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Saudi Pharmaceutical Journal
Journal Prestige (SJR): 0.687
Citation Impact (citeScore): 3
Number of Followers: 0  

  This is an Open Access Journal Open Access journal
ISSN (Print) 1319-0164
Published by Elsevier Homepage  [3163 journals]
  • Assessment of knowledge, attitude and practice of adverse drug reaction
           reporting among healthcare professionals in secondary and tertiary
           hospitals in the capital of Pakistan

    • Authors: Zaka Un Nisa; Ayesha Zafar; Farooq Sher
      Pages: 453 - 461
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Zaka Un Nisa, Ayesha Zafar, Farooq Sher
      Adverse Drug Reactions (ADRs) underreporting is a great challenge to pharmacovigilance. Healthcare professionals should consider ADR reporting as their professional obligation because the effective system of ADR reporting is important to improve patient care and safety. This study was designed to assess the knowledge, attitude, practice and factors associated with ADR reporting by healthcare professionals (physicians and pharmacists) in secondary and tertiary hospitals of Islamabad. A pretested questionnaire comprising of 27 questions (knowledge 12, attitude 4, practice 9 and factors influencing ADR reporting 2) was administered to 384 physicians and pharmacists in public and private hospitals. Respondents were evaluated for their knowledge, attitude and practice related to ADR reporting. Additionally, the factors which encourage and discourage respondents to report ADRs were also determined. The data was analysed by using SPSS statistical software. Among 384 respondents, 367 provided responses to questionnaire, giving a response rate of 95.5%. The mean age was 28.3 (SD = 6.7). Most of the respondents indicated poor ADR reporting knowledge (83.1%). The majority of respondents (78.2%) presented a positive attitude towards ADR reporting and only a few (12.3%) hospitals have good ADR reporting practice. The seriousness of ADR, unusualness of reaction, new drug involvement and confidence in the diagnosis of ADR are the factors which encourage respondents to report ADR whereas lack of knowledge regarding where and how to report ADR, lack of access to ADR reporting form, managing patient is more important than reporting ADR legal liability issues were the major factors which discourage respondents to report ADR. The study reveals poor knowledge and practice regarding ADR reporting. However, most of the respondents have shown a positive attitude towards ADR reporting. There is a serious need for educational training as well as sincere and sustained efforts should be made by Government and Hospital Authorities to ensure proper implementation of ADR reporting system in all of the hospitals.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.014
  • GC quantitative analysis of benzyl isothiocyanate in Salvadora persica
           roots extract and dental care herbal products

    • Authors: Maged Saad Abdel-Kader; Elsadig Hassan Khamis; Ahmed Ibrahim Foudah; Mohammed Hamed Alqarni
      Pages: 462 - 466
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Maged Saad Abdel-Kader, Elsadig Hassan Khamis, Ahmed Ibrahim Foudah, Mohammed Hamed Alqarni
      An accurate, sensitive, precise and simple method was developed utilizing Gas Chromatography for the quantitative analysis of benzyl isothicyanate in Siwak extract and dental care herbal products claimed to contain Siwak. Rtx (30.0 m × 0.25 mm ID, 25 µm thickness) column was used and helium as carrier gas at a flow rate of 0.74 mL/min. The retention time of standard benzyl isothicyanate was 13.470 min under the described conditions. Linear regression data analysis indicated a good linear relationship between peak height measurement and concentration of benzyl isothiocyanate in the range of 10–50 µg/ml (R2 = 0.9971). The regression equation was y = 11,471x. The developed GC method was subjected to validation requirements set by the ICH for precision, accuracy, and robustness. The entitled GC analyses expected to be valuable for the determination of benzyl isothiocyanate in Siwak extracts and other formulations containing Siwak extract. The amount of benzyl isothiocyanate reflects the efficacy of the products.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.013
  • Characterization of forced degradation products of toloxatone by

    • Authors: Robert Skibiński; Jakub Trawiński; Łukasz Komsta; Diana Murzec
      Pages: 467 - 480
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Robert Skibiński, Jakub Trawiński, Łukasz Komsta, Diana Murzec
      Forced degradation of toloxatone in solutions under basic, acidic, neutral, photo UV–VIS, photo UVC and oxidative stress conditions was investigated and structural elucidation of its degradation products was performed with the use of UHPLC system coupled ESI-Q-TOF mass spectrometer. Eight degradation products were found and their masses and formulas were obtained with high accuracy (0.09–3.79 ppm). The structure of unknown degradation products were elucidated from MS/MS fragmentation spectra of all analyzed compounds. Additionally, whole signals of decomposed substances were compared chemometrically. It was found that toloxatone is fragile towards basic hydrolysis, oxidative conditions and UVC irradiation. Finally, the toxicity of transformation products was computationally evaluated and compared in multivariate manner.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.012
  • Clinical pharmacy in Kuwait: Services provided, perceptions and barriers

    • Authors: Jacinthe Lemay; Mohammad Waheedi; Dalal Al-Taweel; Tania Bayoud; Pierre Moreau
      Pages: 481 - 486
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Jacinthe Lemay, Mohammad Waheedi, Dalal Al-Taweel, Tania Bayoud, Pierre Moreau
      Introduction Pharmacy practice has considerably evolved from a dispensing role to a patient-centered profession. Kuwait has minimal clinical pharmacy services established in its healthcare settings. Objectives The objectives of this study were to document existing clinical pharmacy services in public hospitals, identify barriers to their implementation and assess perceptions regarding pharmacists providing clinical services. Material & Method A cross sectional study using self-administered questionnaires among a total of 166 pharmacists and 284 physicians across 6 public hospitals in Kuwait was conducted. Results Over half of pharmacists (54%) provided clinical services, with the most common service being education and drug information (86%). Forty percent (40%) of the pharmacists reported that clinical services offered were of their own initiative but most of them (71%) were not sure whether they would offer additional services in the future. The majority of physicians were receptive to an expanded patient-centered role of the pharmacist (97%), believed pharmacists add to patient clinical care (92%) and considered pharmacists members of the healthcare team (96%). Major barriers reported by pharmacists to implement clinical pharmacy services included lack of policy (49%), time (36%) and clinical skills (28%), which is similar to barriers reported by physicians. Conclusion Although clinical pharmacy is in its infancy in Kuwait, it is well perceived and requested by physicians. Major barriers must be addressed and in this context, having a national framework for pharmacy practice from Ministry of Health, supported by cutting edge education and a pro-active professional association would be key assets to evolve the practice in Kuwait.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.011
  • Evaluation of the hepatoprotective effect of combination between
           hinokiflavone and Glycyrrhizin against CCl4 induced toxicity in rats

    • Authors: Maged S. Abdel-Kader; Ashraf T. Abulhamd; Abubaker M. Hamad; Abdullah H. Alanazi; Rizwan Ali; Saleh I. Alqasoumi
      Pages: 496 - 503
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Maged S. Abdel-Kader, Ashraf T. Abulhamd, Abubaker M. Hamad, Abdullah H. Alanazi, Rizwan Ali, Saleh I. Alqasoumi
      Liver diseases are one of the fatal syndromes due to the vital role of the liver. Most of the effective treatment of liver conditions are of natural origin. Silymarin (SI) is the standard drug used for treatment of impaired liver functions. Two natural compounds possessing promising liver protection and with different chemical structures namely; the bioflavonoid hinokiflavone (HF) isolated from Junipers phoenicea family Cupressaceae and the sweet saponin Glycyrrhizin (GL) present in Glycyrrhiza glabra (liquorice) were selected for the current study. Since the two compounds are of different nature, they may act by different mechanisms and express synergistic effect. Combination of the two compounds using to dose levels were challenged with single doses of HF, GL and SI as well. The comparison was monitored via measuring serum biochemical parameters including, aspartate aminotransferase (AST), alanine aminotransferase (ALT), gamma glutamyltranspeptidase (GGT), alkaline phosphatase (ALP) and total bilirubin, tissue parameters such as MDA, NP-SH and TP, histopathological study using light and electron microscope. Protective effect on kidney was also monitored histopathologically and biochemically through observing the levels of LDH, creatinine, creatinine-kinase, urea and uric acid. The combinations of HF and GL showed protective effect more than the used single doses of HF and GL alone. However, SI was superior to the used combination in the two used doses in all the measured parameters. The liver and kidney cells appearance under normal and electron microscope showed that SI treated groups showed almost normal cells with slight toxic signs. Cells from group treated with the higher doses of the combination of HF and GL showed slight signs of intoxication under light and electron microscope indicating good level of protection. Although the combination of HF and GL expressed good protection in the higher dose, however, the combination did not exceed the protective effect of SI.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.009
  • Phytochemical contents and biological evaluation of Ruta chalepennsis L.
           growing in Saudi Arabia

