فهرست مطالب

Iranian Journal of Pharmaceutical Sciences
Volume:12 Issue: 4, Summer 2016

  • تاریخ انتشار: 1395/06/11
  • تعداد عناوین: 8
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  • Hossein Danafar *, Mehrdad Hamidi Pages 1-14
    Cefixime is a significant member of orally active third generation cephalosporin and has excellent activity against many pathogens. The virtual bioavailability of a newly industrial dispersible tablet as compared with a recognized identified formulation. An open-label, single-dose, randomized, 2-way crossover study was conducted in fasted healthy Iranian male volunteers. Eligible participants were randomly assign in a 1:1 ratio to be given one tablet(400 mg) of the test or reference formulation, followed by a 2-week washout period and administration of the exchange formulation. The study drugs were administered after a 10-hour overnight fast. A simple and available reversed-phase HPLC method with UV detection has been urbanized and validate for cefixime evaluate in human plasma using a C18analytical column and a mobile phase of tetrabutylammonium hydroxide (pH=6.5)-acetonitril (3:1 v/v). The detection wavelength was 280 nm. The cefixime serum concentration time curves were used to find pharmacokinetic parameters counting AUC0–24, AUC0–∞, and Cmax. To method observed major linear response-concentration association all through the cefixime concentration range of 15-100 ng/ml, with the average accuracy within-run and between-run values of 97.29 and 99.27 percent. The average drug recovery from plasma was 98.2 percent throughout the linear concentration range. The limits of detection (LOD) and quantitation (LOQ) of the method were 5 and 15ng/ml, respectively. The mean (SD) Cmax, Tmax, AUC0–24 and AUC0–∞ values after administration of the test and reference formulations, respectively, were in this manner: 4.68 (0.97) versus 4.72 (0.67) µg/mL, 4.28(0.86) versus 4.25 (0.73) hours, 43.37 (1.13) versus 43.39(1.22) µg/mL/h, and 60.17 (1.98) versus 59.96 (2.13) µg/mL/h. The mean (SD) t1/2 was 5.32 (2.01) hours for the test formulation and 5.34 (2.13) hours for the reference formulation. No statistical differences were showed for Cmax and the area under the plasma concentration-time curve for test and reference tablets. The calculated 90 % confidence intervals based on the ANOVA analysis for the mean test/reference ratios of Cmax, AUC0–∞ and AUC0–24 h of cefixime were in the bioequivalence range (97 %–119 %). The method is quick, easy, very steady and precise for the partition, assignment, pharmacokinetic and bioavailability evaluation of cefixime healthy Iranian adult male volunteers.
    Keywords: Cefixime, Bioequivalence, Pharmacokinetics, Reversed-phase HPLC. dissulotion, Tablets, Hardness, tickness
  • Tejal Gandhi *, Khushboo Gandhi, Kinnarkumar Monapara Pages 15-32
    Prostate cancer is a devastating disease for which current therapies are inadequate. Various lines of evidences have suggested the 5-lipoxygenase (5-LOX) pathway and the leukotriene receptor pathway are potential targets for prevention or treatment of Prostate cancer. Thus, search for new anti-cancer drugs targeting 5-LOX and leukotriene is very essential and important. The objective of the present study was to evaluate the in vitro anti- cancer effects of5-LOX inhibitor-Boswellic acid and cysteinyl leukotrienes receptor antagonist-Montelukast sodium by 3-(4,5-dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide (MTT) assay and Sulphorodamine B assay (SRB) assay against human prostate cancer cell line PC-3. Cell viability was assayed by trypan blue dye exclusion assay. A study was carried out in 24, 48 and 72 hrs. In addition, effect of combination of both the above drugs was also determined by same assays. Boswellic acid and Montelukast sodium demonstrated a substantial anti-cancer effect against the PC-3 cell line. The cytotoxicity of both the drugs increased with increase in duration of drug treatment. A combination of both drugs showed significant reduction in cell viability but did not show any synergistic activity. Complete dose-response curves were generated and IC50 values were calculated for all the assays. IC50 Value for Boswellic acid was found to be 49.15- 45.80 µg/ml and 50.14-43.39 µg/ml by MTT assay and SRB assay, respectively at the same time IC50 value for Montelukast sodium was 49.27-46.77 µg/ml and 46.68-46.47 µg/ml by MTT assay and SRB assay respectively. In summary, Boswellic acid and Montelukast sodium are likely to be valuable for the treatment of prostate cancer, but further studies are required for their more extensive biological evaluations.
