glucopyranoside (2); three acyclic monoterpene glycosides, linalyl β- D- glucopyranoside (3) and linalyl 6-O-α-L-arabinopyranosyl -β-D-glucopyranoside (4); 2E)-3,7-dimethylocta-2,6-dienoate-6-O-α-L arabinopyranosyl-β-D-glucopyranoside (5), two oligoglycosides, n- hexyl-α-L arabinopyranosyl-(1→6)-β-D-glucopyranoside (creoside) (7) and n-octyl α-L- arabinopyranosyl-(1→6)-β-D-glucopyranoside (rhodiooctanoside) (8); and ethyl fructofuranoside (10). The structures of the isolated compounds were elucidated based on extensive examination of their spectroscopic 1D and 2D-NMR, MS, UV, and IR data. It is worth mentioning that, some of the isolated linalol glycoside derivatives were reported as aroma precursors.


      PubDate: 2016-05-25T07:14:48Z
       
  • Editorial Board

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3




      PubDate: 2016-05-25T07:14:48Z
       
  • Bioactivity and chemical characterization of Acalypha fruticosa Forssk.
           growing in Saudi Arabia

    • Abstract: Publication date: Available online 24 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Ghada Ahmed Fawzy, Areej Mohammad Al-Taweel, Shagufta Perveen, Shabana Iqrar Khan, Fatma Abdulaziz Al-Omary
      Acalypha is an important genus of the Euphorbiaceae family. The genus is represented by five species in Saudi Arabia. Acalypha fruticosa Forssk. Fl. Aeg is traditionally used as a cure for stomachache, dyspepsia, rheumatism, dermatitis, and swellings of the body. The present study endeavors to provide a phytochemical and biological evaluation of the plant, with the aim of relating activity to constituting secondary metabolites in the plant. Column chromatographic separation of the methanol extract led to the isolation of four compounds namely; 2-methyl-5,7-dihydroxychromone 5-O-β-D-glucopyranoside 1, acalyphin 2, apigenin 3 and kaempferol 3-O-rutinoside 4. The plant extracts and the isolated compounds were subjected to biological assays to screen peroxisome proliferator-activated receptor alpha (PPARα) and PPARγ agonistic, anti-inflammatory and cytotoxic activities. Results proved for the first time, the PPARγ activator effect of acalyphin, as well as its promising anti-inflammatory activity, in addition to the dual PPAR activator effect of the chromone glucoside. The plant extracts and isolated compounds were non-cytotoxic to the tested cell lines. Thus A. fruticosa could be a valuable source of important therapeutics that may hold clinical prospect.


      PubDate: 2016-05-25T07:14:48Z
       
  • Acute toxicity profiling of the ethyl acetate fraction of Swietenia
           macrophylla seeds and in-vitro neuroprotection studies

    • Abstract: Publication date: Available online 7 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Mustak Sayyad, Tiang Ning, Yatinesh Kumari, Goh Beh Hing, Yogini Jaiswal, Rozita Rosli, Leonard Williams, Mohd. Farooq Shaikh
      Swietenia macrophylla (SM) is a medicinally important plant found in tropical and subtropical regions of the world. The ethyl acetate fraction of the seeds of Swietenia macrophylla (SMEAF) is reported to exhibit potent anticancer, antitumor, anti-inflammatory and antifeedant activities. Till date, there have been no studies reported on the acute oral toxicity profile of the ethyl acetate fraction of the seeds of SM. The objective of the present study was to determine the acute toxicity of SMEAF and evaluate the in-vitro neuroprotective activity of SMEAF using primary neuronal cell cultures. In acute oral toxicity study, the SMEAF did not produce any lethal signs of morbidity and mortality. Histo-pathological findings, support the safety of SMEAF, as there were no significant changes observed in any of the parameters studied. Based on the results obtained in MTT assay, we infer that SMEAF has a significant neuroprotective effect, as it increased the cell viability and exhibited protection to the neuronal cells against TBHP induced oxidative stress. Thus, SMEAF can be suggested for use in the development of herbal drug formulations with neuroprotective potential.


      PubDate: 2016-05-13T13:43:32Z
       
  • Compatibility study of paracetamol, chlorpheniramine maleate and
           phenylephrine hydrochloride in physical mixtures

    • Abstract: Publication date: Available online 7 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): G.G.G. de Oliveira, A. Feitosa, K. Loureiro, A.R. Fernandes, E.B. Souto, P. Severino
      Paracetamol (PAR), phenylephrine hydrochloride (PHE) and chlorpheniramine maleate (CPM) are commonly used in clinical practice as antipyretic and analgesic drugs to ameliorate pain and fever in cold and flu conditions. The present work describes the use of thermal analysis for the characterization of the physicochemical compatibility between drugs and excipients during the development of solid dosage forms. Thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC) were used to study the thermal stability of the drug and of the physical mixture (drug/excipients) in solid binary mixtures (1:1). DSC thermograms demonstrated reproducible melting event of the prepared physical mixture. Starch, mannitol, lactose and magnesium stearate influence thermal parameters. Information recorded from the derivative thermogravimetric (DTG) and TGA curves demonstrated the decomposition of drugs in well-defined thermal events, translating the suitability of these techniques for the characterization of the drug/excipients interactions.


      PubDate: 2016-05-13T13:43:32Z
       
  • Preparation and evaluation of rotigotine-loaded implant for the treatment
           of Parkinson’s disease and its evolution study

    • Abstract: Publication date: Available online 5 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Aiping Wang, Yanxiang Liu, Rongcai Liang, Xuemei Zhang, Kaoxiang Sun, Zimei Wu, Wanhui Liu
      Purpose To develop rotigotine-loaded implants (RI) to achieve continuous release of rotigotine for long duration for the treatment of Parkinson’s disease (PD). Methods RI was prepared by hot-melt extrusion method using poly (lactide-co-glycoside) (PLGA) as the matrix. In vitro drug release was optimized by drug loading, melting temperature during preparing process and additives. The surface and internal morphology of RI was imaged by SEM. The in vivo release profile of RI was investigated on rat. Results RI prepared with PLGA 8515 4A showed sustained release of 40 days while suffering a lag phase, which was significantly shortened by blending 5050 2A and mannitol in the matrix. RI prepared by 8515 4A/5050 2A/mannitol = 55:10:5 (rotigotine 30%) showed a 40-day sustained release in vivo with no lag phase. The drug release from RI was also affected by drug loading and melting temperature probably due to the drug state existed in the implant. The evolution of implants during release process was correlated well with the drug release kinetics. Conclusion RI could achieve sustained drug release for 40 days which could supply an alternative of continuous dopamindergic stimulation (CDS) for the treatment of PD.


      PubDate: 2016-05-08T12:54:51Z
       
  • Natural cures for breast cancer treatment: A review

    • Abstract: Publication date: Available online 5 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Munazza Shareef, Muhammad Aqeel Ashraf, Maliha Sarfraz
      For centuries, herbs and plants have been used for medicinal purposes and as food as well. This review concern about different types of plants that retain the immune stimulating and anti-tumor properties. Large variety of active phytochemicals like carotenoids, flavonoids, ligands, polyphenolics, terpenoids, sulfides, lignans and plant sterols have been identified in different types of herbs. These phytochemicals have different mechanisms of action. They either stimulate the protective enzyme like glutathione transferase or prevent the cell proliferation. This review has centered on the biochemical properties of Allium sativum, Echinacea, Curcuma longa, Arctium lappa, Camellia sinensis, Panax ginseng and Flax seed. Extracts and juices of Withania somnifera, Amoora rohituka, Dysoxylum binectariferum and Vaccinium macrocarpon, respectively also used as anti-breast cancer. The volatile oils and extracts of these herbs and plants inhibit the synthesis of mevalonate that lessen the tumor growth and cholesterol synthesis.


