فهرست مطالب

Pharmaceutical Sciences - Volume:22 Issue: 3, Sep 2016

Pharmaceutical Sciences
Volume:22 Issue: 3, Sep 2016

  • تاریخ انتشار: 1395/07/12
  • تعداد عناوین: 10
|
  • Daniel R. Delgado, Mar, Iacute, A. A. Pe, Ntildea., Fleming Martinez*, Abolghasem Jouyban, William E. Acree Jr Pages 143-152
    Background
    Dissolution thermodynamic quantities of sulfapyridine (SP) have been reported in the literature for aqueous alcoholic mixtures. Nevertheless, no attempts to evaluate the preferential solvation of this drug in this binary system, have been reported. In this way, the inverse Kirkwood-Buff integrals (IKBI) were used to evaluate this behavior in solution.
    Methods
    Solubility data for SP dissolved in binary ethanol (EtOH) water mixtures at various temperatures were mathematically represented using the Jouyban-Acree (J-A) model. The preferential solvation parameters of SP by EtOH (δx1,3) in EtOH water mixtures were obtained from some thermodynamic properties of the mixtures by means of the IKBI method.
    Results
    Solubility of SP in EtOH water mixtures is adequately described by the J-A model in second order. Moreover, SP is sensitive to specific solvation effects, so the δx1,3 values are negative in water-rich and EtOH-rich mixtures indicating preferential solvation by water in these mixtures. By contrary, δx1,3 values are positive in the range 0.24
    Conclusion
    It can be assumed that in water-rich mixtures the hydrophobic hydration around the aromatic rings plays a relevant role in the solvation. The higher drug solvation by EtOH in mixtures of similar solvent proportions could be due to polarity effects. Moreover, in EtOH water mixtures SP could be acting as a Lewis acid with the EtOH molecules and in EtOH-rich mixtures the drug could be acting as a Lewis base with water molecules.
    Keywords: Sulfapyridine_Ethanol + water mixtures_Jouyban_Acree model_Preferential solvation
  • Maryam Maghsoodi, Mahdieh Rahmani, Hamed Ghavimi, Seyed Hassan Montazam, Saieede Soltani, Mitra Alami, Sara Salatin, Mitra Jelvehgari* Pages 153-163
    Background
    Sumatriptan succinate is a 5-HT1 receptor agonist which is used in the treatment of migraine. It shows low bioavailability (15%) due to high hepatic first pass metabolism. The present work intended to formulate mucoadhesive sublingual films of sumatriptan combined with metoclopramide and sumatriptan alone with the objective of improving the therapeutic efficacy, patient compliance, and bioavailability.
    Methods
    The sublingual films were formulated by solvent casting technique using mucoadhesive polymer of hydroxypropyl methylcellulose and propylene glycol as plasticizers. This study was also designed to evaluate the physicochemical and mucoadhesive characteristics of the films. The films were evaluated for their mechanical strength, folding endurance, drug content uniformity, swelling, in vitro residence time, in vitro release, in vitro bioadhesion, and in vivo mucoadhesion.
    Results
    They showed good appearance and elasticity. The best drugs of polymer ratio were S3 (1:2) and SM2 (2.7:1:8). The film of S3 and SM2 showed 10.6 and 11.01 mg weight, 2.2 and 22.5 µm thickness, 300 folding endurance, 55.9 and 100% content uniformity, respectively. The Differential Scanning Calorimetry (DSC) showed no stable sample of sumatriptan and metoclopramide in the drug loaded films and revealed amorphous form and transition of hydrate to anhydrous form for metoclopramide. The results showed that the films prepared were fast dissolving. The films (sumatriptan combined with metoclopramide and sumatriptan alone) exhibited very good mucoadhesive properties and shorter retention time (15-30 s).
    Conclusion
    The formulations were found to be suitable candidates for the development of sublingual films for therapeutic uses.