    Keywords: Anti-cancer activity, Boswellic Acid, Montelukast Sodium, MTT assay, PC-3 cell line, SRB assay
  • Najmeh Moradi, Shahram Tofighi *, Marzieh Zanganeh, Ali Akbari Sari, Hossein Khedmat, Leila Zarei Pages 33-42
    The aim of this study is to assess cost-effectiveness of infliximab, compared with conventional treatments in patients with moderate to severe Ulcerative Colitis (UC) in Iran. We developed an analytical decision model with a 5-year-time horizon to follow up 1000 hypothetical patients, in order to estimate treatment costs and outcomes. Hypothetical patients, were individuals with moderate to severe UC, that are resistant to conventional treatments. Remission rate, clinical response, and surgery, were selected as clinical outcomes. For estimating QALY, utility value related to each state, drive form published paper. We also estimated associated probabilities by using patients ’medical records and specialists’ opinion. Costs of treatment such as: Physician visit fee, laboratory tests, hospitalizations, surgery, and drugs were estimated based on the public sector tariffs and drug price list that set by pricing committee of food and drug administration. Infliximab costs at dosage of 5 mg /kg, were considered for UC patients with average weight of 75 kilogram. Incremental Cost-Effectiveness Ratio (ICER) of infliximab treatment in UC patients were 240,903 USD dollars per QALY gained, compared with conventional treatments. According to recommendation of World Health Organization for choosing cost-effective intervention, interventions with relative cost-effectiveness value less than 3 times of Gross Domestic Production (GDP) per capita, are cost–effective. Our result showed that the ICER value of infliximab, is approximately 51 times of Iran’s local GDP per capita, in 2014 – i.e. more than 3 time GDP per capita. Thus, for UC patients, our finding indicates, infliximab, is not a cost- effective treatment.
    Keywords: Conventional treatments, Cost-effectiveness analysis, Economic evaluation, Incremental cost-effectiveness ratio, Infliximab, Ulcerative Colitis
  • Mahnaz Kesmati *, Maryam Rezaei, Mozhgan Torabi Pages 43-54
    One of the main components of the stress system is hypothalamus- pituitary-adrenal (HPA) axis. Acute activation of µ-opioid receptors increases the activity of the HPA axis, leading to release of ACTH and corticosterone. Glucocorticoids can change behaviors, depend on age but there were no evidences about the interaction between age, opioid system and glucocorticoids. In this experiment, effects of dexamethasone (1mg/kg) and RU486 (20mg/kg) as an agonist and antagonist of glucocorticoid receptors, morphine (5mg/kg) and naloxone (20mg/kg) as an agonist and antagonist of the opioid system on anxiety in young and adult male Wistar rats were examined. The percentage of time in the open arms of plus maze was evaluated for anxiety behavior also percentage of the number of entries in closed arms was evaluated for locomotor activity. The results showed that morphine (5mg/kg) and dexamethasone (1mg/kg) had an anxiolytic effect on both young and adult rats while just in young rats reduced locomotor activity. RU486 could prevent the anxiolytic effect of morphine, and the anxiolytic effect of dexamethasone had been inhibited by naloxone in young but it wasn't seen in adult rats. These results show an interactive effect between glucocorticoids and the opioid system on mediating anxiety that can be influenced by age.
    Keywords: anxiety, elevated plus maze, glucocorticoid, Mice, opioid, RU486
  • Hadis Bahramiun, Mohammad Kamalinejad, Fatemeh Elahian, Maryam Noubarani, Fatemeh Balaghi, Fariborz Keyhanfar, MohammadReza Eskandari, Farshad H. Shirazi * Pages 55-62