      PubDate: 2016-05-08T12:54:51Z
       
  • Histatin peptides: Pharmacological functions and its applications in
           dentistry

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Zohaib Khurshid, Shariq Najeeb, Maria Mali, Syed Faraz Moin, Syed Qasim Raza, Sana Zohaib, Farshid Sefat, Muhammad Sohail Zafar
      There are many human oral antimicrobial peptides responsible for playing important roles including maintenance, repairing of oral tissues (hard or soft) and defense against oral microbes. In this review we have highlighted the biochemistry, physiology and proteomics of human oral histatin peptides, secreted from parotid and submandibular salivary glands in human. The significance of these peptides includes; capability for ionic binding that can kill fungal Candida albicans. They have histidine rich amino acids sequences (7-12 family members; corresponding to residues 12-24, 13-24, 12-25, 13-25, 5-11, and 5-12, respectively) for Histatin-3. However, Histatin-3 can be synthesised proteolytically from histatin 5 or 6. Due to their fungicidal response and high biocompatibility (little or no toxicity), these peptides can be considered as therapeutic agents with most probable applications for example, artificial saliva for denture wearers and salivary gland dysfunction conditions. The objectives of current article are to explore the human histatin peptides for its types, chemical and biological aspects. In addition, the potential for therapeutic bio-dental applications has been elaborated.


      PubDate: 2016-05-08T12:54:51Z
       
  • The Transport Mechanism of Monocarboxylate Transporter on Spinosin in
           Caco-2 Cells

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Xiang Le Meng, Yan Li Guo, Hai Yinghuang
      Objectives The aim of this study was to determine the uptake mechanism of spinosin (SPI) by the monocarboxylic acid transporters (MCTs) in Caco-2 cells. Methods The Caco-2 cells were pretreated with various monocarboxylic acids, and the uptake of spinosin from Caco-2 cells was measured by High Performance Liquid Chromatography (HPLC). Key findings Preloading of various monocarboxylic acids enhanced the uptake of SPI, especially salicylic acid (a substrate of MCTs) had a 23.4 times increase in SPI uptake, indicating that the monocarboxylic acid transporters had an efflux effect on SPI uptake and salicylic acid had a strong inhibition on SPI efflux in Caco-2 cells. At the same time, the uptake of SPI through Caco-2 cells was Na+- and temperature-dependent, pretreatment without Na+ significantly increased the uptake of SPI by 1.85 times and incubated at low temperature (4 °C) SPI uptake increased 20% than that of 37 °C. Furthermore, SPI was transported mainly via a carrier-mediated transport: [Vmax=5.364 μg/mg protein, Km=657.0 μg/mL]. Conclusion The uptake of spinosin (SPI) in Caco-2 cells was mainly regulated by the monocarboxylic acid transporters along with Salicylic acid.


      PubDate: 2016-05-08T12:54:51Z
       
  • Structure characteristics of self-bonding boards during hot press for
           leukemia inhibition

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Jiang Zhang, Zhi Lin
      The 80% leukemia were caused by indoor formaldehyde pollution. And the results shown that the absorbances of many connectionbonds (such as C-O-C, C-OOC, and so on) increased. It could be inferred that a lot of bonds were produced and played the role of molecularcrosslinking. After hot press, the content of lignin in Eucalyptus wood fiber were all lower than ones of self-bonding boards. And the change of content of lignin was closely related to time and temperature of hot press.


      PubDate: 2016-05-08T12:54:51Z
       
  • Biomechanical analysis of press-extension technique on degenerative lumbar
           with disc herniation and staggered facet joint

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Hong-gen Du, Sheng-hui Liao, Zhong Jiang, Huan-ming Huang, Xi-tao Ning, Neng-yi Jiang, Jian-wei Pei, Qin Huang, Hui Wei
      This study investigate the effect of a new Chinese massage technique named “press-extension” on degenerative lumbar with disc herniation and facet joint dislocation, and provide a biomechanical explanation of this massage technique. Self-developed biomechanical software used to establish a normal L1-S1 lumbar 3D FE model, which integrated the spine CT and MRI data-based anatomical structure. Then utilize graphics technique to build a degenerative lumbar FE model with disc herniation and facet joint dislocation. According to the actual press-extension experiments, mechanics parameters are collected to set boundary condition for FE analysis. The result demonstrated that press-extension techniques bring the annuli fibrosi obvious induction effect, make the central nucleus pulposus forward close, increasing the pressure in front part. Study conclude that finite element modeling for lumbar spine is suitable for the analysis of press-extension technique impact on lumbar intervertebral disc biomechanics, to provide the basis for the disease mechanism of intervertebral disc herniation using press-extension technique.


      PubDate: 2016-05-08T12:54:51Z
       
  • Treatment on Patients with Nueroglioma by Teniposide and Semustine and Its
           Influence on Twist and E-cadherin Expression

    • Abstract: Publication date: Available online 5 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Yongbo Zhang, Guoyi Liu, Meiling Lang, Jing Zhang, Jia Geng
      This study focus on curative effects of teniposide combining with semustine on patients with neuroglioma and the influences on the expression of Twist and E-cadherin in tissue. Sixty eight patients with neuroglioma taking operation in our hospital were divided into two groups randomly. Single radiotherapy was given to 34 patients in group A, and teniposide (VM-26) and semustine (Me-CCUN) were added to radiotherapy for 34 patients in group B. Then, curative effects, survival rate, living quality and adverse reaction rate after operation were compared between two groups. Moreover, the difference in positive expression rate of Twist and E-cadherin before and after treatment between two groups was analyzed by immunohistochemistry. Results: In group B, the effective rate of treatment was 88.2%, and the disease control rate was 70.6%, higher than 52.9% and 32.4% in group A with statistical significance (P<0.05). Moreover, the survival rate in three years of group B was 44.1%, and the score of living quality was 67.11±4.32, also higher than 23.5% and 63.79±4.53 in group A with statistical significance (P<0.05). However, the difference between two groups in adverse reaction rate has no statistical significance (P>0.05). In addition, the difference in positive expression rate of Twist and E-cadherin between group A and group B has no statistical significance before treatment (P>0.05). After treatment, however, the positive rate of Twist in group B is lower than that in group A, while the positive rate of E-cadherin is higher. Both differences have statistical significance (P<0.05). Chemotherapy of VM-26 combining with Me-CCNU can inhibit Twist expression and improve the expression rate of E-cadherin to help improving the curative effects and living quality and increasing survival rate.


      PubDate: 2016-05-08T12:54:51Z
       
  • Protective effect of Astragaloside IV against sepsis-induced acute lung
           injury in rats

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Ruiqin Huang, Min LI, Min Li
      The study aimed to explore the protective effects of AS-IV against sepsis-induced ALI. Sepsis was induced by cecal ligation and puncture (CLP) method in Sprageue Dawley rats. Rats were randomly assigned into five groups: animals undergoing a sham CLP (sham group); animals undergoing CLP (CLP group); animals undergoing CLP and treated with AS-IV at 2.5mg/kg.bw (low-dose AS-IV [L-AS] group), at 5mg/kg.bw (mid-dose AS-IV [M-AS] group), and at 10mg/kg.bw (high-dose AS-IV [H-AS] group). At 6 h, 12 h and 24 h post-CLP surgery, six rats were respectively sacrificed to collect blood and lung tissue samples. The levels of arterial blood gas index, lung water content, protein level and leukocyte counts (total amount, neutrophils and lymphotes) in bronchoalveolar lavage fluid (BALF) and cytokines such as TNF-α and IL-6 in BALF were measured at each time point in different groups. HE-staining and optical microscopy were performed to examine the pathologic changes in lungs. The 72 h-survival rate of each group was also recorded. PaO2 was decreased significantly, while the lung water content, BALF protein level, cell numbers, BALF cytokine TNF-α and IL-6 levels were increased significantly for CLP group as compared with sham group. Moreover, pathological injury was observed in lung tissue indicating the successful sepsis-induced ALI model. Speaking of the effect of AS-IV, we founded that, compared with the CLP group, the AS-IV treatment groups could significantly alleviate all the abovenegative changes exited in the CLP group in a dose-dependent manner. What’s more, the pathological injury was also gradually improved by AS-IV treatment compared with the CLP rats. AS-IV exerts its protective effect against sepsis-induced ALI in rats via improving pulmonary ventilation function, decreasing the permeability of alveolar epithelium and capillary as well as repressing lung inflammation.