    • Authors: Shorok M. Alotaibi; Monerah S. Saleem; Jehan G. Al-humaidi
      Pages: 504 - 508
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Shorok M. Alotaibi, Monerah S. Saleem, Jehan G. Al-humaidi
      Phytochemical screening of Ruta chalepensis L. exhibited the presence of different chemical groups. The dried aerial parts of the plant was total extracted by ethanol and successively using chloroform, ethyl acetate and Butanol, out of the successive extracts four compounds namely, scopletin, kaempferol, quercetin, quercetin 3-O-α-L-rhamno glucopyranosyl (Rutin) were isolated and biological evaluations. Total ethanol and successive extracts; chloroform, ethyl acetate and Butanol were produced excellent antimicrobial activities against gram negative bacteria, gram positive bacteria and fungi. Ethyl acetate extract was the best for inhibition of the microorganism’s growth. All extracts (total ethanol, and successive extracts) showed DPPH radical scavenging activity in a concentration–dependent manner. The best antioxidant activity was obtained by ethyl acetate & n-butanol extract (94.28%, IC50 = 56.6 µg/ml). Also All extracts (total ethanol, and successive extracts) showed anticoagulant activity at higher concentration with prolonged clotting time 6:30 and 4:30 s at 10 mg/ml concentrations, respectively.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.008
  • Pharmaceutical significance of Leuconostoc mesenteroides KS-TN11 isolated
           from Nile Tilapia, Oreochromis niloticus

    • Authors: Bilal Ahmad Paray; Irfan A. Rather; Mohammad K. Al-Sadoon; Al-Shammari Fanar Hamad
      Pages: 509 - 514
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Bilal Ahmad Paray, Irfan A. Rather, Mohammad K. Al-Sadoon, Al-Shammari Fanar Hamad
      Aquatic animals are known for their myriad of beneficial bacteria with diverse biologically active compounds. The current study was aimed to isolate and characterize potentially beneficial lactic acid bacteria from Nile Tilapia and evaluate their pharmaceutical applications. The fish samples were dissected and stomach, intestine, and gills were collected and serially diluted for the isolation of lactic acid bacteria (LAB) on BCP agar media. Identification of isolate was carried by biochemical and molecular characterization using API kit and 16S rRNA gene sequencing analysis, respectively. Further, KS-TN11 was assessed for α-glucosidase inhibitory potential using the chromogenic method. A lactic acid bacterium KS-TN11 was isolated from the stomach of Nile Tilapia and identified as Leuconostoc mesenteroides. Effect of KS-TN11 on lipid accumulation in adipocytes was done by using Oil Red O staining. The isolate showed strong antibacterial activity against a number of pathogenic bacteria in vitro. In addition, L. mesenteroides KS-TN11 KS-TN11 (50 mg/ml and 100 mg/ml) tends to inhibit adipogenesis in 3T3-L1 adipocytes and thus may have possible anti-obesity effects. Moreover, L. mesenteroides KS-TN11 exhibited substantial α–glucosidase inhibitory activities by 41.33% at 50 mg/ml and 64% at 100 mg/ml, respectively. The bacterium showed potent antibacterial activity against a number of pathogenic bacteria; in addition to alpha-glucosidase activity, and inhibition of lipid accumulation in 3T3-L1 cell line. These results reinforce KS-TN11 as a novel bacterium with an impending pharmaceutical application.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.006
  • Aggregation and conformational stability evaluation of myoglobin in the
           presence of ionic surfactant

    • Authors: Mohammad A. Alsenaidy
      Pages: 515 - 519
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Mohammad A. Alsenaidy
      Sodium lauroyl sarcosinate (SLS) is frequently used for the solubilization of inclusion bodies in vitro due to its structural similarity to lipid plasma membrane. There are many factors that could influence protein aggregation propensity, including overall protein surface charge and hydrophobicity. Here, the aggregation pathway of myoglobin protein was studied under different conditions (pH 3.5 and 7.4) in the presence of varying concentrations of SLS to evaluate the underlying forces dictating protein aggregation. Data obtained from Rayleigh light scattering, ThT binding assay, and far-UV CD indicated that SLS have different effects on the protein depending on its concentration and environmental conditions. In the presence of low concentrations of SLS (0.05–0.1 mM), no aggregation was detected at both pH conditions tested. Whereas, as we reach higher SLS concentrations (0.5–10.0 mM), myoglobin started forming larger-sized aggregates at pH 3.5 and not pH 7.4. These results suggest that electrostatics interactions as well as hydrophobic forces play an important role in SLS-induced myoglobin aggregation.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.005
  • Revisiting the systemic lipopolysaccharide mediated neuroinflammation:
           Appraising the effect of l-cysteine mediated hydrogen sulphide on it

    • Authors: Abdulaziz S. Al-Saeedan; Varsha Gautam; Mohd Nazam Ansari; Manjari Singh; Rajnish K. Yadav; Jitendra K. Rawat; Uma Devi; Swetlana Gautam; Subhadeep Roy; Gaurav Kaithwas
      Pages: 520 - 527
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Abdulaziz S. Al-Saeedan, Varsha Gautam, Mohd Nazam Ansari, Manjari Singh, Rajnish K. Yadav, Jitendra K. Rawat, Uma Devi, Swetlana Gautam, Subhadeep Roy, Gaurav Kaithwas
      The present research was ventured to examine the effect of l-cysteine on neuro-inflammation persuaded by peripheral lipopolysaccharides (LPS, 125 μg/kg, i.p.) administration. No behavioral, biochemical, and inflammatory abnormality was perceived in the brain tissues of experimental animals after LPS administration. l-cysteine precipitated marginal symptoms of toxicity in the brain tissue. Similar pattern of wholesome effect of LPS were perceived when evaluated through the brain tissue fatty acid profile, histopathologically and NF-ĸBP65 protein expression. LPS was unsuccessful to alter the levels of hydrogen sulphide (H2S), cyclooxygenase (COX) and lipoxygenase (LOX) enzyme in brain tissue. LPS afforded significant peripheral toxicity, when figured out through inflammatory markers (COX, LOX), gaseous signaling molecules nitric oxide (NO), H2S, liver toxicity (SGOT, SGPT), and inflammatory transcription factor (NF-ĸBP65) and l-cysteine also provided a momentous protection against the same as well. The study inculcated two major finding, firstly LPS (i.p.) cannot impart inflammatory changes to brain and secondly, l-cysteine can afford peripheral protection against deleterious effect of LPS (i.p.)

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.004
  • Self-emulsifying drug delivery system improves preventive effect of
           curcuminoids on chronic heart failure in rats

    • Authors: Yunbin Jiang; Junzhi Wang; Yunhong Wang; Xiumei Ke; Chuanhui Zhang; Rongping Yang
      Pages: 528 - 534
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Yunbin Jiang, Junzhi Wang, Yunhong Wang, Xiumei Ke, Chuanhui Zhang, Rongping Yang
      Several studies have reported the preventive or therapeutic effect of curcuminoids on chronic heart failure (CHF), but their application was limited due to low solubility and bioavailability. Our previous study indicates that self-emulsifying drug delivery system (SEDDS) improves the solubility and bioavailability of curcuminoids. Thus, the aim of this work was to investigate whether SEDDS could improve preventive effect of curcuminoids on CHF in rats. CHF model was were established by coronary artery ligation. Ninety rats were randomly and averagely divided into sham, model, low- or high-dose suspension or SEDDS of curcuminoids (66.68 or 266.68 mg/kg) groups. Hemodynamic indices were recorded by multipurpose polygraph. Serum oxidative indices, B-type natriuretic peptide (BNP) and heart weight index were determined by kits and electronic balance. Myocardial infarct area, ventricular dilatation degree and collagen volume fraction of myocardial interstitium were analyzed by Masson staining, picric acid and sirius red staining, light microscopy and image analysis system. Myocardial histopathology was observed by hematoxylin and eosin staining, Masson staining and light microscopy. Reduction of ventricular pump function, increase of BNP level and heart weight index, myocardial lipid peroxidation damage, myocardial infarction, myocardial fibrosis, and cardiac enlargement were detected or observed in model group relative to those in sham group. After treatment with suspension or SEDDS of curcuminoids, the above-mentioned pathological changes were obviously reversed relative to those in model group. Meanwhile, the ameliorative effect of SEDDS of curcuminoids was markedly better than that of suspension of curcuminoids. This work provides a valuable reference from pharmacodynamics for development of curcuminoids pharmaceutics.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.003
  • In – Vitro activity of Desmostachya bipinnata (L.) Stapf successive
           extracts against Helicobacter pylori clinical isolates

    • Authors: Nermin H. Ibrahim; Amani S. Awaad; Rawan A. Alnafisah; Saleh I. Alqasoumi; Reham.M. El-Meligy; Amani Z. Mahmoud
      Pages: 535 - 540
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Nermin H. Ibrahim, Amani S. Awaad, Rawan A. Alnafisah, Saleh I. Alqasoumi, Reham.M. El-Meligy, Amani Z. Mahmoud
      Helicobacter pylori are well acknowledged as a major cause of gastrointestinal ailments and gastric cancers. Therefore, the present study aimed to investigate the potential in vitro activity of Desmostachya bipinnata against H. pylori, focusing on the determination of the most active extract responsible for the anti-helicobacter activity to produce new active drug from natural source. Desmostachya bipinnata total alcohol and successive extracts were in vitro tested against H. pylori. All extracts showed promising anti Helicobacter pylori activities. The most effective extract was diethyl ether extract, it showed 75% growth inhibition of the clinical Isolates bacterial Helicobacter pylori, in addition it showed high count reduction on the selected organisms in the different concentrations used (2xMIC, MIC & ½ MIC) compared with the untreated controls as well as the other extracts (chloroform, ethyl acetate and n-butanol). The oral median lethal dose (LD50) of the alcohol extract of the plant by doses up to 5000 mg/kg didn’t showed any mortality or morbidity, in addition no side effects were recorded on both liver and kidney functions this means that the extract was safe for use.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.002
  • The possible mechanisms of protocatechuic acid-induced central analgesia

