Journal of Pharmacy And Bioallied Sciences
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   Table of Contents - Current issue
April-June 2016
Volume 8 | Issue 2
Page Nos. 83-171

Online since Monday, March 28, 2016

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Exploring the ocean for new drug developments: Marine pharmacology Highly accessed article p. 83
Harshad Malve
Disease ailments are changing the patterns, and the new diseases are emerging due to changing environments. The enormous growth of world population has overburdened the existing resources for the drugs. And hence, the drug manufacturers are always on the lookout for new resources to develop effective and safe drugs for the increasing demands of the world population. Seventy-five percentage of earth's surface is covered by water but research into the pharmacology of marine organisms is limited, and most of it still remains unexplored. Marine environment represents countless and diverse resource for new drugs to combat major diseases such as cancer or malaria. It also offers an ecological resource comprising a variety of aquatic plants and animals. These aquatic organisms are screened for antibacterial, immunomodulator, anti-fungal, anti-inflammatory, anticancer, antimicrobial, neuroprotective, analgesic, and antimalarial properties. They are used for new drug developments extensively across the world. Marine pharmacology offers the scope for research on these drugs of marine origin. Few institutes in India offer such opportunities which can help us in the quest for new drugs. This is an extensive review of the drugs developed and the potential new drug candidates from marine origin along with the opportunities for research on marine derived products. It also gives the information about the institutes in India which offer marine pharmacology related courses.
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Forensic pharmacology: An important and evolving subspecialty needs recognition in India Highly accessed article p. 92
Harshad Onkarrao Malve
With training in pharmacology, a pharmacologist has an expert knowledge as well as working experience in the subjects of therapeutics, pharmacokinetics, and toxicology along with exposure to subjects such as forensic medicine during the medical education. All these knowledge domains can be applied and act as an interface to the forensic situations. The skills and expertise of a forensic pharmacologist can be useful in a large and diverse number of legal cases. With an ever increasing incidence of criminal and civil cases in India, the development and inclusion of forensic pharmacologist in the judicial system of India are the need of the hour. The research in pharmacology has witnessed great technological advancement that allows it to expand its scope beyond the domain of therapeutics, thus enabling Indian pharmacologists to explore the niche area of Forensic Pharmacology. Differing pharmacokinetics and pharmacodynamics of drugs in living and dead, drug interactions, abuse of drugs, personal injury or death due to drug exposure leading to medico-legal issues, environmental exposure to chemicals, and doping and forensic pharmacovigilance are the diverse aspects of Forensic Pharmacology.
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Vorapaxar: A novel agent to be considered in the secondary prevention of myocardial infarction p. 98
Obamiro Kehinde, Rotimi Kunle
Patients receiving therapy for the secondary prevention of myocardial infarction (MI) are still at high risk of a major cardiovascular event or death despite the use of currently available treatment strategy. Vorapaxar, an oral protease-activated receptor antagonist, is a novel antiplatelet drug that has been recently approved to provide further risk reduction. The results of two Phase III trials (thrombin receptor antagonists for clinical event reduction and the TRA 2 °P-TIMI 50) have showed that vorapaxar, in addition to standard of care therapy, has the potential to provide further risk reduction in patients with prior MI. A search was made on PubMed on articles related to clinical trials and clinical consideration with the use of vorapaxar. This review article summarizes the results of Phase II trials, Phase III trials, subgroup analysis, precautions, and drug interaction with the use of vorapaxar.