      PubDate: 2016-05-08T12:54:51Z
       
  • New discovery of cryptorchidism: Decreased retinoic acid in testicle

    • Abstract: Publication date: Available online 5 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Jinpu Peng, Lianju Shen, Jinjun Chen, Xining Cao, Yue Zhou, Huali Weng, Chunlan Long, Deying Zhang, Shengfen Tu, Yan Zhang, Dawei He, Tao Lin, Guanghui Wei
      This study focus on investigatation of cryptorchidism induced by flutamide (Flu) and its histopathological damage, and detect retinoic acid concentration in testicle tissue, in order to find a new method for clinical treatment to infertility caused by cryptorchidism. Twenty SD (Sprague Dawley) pregnant rats were randomly divided into Flu cryptorchidism group (n=10) and normal control group (n=10). HE stained for observing morphological difference. TEM(transmission electron microscope) was used for observing the tight junction structure between Sertoli cells. Epididymal caudal sperms were counted and observed in morphology. The expression of stimulated by retinoic acid gene 8 (Stra8) was detected using immunohistochemistry, western blot, and Q-PCR. High performance liquid chromatography (HPLC) analysis was made on retinoic acid content. Sperm count and morphology observation confirmed cryptorchidism group was lower than normal group in sperm quantity and quality. The observation by TEM showed a loose structure of tight junctions between Sertoli cells. Immunohistochemistry, western blot, and Q-PCR showed that cryptorchidism group was significantly lower than normal group in the expression of Stra8. HPLC showed that retinoic acid content was significantly lower in cryptorchid testis than normal testis. In the cryptorchidism model, retinoic acid content in testicular tissue has a significant reduction; testicles have significant pathological changes; damage exists in the structure of tight junctions between Sertoli cells; Stra8 expression has a significant reduction, perhaps mainly contributing to spermatogenesis disorder.


      PubDate: 2016-05-08T12:54:51Z
       
  • The Pharmacological Potential of Rutin

    • Abstract: Publication date: Available online 30 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Aditya Ganeshpurkar, Ajay K. Saluja
      The contemporary scientific community has presently recognized flavonoids to be a unique class of therapeutic molecules due to their diverse therapeutic properties. Of these, rutin, also known as vitamin P or rutoside, has been explored for a number of pharmacological effects. Tea leaves apples, and many more possess rutin as one of the active constituents. Today, rutin has been observed for its nutraceutical effect. The present review highlights current information and health-promoting effects of rutin. Along with this, safety pharmacology issues and SAR of the same have also been discussed.


      PubDate: 2016-05-04T13:40:02Z
       
  • Identification and characterization of Endophytic filamentous fungi from a
           Catharanthus roseus

    • Abstract: Publication date: Available online 29 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Farah Wahida Ayob, Khanom Simarani
      This paper reported on the various filamentaous fungi strains that were isolated from a wild grown Catharanthus roseus. Based on the morphological characteristics and molecular technique through a Polymerase Chain Reaction and DNA sequencing method using internal transcribed spacer (ITS), these fungi had been identified as a Colletotrichum sp, Macrophomina phaseolina, Nigrospora sphaerica and Fusarium solani. The ultrastructures of spores and hyphae were observed under a Scanning Electron Microscope. The hydrolytic enzyme test showed that all strains were positive in secreting cellulase. Colletotrichum sp and Fusarium solani strains also gave a positive result for amylase while only Fusarium solani capable to secrete protease. These fungi were putatively classified as endophytic fungi since they produced extracellular enzymes that allow them to penetrate plants cell walls and colonized with symbiotic properties.


      PubDate: 2016-05-04T13:40:02Z
       
  • The therapeutic usage of botulinum toxin (Botox) in non-cosmetic head and
           neck conditions – an evidence based review

    • Abstract: Publication date: Available online 30 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Kamran Habib Awan
      Botulinum toxin (Botox) is an exotoxin produced from Clostridium botulinum. It blocks the release of acetylcholine from the cholinergic nerve end plates resulting in inactivity of the muscles or glands innervated. The efficacy of Botox in facial aesthetics is well established, however, recent literature has highlighted its utilization in multiple non-cosmetic medical and surgical conditions. The present article reviews the current evidence pertaining to Botox use in the non-cosmetic head and neck conditions. A literature search was conducted using Medline, EMBASE, ISI Web of Science and the Cochrane databases limited to English Language articles published from January 1980 to December 2014. The findings showed that there is level 1 evidence supporting the efficacy of Botox in the treatment of laryngeal dystonia, headache, cervical dystonia, masticatory myalgia, sialorrhoea, temporomandibular joint disorders, bruxism, blepharospasm, hemifacial spasm and rhinitis. For chronic neck pain there is level 1 evidence to show that Botox is ineffective. Level 2 evidence exists for vocal tics and trigeminal. For stuttering, facial nerve paresis, Frey’s syndrome and oromandibular dystonia the evidence is level 4. Thus, there is compelling evidence in the published literature to demonstrate the beneficial role of Botox in a wide range of non-cosmetic conditions pertaining to the head and neck (mainly level 1 evidence). With more and more research, the range of clinical applications and number of individuals getting Botox will doubtlessly increase. Botox appears to justify its title as ‘the poison that heals’.


      PubDate: 2016-05-04T13:40:02Z
       
  • The standard aqueous stem bark extract of Mangifera indica L. inhibits
           toxic PLA2 – NN-XIb-PLA2 of Indian cobra venom

    • Abstract: Publication date: Available online 30 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Bhadrapura Lakkappa Dhananjaya, Shivalingaiah Sudarshan, Yashad Dongol, Sunil S. More
      The aqueous extract of Mangifera indica is known to possess diverse medicinal properties, which also includes anti-snake venom activities. However, its inhibitory potency and mechanism of action on multi-toxic snake venom Phospholipases A2s is still unknown. Therefore, the objective of this study was to evaluate the modulatory effect of standard aqueous bark extract of M. indica on NN-XIb-PLA2 of Indian cobra venom. The in vitro sPLA2, in situ hemolytic and in vivo edema inhibition effect were carried out as described. Also the effect of substrate and calcium concentration was carried out. M. indica extract dose dependently inhibited the GIA sPLA2 (NN-XIb-PLA2) activity with an IC50 value of 7.6 μg/ml. M. indica extract effectively inhibited the indirect hemolytic activity up to 98% at ∼40 μg/ml concentration. Further, M. indica extract (0-50 μg/ml) inhibited the edema formed in a dose dependent manner. When examined as a function of increased substrate and calcium concentration, there was no relieve of inhibitory effect of M. indica extract on the NN-XIb-PLA2. Further, the inhibition was irreversible as evident from binding studies. The in vitro inhibition is well correlated with in situ and in vivo edema inhibiting activities of M. indica. As the inhibition is independent of substrate and calcium and was irreversible, it can be concluded that M. indica extracts mode of inhibition could be due to direct interaction of components present in the extract with the PLA2 enzyme. The aqueous extract of M. indica effectively inhibits svPLA2 enzymatic and its associated toxic activities, which substantiate their anti-snake venom properties. Further in-depth studies on the role and mechanism of the principal constituents present in the extract, responsible for the anti-PLA2 activity will be interesting to develop them into potent antisnake component and also as an anti-inflammatory agent.


      PubDate: 2016-05-04T13:40:02Z
       
  • The effect of chitooligosaccharides on oleic acid-induced lipid
           accumulation in HepG2 cells

    • Abstract: Publication date: Available online 29 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Peiqiu Cao, Guidong Huang, Qingyun Yang, Jiao Guo, Zhengquan Su
      This experiment aimed to evaluate the capacities of two types of chitooligosaccharides (COS) with different molecular weights for the ability to eliminate lipid accumulation in hepatocytes. We have established a lipid accumulation model in HepG2 cells for these studies in vitro, which was established by induction with oleic acid. The capacity of COS to eliminate lipid accumulation were evaluated using three metrics: the thiazolyl blue dye absorbance (MTT value), the morphology of intracellular lipid droplets and the triglyceride level (TG). Two types of COS with different molecular weights (1000Da and 3000Da) can significantly reduce intracellular lipid accumulation and decrease TG content in HepG2 cells, in a dose-dependent fashion. We found that low molecular weight COS is more efficacious than high molecular weight COS. Two types of COS can eliminate lipid accumulation induced by oleic acid in HepG2 cells, leading to an obvious hypolipidemic effect in vitro. These results suggest that COS may be effective preventive agents in fatty liver disease.