    • Authors: Rana Arslan; Sule Aydin; Dilara Nemutlu Samur; Nurcan Bektas
      Pages: 541 - 545
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Rana Arslan, Sule Aydin, Dilara Nemutlu Samur, Nurcan Bektas
      It is aimed to investigate the central antinociceptive effect of protocatechuic acid and the involvement of stimulation of opioidergic, serotonin 5-HT2A/2C, α2-adrenergic and muscarinic receptors in protocatechuic acid-induced central analgesia in mice. Time-dependent antinociceptive effects of protocatechuic acid at the oral doses of 75, 150 and 300 mg/kg were tested in hot-plate (integrated supraspinal response) and tail-immersion (spinal reflex) tests in mice. To investigate the mechanisms of action; the mice administered 300 mg/kg protocatechuic acid (p.o.) were pre-treated with non-specific opioid antagonist naloxone (5 mg/kg, i.p.), serotonin 5-HT2A/2C receptor antagonist ketanserin (1 mg/kg, i.p.), α2-adrenoceptor antagonist yohimbine (1 mg/kg, i.p.) and non-specific muscarinic antagonist atropine (5 mg/kg, i.p.), respectively. The antinociceptive effect of protocatechuic acid was observed at the doses of 75, 150 and 300 mg/kg in tail-immersion test, at the doses of 150 and 300 mg/kg in hot-plate test at different time interval. The enhancement in the latency of protocatechuic acid-induced response to thermal stimuli was antagonized by yohimbine, naloxone and atropine in tail-immersion test, while it was antagonized only by yohimbine and naloxone pretreatments in hot-plate test. These results indicated that protocatechuic acid has the central antinociceptive action that is probably organized by spinal mediated cholinergic and opiodiergic, also spinal and supraspinal mediated noradrenergic modulation. However, further studies are required to understand how protocatechuic acid organizes the interactions of these modulatory systems. As a whole, these findings reinforce that protocatechuic acid is a potential agent that might be used for pain relief. Additionally, the clarification of the effect and mechanisms of action of protocatechuic acid will contribute to new therapeutic approaches and provide guidance for new drug development studies.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.001
  • Inverse docking based screening and identification of protein targets for
           Cassiarin alkaloids against Plasmodium falciparum

    • Authors: Arvind Negi; Nitisha Bhandari; Bharti Rajesh Kumar Shyamlal; Sandeep Chaudhary
      Pages: 546 - 567
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Arvind Negi, Nitisha Bhandari, Bharti Rajesh Kumar Shyamlal, Sandeep Chaudhary
      Various reports have shown Cassiarin alkaloids, selective in vitro activities against various strains of Plasmodium falciparum with low cytotoxicity, which indicates their possible candidature as antimalarial drug. However, poor recognition of their protein targets and molecular binding behaviour, certainly limits their exploration as antimalarial drug candidature. To address this, we utilises inverse screening, based on three different docking methodologies in order to find their most putative protein targets. In our study, we screened 1047 protein structures from protein data bank, which belongs to 147 different proteins. Our investigation identified 16 protein targets for Cassiarins. In few cases of identified protein targets, the binding site was poorly studied, which encouraged us to perform comparative sequence and structural studies with their homologous proteins, like as in case of Kelch motif associated protein, Armadillo repeats only protein and Methionine aminopeptidase 1b. In our study, we also found Tryptophanyl-tRNA synthetase and 1-Deoxy-D-Xylose-5-phosphate reductoisomerase proteins are the most common targets for Cassiarins.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.01.017
  • Synthesis and antibacterial activity of new
           (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid derivatives with
           thiazolidine-2,4-dione, rhodanine and 2-thiohydantoin moieties

    • Authors: Nazar Trotsko; Urszula Kosikowska; Agata Paneth; Monika Wujec; Anna Malm
      Pages: 568 - 577
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Nazar Trotsko, Urszula Kosikowska, Agata Paneth, Monika Wujec, Anna Malm
      A series of new (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid derivatives with thiazolidine-2,4-dione, rhodanine and 2-thiohydantoin moiety (28–65) were synthesized by the reaction of (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid chlorides with 5-(hydroxybenzylidene) thiazolidine-2,4-dione, rhodanine and 2-thiohydantoin derivatives. Obtained compounds (28–65) were tested on reference strains of Gram-positive bacteria and ones of the Gram-negative bacteria. The antibacterial activity of target compounds was determined by broth microdilution method. These derivatives showed antibacterial activity generally against Gram-positive bacterial strains. Most active compounds possess MIC = 3.91 mg/L. Our results suggest that presence of electron-withdrawing substituent at phenyl ring is favorable while geometry of molecule does not play important role in antibacterial response. It was confirmed the lack of direct influence of substitution pattern at phenyl ring on antibacterial activity of closely related compounds of series 1–3. The antibacterial activity of some compounds was similar or higher than the activity of commonly used reference drugs such as oxacillin and cefuroxime.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.01.016
  • Comparison between the dissolution profiles of nine meloxicam tablet
           brands commercially available in Buenos Aires, Argentina

    • Authors: Laura D. Simionato; Luciana Petrone; Mariela Baldut; Silvina L. Bonafede; Adriana Inés Segall
      Pages: 578 - 584
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Laura D. Simionato, Luciana Petrone, Mariela Baldut, Silvina L. Bonafede, Adriana Inés Segall
      In this work, the dissolution profiles of nine meloxicam tablet brands marketed in Argentina have been evaluated. As meloxicam is a Class 2 Biopharmaceutical Classification System (BSC) drug, interchangeability between commercial products must be demonstrated through in vivo bioequivalence studies. However, in our country, such studies remain to be performed. Dissolution studies have been performed according to USP 38 and evaluated by fitting experimental data to the zero and first-order, the Hixson-Crowell, the Higuchi, and the Weibull model-dependent methods. To test the pertinence of these release models, the Akaike Information Criteria (AIC) were used. All brands satisfied the dissolution profiles (phosphate buffer, pH 7.5) established in the USP. The comparison between the dissolution profiles was carried out by model-dependent and model-independent methods. The Weibull model provided the best kinetic curve adjustment. Brands I, II, IV and VI had the best fitting, with the maximum determination coefficient and the smallest AIC values. Model-independent methods included ratio test and the fit factors. The Dissolution Efficiency (DE) and Mean Dissolution Time (MDT) were analysed with ANOVA and the DGC method. In both cases, brand I did not show similarity with the rest of the brands. Using fit factors, only brands I, II and V were similar to each other. Significant differences were found among the in vitro dissolution profiles of meloxicam tablets belonging to the nine brands. As meloxicam is a class 2 BCS drug, interchangeability between commercial products must be demonstrated through in vivo bioequivalence studies. However, in Argentina, such studies remain to be performed. Our results demonstrate that caution must be exercised as regards interchangeability of generic products.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.01.015
  • Newly developed controlled release subcutaneous formulation for tramadol

    • Authors: Mostafa Mabrouk; Hanan H. Beherei; Shaimaa ElShebiney; Masaru Tanaka
      Pages: 585 - 592
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Mostafa Mabrouk, Hanan H. Beherei, Shaimaa ElShebiney, Masaru Tanaka
      This study presents a drug delivery system of poly (Ɛ-caprolactone) (PCL) ribbons to optimize the pharmaceutical action of tramadol for the first time according to our knowledge. PCL ribbons were fabricated and loaded with tramadol HCl. Ribbons were prepared by slip casting technique and coated with dipping technique with β-cyclodextrin. The chemical integrity and surface morphology of the ribbons were confirmed using FTIR and SEM coupled with EDX. In addition, thermodynamic behavior of the fabricated ribbons was investigated using DSC/TGA. Tramadol loading into PCL ribbons, biodegradation of ribbons and tramadol release kinetics were studied in PBS.The results revealed that the formulated composition did not affect the chemical integrity of the drug. Furthermore, SEM/EDX confirmed the inclusion of tramadol into the PCL matrix in homogenous distribution pattern without any observation of porous structure. The particle size of loaded tramadol was found to be in the range of (2–4 nm). The formulated composition did not affect the chemical integrity of the drug and should be further investigated for bioavailability. Tramadol exhibited controlled release behavior from PCL ribbons up to 45 days governed mainly by diffusion mechanism. The fabricated ribbons have a great potentiality to be implemented in the long term subcutaneous delivery of tramadol.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.01.014
  • Investigate the effect of solvents on wet granulation of microcrystalline
           cellulose using hydroxypropyl methylcellulose as a binder and evaluation
           of rheological and thermal characteristics of granules