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Severity and clustering of menopausal symptoms among obese and nonobese postmenopausal women in India p. 106
ES Sharanya Shre, Kate Trout, Sonia Pant Singh, Awnish Kumar Singh, Surapaneni Krishna Mohan, Ashish Joshi
Background: The symptoms of menopause have a negative impact on quality of life, especially in women transitioning to menopause and earlier transitions. This study was conducted with the objective of assessing the effect of obesity on the severity of menopausal symptoms and the clustering of symptoms in postmenopausal women in India. Methodology: The Menopausal Rating Scale (MRS) was used to assess the severity of menopausal symptoms of postmenopausal women of Chennai, visiting Saveetha Medical College, Chennai, India. This cross-sectional study was conducted from August to November 2013 in Chennai, India. Sociodemographic characteristics, anthropometric measurements, blood pressure level, menopausal history, personal health history, and hormonal disorder issues were investigated. Results: The results have shown that 24% of the participants had complaint of mild to severe hot flushes, half of them had reported heart ailments (49%; n = 74), and disturbed sleep (48%; n = 72). The proportion of overweight/obese participants was higher in married (64%) than widows (41%), and this difference was found statistically significant (P = 0.005). There were no significant differences in MRS scores of obese and nonobese postmenopausal participants. Conclusion: There is a need of developing interactive, user friendly, technology based education module for addressing the chronic ailments of postmenopausal women.
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Antihyperlipidemic effects of Citrus sinensis, Citrus paradisi, and their combinations p. 112
Neelam Mallick, Rafeeq Alam Khan
Objective: Hyperlipidemia, extensively contributes in the progression of coronary heart diseases and atherosclerosis, but may be managed through alterations in the nutritional pattern. Several studies show that diet rich in polyphenols and antioxidants have antiatherogenic effects. Citrus sinensis and Citrus paradisi are widely known for health benefits and have found to produce antioxidant, anti-inflammatory, and hypolipidemic effects, hence current research was planned to determine the hypolipidemic effects of C. sinensis and C. paradisi in rats receiving diet rich in cholesterol. Materials and Methods: All rats were divided into 11 groups each comprising 10 animals: Normal control group and hyperlipidemic control. C. sinensis treated three groups, C. paradisi treated three groups, C. sinensis and C. paradisi combination treated two groups, and group treated atorvastatin. All rats in the respective groups were treated orally with sterile water, juices, and standard drug for 8 weeks and lipid profile was estimated at the end of dosing. Results: Cholesterol, triglycerides (TGs), and low-density lipoprotein (LDL) were decreased at all the three doses of C. sinensis and C. paradisi but rise in high-density lipoprotein (HDL) was only significant at 8 ml/kg, and 0.3 ml/kg, respectively. Animals received the combination doses of C. sinensis and C. paradisi also showed a highly significant fall in cholesterol, LDL, and TGs, however HDL level was significantly elevated by SPJ-2 combination. Conclusion: Results suggest that C. sinensis and C. paradisi possess antihyperlipidemic activity due to phytochemicals and other essential nutrients, hence may serve as cardioprotective by preventing thrombosis.
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Evaluation of antioxidant activity of Manihot esculenta Crantz in wistar rats p. 119
Satish Eknath Bahekar, Ranjana Sushil Kale
Aims: The study aimed to explore the antioxidant activity of ethanolic leaf extract of Manihot esculenta Crantz leaves (MEC) in wistar rats. Materials and Methods: Ethanolic extract of MEC leaves in the doses of 50 mg/kg, 100 mg/kg, and 200 mg/kg were used in wistar rats of either sex. The oxidative stress was produced by overdose of acetaminophen and estimation of serum concentration of various enzymes such as malonaldehyde (MDA), superoxide dismutase (SOD), reduced glutathione (GSH), and catalase (CAT) were measured by standard biochemical methods. Silymarin (100 mg/kg) was used as a standard drug for assessment of antioxidant status. Statistical Analysis Used: Results were analyzed by one-way analysis of variance followed by Student's unpaired t-test. Results: When compared with the standard antioxidant silymarin, MEC extract did not exhibit antioxidant activity in terms of MDA level reduction. However, it significantly increased serum levels of the antioxidant enzymes (SOD, GSH, and CAT) exerting a potent antioxidant effect in a graded manner. Conclusions: The observed results suggest that MEC could be a potential source of antioxidants. However, further studies are required to explore this therapeutic property of plant.