    Keywords: Sumatriptan succinate, Metoclopramide, Mucoadhesive, Hydroxypropyl methylcellulose, Film
  • Ashish Kumar Gupta, Ritam Muhury, Deepak Ganjewala* Pages 164-169
    Background
    Cymbopogon flexuosus popularly known as lemongrass provides a lemon scented essential oil which is widely used in flavour and fragrance, perfumery, food and pharmaceuticals. The aim of the present study was to assess antimicrobial activities of essential oils of three lemongrass cultivars viz., Pragati, Praman and Suvarna.
    Methods
    Essential oils were isolated from one month old plants by hydro-distillation in mini Clevenger apparatus for 2 h. Antimicrobial activities were determined by agar well diffusion
    Results
    Lemongrass oils exhibited strong antimicrobial activity against all the microbes except E coli. Mean inhibition zone diameter (mm) against bacteria was ranged 27-38 mm. B. Subtilis was the most sensitive bacterium to all essential oils. Essential oils also showed strong antifungal effects against both A. niger and C. albicans with mean inhibition zone diameter (mm) values 20-26 and 27-29 mm, respectively. Statistical analyses revealed that antimicrobial activity shown by essential oils were significant (p > 0.05).
    Conclusion
    The study revealed strong antimicrobial potential of the essential oil against pathogenic microbial strains which may be of high clinical importance in future.
    Keywords: Cymbopogon flexuosus, Lemongrass, Essential oil, Citral, Agar well diffusion, Antimicrobial
  • Akram Jamshidzadeh, Reza Heidari*, Farzaneh Abazari, Maral Ramezani, Forouzan Khodaei, Mohammad Mehdi Ommati, Maryam Ayarzadeh, Roya Firuzi, Arastoo Saeedi, Negar Azarpira, Asma Najibi Pages 170-180
    Background
    Chloroquine and amodiaquine are used in the prophylaxis and treatment of malaria. However, hepatic injury is associated with malaria drug therapy. On the other hand, there is no promising hepatoprotective agent for prophylaxis or treatment of antimalarial drugs‑induced liver injury. Carnosine is a naturally occurring peptide with pleiotropic protective properties in different tissues. This investigation aimed to evaluate the effect of carnosine administration in antimalarial drugs-induced hepatic injury in rats.
    Methods
    Animals were treated with amodiaquine (180 mg/kg, oral) or chloroquine (970 mg/kg, oral). Carnosine (250, 500 and 1000 mg/kg, i.p) was administered as the hepatoprotective agent against antimalarial drugs liver injury.
    Results
    Liver injury was manifested biochemically by a significant increase in serum level of ALT, LDH, and AST. In addition, hepatic tissue from antimalarial drugs‐treated rats showed a significant increase in reactive oxygen species (ROS), lipid peroxidation and protein carbonylation along with a decrease in hepatic glutathione reservoirs and total antioxidant capacity. Moreover, the liver histopathologic evaluation revealed significant congestion, inflammation, and necrosis in amodiaquine and/or chloroquine-treated animals. Carnosine administration significantly alleviated antimalarial drugs-induced pathologic changes in serum biochemistry and liver tissue.
    Conclusion
    Our data suggest that carnosine possesses protective properties against amodiaquine and/or chloroquine‑induced liver injury possibly through mitigation of drug-induced oxidative stress and its consequent events.
    Keywords: Antimalarial agents, Drug, induced liver injury, Hepatoprotection, Malaria, Peptide
  • Vali Ahmadi, Jalil Karnoosh, Yamchi, Akbar Aliasgharzadeh, Alireza Ostad, Rahimi, Zeinab Nikniaz, Roya Salehi, Majid Mobasseri* Pages 181-185
    Background
    This pilot study was designed to investigate the effect of orally delivered nanohydrogel insulin on serum glucose and insulin levels in patients with type 2 diabetes (T2DM).
    Methods
    In this pilot before-after study, 8 T2DM patients received 300 IU insulin loaded nanohydrogel orally and the serum concentration of glucose and insulin were measured before treatment and consecutively during treatment. The area under the curve (AUC) was calculated for serum glucose and insulin and repeated measures of ANOVA, paired t-test were used for statistical analysis.