    • Authors: Dharti Tank; Kapish Karan; Bhavin Y. Gajera; Rutesh H. Dave
      Pages: 593 - 602
      Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4
      Author(s): Dharti Tank, Kapish Karan, Bhavin Y. Gajera, Rutesh H. Dave
      Wet granulation is the most commonly used technique in the pharmaceutical industry for delivering oral solid dosage forms. In wet granulation, the binder solvent is one of the critical factors affecting granule properties. In the current study, an attempt was made to investigate the effect of solvents (aqueous and hydro-alcoholic) on thermal and flow properties of Microcrystalline Cellulose (MCC) granules prepared using two different grades of Hydroxypropyl Methylcellulose (HPMC), which served as an effective binder. The granulation endpoint was evaluated using thermal effusivity sensor. Rheometer and Modulated Differential Scanning Calorimetry (mDSC) was used to study the flow and thermal properties of wet and dried granules. Furthermore, physical characterization was carried out by granule strength, particle size distribution and tablet hardness for all granules under the study. Thermal effusivity sensor results indicate 55% w/w concentration of binder solution as the endpoint by measuring thermal effusivity for both binders. Additionally, powder rheometer results show that the wet granules of hydro-alcoholic batches show greater resistance to flow whereas the dried granules display excellent flow characteristics as evident from Basic flowability energy values and specific energy values. Permeability results suggest that the granules formed with hydro-alcoholic binder solvent exhibit better porosity and permeability. Tablet hardness data showed that tablets formulated using hydro-alcoholic solvent granules have greater hardness than tablets formulated using water based solvent granules. The granule strength for water based granules is relatively higher than that of hydro-alcoholic based granules. mDSC thermograms show a sharp rise in enthalpy value at 55% w/w binder solution which is indicative of a more significant amount of solvent being present on the surface of granules and formation of optimal granules. To summarize, we have determined a technique to measure endpoint determination and simultaneously investigate the role of solvent systems on the rheology of MCC granules, which could assist in selecting an appropriate solvent system for granulation.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.02.007
  • STAT3-siRNA induced B16.F10 melanoma cell death: Association with VEGF
           downregulation than p-STAT3 knockdown

    • Authors: Aws Alshamsan
      Abstract: Publication date: Available online 30 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Aws Alshamsan
      STAT3 knockdown by small interfering RNA (siRNA) has been described to inhibit carcinogenic growth in various types of tumors. Earlier we have reported delivery of siRNA by oleic acid- and stearic acid-modified-polyethylenimine and enhancement of silencing of STAT3 by small interfering RNA (siRNA) in B16.F10 melanoma cell lines and consequent tumor suppression. Present investigation mainly focused on the downstream events involved in B16.F10 melanoma cell death and consequent tumor suppression following knockdown of p-STAT3 by siRNA. Lipid-substituted polyethylenimine (PEI)-p-STAT3-siRNA were prepared and characterized by measuring its N/P ratio, zeta potential, size, association and dissociation with siRNA. B16.F10 melanoma cells were treated with six different concentrations of PEI-p-STAT3-siRNA (200, 100, 50, 25, 12.5 and 6.25 nM). Downregulation of p-STAT3 and VEGF were studied using western blot and ELISA in association with the melanoma cell death. PEI-p-STAT3-siRNA hydrodynamic diameter ranged from 110 to 270 nm. PEI assisted p-STAT3-siRNA delivery exhibited increased uptake by B16.F10, when analyzed by fluorescent and confocal microscopy along with flowcytometry. It induced concentration-dependent knockdown of the p-STAT3 that also downregulated VEGF expression in similar fashion and induced B16.F10 cell death. Higher concentrations of p-STAT3-siRNA appear to significantly downregulate the VEGF expression via p-STAT3 knockdown. Decreasing survival of B16.F10 cells with the increasing concentration of p-STAT3-siRNA significantly correlated with VEGF downregulation, not with p-STAT3 expression. Data suggest that VEGF downregulation following knockdown of p-STAT3 may be a key event in survival reduction in B16.F10 melanoma cells and.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.018
  • Effect of poplar-type propolis on oxidative stability and rheological
           properties of O/W emulsions

    • Authors: Soukaina El-Guendouz; Smail Aazza; Badiaa Lyoussi; Nessrine Majdoub; Vassya Bankova; Milena Popova; Sara Raposo; Maria Dulce Antunes; Maria Graça Miguel
      Abstract: Publication date: Available online 29 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Soukaina El-Guendouz, Smail Aazza, Badiaa Lyoussi, Nessrine Majdoub, Vassya Bankova, Milena Popova, Sara Raposo, Maria Dulce Antunes, Maria Graça Miguel
      Propolis is known to possess antioxidant activity. However, there is no information on this activity in emulsions O/W. The protective effect of propolis on the oxidation and rheological properties of emulsions O/W containing wheat germ and almond oils was evaluated. Emulsions O/W were prepared with different concentration of propolis extract, almond oil and wheat germ oil. All emulsions physically stable without phase separation were stored at 37°C for 9 weeks. Chemical composition of propolis was established by Gas chromatography coupled to mass spectrometry. Rheological characterization of different emulsions was performed evaluating consistency index and flow behaviour index. The oxidation was monitored by measuring the lipid hydroperoxides and thiobarbituric acid-reactive substances (TBARS) methods. Flavonoids, phenolic acid esters, and aromatic acids were the main groups of compounds found in propolis. The results showed that popolis was good antioxidant in the concentration of 0.02 and 0.04% when lipid phase was constituted by almond oil. The rheological behaviour is typical of a non-Newtonian fluid, being almond oil more adequate for having a higher stable O/W emulsion.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.017
  • Anticancer activity and concurrent analysis of ursolic acid, β-sitosterol
           and lupeol in three different Hibiscus species (aerial parts) by validated
           HPTLC method

    • Authors: Perwez Alam; Hanan M. Al-Yousef; Nasir A. Siddiqui; Tawfeq A. Alhowiriny; Saleh I. Alqasoumi; Musarat Amina; Wafaa Hassan Badr Hassan; Sahar Abdelaziz; Rehab H. Abdalla
      Abstract: Publication date: Available online 23 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Perwez Alam, Hanan M. Al-Yousef, Nasir A. Siddiqui, Tawfeq A. Alhowiriny, Saleh I. Alqasoumi, Musarat Amina, Wafaa Hassan Badr Hassan, Sahar Abdelaziz, Rehab H. Abdalla
      The genus Hibiscus contains about 275 species of flowering plants widely grown in the tropics and sub-tropics. The available literature revealed that several Hibiscus species exhibited excellent anticancer activity against several cancer cells like lung, breast, and liver. This motivated the authors to explore the anticancer property of other Hibiscus species (Hibiscus calyphyllus, H. deflersii and H. micranthus) along with development of a validated HPTLC method for the concurrent analysis of three anticancer biomarkers (ursolic acid, β-sitosterol and lupeol) in different Hibiscus species. The anticancer activity of various fractions (petroleum ether, toluene, dichloromethane, ethyl acetate and n-butanol) of all the Hibiscus species (aerial parts) were evaluated in vitro against HepG2 and MCF-7 cell lines using MTT assay. The HPTLC analysis was carried out using chloroform and methanol as mobile phase (97:3; v/v) on 20 × 10 cm glass-backed silica gel 60F254 plates and analyzed different phytoconstituents present in all fractions at λ = 575 nm wavelength. Of the tested fractions of H. calyphyllus, H. deflersii and H. micranthus, HdP (H. deflersii petroleum ether fraction) exhibited the most potent cytotoxic effect on HepG2 and MCF-7 (IC50: 14.4 and 11.1 μg/mL, respectively) cell lines. Using the developed HPTLC method a compact and intense peak of ursolic acid, β-sitosterol and lupeol were obtained at Rf = 0.22, 0.39 and 0.51, respectively. The LOD/LOQ (ng) for ursolic acid, β-sitosterol and lupeol were found as 42.30/128.20, 13.20/40.01 and 31.57/95.68, respectively in the linearity range 100–1200 ng/spot. The obtained result showed maximum presence of ursolic acid, β-sitosterol and lupeol (5.50, 11.85 and 7.47 μg/mg, respectively) in HdP which also supported its strong anticancer effect. Our data suggest that H. deflersii petroleum ether fraction (HdP) can be further subjected to the isolation of active cytotoxic phytoconstituents and establishment of their mechanism of action. The maiden developed HPTLC method for concurrent analysis of anticancer biomarkers may be further employed in the in process quality control of herbal formulation containing the said biomarkers.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.015
  • Quantitative determination of doxorubicin in the exosomes of A549/MCF-7
           cancer cells and human plasma using ultra performance liquid
           chromatography-tandem mass spectrometry