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Nonadherence and factors affecting adherence of diabetic patients to anti-diabetic medication in Assela General Hospital, Oromia Region, Ethiopia p. 124
Ashebir Kassahun, Fanta Gashe, Eshetu Mulisa, Wote Amelo Rike
Background: Diabetes mellitus is a major global health problem covering approximately 347 million persons worldwide. Glycemic control has a main role in its management which mainly depends upon patient adherence to the treatment plan. Accurate assessment of medication adherence is necessary for effective management of diabetes. Objective: To assess nonadherence and factors affecting adherence of diabetic patients to anti-diabetic medication in Assela General Hospital (AGH), Oromia Region, Ethiopia. Materials and Methods: A descriptive cross-sectional study was conducted on patients seeking anti-diabetic drug treatment and follow-up at AGH using structured questionnaire and reviewing the patient record card using check list from January 24, 2014 to February 7, 2014. Descriptive analysis was used to describe the percentages and number of distributions of the variables in the study; and association was identified for categorical data. P ≤ 0.05 was considered as statistically significant. Result: Of all respondents, 149 (52.3%) and 136 (47.7%) were female and male, respectively. The majority of the study participants 189 (66.3%) were in the age group of 30–60 years. Two-hundred nineteen (76.8%) of respondents were married currently. The majority, 237 (83.2%) of respondents did not have blood glucose self-monitoring equipment (glucometer). A total of 196 (68.8%) respondents were adhered to anti-diabetic medication. There was a significant association between adherence to the medication and side effect, level of education, monthly income and presence of glucometer at home (P < 0.05). Conclusion: The participants in the area of study were moderately adherent to their anti-diabetic medications with nonadherence rate of 31.2%. Different factors of medication nonadherence were identified such as side effect and complexity of regimen, failure to remember, and sociodemographic factors such as educational level and monthly income.
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Therapeutic effects of Citrullus colocynthis fruit in patients with type II diabetes: A clinical trial study p. 130
Batol Barghamdi, Fereshteh Ghorat, Khairollah Asadollahi, Kourosh Sayehmiri, Robab Peyghambari, Ghobad Abangah
Aim: Citrullus colocynthis plant was traditionally used for the treatment of diabetes in Sabzevar city, Iran. This study aimed to investigate the effects of C. colocythis on fasting blood sugar (FBS) and HbA1c in patients with type II diabetes. Materials and Methods: Totally 70 patients with type II diabetes attending the diabetes clinic in Sabzevar city were investigated. Patients were divided into two groups of intervention and placebo randomly and were studied for 2 months. Mean serum level of FBS and HbA1c was compared within and between groups at the end of the study. Data were analyzed using student and paired t-tests via SPSS software version 16. Results: A significant difference was revealed between before and after intervention for HbA1c and FBS levels in the intervention group (P = 0.01 and P = 0.04, respectively). The difference between before and after intervention for FBS and HbA1c levels in the placebo group were not significant (P = 0.8, P = 0.68 respectively). This study showed a negative relationship between either the mean ± standard deviation serum level of FBS or HbA1c and body mass index in the treatment group significantly (P = 0.03, 0.008, respectively). The present study did not identify any side effects during the study period among the treatment group. Conclusion: According to the findings of this study, application of 125 mg C. colocynthis once per day for 2 months can lead to considerable decrease in the mean levels of HbA1c and FBS among the patients with type II diabetes without any side effects.