    Olea europaea L. commonly known as olive has been traditionally used for the prevention and treatment of many diseases since ancient times. Olive has been reported to possess a broad spectrum of pharmacological properties. In the present study we investigated the activity of aqueous extract of Olea europaea L. fruit at various concentrations on A2780, A172 and HFFF2 cell lines proliferation by MTT assay. Aqueous extract of olive significantly increased cell proliferation in a dose dependent manner in the cell lines. It has been previously reported that olive has chemoproventive and anti-tumor effects. These disagreements can be explained by differences in cell line properties, type of olive and different solvents in the extracts. However, further investigation is needed to clarify the exact role of olive in cell proliferation and cancer. In this study fruit extract of Olea europaea L. showed more activatory effects on A2780 cell line in comparison with A172 and HFFF2. These differences in the activatory effects may be related to the activation of different signaling pathways in different cell lines.

    Keywords: Olea europaea L, Olive, Cell proliferation, Activatory effects, A2780, A172, HFFF2
  • Rouhollah Bahmani, Ghazaal Moghaddam, Maryam Noubarani * Pages 63-68
    The aim of the present study was to provide a clear picture of the prescribing pattern of corticosteroids in Zanjan, Iran. A retrospective and cross-sectional study was conducted to describe the pattern of corticosteroids prescription at Beheshti pharmacy (Zanjan, Iran) over a period of six months between March 21 and September 22 of 2013. Descriptive analyses were stratified by gender, age, type of prescribed corticosteroid and rout of administration. Separate analyses were performed to determine the most common indications leading to the prescription of injection dexamethasone. Corticosteroids were prescribed mostly (74.56%) as injection. The overall corticosteroid prescribing rate was 25.73%; 55.86% and 44.14% in females and males, respectively. Corticosteroids were prescribed frequently for adults in both males and females. In young and middle-aged women, corticosteroids were prescribed substantially higher than in men of the same age. Dexamethasone as the most prescribed corticosteroid in both male and females was mostly prescribed for respiratory bacterial infections. The current study grows the knowledge about the use of corticosteroids in Iran and suggests more attempts to reduce corticosteroids prescription. Educational interventions to promote hygiene in the society could improve rational use of corticosteroids.
    Keywords: age, Ambulatory care, Dexamethasone, Gender, Prescribing pattern, Respiratory infections
  • Fatemeh Moeini, AliAkbar Jafarian, Najmeh Aletaha, Mohammad Kamalinejad *, Nima Naderi, Mohammad Babaeian Pages 69-76
    Background and objectives

    Gastroesophageal reflux is a common chronic disease that impairs individuals’ quality of life, wherein patients should receive prolonged, and sometimes lifelong, treatment with chemical drugs, that in addition to high costs they can lead to side effects in the long term .Hawthorn fruit is one of the drugs used in traditional medicine to relieve reflux symptoms and to boost stomach function, but no clinical studies has been done so far on its efficacy and adverse effects in controlling reflux symptoms. This project aims to investigate the effectiveness and safety of hawthorn fruit in the treatment of patients with gastroesophageal reflux disease.

    Method

    80 male and female patients with reflux disease were included in the study. Diagnosis of the disease was clinical and based on either of its main symptoms, heartburn and regurgitation, at least twice a week. The patients were randomly assigned to experimental (treatment) and control groups. Patients in the experimental group were given hawthorn syrup and those in the control group received placebo for 4 weeks (5 ml after each meal). Severity of the disease was assessed, based on an available valid questionnaire, before and after the treatment in both groups. The side effects were assessed according to old and new medical resources. To assess the effects on hepatorenal function, the ALT, AST, BUN, and creatinine blood test values were measured and recorded before and after the treatment.

    Results

    After 4 weeks of taking the medicine and placebo, significant improvement of the two main symptoms of reflux disease was observed in the experimental group. For heartburn the p-value

    Conclusion

    Hawthorn syrup is remarkably effective in controlling the major symptoms of gastroesophageal reflux disease (heartburn and regurgitation). After 4 weeks of administration, heartburn and regurgitation were recovered 93.5% and 94.2%, respectively. Out of 80 patients only one patient complained of aggravated bloating and one other of nausea in the early days of taking the medicine. No adverse effects of the medicine were found on the functions of liver and kidney.

    Keywords: hawthorn, Syrup, Gastroesophageal reflux disease, Regurgitation, Heartburn, herbal
  • Anahita Rafie Tabar, Navideh Anarjan, Saeed Ghanbarzadeh, Hamed Hamishehkar * Pages 77-92
    Incorporation of functional foods and nutraceuticals such as carotenoids which suffer from poor water solubility and low bioavailability into nano-sized delivery systems can improve their solubility, stability and oral bioavailability. The aim of this study was to prepare β-Carotene nanodispersion and investigate the effects of preparation parameters by means of response surface methodology using central composite design. Therefore, the impact of the preparation conditions namely the homogenizer speed, evaporation temperature and rotation speed (as independent variables) on the mean particle size, particle size distribution and β-carotene amount of the prepared β-carotene nanodispersion (as responses) were evaluated. A multiple-optimization procedure showed that the optimum conditions of homogenization speed as well as evaporation temperature and rotary speed were 15000 rpm, 32 °C and 140 rpm, respectively. A statistical assessment showed insignificant (p > 0.05) differences between experimental and predicted responses values, verifying the fitness of the final reduced models for explaining the variation of nanoemulsion properties. Using statistical methods can reduce the number of experiments by optimizing of formulations during development and lead to significant save in time and cost.
    Keywords: Nanodispersion, β-Carotene, Response surface methodology, Optimization, Formulation, Central composite design, Factorial design