    • Authors: Mohammad H. Semreen; Hasan Y. Alniss; Muath K. Mousa; Rafaat El-Awady; Farman Khan; Khalid Abu Al-Rub
      Abstract: Publication date: Available online 23 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Mohammad H. Semreen, Hasan Y. Alniss, Muath K. Mousa, Rafaat El-Awady, Farman Khan, Khalid Abu Al-Rub
      In cancer therapy, exosomes efflux enhances resistance of cancer cells toward anticancer agents through mediating the transport of anticancer drugs outside the cells. In this study, a rapid, simple and highly sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for the determination of Doxorubicin (DOX) in exosomes of cancer cells and human plasma using Ketotifen as an internal standard (IS). Plasma samples spiked with DOX and two cancer cell lines (A549 & MCF-7) were incubated with different concentrations of DOX and IS. The analytes were then extracted with methanol after protein precipitation and the chromatographic separation was carried out using a C18 column, with a mixture of acetonitrile–water- formic acid (85:15:0.1%, v/v/v) as mobile phase. Multiple reaction monitoring (MRM) was utilized to monitor the protonated precursor to product ion transitions of m/z 544.25 > 397.16 and m/z 310.08 > 96.97 for the quantification of DOX and IS, respectively. The method was linear over ranges of 1–1000 ng/mL for DOX in plasma and 2–1000 ng/mL for DOX in exosome samples. The lower limit of quantification of this method was 1 ng/mL, 2 ng/mL and 2 ng/mL in human plasma, A549 & MCF-7 cells respectively. Intra- and inter day precision of all quality control concentrations were less than 10.33% and the accuracy values ranged from −4.82 to 12.60%. The optimized UPLC-MS/MS method proved to be fast, specific, simple and highly sensitive and was successfully applied for the estimation of DOX in the exosomes of cancer cells and plasma.
      Graphical abstract image

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.011
  • Development and validation of UPLC-PDA method for concurrent analysis of
           Bergenin and Menisdaurin in aerial parts of Flueggea virosa (Roxb. ex

    • Authors: Afzal Hussain; Perwez Alam; Nasir Ali Siddiqui; Mohamed Fahad Alajmi; Md Tabish Rehman; Mohd Abul Kalam; Adnan Jathlan Al-Rehaily
      Abstract: Publication date: Available online 22 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Afzal Hussain, Perwez Alam, Nasir Ali Siddiqui, Mohamed Fahad Alajmi, Md Tabish Rehman, Mohd Abul Kalam, Adnan Jathlan Al-Rehaily
      Bergenin and menisdaurin are biologically active components which are found in plant Flueggea virosa (Phyllanthaceae). Bergenin has pharmacological actions such as chemopreventive and antihepatotoxic while menisdaurin has an anti-viral activity which needs its evaluation by an analytical method (UPLC-PDA method) that can be applied to the quality control of pharmaceutical preparations. The developed UPLC-PDA method was applied for identification and quantification of standards bergenin and menisdaurin in the methanol extract of F. virosa (FVME). The analysis was carried out using Eclipse C18 (4.6 × 100 mm, 3.5 µm) UPLC column. The optimized chromatographic condition was achieved at 0.16 mL/min flow rate using gradient system with acetonitrile and water as mobile phase. Both biomarkers were measured at λmax 235 nm in PDA detector at ambient temperature. The developed method furnished sharp and intense peaks of menisdaurin and bergenin at Rt = 2.723 and 3.068 min, respectively along with r2 >0.99 for both. The recoveries of bergenin and menisdaurin were found in the range of 99.37-101.49% and 98.20-100.08%, respectively. With other validation data, including precision, specificity, accuracy, and robustness, this method demonstrated excellent reliability and sensitivity. The separation parameters i.e. retention, separation, and resolution factors for resolved standards (bergenin and menisdaurin) were >1, which showed good separation. The quantity of bergenin and menisdaurin in the FVME sample was found as 15.16 and 3.28% w/w, respectively. The developed UPLC-PDA method could be conveniently adopted for the routine quality control analysis.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.007
  • The effect of polymer length on the in vitro characteristics of a drug
           loaded and targeted silica nanoparticles

    • Authors: Areen M. Khattabi; Wamidh H. Talib; Diala A. Alqdeimat
      Abstract: Publication date: Available online 22 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Areen M. Khattabi, Wamidh H. Talib, Diala A. Alqdeimat
      The objective of this research was to investigate the effect of polymer length on the in vitro characteristics of thymoquinone-melatonin (TQ-MLT) when loaded into our previously prepared targeted drug delivery system (TDDS). Our system constructed from silica nanoparticles (NPs) and modified with diamine polymer (D4000), carboxymethyl-β-cyclodextrin (CM-β-CD) and folic acid (FA), respectively. In this study, three other different lengths of polymers (D230, D400 and D2000) were used and compared to D4000. The surface modification was characterized using fourier transform infrared spectroscopy (FTIR) and the mean particle size as well as polydispersity (PD) was measured using dynamic light scattering (DLS). The results, in general, showed that the release rate increases as the polymer length decreases. Also, shorter polymers showed an obvious burst release of most of the drug within the first hour. On the other hand, longer polymers exhibited a more sustained release in a pulsatile manner, with two moderate drug burst patterns occurred within the first and the last few hours. The in vitro cell viability assay showed that the percentage of cell toxicity toward HeLa cells increases with increasing the polymer length.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.010
  • Evaluation of anti-ulcer and ulcerative colitis of Sonchus oleraceus L

    • Authors: Esraa A. Alothman; Amani S. Awaad; Amal A. Safhi; Shekhah S. Almoqren; Reham M. El-Meligy; Yara M. Zain; Fatemal A. Alasmary; Saleh I. Alqasoumi
      Abstract: Publication date: Available online 12 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Esraa A. Alothman, Amani S. Awaad, Amal A. Safhi, Shekhah S. Almoqren, Reham M. El-Meligy, Yara M. Zain, Fatemal A. Alasmary, Saleh I. Alqasoumi
      Sonchus oleraceus L. was evaluated for its gastro antiulcerogenic and anti-ulcerative colitis activities Different extracts and fractions from Sonchus oleraceus aerial parts and roots were evaluated at different dose; total alcohol extracts of aerial parts SA and roots SR were evaluated doses 250 & 500 mg/kg, While Successive extracts (SAL, SRL, CSA, CSR, BSA & BSR) were evaluated at dose of 150 mg/kg. Absolute ethanol-induced ulcer model was used for evaluation of the anti-ulcerogenic activity. The root extract showed promising antiulcerogenic activity as the total alcohol extract of the root SR (500 mg/kg) produced 88.5% protection from control ulcer which is significantly more effective than the standard drug omeprazole (20 mg/kg), in addition, the butanol fraction of the root extract BSR also produced 76.66% protection from control ulcer. On the other hand, the aerial parts total extract SA showed low antiulcerogenic activity in both tested doses (250 & 500 mg/kg) as it produced 25% & 28.33% protection from control ulcer respectively. Only the butanol fraction of the aerial parts extract BSA showed promising activity 54.16%. In the acetic acid-induced ulcerative colitis model, among the investigated extracts of Sonchus oleraceus; only the total extract of the aerial parts (SA) at dose 500 mg/kg showed strong anti-ulcerative colitis activity and this activity is followed by the activity of the butanol and chloroform fractions of the aerial parts, they produced 77.28%, 57.4% & 47.68% protection from control colitis respectively. The standard drug dexamethasone produced 63.36% protection from control colitis. The total alcohol extracts SR & SA showed no alteration on liver and kidney functions and these extracts are safe up to 5000 mg/kg. Phytochemical screening of the investigated extracts revealed the presence of carbohydrates, flavonoids, tannins, unsaturated sterols, proteins and lactones which could be responsible for the activities.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.004
  • Drug Shortages in Saudi Arabia: Root Causes and Recommendations

    • Authors: Yazed S. Alruthia; Monira Alwhaibi; Mashal F. Alotaibi; Shatha A. Asiri; Bushra M. Alghamdi; Ghadah S. Almuaythir; Wejdan R. Alsharif; Hala H. Alrasheed; Yahya A. Alswayeh; Abdulaziz J. Alotaibi; Mohammad Almeshal; Saleh N. Aldekhail; Abdulrahman Alhusaini; Sulaiman A. Alrashed; Ali M. Alrumaih; Mohammed A. Dahhas; Mohammed A. Alghamdi; Mohammad S. Aleheidib; Mohamed H. Alhaidari; Jameel A. Alharbi; Aws Alshamsan
      Abstract: Publication date: Available online 12 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Yazed S. Alruthia, Monira Alwhaibi, Mashal F. Alotaibi, Shatha A. Asiri, Bushra M. Alghamdi, Ghadah S. Almuaythir, Wejdan R. Alsharif, Hala H. Alrasheed, Yahya A. Alswayeh, Abdulaziz J. Alotaibi, Mohammad Almeshal, Saleh N. Aldekhail, Abdulrahman Alhusaini, Sulaiman A. Alrashed, Ali M. Alrumaih, Mohammed A. Dahhas, Mohammed A. Alghamdi, Mohammad S. Aleheidib, Mohamed H. Alhaidari, Jameel A. Alharbi, Aws Alshamsan
      Drug shortages are a multifaceted problem that has been recurring in Saudi Arabia over the past decade with its significant negative impact on patient care. However, there is a dearth of evidence about possible domestic reasons, if any, behind this recurring problem. Recently, the Pharmacy Education Unit at King Saud University College of Pharmacy has called for a meeting with multiple stakeholders from academia, pharmaceutical care, pharmaceutical industry, purchasing and planning, and regulatory bodies to unveil the root domestic causes of the drug shortages in the Kingdom. Four major topics were used to guide the discussion in this meeting, including: current situation of drug shortages in Saudi Arabia, major factors contributing to drug shortages, challenges and obstacles to improve drug supply, and stakeholders’ recommendations to manage drug shortages. The meeting was audio-recorded and transcribed into verbatim by five authors. The text was then reviewed and analyzed to identify different themes by the first author. Multiple causes were identified and several recommendations were proposed. The main domestic causes of drug shortages that were explored in this study included poor medication supply chain management, lack of government regulation that mandates early notification of drug shortages, a government procurement policy that does not keep pace with the changes in the pharmaceutical market, low profit margins of some essential drugs, weak and ineffective law-violation penalties against pharmaceutical companies and licensed drug importers and distributors, and overdependence on drug imports. The participants have also proposed multiple recommendations to address drug shortages. Policy makers should consider these factors that contribute to drug shortages in Saudi Arabia as well as the recommendations when designing future initiatives and interventions to prevent drug shortages.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.002
  • Anticancer effect of Cenchrus ciliaris L