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Development of pH sensitive polymeric nanoparticles of erythromycin stearate p. 135
Sulekha Bhadra, Atin B Prajapati, Dipankar Bhadra
Context: Bioavailability of conventional tablet of erythromycin stearate is low as it is unstable at acidic pH and also shows a low dissolution rate. Objective: It was proposed to protect it from the acidic condition of the stomach along with an increase in dissolution rate by formulating pH sensitive nanoparticles. Materials and Methods: The nanoparticles were prepared by the solvent evaporation technique using different quantities of Eudragit L100-55 and polyvinyl alcohol (PVA). Size reduction was achieved by high speed homogenization technique using Digital Ultra Turrax homogenizer. The formulation was optimized using 32 factorial design, keeping drug polymer ratio and surfactant concentration as independent variables. Particle size, entrapment efficiency, and drug-release (DR) were studied as dependent variables. Results: Optimized batch containing 1:0.3 erythromycin stearate: Eudragit L100-55 ratio and 1.0% PVA showed 8.24 ± 0.71% DR in pH 1.2 in 1-h and 90.38 ± 5.97% in pH 5.5 and pH 6.8 within 2-h, respectively. Discussion: The optimized batch exhibited lower release in acidic pH and faster release in higher pH compared to the marketed preparation. Conclusion: Thus the present study concludes that pH sensitive nanoparticles of erythromycin stearate increases the dissolution of the drug in intestinal pH and also protect it from acidic pH, which may help in improving the bioavailability of erythromycin.
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In vitro screening on amyloid beta modulation of aqueous extracts from plant seeds p. 141
Yoshinori Okada, Mizue Okada
Introduction: Glycation process might contribute to both extensive protein cross-linking and oxidative stress in Alzheimer's disease (AD). The amyloid-like aggregation of glycated bovine serum albumin induces apoptosis in the neuronal cell. Dietary supplementation of antioxidants, vitamins, and polyphenols are beneficial to AD, and consumption of fruits and vegetables reduce the risk of AD. We conducted a screening of 14 aqueous extracts from plant seeds (PSAE) for inhibitory activity on amyloid beta (Aβ). Materials and Methods: To examine the effects of PSAE on the Aβ (1–42) concentration, PSAE were analyzed by Aβ (1–42) enzyme-linked immunosorbent assay. Furthermore, we carried out an antiglycation experiment of PSAE and an antiaggregation experiment of PSAE to confirm the modification mechanism of PSAE. PSAE were added to buffer containing D-ribose and albumins. The solutions were incubated at 37 °C for 10 days. After incubation, the products were assayed on a fluorophotometer. Results: PSAE associated differential reduction in the levels of Aβ (1–42) (lettuce; 98.7% ± 2.4%, bitter melon; 95.9% ± 2.6%, and corn; 93.9% ± 2.1%), demonstrating that treatment with lettuce seeds extracts (LSE) effectively decreases Aβ (1–42) concentration. Among the 14 PSAE, LSE exhibited the second greatest potential for antiglycation. Inhibition of aggregates was not recognized in LSE. Conclusion: These results suggest that LSE reduces the toxicity of Aβ by modifying Aβ.
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Knowledge and perception about health risks of cigarette smoking among Iraqi smokers p. 146
Omar Thanoon Dawood, Mohammed Abd Ahmed Rashan, Mohamed Azmi Hassali, Fahad Saleem
Background: Smoking is a major public health problem, especially in Iraq. There is very little information had been documented regarding smoking risk factors and quit intention among Iraqi smokers. Objectives: The main objectives of this study are to determine smokers' knowledge and perception about smoking health risks; and to determine smoking behavior and quitting intentions among Iraqi smokers; as well as to predict the factors that may associate with quit intentions. Methods: A cross-sectional study was conducted at the outpatient clinic in Tikrit Teaching Hospital, Tikrit City, Iraq. Adult smokers who are smoking cigarette everyday and able to communicate with the researcher were invited to participate in the study. A self-administered questionnaire was used to collect data from 386 participants. Results: This study showed that smokers had low awareness about some risk effects of smoking such as lung cancer in nonsmokers (30.1%), impotence in male smokers (52.6%), premature ageing (64%), and stroke (66.3%). In addition, the high score of knowledge and perception was significantly associated with quitting intention. Conclusion: Smokers' knowledge and perception regarding smoking health effects were low, especially in terms of secondhand smokers. Many efforts needed from health policy-makers and health care professionals to disseminate information about the risks of smoking and health benefits of give up smoking.