      PubDate: 2016-04-29T13:15:42Z
       
  • Diagnosis of Genus Helicobacter through A hemi-nested PCR assay of 16S
           rRNA

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Heping Qin, Guodu Tang, Ping Yi, Xinyi Pan, Huali Huang, Renjie Chang, Zhe Shi, Muhammad Aqeel Ashraf
      The present study aimed to establish a genus-specific PCR-based assay to detect helicobacters using 16S rRNA gene as the target template. We designed the hemi-nested primers based on sequences of 16S rRNA gene of 34 types of Helicobacter species. The inclusivity, sensitivity, and specificity of the PCR assay using these primers were examined in three different models, comprising feces simulated samples, BLAB/c mice infection model and clinic patients samples. The detection sensitivity of H.pylori, H.hepaticus and H.bilis strains from feces simulated samples was all 102 CFU/ml. We successfully detected H.hepaticus and H.bilis in the liver, caecum and feces of experimentally infected mice. H.pylori was successfully detected in the feces samples from 3 patients infected with H.pylori while not in the feces samples from 3 healthy human. However, the C97/C05-C97/C98 PCR assay detected H.pylori in the 2 positive samples. Due to the PCR assay’s excellent inclusivity, high sensitivity and specificity it may be used to detect the presence of Helicobacters.


      PubDate: 2016-04-29T13:15:42Z
       
  • Serum TNF-α, GTH and MDA of High-Fat Diet-Induced Obesity and Obesity
           Resistant Rats

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Peixian Wu, Fan Zhang, Yali Dai, Lingchuan Han, Shuo Chen
      Objective Mechanism of high fat diet-induced obesity is analyzed and serum tumor necrosis factor, malondialdehyde and glutathione levels of obesity resistant rats are effectively analyzed. Methods 120 male SD rats were grouped into obesity group and control group, each group with 60 rats. Obese rats were fed with high fat diet, while control rats were fed with ordinary fodder. After six months of feeding, observe growth degree of two groups of rats, and divide the rats into obesity group and obesity resistant group based on extent of growth. Then detect glutathione, tumor necrosis factor-α and MDA content in bat serum with enzyme-linked immunosorbent assay. Results The content of tumor necrosis factor α in obese rats and obesity resistant rats is far higher than that in control group (P <0.05), there exists no statistical significance (P> 0.05) in tumor necrosis factor α in obesity group and obesity resistant group, glutathione level of obesity group rats and obesity resistant group rats are significantly increased (P <0.05) compared with that of control group, also serum MDA level of the two groups have significant statistical significance compared with that of normal control group, (P <0.05). Conclusion Among rats fed with high fat diet, in comparison of weight of obesity resistant rats and control group rats, there is no statistically significant difference, (P> 0.05). However, high fat diet will impact mechanisms in vivo in rats, which then induces oxidative stress response and inflammatory response in rats.


      PubDate: 2016-04-29T13:15:42Z
       
  • Forgotten Topological Index of Chemical Structure in Drugs

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Wei Gao, Muhammad Kamran Siddiqui, Muhammad Imran, Muhammad Kamran Jamil, Mohammad Reza Farahani
      A massive of early drug tests implys that there exist strong inner relationships between the bio-medical and pharmacology characteristics of drugs and their molecular structures. The forgotten topological index was defined to be used in the analysis of drug molecular structures, which is quite helpful for pharmaceutical and medical scientists to grasp the biological and chemical characteristics of new drugs. Such tricks are popularly employed in developing countries where enough money is lacked to afford the relevant chemical reagents and equipment. In our article, by means of drug molecular structure analysis and edge dividing technology, we present the forgotten topological index of several widely used chemical structures which often appear in drug molecular graphs.


      PubDate: 2016-04-29T13:15:42Z
       
  • Release property study on the novel divalproex sodium enteric-coated
           capsules

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Shuoye Yang, Xin Wang, Jiangsong Jia, Pengyuan Li
      In present study, a novel divalproex sodium (DS) enteric-coated capsule was prepared, high performance liquid chromatography (HPLC) assay method for DS was developed. Their uniformity, release curve and release characteristics in different solvents were examined. The release studies were performed using marketed sample as a reference and data were analyzed in terms of cumulative release amounts as a function of time. It was demonstrated by the results that assay developed was specific, rapid and reliable, which can be used to determine DS in vitro accurately, our developed samples was similar to reference preparation in in vitro release characteristics. The release characteristics of different batches of samples were quite similar with each other, the total release percents of DS from enteric-coated capsule were within 0-10 % in HCl, and reached close to 100 % in phosphate buffer. Similarity factors (f2) of three batches between two preparations were all higher than 50. The developed enteric-coated capsule may be a promising alternative dosage form for treatment of related diseases.


      PubDate: 2016-04-29T13:15:42Z
       
  • Treatment with Glial derived neurotropic factor (GDNF) attenuates
           oxidative damages of spinal injury in rat model

    • Abstract: Publication date: Available online 25 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Tao Li, Qi Li, Hui Gong, Zhuo-fu Chen, Xia-wu Peng
      Spinal cord injury (SCI) is a serious and debilitating issue being suffered by wide population worldwide. Extensive treatment approaches have been tested and being verified for their efficacy. Owing to the nature of central nervous system (CNS), the resident stem cells would be triggered in response to any sort of trauma with nerve factors as their communication signals. Apart from physical injuries, damages due to oxidative stress also needs to be addressed while CNS repair mechanism takes place. This study looks at the potential of glial derived nerve factor (GDNF) in addressing the SCI in regards to oxidative damages. A total of 60 Wistar rats were clustered into five groups and GDNF at various concentration were tested in each group. Assessments in terms of oxidative stress parameters were noted and analyzed accordingly. It was noted that GDNF had reduced oxidative damages and increased the levels of anti-oxidants in dose-dependent manner (p<0.05). Though treatment with 10mg/mL and 20mg/mL showed significant changes as compared to control group, these treatment modalities remained insignificant among each other. In conclusion, we demonstrated that GDNF exerted a neuro-protective effect on CNS by inducing anti-oxidants and reducing the levels of oxidative stress in SCI induced rat models.


      PubDate: 2016-04-29T13:15:42Z
       
  • Research on AIDS Patients’ Survival Time after Highly Active
           Antiretroviral Therapy, Treatment Effect and Treatment Modes

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Riying Lv, Guojian Li, jizhou Wu, Yujia Zhu, XiongLin Qin, Shixiong Li
      To fully define clinical efficacy of highly active antiretroviral therapy for AIDS, analyze patients’ survival time and treatment mode after receiving treatment, and provide scientific theory to guide improvement of antiviral therapy, this paper selected 3100 cases of patients diagnosed with AIDS during April 2006 and April 2014 as object of this study. All patients were treated with highly active antiretroviral therapy. The main analysis contents of this study include CD4 + T lymphocyte count, viral load changes, incidence of opportunistic infections, specific cause of death and the like. The results show that patients’ CD4 +, T lymphocyte levels are significantly increased 3,18,24 months after treatment, difference between the situation after and before receiving treatment, P <0.05, with statistically significant difference. Analyzed from effective inhibition of virus, effective inhibition rate is 72.58.0% (2250/3100). Main causes of death in patients is usually respiratory failure. It thus can be concluded that highly active antiretroviral therapy for AIDS is with good clinical effect, which can effectively improve survival time of patients. So it enjoys application value of being widely used in clinical treatment of AIDS.