    • Authors: Esraa A. Alothman; Amani S Awaad; Norah A. Al-Qurayn; Haya F. Al-Kanhal; Reham M. El-Meligy; Yara M. Zain; Fatemal Ali Alasmary; Saleh I. Alqasoumi
      Abstract: Publication date: Available online 12 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Esraa A. Alothman, Amani S Awaad, Norah A. Al-Qurayn, Haya F. Al-Kanhal, Reham M. El-Meligy, Yara M. Zain, Fatemal Ali Alasmary, Saleh I. Alqasoumi
      Cenchrus ciliaris L total alcohol and successive extracts of both aerial and root parts were tested for their anticancer activities against lung (A-549), intestinal (CACO), colon (HCT-116), cervical (Hela), hepatocellular (HepG-2), and breast (MCF-7) (PC3) cell lines and compared with the standard drug vinblastine sulphate. The obtained results exhibited direct cytotoxic effect with variable inhibiting effect on the growth of the listed cell lines comparing to vinblastine sulphate as reference standard drug, these effects showed different IC50 ranged from 11.1 ± 0.3 to 267 ± µg/ml. All root extracts showed the best activities against most of the tested cell lines specially HepG-2 (Hepatocellular carcinoma) (9 ± 2.1 µg/ml) which was somewhat closely related to the effect of vinblastine sulphate (2.93 ± 0.3 µg/ml). The highest anticancer effect of Cenchrus ciliaris L aerial parts and root extracts were recorded on HepG-2 (Hepatocellular carcinoma) their IC50 were 12 ± 0.8 & 9 ± 2.1 respectively, CACO (colorectal carcinoma) their IC50 were 27.2 ± 1.6 & 20.5 ± 0.6 respectively, A-549 (Lung carcinoma) their IC50 were 14.5 ± 0.7& 11.1 ± 0.3 respectively which were better than the standard drug especially in case the anticancer effect on CACO (colorectal carcinoma) and A-549 (Lung carcinoma). Chloroform extracts of both aerial and roots achieved the best anticancer activities on all of the cell lines especially with colorectal (CACO) and Lung carcinoma (A-549). Cenchrus ciliaris could be a promising source of new chemical moieties used to target cancer cells.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.003
  • The relationship between blood eosinophil count and disease activity in
           ankylosing spondylitis patients treated with TNF-α inhibitors

    • Authors: Gokhan Sargin; Taskin Senturk; Irfan Yavasoglu
      Abstract: Publication date: Available online 4 May 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Gokhan Sargin, Taskin Senturk, Irfan Yavasoglu
      Aim Anti-tumor necrosis factor-alpha (Anti-TNF-α) therapy has achieved an important position, are widely used for ankylosing spondylitis (AS) patients. TNF-α inhibition improves clinical outcomes and has differential effects on haematopoiesis. Information about effects on eosinophils is limited. The aim of our study is to determine the relationship between blood eosinophil counts in AS patients treated with TNF-α inhibitors. Methods Seventy-five patients diagnosed with AS according to modified New York criteria were enrolled in this study. Disease activity was assessed by BASDAI, and erythrocyte sedimentation rate, C-reactive protein of patients were evaluated. All data were analyzed with Spearman’s correlation and Friedman's Two-Way by using SPSS version 19.0 statistical software, and p < 0.05 was considered as statistically significant. Results Seventy-five AS (F/M: 27/48, the mean age of 41 ± 10 years) patients were evaluated. On the 3rd month of treatment, there was a correlation between BASDAI and CRP (r = 0.32, p = 0.005), but no correlation between BASDAI and ESR (r = 0.21, p = 0.06). Blood eosinophil count was not correlated with BASDAI, ESR and CRP on pre-, post-therapy (p > 0.05). It counts lower before anti-TNF-α therapy compare with post-treatment (130/mm3, 140/mm3 and 190/mm3, respectively). There was no statistically significant difference between pre- and 3rd month (p > 0.05), while correlation was found between pre- and 6th month, and also 3rd month and 6th month (p < 0.001, p = 0.002, respectively) for blood eosinophil count. Conclusion To the best of our knowledge, our study is the first to evaluate blood eosinophil counts and disease activity with anti-TNF-α therapy. Blood eosinophil count may be affected by TNF-α inhibition in patients with AS.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.05.001
  • Inside Front Cover - Editorial Board

    • Abstract: Publication date: May 2018
      Source:Saudi Pharmaceutical Journal, Volume 26, Issue 4

      PubDate: 2018-05-31T16:08:43Z
  • Knowledge, attitudes & practices of healthcare professionals in
           hospitals towards the reporting of adverse drug reactions in Saudi Arabia:
           A multi-centre cross sectional study

    • Authors: Thamir M. AlShammari; Mohammed J. Almoslem
      Abstract: Publication date: Available online 26 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Thamir M. AlShammari, Mohammed J. Almoslem
      Introduction Adverse drug reactions (ADRs) are a major global clinical problem, causing substantial mortality and morbidity especially in hospitals. Healthcare professionals (HCPs) knowledges’, attitude and practices are crucial points to evaluate the hospital safety environment. Objective of the study was to investigate the knowledge, attitudes, and practices of HCPs regarding the ADRs reporting system. Methods A cross-sectional survey was conducted between January and February of 2013 in nine tertiary care hospitals (governmental and private) that provide highly specialized medical services in Riyadh, Qassim, and the Eastern region of the Kingdom of Saudi Arabia. A validated questionnaire was used to assess the knowledge, attitudes, and practices of HCPs regarding the ADR reporting system. All statistical analyses were performed using SAS version 9.2. Results In total, 480 questionnaires were distributed, and the response rate was 70% (n = 336). Only 33% of the participants were aware of the National Pharmacovigilance Centre (NPC). Of those HCPs who were familiar with the NPC and their responsibility to report ADRs, most (50%) were pharmacists, followed by physicians (24%) and nurses (16%), and these differences were statistically significant (p < 0.01). Twenty-seven percent of the participants were involved in reporting ADRs; among these HCPs, 62% were pharmacists, 26% were nurses, and 6% were physicians. Most participants (95%) favoured reporting ADRs caused by antibiotics and new/old drugs. The prominent factors discouraging ADR reporting included fear that the report might be incorrect (46%) and lack of time (44%). Conclusions A significant lack of knowledge, positive attitudes, and practices regarding ADRs and reporting was observed in hospital HCPs. This finding represents an international concern, and urgent action is needed to promote drug safety and pharmacovigilance in this region.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.04.012
  • Physical and chemical screening of honey samples available in the Saudi
           market: An important aspect in the authentication process and quality

    • Authors: Haya I. Aljohar; Hadir M. Maher; Jawza Albaqami; Maha Al-Mehaizie; Rawan Orfali; Razan Orfali; Sarah Alrubia
      Abstract: Publication date: Available online 25 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Haya I. Aljohar, Hadir M. Maher, Jawza Albaqami, Maha Al-Mehaizie, Rawan Orfali, Razan Orfali, Sarah Alrubia
      Honey is becoming accepted as a reputable and effective therapeutic agent by practitioners of conventional medicine and by the general public. It has many biological activities and has been effectively used in the treatment of many diseases, e.g. gastrointestinal diseases, skin diseases, cancer, heart diseases, and neurological degeneration. Honey is an excellent source of energy containing mainly carbohydrates and water, as well as, small amounts of organic acids, vitamins, minerals, flavonoids, and enzymes. As a natural product with a relatively high price, honey has been for a long time a target for adulteration. The authenticity of honey is of great importance from commercial and health aspects. The study of the physical and chemical properties of honey has been increasingly applied as a certification process for the purpose of qualification of honey samples. The current work focusses on studying the authenticity of various types of honey sold in Riyadh market (24 samples). For this purpose, physical properties (pH, hydroxylmethylfurfural HMF, and pollen test) were measured. Besides, sugar composition was evaluated using Fehling test and an HPLC method. Elemental analysis was carried out using inductively coupled plasma (ICP). In addition, the presence of drug additives was assessed by means of GC–MS. The obtained results were compared with the Saudi Arabian standards, Codex Alimentarius Commission (2001), and harmonized methods of the international honey commission.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.04.013
  • Development of differentiated pharmaceutical packaging for greater
           autonomy and quality of life for physically and visually impaired patients

    • Authors: Beatriz Gamberini Cernic; Ana Carolina Kogawa; Hérida Regina Nunes Salgado
      Abstract: Publication date: Available online 25 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Beatriz Gamberini Cernic, Ana Carolina Kogawa, Hérida Regina Nunes Salgado
      20–45% of the world population present special needs, permanent or provisional. This index is higher than that presented by the WHO, which determines that 10% of a country's population has some kind of disabled, in times of peace. This work proposes, focused on Assistive Technology, to seek solutions to daily problems encountered during the distribution of toothpaste for the toothbrushing of persons with visual impairment or with reduced mobility, through the development of a device that assists in the autonomy and independence of the individual, allowing their well-being and social inclusion. For this, an innovative packaging for toothpaste with important characteristics for the support was proposed, such as the presence of a pump valve and an adapter that guides the user to locate the exit of a predefined quantity of the toothpaste, without the need to handle the bristles of the brush, avoiding contaminations. The developed packaging material allows the user independence in day-to-day activities, which strengthens their self-esteem and quality of life, leading, consequently, to family well-being.