    Results
    The changes in serum glucose level was not significant pretreatment (p=0.10) and during oral insulin treatment (p=0.71). Compared with pretreatment value, the serum glucose level was significantly lower in 7 A.M. (immediately after insulin therapy) and 8.30 A.M. during oral insulin treatment. The maximum reduction was observed 1.5 hours after insulin therapy and its effect lasted for more than 6 hours. The mean AUC of glucose was insignificantly decreased (p=0.16). The pretreatment (p=0.10) and during treatment (p=0.30) changes in serum insulin level were not statistically significant. The serum insulin level was increased significantly immediately after oral insulin therapy compared with pretreatment values. The mean AUC of insulin increased marginally significant (p=0.056).
    Conclusion
    The results of the present pilot study showed that 300IU nanohydrogel oral insulin was effective in rapid lowering of serum glucose and its glucose lowering effect lasting for more than 6 hours. However, for any precise conclusions further studies with longer duration are needed.
    Keywords: Nanohydrogels, Insulin, Diabetes mellitus type 2
  • Elaheh Shafiee, Haleh Rezaee, Taher Entezari, Hadi Hamishehkar* Pages 186-189
    Background
    Albumin is an expensive protein colloidal solution with various indications, especially in critically ill patients. The vast use of albumin in health care centers (particularly ICUs), the theoretical danger of contaminant transmission (as with any blood derivative), and the existence of more economical alternatives of equal efficacy evidence the importance of conducting a drug-utilization evaluation. The objective of this study was to assess the usage of albumin in patients at a hospital in Iran.
    Methods
    Albumin administration was evaluated in 210 patients from different wards on randomly selected days during one year. Reasons for the prescription, the consumed dose, length of administration, and related laboratory tests were recorded.
    Results
    Albumin was prescribed inappropriately in 76.2% and appropriately in 23.8% of inpatients. The most frequent inappropriate prescribing motives were hypoalbuminemia (35.6%), nutritional support (32.5%), and edema (24.4%), while the most appropriate prescriptions were edema (46%), nephrotic syndrome (18%), and plasmapheresis (16%). The total amount of albumin used for 210 patients was 68930 g, from which 51290 g costing $274607.1429 was administered for inappropriate indications.
    Conclusion
    Despite the many valid guidelines defining the appropriate indications of albumin, this study demonstrated the extensive inappropriate use of this expensive preparation in one of the largest university-affiliated hospitals in northwestern Iran. It seems advisable to have the consumption of albumin continuously monitored.
    Keywords: Albumin, Drug utilization Evaluation (DUE), Rational Therapy, Clinical Practice Guidelines
  • Yunes Panahi, Jafar Aslani, Ali Hajihashemi, Mahdieh Kalkhorani, Mostafa Ghanei, Amirhossein Sahebkar* Pages 190-194
    Background
    Gastro-esophageal reflux disease (GERD) is a common complaint of sulphur mustard (SM)-exposed subjects. Routine treatments such as proton-pump inhibitors (PPIs), H2-blockers and anti-acids cannot control GERD symptoms completely. Aloe vera is a medicinal plant that has been shown to reduce gastric acid secretion. The efficacy of pantoprazole with or without A. Vera juice in alleviating GERD symptoms was investigated in SM-exposed subjects.
    Methods
    Male patients with a history of SM exposure and diagnosed GERD were enrolled and assigned to treatment with pantoprazole (40 mg before breakfast) plus A. vera syrup (5 mL bid before breakfast and at bedtime) (n=44), or pantoprazole alone (40 mg before breakfast) (n=41) for a period of 6 weeks. GERD symptoms were assessed at baseline and weeks 3 and 6 of study using the Reflux Symptom Index (RSI) questionnaire.
    Results
    Seventy-five patients (n=38 and 37 in the A. vera pantoprazloe and pantoprazole group, respectively) completed the study. No significant difference was found between the groups regarding demographic characteristics and baseline RSI score (p>0.05). A decreasing trend in RSI score was observed in both groups by the 3rd and 6th week of study (p
    Conclusion
    Findings of the present study suggested a significant improvement in the severity of GERD symptoms in SM-exposed subjects following addition of A. Vera to pantoprazole.