      PubDate: 2016-04-29T13:15:42Z
       
  • Analgesic effect and possible mechanism of SCH772984 intrathecal injection
           on rats with bone cancer pain

    • Abstract: Publication date: Available online 26 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Bian Juhua, Zhu Shanshan, Ma Wenwen, Li Chunwei, Muhammad Aqeel Ashraf
      This study is to establish a model of rat tibial osteocarcinoma pain, intrathecally inject specific ERK1/2 inhibitors SCH772984, observe the analgesic effect, and discuss the influence of ERK-P90RSK-Fos signal path in bone cancer pain. Forty female SD rats were randomly divided into 5 groups. Establish a bone cancer pain model after putting the intrathecal tube 5d, determine the rats’ mechanical withdrawal threshold(MWT) after tube 5d 40 SD rats with intrathecal tube back 5d were randomly divided into 5 groups. Sham Group receives no medication, the other four respectively receives 5% DMSO 10 μl, SCH 0.1, 1.0, 10 μ g (SCH dissolved in 10 μl 5% DMSO) intrathecally. Determine the rats’ mechanical withdrawal threshold(MWT) before and after giving medication 1, 3, 6, 9, 12, 15, 18, 24h, and 2min spontaneous paw withdrawal. Western Blot and immuno-fluorescence determine the expression condition of spinal cord dorsal horn of p-ERK, p-p90RSK and Fos protein. Intrathecal injection of SCH772984 has analgesic effects on rats with bone cancer pain, and the effects enhance with increasing dose; intrathecal injection of SCH772984 10 μg could greatly reduce the expression of spinal dorsal horn Fos protein. Injecting walker 256 tumor cells into rats’ tibia could cause behavior changes, such as idiopathic pain sensitivity and pain; the intrathecal tube almost has no effect on motor function of rats; ERK1/2 is involved in bone cancer pain, intrathecal injection of ERK1/2 specific inhibitors SCH772984 10 μg may effectively relieve bone cancer pain.


      PubDate: 2016-04-29T13:15:42Z
       
  • Pathogen Distribution and Drug Resistance of Nephrology Patients with
           Urinary Tract Infections

    • Abstract: Publication date: Available online 23 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Yunqian Wang, Huicong Li, Baoping Chen
      Objective Pathogen distribution characteristics of nephrology patients with urinary tract infections are studied, and drug resistance of nephrology and urinary tract infections disease are analyzed, so as to provide sufficient evidence for treatment of patients. Methods: Conduct randomized control study of 3,500 cases of nephrology patients with urinary tract infections treated in different hospitals from December 2013 to December 2015, isolate pathogens in patients’ urine samples, perform identification and drug sensitive test and then conduct detailed analysis of drug resistance of pathogens. Results: Through isolation of pathogens, it can be found that all pathogens include Escherichia coli, Gram-positive cocci, gram-negative bacteria, fungi, Acinetobacter baumannii, Enterococcus faecalis, urinary Enterococcus. Among them, proportion of Escherichia coli is the largest. Patients have relatively high drug resistance to ceftriaxone, gentamicin, ciprofloxacin and cotrimoxazole. Conclusion: For nephrology patients with urinary tract infection, the main pathogen is escherichia coli, which has had some drug resistance. Drug resistance detection of pathogen should be strengthened in clinics, so as to provide strong guidance for clinical treatment and promote effective treatment of patients.


      PubDate: 2016-04-25T12:38:27Z
       
  • Effect of Cynomorium Flavonoids on morphology of Perimenopausal Depression
           mice model

    • Abstract: Publication date: Available online 24 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Tan Wang, Mingsan Miao, Yan Li, Min Li, Ying Zhang, Shuo Tian
      Objective In this report, the effects of cynomorium flavonoids on mouse model of perimenopausal depression were investigated. Method 60 ovariectomized female mice were randomly divided into 6 groups evenly: high, medium and low doses of cynomorium flavonoids groups (400mg·kg-1, 200mg·kg-1, 100mg·kg-1), Gengnian’an capsule group (675mg·kg-1), soy isoflavones soft capsule group (250mg·kg-1), and model group. Give the corresponding drug fifth days after surgery for once a day, consecutive thirty days. The model group and control group given the water of same volume. The model related groups were applied with different stress for consecutive eighteen days. Kill the mice and remove the thymus, spleen, uterus and one hand of brain when it is 2 hours after the last administration in mice of each group. Observe the histological changes of each group under light microscope. Results By observing the pathological section. Compared with model group, the pathological changes of the uterus and hypothalamus of mice were significantly improved. The thymic cortex markedly thickened, volume of splenic nodule also significantly increases, the number of lymphocytes significantly increased (P < 0.01). Simulation results that the high dose of cynomorium flavonoids group has the best effective. Conclusion Cynomorium flavonoids on mouse uterus, hypothalamus, thymus and spleen lesions have a significant role in the improvement. Cynomorium flavonoids have a good therapeutic effect on mice with perimenopausal depression


      PubDate: 2016-04-25T12:38:27Z
       
  • Study on Fluorouracil - Chitosan Nanoparticle Preparation and its
           Antitumor Effect

    • Abstract: Publication date: Available online 23 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Gaimin Chen, Rudong Gong
      To successfully prepare fluorouracil - chitosan nanoparticles, and further analyze its anti-tumor activity mechanism, this paper makes a comprehensive study of existing preparation prescription and makes a detailed analysis of fluorouracil - chitosan in vitro release and pharmacodynamic behavior of animals. Two-step synthesis method is adopted to prepare 5-FU-CS-mPEG prodrugs, and infrared, 1H-NMR and differential thermal analysis are adopted to analyze characterization synthetic products of prepared drugs. To ensure clinical efficacy of prepared drugs, UV spectrophotometry is adopted for determination of drug loading capacity of prepared drugs, transmission electron microscopy is adopted to observe the appearance, dynamic dialysis method is used to observe in vitro drug release of prepared drugs and fitting of various release models is done. Anti-tumor effect is studied via level of animal pharmacodynamics. After the end of the experiment, tumor inhibition rate, spleen index and thymus index of drugs are calculated. Experimental results show that the prepared drugs are qualified in terms of regular shape, dispersion, drug content, etc.. Animal pharmacodynamics experiments have shown that concentration level of drug loading capacity of prepared drugs has a direct impact on anti-tumor rate. The higher concentration, the higher anti-tumor rate. Results of pathological tissue sections of mice show that the prepared drugs cause varying degrees of damage to receptor cells, resulting in cell necrosis or apoptosis problem. It can thus be concluded that ion gel method is an effective method to prepare drug-loading nanoparticles, with prepared nanoparticles evenly distributed in regular shape which demonstrate good slow-release characteristics in receptor vitro and vivo. At the same time, after completion of drug preparation, relatively strong anti-tumor activity can be generated for the receptor, so this mode of preparation enjoys broad prospects for development.


      PubDate: 2016-04-25T12:38:27Z
       
  • Ablation Effects of Noninvasive Radiofrequency Field -Induced Hyperthermia
           on Liver Cancer Cells

    • Abstract: Publication date: Available online 23 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Kaiyun Chen, Shuguang Zhu, Guoan Xiang, Xiaopeng Duan, Jiwen He, Guihua Chen
      To have in-depth analysis of clinical ablation effect of noninvasive radiofrequency field- induced hyperthermia on liver cancer cells, this paper collected liver cancer patients’ treatment information from10 hospitals during January 2010 and December 2011, from which 1050 cases of patients were randomly selected as study object of observation group who underwent noninvasive radiofrequency field- induced hyperthermia treatment; in addition, 500 cases of liver cancer patients were randomly selected as study object of control group who underwent clinical surgical treatment. After treatment was completed, three years of return visit was done, survival rates of the two groups of patients after 1 year, 2 years, 3 years were compared, and clinical effects of radiofrequency ablation of liver cancer was evaluated. Zoom results show that the two groups are similar in terms of survival rate, and the difference is without statistical significance. 125 patients in observation group had varying degrees of adverse reactions, while 253 patients in control group had adverse reactions. Difference between groups P<0.05, with significant statistical significance. It can be concluded that radiofrequency ablation of liver cancer is more secure. Therefore, the results of this study fully demonstrate that liver cancer treatment with noninvasive radiofrequency field-induced hyperthermia is with safety effect and satisfactory survival rate, thus with relatively high clinical value in clinical practice.