      PubDate: 2018-05-31T16:08:43Z
      DOI: 10.1016/j.jsps.2018.04.011
  • Patterns of antibiotic use and administration in hospitalized patients in

    • Authors: Anan S. Jarab; Tareq L. Mukattash; Buthaina Nusairat; Mohammad Shawaqfeh; Rana Abu Farha
      Abstract: Publication date: Available online 18 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Anan S. Jarab, Tareq L. Mukattash, Buthaina Nusairat, Mohammad Shawaqfeh, Rana Abu Farha

      PubDate: 2018-04-25T16:18:09Z
      DOI: 10.1016/j.jsps.2018.04.009
  • Sodium polystyrene sulfonate induced intestinal necrosis; a case report

    • Authors: Abdulaziz Saleh Almulhim; Edina Hall; Bassam Mershid Al Rehaili; Abdulmuhsin Saleh Almulhim
      Abstract: Publication date: Available online 12 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Abdulaziz Saleh Almulhim, Edina Hall, Bassam Mershid Al Rehaili, Abdulmuhsin Saleh Almulhim
      Background Hyperkalemia is a commonly encountered medical problem. The treatment of hyperkalemia involves the use of pharmacological agents with different mechanism of actions. Sodium Polystyrene sulfonate (SPS) is a cation-exchange resin that exchanges sodium for potassium. In 2009, the United States Food and Drug Administration issued warning against the use of SPS with sorbitol due to risk of colonic necrosis. We present a case of SPS induced colonic necrosis in the absence of sorbitol and risk factors deemed to increase risk of colonic necrosis. Case report Here we report a 64-year old male with past medical history of kidney stones who was admitted for treatment of colitis which was complicated by septic shock requiring vasopressors. His course was further complicated by hyperkalemia attributed to acute kidney injury. One dose 30 gm of SPS was administered which normalized his serum potassium. The patient’s course was complicated by duodenal ulcer, and colonic perforation. The initial pathology findings of the resected specimen were suggestive of inflammatory bowel disease which resulted in starting patient on mesalamine. The patient then developed fistula which was resected and sent for pathology. SPS induced colonic necrosis was made based on the pathology findings. Conclusion SPS is commonly used to decrease potassium levels. SPS has been reported to be associated with several gastrointestinal complications. FDA issued warning against the use of SPS in patients at risk for complications. Here we report a case with SPS induced colonic necrosis in the absence of risk factors reported in the literature.

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.04.008
  • A Survey on Traditional Plants Used in Al Khobah Village

    • Authors: Maged S. Abdel-Kader; Ali M.A. Hazazi; Osman A. Elmakki; Saleh I. Alqasoumi
      Abstract: Publication date: Available online 11 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Maged S. Abdel-Kader, Ali M.A. Hazazi, Osman A. Elmakki, Saleh I. Alqasoumi
      The use of traditional medicine for treatment of various diseases is a common practise in most of the developing countries including the Kingdom of Saudi Arabia especially in rural areas. In this survey, Al Khobah village was selected to study the status of Traditional Medicine. Al Khobah village is located on the Southern boarders of the kingdom and characterized by diverse topography and moderate weather. The plants with medicinal uses were collected, identified and their methods of preparation and uses were recorded. After gathering all these information from the local people, literature survey was conducted on each plant to get information about pharmacological activities and weather they support the traditional use or not. The survey revealed that the uses of some plants are consistent with the experimental data in the literature. Some other plants were studied; however, they still need pharmacological investigation to prove the claimed uses. Other plant did not subject to any scientific investigation.

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.04.001
  • An Exploration of Parents’ Knowledge, Attitudes and Practices Towards
           the Use of Antibiotics in Childhood Upper Respiratory Tract Infections in
           a Tertiary Jordanian Hospital

    • Authors: Khawla Abu Hammour; Mariam Abdel Jalil; Walid Abu Hammour
      Abstract: Publication date: Available online 7 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Khawla Abu Hammour, Mariam Abdel Jalil, Walid Abu Hammour
      Objectives The present study aimed to evaluate the parents' knowledge, attitudes and practices (KAP) towards the use of antibiotics for childhood upper respiratory tract infections (URTIs), at the Jordanian University Hospital. Methods This was a cross-sectional study. During the study period, 1301 parents of young children completed a validated –structured questionnaire. Results Gaps in common knowledge related to antibiotics and their use were noted among participants. Nearly half of respondents believed that antibiotics are void from adverse effects, while 72.4% of them believed that a child should be given an antibiotic if it develops fever, even though 60% they were aware that most URTIs were viral in nature. Parents reported that they administered antibiotics to children without medical advice most of the time for various causes, including using a previously prescribed antibiotic for a similar illness (27.1%), or based on pharmacist's recommendation (23.8%). Conclusion The results demonstrated the need for educational interventions to increase the awareness of parents about antibiotics to reduce inappropriate use and its consequences

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.04.006
  • New derivatives of hydrogenated pyrido[4,3-b]indoles as potential
           neuroprotectors: Synthesis, biological testing and solubility in
           pharmaceutically relevant solvents

    • Authors: Svetlana Blokhina; Angelica Sharapova; Marina Ol'khovich; Anatoly Ustinov; German Perlovich
      Abstract: Publication date: Available online 6 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Svetlana Blokhina, Angelica Sharapova, Marina Ol'khovich, Anatoly Ustinov, German Perlovich
      The derivatives of hydrogenated pyrido[4,3-b]indoles as potential neuroprotectors have been synthesized. The different substituents were introduced into position 8 of the carboline fragment of the molecule: methyl-, methoxy-, fluorine- and chlorine-. Biological tests have shown that all the studied compounds can modulate glutamate-dependent uptake of calcium ions in rats’ cerebral cortex synaptosomes. The shake-flask method was used to measure the solubility of the compounds in the buffer solution (pH 7.4), hexane and 1-octanol within the temperature interval of 293.15–313.15 К. All the derivatives have been found to have low solubility (not exceeding 8 ∙ 10−4 mole fractions) in the mentioned solvents. The effect of thermophysical and protolytic properties of the compounds on the solubility have been studied and the thermodynamic functions of compounds dissolution in the solvents used have been calculated.

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.04.003
  • Vitamin B12 protects against DNA damage induced by hydrochlorothiazide

    • Authors: Karem H. Alzoubi; Erva Bayraktar; Omar Khabour; Sayer I. Al-Azzam
      Abstract: Publication date: Available online 3 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Karem H. Alzoubi, Erva Bayraktar, Omar Khabour, Sayer I. Al-Azzam
      DNA damage induced by hydrochlorothiazide was previously reported in cultured human lymphocytes. In this study, we aimed to investigate the harmful effects of hydrochlorothiazide on DNA by measuring the spontaneous frequency of sister chromatid exchanges (SCEs) in cultured human lymphocytes. We also aimed to investigate the possible protection of that damage by vitamin B12. The results showed that hydrochlorothiazide (5 µg/mL) significantly increased the frequency of sister chromatid exchanges (P < 0.001) in human lymphocytes in comparison with control. Additionally, the frequency of hydrochlorothiazide-induced SCEs was significantly decreased by co-treatment with vitamin B12 at concentration of 13.5 µg/mL (P < 0.001). In conclusion, hydrochlorothiazide is genotoxic to human lymphocytes and its toxicity is reduced by vitamin B12.

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.04.005
  • Antibacterial prophylaxis in pediatric patients with leukemia

    • Authors: Suha Al Omar; Deema Moumani; Rawad Rihani
      Abstract: Publication date: Available online 3 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Suha Al Omar, Deema Moumani, Rawad Rihani
      Background Bacterial infections in pediatric patients with leukemia are associated with increased risks for morbidity and mortality. Few Recommendations have been made on the use of antibacterial prophylaxis in pediatrics with acute lymphoblastic leukemia (ALL) or acute myeloid leukemia (AML). Objectives To determine the role of antibacterial prophylaxis in pediatric patients with leukemia and the most appropriate regimen that can be safely and effectively used. Methods Literature search was conducted independently by 3 reviewers to find studies on the safety and effectiveness of antibacterial prophylactic regimens. Results The search strategy resulted in 13 studies; most of them were observational studies. The available evidence recommends use of antibiotics with Gram-positive bacterial coverage in AML patients. In ALL patients, prophylaxis was used during the intensive phases of chemotherapy with ciprofloxacin being recommended most commonly. Conclusion Antibacterial prophylaxis mainly with coverage against Gram-positive bacteria is recommended in pediatric patients with AML. For ALL patients, prophylaxis may be considered for patients who are undergoing intensive chemotherapy phases and are at high risk for infections with ciprofloxacin being the most commonly used agent. In general more studies are needed to determine the role of antibacterial prophylaxis in pediatric patients with leukemia.