    Keywords: Aloe Vera, Pantoprazole, Mustard gas, GERD, Reflux Symptom Index
  • Hojjat Kouchakkhani, Parvin Dehghan*, Mir, Hassan Moosavy, Bahareh Sarmadi Pages 195-202
    Background
    Escherichia coli O157:H7 is one of the high risk bacteria, found in foods, especially in ready-to-eat products, which causes many disorders such as hemorrhagic colitis, hemolytic uremic syndrome and dysentery in humans. The objective of this study was to determine the contamination of Escherichia coli O157:H7 and antibiotic resistance in ready-to-eat vegetable salads.
    Methods
    In this study, 6o ready-to-eat salad vegetable samples were collected from restaurants for determining their isolated Escherichia coli O157:H7 and their antibiotic resistance by SYBR Green I Based real-time PCR and disc diffusion method, respectively.
    Results
    Out of the 60 samples, 10 samples (16.66%) were positive for Escherichia coli O157:H7. All identified isolates were resistant to more than five antibiotics. A high rate of resistance was observed to the clindamycin, vancomycin, erythromycin, penicillin, amoxicillin and cephalothin (100%), cefixime (40%), amikacin (20%), cefotaxime and cetracycline (10%).
    Conclusion
    The presence of toxigenic Escherichia coli O157:H7 in ready-to-eat vegetable salads can be considered a public health threat. Providing the useful strategies for improving food safety and inspection services is necessary. Further studies are suggested to identify specific ready-to-eat vegetable salads-related hazards.
    Keywords: Ready, to, eat vegetable salads, Antibiotic resistant, Escherichia coli O157:H7, Tabriz, Real, time PCR
  • Mehdi Mohammadzadeh, Mohammad Poloee, Tayebeh Ghari* Pages 203-209
    Background
    In the area of exporting, in developing countries, including Iran, the concept of export readiness is unknown to many decision makers and field of activity of Iranian pharmaceutical companies have been limited to the domestic market. Therefore, the main objective of this study is to compare the export performance of ten Iranian pharmaceutical companies with their export readiness.
    Methods
    In order to do this, the top ten of Iranian pharmaceutical companies were selected as the sample. The companie's export readiness was measured, and compared with their export volume as well as their export growth (as two factors for determining the export performance) in five years, to practically check the model and find the strengths and weaknesses of these Iranian pharmaceutical companies in the export factors.
    Results
    Base on the results of the study, the export readiness of these companies does not have significant correlation with companie's export volume in the current circumstances, but it can predict the export growth in the firm's export rate with 95% certainty.
    Conclusion
    The most important thing is that according to the data collected in our study, most of these ten Iranian pharmaceutical companies are not ready to attend in exporting and international markets and only two companies were ready to export. It seems that making improvement in some variables like obtaining international standards, marketing and exporting education, having a transparent and documented plan and having the responsible person for export could increase export readiness of pharmaceutical companies.
    Keywords: Iranian Pharmaceutical Companies, Export readiness, PARO model
  • Ahmad Ghanbari, Yashar Sarbaz, Vahid Jouyban, Gharamaleki, Karim Jouyban, Gharamaleki, Jafar Soleymani, Abolghasem Jouyban* Pages 210-214
    Background
    Solubility of a drug/drug candidate is an essential information in the pharmaceutical area. Classical solubility determination method used in the laboratories are expensive and time-consuming. Attempts were made to provide an automated solubility determination setup based on a laser monitoring technique.
    Methods
    In a previously developed setup, drug powder was added to a given quantity of the solvent which made some troubles in practical applications. The present work reports another setup which adds solvent to a given mass of the drug. The validity of the measured solubilities is checked by comparing the measured solubilities of acetaminophen at two temperatures in water and ethanol mixtures with the corresponding data from the literature.
    Results
    The results reveal that the improved setup could overcome the limitations of the previously developed setup and could be used for drug solubility determination.
    Conclusion
    The improved setup overcomes the troubles made in the previous setup and could be used in generating large amount of solubility data to be used in the pharmaceutical industry.
    Keywords: Aqueous solubility, Determination, Drug, Laser monitoring