      PubDate: 2016-04-25T12:38:27Z
       
  • Preparation and Application of Functionalized Nano Drug Carriers

    • Abstract: Publication date: Available online 23 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Rudong Gong, Gaimin Chen
      Objective Targeting at category memory characteristics and preparation methods of functionalized nano drugs, preparation technology of functionalized nano drug carriers are studied, and then important role of functionalized nano drug carrier in preparation of medicine is studied. Methods Carry out the relevant literature search with computer, change limited language in the paper to Chinese and necessarily remove repetitive studies. Results After first review of 1260 retrieved literature, it can be found that nano drug is with accurate quantity, relatively good targeting, specificity and absorbency. Necessary research of nano drug carriers can prevent and treat disease to a certain extent. Conclusion Preparation of functionalized nanocarrier is simple and convenient, which can improve frequency of use of nano preparation technology and provide better development space for medical use. Therefore, nanocarriers should be combined with drugs with relatively strong specificity in clinics, in order to be able to conduct effective research on nanometer intelligent drug, effectively promote long-term development of nano biotechnology, and then provide favorable, reliable basis for clinical diagnosis and treatment.


      PubDate: 2016-04-25T12:38:27Z
       
  • Corrigendum to “Mycosynthesis of silver nanoparticles bearing
           antibacterial activity” [Saudi Pharm. J. 24 (2016) 140–146]

    • Abstract: Publication date: Available online 12 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Pasha Azmath, Syed Baker, Devaraju Rakshith, Sreedharamurthy Satish



      PubDate: 2016-04-25T12:38:27Z
       
  • Separation and Purification and in Vitro Anti-Proliferative Activity of
           Leukemia Cell K562 of Galium Aparine L. Petroleum Ether Phase

    • Abstract: Publication date: Available online 24 April 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Guoqing Shi, Jiang Liu, Wen’en Zhao, Yanqi Liu, Xinfeng Tian
      To explore material basis of in vitro anti-proliferative activity of leukemia cell K562 of petroleum ether phase of product resulting from galium aparine L. 60% ethanol extraction, the experiment adopts column chromatography combined with thin layer preparation, isolates and purifies petroleum ether, conducts structural identification of obtained single compound and applies MTT method for viability assay of in vitro anti-proliferative activity of leukemia cell K562. Experimental results show that galium aparine L. petroleum ether contains mainly β- sitosterol, daucosterol and dibutyl phthalate and other substances. Under experimental conditions, the three could inhibit the proliferation of leukemia cell K562 with dose-effect and time-effect relationship, of which dibutyl phthalate has strongest activity. Dibutyl phthalate with excellent activity, β- sitosterol with rich content and moderate effect should be the main contributor to its biological activity.


      PubDate: 2016-04-25T12:38:27Z
       
  • Nanogels as potential nanomedicine carrier for treatment of cancer: A mini
           review of the state of the art

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Govind Soni, Khushwant S. Yadav
      Nanogels are being explored as drug delivery agents for targeting cancer due to their easy tailoring properties and ability to efficiently encapsulate therapeutics of diverse nature through simple mechanisms. Nanogels are proficiently internalized by the target cells, avoid accumulating in nontarget tissues thereby lower the therapeutic dosage and minimize harmful side effects. However, there is an urgent need for relevant clinical data from nanogels so as to allow translation of the nanogel concept into a viable therapeutic application for the treatment of cancer. This review highlights some of the recent progress in nanogels as a carrier in the field of nanomedicine for the treatment of cancer. The present review critically analyzes the use of extracellular pH targeting for nanogels, siRNA delivery, PEGylated nanogels, multi-responsive nanogels and intracellular delivery of nanogels for improved therapy of cancer.


      PubDate: 2016-03-17T08:23:03Z
       
  • Mycosynthesis of silver nanoparticles bearing antibacterial activity

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Pasha Azmath, Syed Baker, Devaraju Rakshith, Sreedharamurthy Satish
      Mycosynthesis of silver nanoparticles was achieved by endophytic Colletotrichum sp. ALF2-6 inhabiting Andrographis paniculata. Well dispersed nanoparticles were characterized using UV–Visible spectrometry with maximum absorption conferring at 420nm. FTIR analysis revealed possible biomolecules reducing the metal salt and stabilization of nanoparticles. XRD analysis depicted the diffraction intensities exhibiting between 20 and 80°C at 2theta angle thus conferring the crystalline nature of nanoparticles. Morphological characteristic using TEM revealed the polydispersity of nanoparticles with size ranging from 20 to 50nm. Synthesized nanoparticles exhibited bactericidal activity against selected human pathogens. Nanoparticles mode of action was carried out to reveal DNA damage activity. Thus the present investigation reports facile fabrication of silver nanoparticles from endophytic fungi.


      PubDate: 2016-03-17T08:23:03Z
       
  • Investigation of the efficacy of generic and brand-name tiotropium bromide
           in the management of chronic obstructive pulmonary disease: A randomized
           comparative trial

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Yunes Panahi, Mostafa Ghanei, Mohammad Behzadi, Maryam Salehi, Sara Saffar Soflaei, Amirhossein Sahebkar
      Introduction: The beneficial effects of tiotropium bromide, a long acting anticholinergic bronchodilator, in the management of chronic obstructive pulmonary disease have been shown in previous studies. The present study aimed to compare the efficacy and safety of generic (Tiova®) and brand-name (Spiriva®) tiotropium preparations in patients with COPD. Methods and materials: In this randomized double-blind parallel-group trial, 79 patients with documented COPD were assigned to Tiova® or Spiriva® for a period of 4weeks. Assessment of pulmonary function (using spirometry), quality-of-life (using St. George respiratory Questionnaire [SGRQ]) and severity of respiratory symptoms (using breathlessness, cough and sputum scale [BCSS]) was performed at baseline and at the end of treatment period. Results: There were significant increases in FEV1 and reductions in FVC by the end of study in both Tiova® and Spiriva® groups. FEV1/FVC ratio did not change significantly neither in the Tiova® nor in Spiriva® group. Overall SGRQ score as well as subscale scores of symptoms, activity and impacts were improved by both drugs. In the BCSS scale, the frequency and severity of three main symptoms (dyspnea, cough and sputum) was decreased by both drugs. Baseline as well as post-treatment values of spirometric parameters, SGRQ and BCSS scores was comparable between the groups, apart from a lower post-treatment frequency of cough and sputum in the Spiriva® versus Tiova® group. There was no report of adverse events in either of the study groups. Conclusion: The findings of this comparative trial showed equivalent efficacy and safety of Spiriva® and Tiova® in lessening the symptoms as well as improving the quality of life in patients with COPD. This finding has an important translational value given the significantly lower costs of generic versus brand-name products.


      PubDate: 2016-03-17T08:23:03Z
       
  • Assessment of potential drug–drug interactions and its associated
           factors in the hospitalized cardiac patients

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Ghulam Murtaza, Muhammad Yasir Ghani Khan, Saira Azhar, Shujaat Ali Khan, Tahir M. Khan
      Drug–drug interactions (DDIs) may result in the alteration of therapeutic response. Sometimes they may increase the untoward effects of many drugs. Hospitalized cardiac patients need more attention regarding drug–drug interactions due to complexity of their disease and therapeutic regimen. This research was performed to find out types, prevalence and association between various predictors of potential drug–drug interactions (pDDIs) in the Department of Cardiology and to report common interactions. This study was performed in the hospitalized cardiac patients at Ayub Teaching Hospital, Abbottabad, Pakistan. Patient charts of 2342 patients were assessed for pDDIs using Micromedex® Drug Information. Logistic regression was applied to find predictors of pDDIs. The main outcome measure in the study was the association of the potential drug–drug interactions with various factors such as age, gender, polypharmacy, and hospital stay of the patients. We identified 53 interacting-combinations that were present in total 5109 pDDIs with median number of 02 pDDIs per patient. Overall, 91.6% patients had at least one pDDI; 86.3% were having at least one major pDDI, and 84.5% patients had at least one moderate pDDI. Among 5109 identified pDDIs, most were of moderate (55%) or major severity (45%); established (24.2%), theoretical (18.8%) or probable (57%) type of scientific evidence. Top 10 common pDDIs included 3 major and 7 moderate interactions. Results obtained by multivariate logistic regression revealed a significant association of the occurrence of pDDIs in patient with age of 60years or more (p <0.001), hospital stay of 7days or longer (p <0.001) and taking 7 or more drugs (p <0.001). We found a high prevalence for pDDIs in the Department of Cardiology, most of which were of moderate severity. Older patients, patients with longer hospital stay and with elevated number of prescribed drugs were at higher risk of pDDIs.