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.04.002
  • Nanostructured liquid crystalline formulation as a remarkable new drug
           delivery system of anti-epileptic drugs for treating children patients

    • Authors: Hadel Abo El-Enin; Areej Hamed AL-Shanbari
      Abstract: Publication date: Available online 3 April 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Hadel Abo El-Enin, Areej Hamed AL-Shanbari
      Purpose Development of a new dosage-form of antiepileptic-drugs appropriated for children. Methods Clonazepam (Cl) was formulated as cubosomal-gel (cub-gel) to be used as a patch reservoir through transdermal-route. Cubosomes prepared using glycerol-mono-oleate(GMO)/Pluronic-F127(PF127) mixture. An actual-statistical design was used to investigate the effect of different stabilizing agents (Ethanol and PVA) and surfactant concentration on cubosomes’ particle size and entrapping-efficiency. The selected formulae were evaluated by testing particle-morphology, in vitro drug release and stability. Cub-gel was prepared using selected cubosome formulae. The optimal cub-gel subjected to in vitro dissolution, ex-vivo permeation and skin deposition studies followed by studying its pharmacological effect. Results Using PVA or Et as stabilizers with PF127 significantly decreases the average cubosomes’PS (352 ±  2.8 and 264 ± 2.16 nm) and increases EE (58.97 ± 4.57% and 54.21 ± 3.89%). Cubosomes increase the initial release rate of Cl to ensure rapid therapeutic effect (37.39% and 46.04% in the first hour) followed by a prolonged release till 4 h. Cub-gel containing PVA showed significantly higher Cl-transdermal permeation when compared to Cl-suspension. Moreover, increases the retention-time (89.57% at 48 h) and skin-deposition up to 6-times. It also reduces the epileptic seizures and alters the behavioral parameters induced by pilocarpine. Conclusions Cubosomal-gel could be considered an innovative dosage-form for Cl through the transdermal route.

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.04.004
  • Investigation of antioxidant compounds in commercial pomegranate molasses

    • Authors: Y.T. Kamal; Prawez Alam; Saleh Ibrahim Alqasoumi; Ahmed Ibrahim Foudah; Mohammed Hamed Alqarni; Hasan Soliman Yusufoglu
      Abstract: Publication date: Available online 30 March 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Y.T. Kamal, Prawez Alam, Saleh Ibrahim Alqasoumi, Ahmed Ibrahim Foudah, Mohammed Hamed Alqarni, Hasan Soliman Yusufoglu
      Pomegranate is a well known fruit for its unique flavor, taste and health benefits. The medicinal properties of this fruits directly associated with the phenolic content present, with great anti-oxidant potential. The research is intended to develop matrix solid phase dispersion method (MSPD) and HPLC quantification of four major anti-oxidant marker constituents (vitamin C, gallic acid, rutin & ellagic acid) in pomegranate molasses samples. The effects of several important experimental parameters like type of dispersant, sample-dispersant ratio, solvents and its volume, time of extraction were investigated. A C18 column with the specification (5 µm, 250 × 4.0 mm) was used for the separation. A gradient flow of mobile phase was selected after many trials containing 0.1%, v/v solution of orthophosphoric acid and acetonitrile. The flow rate was 1.0 mL/min; and the chromatograms were recorded at 254 nm. The validation parameters, like linearity (r2 = 0.9985, 0.9965, 0.9925 & 0.9986), accuracy (100.3, 99.5, 100.9 & 101.9%), intra-day precision (%RSD = 1.09, 1.02, 1.26 & 0.97), inter-day precision (%RSD = 1.32, 0.83, 1.07, & 1.15) LOD (0.07, 4.50, 0.45 & 0.40 µg/mL), LOQ (0.095, 9.50, 0.85 & 9.5 µg/mL) and robustness (% RSD = 0.92, 0.76, 0.81 & 0.83) respectively for vitamin C, gallic acid, rutin & ellagic acid, were found satisfactory as per ICH guidelines.

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.03.015
  • Use of herbal extract from Artemisia herba-alba (Shih) in pharmaceutical
           preparations for dental hygiene

    • Authors: Amanullah Mohammed; Sadatullah Syed; M.Yaseen Syed; Azhar Dawasaz Ali
      Abstract: Publication date: Available online 30 March 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): Amanullah Mohammed, Sadatullah Syed, M.Yaseen Syed, Azhar Dawasaz Ali
      Antibiotic resistance in bacterial species is opening new avenues to search for alternative modes of antimicrobial treatment, medicinal plant extracts being one among them. The aim of this study was to access the possibility of medicinal plant extract from Shih in the manufacture of pharmaceutical preparations for oral hygiene specifically for the prevention and treatment of dental caries due to Streptococcus mutans. Antimicrobial effects of crude organic extract of Shih on S. mutans isolated from the saliva were examined by taking S. mutans with culture media only (−ve control); S. mutans treated with the antibiotic gentamicin (+ve control) and S. mutans treated with Shih. Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) were Determination by Iodonitrotetrazolium chloride (INT) colorimetric assay Time-kill dynamic assay was performed using broth microdilution method. The metabolic reason behind the bacteriostatic and bactericidal effect were studied by measuring the glucose utilization by the microbes, pH as a measure of acid production, nucleic acids quantitation to check the DNA status and inhibition of water-insoluble glucan synthesis were undertaken. Shih MIC for S. mutans was at 2.5 mg/ml and MBC was 4 mg/ml. S. mutans bacterial population started reclining within 60 min of incubation with Shih at MBC. Utilization of added glucose was very high at MIC due to bacteria overcoming the stress, whereas at MBC its utilization was less. Accordingly pH also became acidic to 2.9 with MIC and 4.03 with MBC. There was a great degree of inhibition in the formation of nucleic acids indicating this crude extract interferes with DNA replication. Inhibition of glucan synthesis was to the tune of 45% as compared to control. Thus we conclude that Shih has potentially effective antibacterial activity hence it can be proposed as a potentially effective antiplaque and anticariogenic agent in the form of mouth wash or gum paint. However, the cytotoxicity of the extract needs to be evaluated in in-vitro and in-vivo conditions before it is considered as a safe antiplaque and anticariogenic agent.

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.03.017
  • Evaluation of teratogenicity and genotoxicity induced by kramecyne (KACY)

    • Authors: J.M. Cristóbal-Luna; N. Paniagua-Castro; G.N. Escalona-Cardoso; M.S. Pérez-Gutiérrez; I. Álvarez-González; E. Madrigal-Bujaidar; G. Chamorro-Cevallos
      Abstract: Publication date: Available online 29 March 2018
      Source:Saudi Pharmaceutical Journal
      Author(s): J.M. Cristóbal-Luna, N. Paniagua-Castro, G.N. Escalona-Cardoso, M.S. Pérez-Gutiérrez, I. Álvarez-González, E. Madrigal-Bujaidar, G. Chamorro-Cevallos
      Kramecyne (KACY), a polymer isolated from Krameria cytisoides Cav, has anti-inflammatory, anti-nociceptive, anti-arthritic and anti-ulcerogenic properties. As a part of standard preclinical safety tests, the present study sought to determine potential developmental toxicity (in female rats) and genotoxicity (in male mice) of KACY. Pregnant female rats were divided into six groups: the negative control (vehicle), the positive control (250 mg/kg of acetylsalicylic acid (ASA)), and four experimental groups (50, 250, 500 and 1000 mg/kg of KACY). To evaluate genotoxicity by in vivo micronuclei (MN) and sister chromatid exchange (SCE) tests, male mice were divided into five groups: the negative control (vehicle), the positive control (1.5 and 2.5 mg/kg of doxorubicin for MN and SCE, respectively), and three experimental groups (50, 500 and 1000 mg/kg of KACY). All treatments were administered by oral gavage. A slight maternal toxicity was evidenced by lower weight gain for rats receiving 500 and 1000 mg/kg of KACY, but no fetal malformations were found. However, there were less live fetuses/litter and greater post-implantation loss/litter at these two doses. Manifestations of developmental toxicity were limited to a higher rate of skeletal alterations. The MN tests did not evidence genotoxicity or cytotoxicity. KACY caused a slightly but significantly increased frequency of SCE. Although KACY-treated rats had skeletal alterations, these apparently were not caused by a mechanism of genotoxicity. Furthermore, the same administration in adult male mice did not produce genotoxicity. Hence, KACY herein proved to be safe for rats during the period of organogenesis.

      PubDate: 2018-04-15T10:09:19Z
      DOI: 10.1016/j.jsps.2018.03.016
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