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Diffuse reflectance near infrared-chemometric methods development and validation of amoxicillin capsule formulations p. 152
Ahmed Nawaz Khan, Roop Krishen Khar, PV Ajayakumar
Objective: The aim of present study was to establish near infrared-chemometric methods that could be effectively used for quality profiling through identification and quantification of amoxicillin (AMOX) in formulated capsule which were similar to commercial products. In order to evaluate a large number of market products easily and quickly, these methods were modeled. Materials and Methods: Thermo Scientific Antaris II near infrared analyzer with TQ Analyst Chemometric Software were used for the development and validation of the identification and quantification models. Several AMOX formulations were composed with four excipients microcrystalline cellulose, magnesium stearate, croscarmellose sodium and colloidal silicon dioxide. Development includes quadratic mixture formulation design, near infrared spectrum acquisition, spectral pretreatment and outlier detection. According to prescribed guidelines by International Conference on Harmonization (ICH) and European Medicine Agency (EMA) developed methods were validated in terms of specificity, accuracy, precision, linearity, and robustness. Results: On diffuse reflectance mode, an identification model based on discriminant analysis was successfully processed with 76 formulations; and same samples were also used for quantitative analysis using partial least square algorithm with four latent variables and 0.9937 correlation of coefficient followed by 2.17% root mean square error of calibration (RMSEC), 2.38% root mean square error of prediction (RMSEP), 2.43% root mean square error of cross-validation (RMSECV). Conclusion: Proposed model established a good relationship between the spectral information and AMOX identity as well as content. Resulted values show the performance of the proposed models which offers alternate choice for AMOX capsule evaluation, relative to that of well-established high-performance liquid chromatography method. Ultimately three commercial products were successfully evaluated using developed methods.
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Characterization of pioglitazone cyclodextrin complexes: Molecular modeling to in vivo evaluation p. 161
Dinesh M Bramhane, Preethi A Kulkarni, Elvis A.F Martis, Raghuvir R. S Pissurlenkar, Evans C Coutinho, Mangal S Nagarsenker
Aims: The objective of present study was to study the influence of different β-cyclodextrin derivatives and different methods of complexation on aqueous solubility and consequent translation in in vivo performance of Pioglitazone (PE). Material and Methods: Three cyclodextrins: β-cyclodextrin (BCD), hydroxypropyl-β-cyclodextrin (HPBCD) and Sulfobutylether-7-β-cyclodextrin (SBEBCD) were employed in preparation of 1:1 Pioglitazone complexes by three methods viz. co-grinding, kneading and co-evaporation. Complexation was confirmed by phase solubility, proton NMR, Fourier Transform Infrared spectroscopy, Differential Scanning Calorimetry (DSC) and X-Ray diffraction (XRD). Mode of complexation was investigated by molecular dynamic studies. Pharmacodynamic study of blood glucose lowering activity of PE complexes was performed in Alloxan induced diabetic rat model. Results: Aqueous solubility of PE was significantly improved in presence of cyclodextrin. Apparent solubility constants were observed to be 254.33 M–1 for BCD-PE, 737.48 M–1 for HPBCD-PE and 5959.06 M–1 for SBEBCD-PE. The in silico predictions of mode of inclusion were in close agreement with the experimental proton NMR observation. DSC and XRD demonstrated complete amorphization of crystalline PE upon inclusion. All complexes exhibited >95% dissolution within 10 min compared to drug powder that showed <40% at the same time. Marked lowering of blood glucose was recorded for all complexes. Conclusion: Complexation of PE with different BCD significantly influenced its aqueous solubility, improved in vitro dissolution and consequently translated into enhanced pharmacodynamic activity in rats
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Management of burning mouth syndrome p. 170
Vagish Kumar Laxman Shanbhag
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Lycopene in cancer therapy p. 170
Vagish Kumar Laxman Shanbhag
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