      PubDate: 2016-03-17T08:23:03Z
       
  • Leukemia and rosiglitazone

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Irfan Yavasoglu, Gurhan Kadikoylu, Zahit Bolaman



      PubDate: 2016-03-17T08:23:03Z
       
  • Monitoring model drug microencapsulation in PLGA scaffolds using X-ray
           powder diffraction

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Adeyinka Aina, Manish Gupta, Yamina Boukari, Andrew Morris, Nashiru Billa, Stephen Doughty
      The microencapsulation of three model drugs; metronidazole, paracetamol and sulphapyridine into Poly (dl-Lactide-Co-Glycolide) (PLGA) scaffolds were probed using X-ray Powder Diffraction (XRPD). Changes in the diffraction patterns of the PLGA scaffolds after encapsulation was suggestive of a chemical interaction between the pure drugs and the scaffolds and not a physical intermixture.


      PubDate: 2016-03-17T08:23:03Z
       
  • Corrigendum to “Medication safety practices in hospitals: A national
           survey in Saudi Arabia” [Saudi Pharm. J. 21(2) (2013) 159–164]
           

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Hisham Aljadhey, Abdulaziz Alhossan, Khalid Alburikan, Mansour Adam, Michael D. Murray, David W. Bates



      PubDate: 2016-03-17T08:23:03Z
       
  • Alignment independent 3D-QSAR, quantum calculations and molecular docking
           of Mer specific tyrosine kinase inhibitors as anticancer drugs

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Fereshteh Shiri, Somayeh Pirhadi, Jahan B. Ghasemi
      Mer receptor tyrosine kinase is a promising novel cancer therapeutic target in many human cancers, because abnormal activation of Mer has been implicated in survival signaling and chemoresistance. 3D-QSAR analyses based on alignment independent descriptors were performed on a series of 81 Mer specific tyrosine kinase inhibitors. The fractional factorial design (FFD) and the enhanced replacement method (ERM) were applied and tested as variable selection algorithms for the selection of optimal subsets of molecular descriptors from a much greater pool of such regression variables. The data set was split into 65 molecules as the training set and 16 compounds as the test set. All descriptors were generated by using the GRid INdependent descriptors (GRIND) approach. After variable selection, GRIND were correlated with activity values (pIC50) by PLS regression. Of the two applied variable selection methods, ERM had a noticeable improvement on the statistical parameters of PLS model, and yielded a q 2 value of 0.77, an r pred 2 of 0.94, and a low RMSEP value of 0.25. The GRIND information contents influencing the affinity on Mer specific tyrosine kinase were also confirmed by docking studies. In a quantum calculation study, the energy difference between HOMO and LUMO (gap) implied the high interaction of the most active molecule in the active site of the protein. In addition, the molecular electrostatic potential energy at DFT level confirmed results obtained from the molecular docking. The identified key features obtained from the molecular modeling, enabled us to design novel kinase inhibitors.


      PubDate: 2016-03-17T08:23:03Z
       
  • Prescription and consumption of solid oral drugs dispensed as unitary
           doses in a third level hospital

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): David Calderón-Guzmán, Hugo Juárez-Olguín, Ernestina Hernández-García, Alejandro Medina-Andrade, Belen Juarez Tapia
      Background: The knowledge about the pattern of prescription and consumption of solid oral drugs dispensed as unitary doses (UD) in Mexico is sparing. Purpose: The aim of this study was to describe the pattern of prescription and consumption of solid oral drugs dispensed as unitary doses (UD) in a third level private hospital of Mexico. A retrospective study of a 60-month period (from 2007 to 2011) was carried out to know the pattern of drugs dispensed as UD in a third level hospital. Results: Among the principal drugs consumed were analgesic, antihypertensive, antibiotic, anti-inflammatory, antiepileptic, and diuretics. The dispensation of drugs per year was as follows: 181 drugs with 85,167 UD in 2007; 199 with 90,519 UD in 2008; 193 with 101,479 UD in 2009; 195 with 100,798 UD in 2010; and 198 with 103,913 UD in 2011. Conclusion: The findings confirmed that prescription and consumption of unitary doses in the hospitalization service increased, and revealed the extensive use of analgesics as the principal prescribed drug in this kind of hospital.


      PubDate: 2016-03-17T08:23:03Z
       
  • Evaluation and implementation of behavioral and educational tools that
           improves the patients’ intentional and unintentional non-adherence
           to cardiovascular medications in family medicine clinics

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Abdulla Shehab, Asim Ahmed Elnour, Shirina Al Swaidi, Akshaya Srikanth Bhagavathula, Farah Hamad, Omar Shehab, Mahmoud AbuMandil, AboBakr Abasaeed, Ahmed Dahab, Naama Al Kalbani, Rouda Abdulla, Sahar Asim, Pinar Erkekoglu, Saif Al Nuaimi, Aaesha Al Suwaidi
      Objective: There are limited number of studies describing the reasons and interventions of non-adherence to cardiovascular medications in United Arab Emirates (UAE). We aimed to implement and evaluate the behavioral and educational tools that indicate the reasons of non-adherence in patients with cardiovascular diseases and improve patient’s adherence to their cardiovascular medications. Methods: In this prospective interventional study, we recruited patients (n =300) with cardiovascular diseases from three family medicine clinics in Al Ain, UAE in 2010. We assessed patients’ responses to a validated brief medication questionnaire (BMQ). Results: At the end of the study, we observed a significant improvement in adherence. When we compared pre- and post-interventions, the mean (± standard deviation, SD) score for non-adherence to current regimen were 4.1±0.2 vs. 3.0±0.3 (p =0.034); indication of negative believes or motivational barriers scores was 1.8±0.4 vs. 0.9±0.1 (p =0.027); the indication of recall barrier scores was 1.6±0.1 vs. 0.8±0.1 (p =0.014); and the indication of access barrier scores was 1.6±0.2 vs. 0.7±0.2 (p =0.019). Mean blood pressure, fasting blood glucose, glycosylated hemoglobin, low density lipoprotein and postprandial blood glucose decreased significantly (p <0.01) post-intervention. Conclusion: We reported that implemented multifaceted tools targeting patients, provider and healthcare system have improved the adherence to cardiovascular medications. Our interventions managed to improve patients’ clinical outcome via improving adherence to prescribed cardiovascular medications.


      PubDate: 2016-03-17T08:23:03Z
       
  • Evaluation of rational use of medicines (RUM) in four government hospitals
           in UAE

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Amal Mahmood, Asim Ahmed Elnour, Abdel Azim Ahmed Ali, Nageeb A.G.M. Hassan, Abdulla Shehab, Akshaya Srikanth Bhagavathula
      Rational: Studies conducted showed that there were gaps regarding the rational use of medicines (RUM). Aims and objectives: Evaluate RUM in main government hospitals in four emirates in UAE, using WHO prescribing indicators. Method: Multicenter prospective cross-sectional comparative study was conducted in 4 hospitals in 4 different Emirates in UAE. Using consecutive random sampling method, a total of 1100 prescriptions (2741 prescribed drugs) were collected and analyzed from surveyed hospitals from April to October 2012. Index of Rational Drug Prescribing (IRDP) was used as an indicator of RUM. Results: The main finding of this study was that, the mean values of prescribing indicators of RUM in the surveyed hospitals were estimated to be within the WHO optimal values for generics (100.0 vs. 100.0), antibiotics (9.8±4.8 vs. ⩽30), injections (3.14±1.7 vs. ⩽10) and formulary (EML) prescribing (100.0 vs. 100.0). However, the only discrepancy was reported regarding the number of drugs per prescription which was found to be more than the WHO optimal value (2.49±0.9 vs. ⩽2); respectively. The mean IRDP was 4.55 which was less than the WHO optimal value of 5. Conclusions: Strategies and interventions are desirable to promote RUM and minimize the consequences of poly-pharmacy.


      PubDate: 2016-03-17T08:23:03Z
       
  • Pediatrician’s cough and cold medication prescription for
           hypothetical cases – A cross-sectional multi-centric study

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Sudha Chandelia, Mukesh Dhankar, Meetu Salhan
      Background: Concerns over inappropriate use of cough and cold medication (CCM) in children have been raised. In addition to being ineffective, these are now considered toxic for young children. Despite this fact studies from some regions have shown high use of these medications by physicians. However data on pediatricians and from India are negligible. Aim: To study the burden and patterns of cough and cold medications use by pediatricians for hypothetical cases. Methods: In this cross-sectional study; 172 pediatricians of various hospitals of Delhi and Haryana were enrolled from February 15 to March 15, 2012. They were contacted personally by authors and asked to write their prescriptions for two hypothetical case scenarios [having cough and cold] of two different age groups; (1) less than 2years and (2) 2–5years. We made two categories as recommendations exist for children less than 2years while recommendations for the second category are underway. Results were summarized as percentages, counts and; presented in tables and figures. Chi square test was used to establish association between categorical variables of subgroups. Results: Response rate was 93%. The most used CCM was antihistaminics (82%) and systemic sympathomimetics (48%). The use of CCM was significantly less in teaching hospitals as compared to non-teaching (77% vs. 95%; p-value – 0.025). However there was no statistical difference in the practice of post graduates and more senior pediatricians (p value-0.895). No difference in CCM use in two age groups {(82% (less than 2years) vs. 85% (2–5years); p-value – 0.531} was observed. Conclusion: Overall use of CCM is still high irrespective of patient age, pediatrician’s seniority or hospital setting. Efforts should be made to create awareness among the pediatricians regarding cautious use of these medications.


      PubDate: 2016-03-17T08:23:03Z
       
  • Formulation development and evaluation of medicated chewing gum of
           anti-emetic drug

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Mansi Paradkar, Balaram Gajra, Bhautik Patel
      Context: Medicated chewing gum (MCG) of Domperidone Maleate (DM) was developed by direct compression method with the goal to achieve quick onset of action and to improve patient compliance. Objective: Formulation development of MCG of DM and optimization of the formulation by screening of different excipients. Material and methods: MCG containing DM was prepared by screening different concentrations of sweeteners, flavouring agents, softening agents, lubricants and anti-adherents by changing one variable at a time. Performance evaluation was carried out by evaluating size, shape, thickness, taste, scanning electron microscopy, texture analysis, in vivo drug release study, ex vivo buccal permeation study and by studying statistical analysis for quality. Results and discussion: The statistical analysis showed significant improvement in organoleptic properties such as chewable mass, product taste, product consistency, product softness, total flavour lasting time and pharmaceutical properties like micromeritic properties after incorporation of appropriate excipients in an optimum amount in final optimized MCG formulation. In vivo drug release study showed 97% DM release whereas ex vivo buccal permeation study through goat buccal mucosa exhibited 11.27% DM permeation within 15min indicating its potential for increasing bioavailability by decreasing time of onset. The optimized formulation showed good surface properties and the peak load required for drug release was found to be acceptable for crumbling action. Conclusion: The developed formulation of medicated chewing gum can be a better alternative to mouth dissolving and conventional tablet formulation. It may be proved as a promising approach to improve the bioavailability as well as to improve patient compliance.


      PubDate: 2016-03-17T08:23:03Z
       
  • Remote loading of doxorubicin into liposomes by transmembrane pH gradient
           to reduce toxicity toward H9c2 cells

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Mohamed Alyane, Gillian Barratt, Mesbah Lahouel
      The use of doxorubicin (DOX) is limited by its dose-dependent cardiotoxicity. Entrapped DOX in liposome has been shown to reduce cardiotoxicity. Results showed that about 92% of the total drug was encapsulated in liposome. The release experiments showed a weak DOX leakage in both culture medium and in PBS, more than 98% and 90% of the encapsulated DOX respectively was still retained in liposomes after 24h of incubation. When the release experiments were carried out in phosphate buffer pH5.3, the leakage of DOX from liposomes reached 37% after 24h of incubation. Evaluation of cellular uptake of the liposomal DOX indicated the possible endocytosis of liposomes because the majority of visible fluorescence of DOX was mainly in the cytoplasm, whereas the nuclear compartment showed a weak intensity. When using unloaded fluorescent-liposomes, the fluorescence was absent in nuclei suggests that liposomes cannot cross the nuclear membrane. MTT assay and measurement of LDH release suggest that necrosis is the form of cellular death predominates in H9c2 cells exposed to high doses of DOX, while for weak doses apoptosis could be the predominate form. Entrapped DOX reduced significantly DOX toxicity after 3 and 6h of incubation, but after 20h entrapped DOX is more toxic than free one.


      PubDate: 2016-03-17T08:23:03Z
       
  • Inside Front Cover - Editorial Board

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2




      PubDate: 2016-03-17T08:23:03Z
       
  • Design and synthesis of some substituted thiazolo[3,2-a]pyrimidine
           derivatives of potential biological activities

    • Abstract: Publication date: March 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 2
      Author(s): Samia G. Abdel Moty, Mostafa A. Hussein, Salah A. Abdel Aziz, Mahrous A. Abou-Salim
      In continuation to our previous work, thiazolopyrimidines 2a–x were synthesized through intramolecular cyclization of 2-phenacylthio-dihydropyrimidine hydrobromides 1a–x using polyphosphoric acid. On the other hand, thiazolo[3,2-a]pyrimidine-3-one 3 was coupled with aryldiazonium salts or condensed with isatin to afford compounds 4a–c or 5, respectively. Chemical structure of the target compounds was substantiated by IR, FT-IR, 1H-, 13C and DEPT-13C NMR, MS as well as microanalyses. Moreover, the lipophilicity of the target compounds is expressed as Clog P. The antimicrobial screening of the test compounds 2a–x, 4a–c and 5 revealed moderate activity in comparison to reference drugs. Compounds 2a–c, 2e, 2o and 2v showed a gradual increase in their anti-inflammatory activity reaching its maximum at 5h compared to indomethacin. Furthermore, the analgesic activity of compounds 2a–c, 2e, 2o and 2v revealed a maximum activity after 5h of injection compared to aspirin and the LD50 of compounds 2e and 2v was determined.


      PubDate: 2016-03-17T08:23:03Z
       
  • Pharmacy Education in Saudi Arabia: A Vision of the Future

    • Abstract: Publication date: Available online 20 February 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Hisham Aljadhey, Yousef Asiri, Yaser Albogami, George Spratto, Mohammed Alshehri
      Background Pharmacy education in developing countries faces many challenges. An assessment of the challenges and opportunities for the future of pharmacy education in Saudi Arabia has not been conducted. Objectives The purpose of the study was to ascertain the views and opinions of pharmacy education stakeholders regarding the current issues challenging pharmacy education, and to discuss the future of pharmacy education in Saudi Arabia. Methods A total of 48 participants attended a one-day meeting in October 2011, designed especially for the purpose of this study. The participants were divided into six round-table discussion sessions with eight persons in each group. Six major themes were explored in these sessions, including the need to improve pharmacy education, program educational outcomes, adoption of an integrated curriculum, the use of advanced teaching methodologies, the need to review assessment methods, and challenges and opportunities to improve pharmacy experiential training. The round-table discussion sessions were videotaped and transcribed verbatim and analyzed by two independent researchers. Results Participants agreed that pharmacy education in the country needs improvement. Participants agreed on the need for clear, measureable, and national educational outcomes for pharmacy programs in the Kingdom. Participants raised the importance of collaboration between faculty members and departments to design and implement an integrated curriculum. They also emphasized the use of new teaching methodologies focusing on student self-learning and active learning. Assessments were discussed with a focus on the use of new tools, confidentiality of exams, and providing feedback to students. Several points were raised regarding the opportunities to improve pharmacy experiential training, including the need for more experiential sites and qualified preceptors, addressing variations in training quality between experiential sites, the need for accreditation of experiential sites, and the use of technology to track experiential activities and assessments. Conclusion Several challenges for improving pharmacy education in Saudi Arabia were discussed by stakeholders. To tackle these challenges facing most pharmacy schools in the Kingdom, national efforts need to be considered by involving all stakeholders.


      PubDate: 2016-02-25T04:09:17Z
       
 
 
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