Open Access Original Research Article

Pharmaceutical and Analytical Evaluation of Prolonged Release Rosuvastatin-Ca Buccoadhesive Tablets

Maha A. Marzouk, Sawsan A. Abdel-Razeq, Marwa M. Soliman

Journal of Pharmaceutical Research International, Page 1146-1162
DOI: 10.9734/BJPR/2014/9257

Rosuvastatin-Ca was prepared in solid dispersion as buccoadhesive tablets to increase its bioavailability and the release of the drug from its buccoadhesive formulae due to its poor aqueous solubility. The solid dispersions were prepared using β-cyclodextrin, polyethylene glycol 6000 and polyethylene glycol 4000 by kneading and solvent evaporation methods and were characterized by differential scanning calorimetry (DSC). They were also prepared using poloxamer 407 as a biocompatible and mucoadhesive carrier by freeze drying method. The buccoadhesive tablets of the drug were formulated using sodium carboxymethyl cellulose, hydroxypropylmethyl cellulose and sodium alginate by direct compression method. The prepared tablets were evaluated for their physical, dissolution, mucoadhesive and swelling properties. An in-vitro release study showed slow and prolonged release of the drug from tablets as compared to marketed formulation. Five formulae were selected for applying the recently reported analytical methods and results were compared statistically with a compendial one.

Open Access Original Research Article

Formulation and Evaluation of Oral Elementary Osmotic Pump Tablets of Sumatriptan Succinate

J. Kishan Pavani, S. Pavani, Y. Shravan Kumar, A. Venkatesh, Y. Madhusudan Rao

Journal of Pharmaceutical Research International, Page 1163-1173
DOI: 10.9734/BJPR/2014/8666

Aim: In the present study, Sumatriptan succinate was formulated as oral elementary osmotic pump with a zero-order drug release profile.
Methodology: The effect of different formulation variables i.e. different types of osmogens, concentrations of osmogen and concentration of coating solution were studied. The in vitro evaluation was carried out in different release media.
Result: Highest percentage of drug release was observed at high concentration of mannitol i.e., 1:3 (drug: mannitol). Osmogen with low osmotic pressure (38 atm) showed 71.01% zero-order drug release for 12 hours when compared to that of the osmogen with high osmotic pressure (356 atm) which showed 67.38% of release by zero order.
Conclusion: Elementary osmotic pump tablets of Sumatriptan succinate were able to deliver zero-order release up to 12 hours independent of pH of dissolution media and have overcome the problem of chronotherapeutic effect.

Open Access Original Research Article

Simple Controlled Release Delivery System for an Anti-hypertensive Drug via Buccal Route

Waleed M. Khattab, Shadeed Gad, Mohamed M. El-Sayed, Mamdouh M. Ghorab

Journal of Pharmaceutical Research International, Page 1174-1195
DOI: 10.9734/BJPR/2014/9789

Objective: This study aims to develop controlled release buccal tablets of losartan potassium based on bioadhesion using direct compression technique.
Materials and Methods: The bioadhesive buccal tablets of losartan potassium were prepared after preliminary drug-excipients compatibility studies and micromeretics study for powder blends. The tablets were prepared by direct compression utilizing carbopol 934LR as a primary bioadhesive polymer either with or without chitosan or hydroxypropyl methylcellulose E15LV as secondary polymers. Other excipients included PVP K30 as a binder, magnesium stearate as a lubricant and mannitol as a diluent. The tablets were evaluated for weight variation, thickness and diameter, hardness, friability, drug content, surface pH, Ex-vivo residence time and bioadhesion force, In-vitro swelling and drug release study. The analysis of the release profiles in the light of distinct kinetic models (zero order, first order, Higuchi, Hixson-Crowell and Korsmeyer–Peppas) was carried out.
Results and Discussion: The formula containing 40% w/w bioadhesive polymers of carbopol 934LR and chitosan (1:2) was selected as the optimum one based on a ranking methodology and then, it was subjected to Ex-vivo permeation and physical stability study in human saliva. Swelling index was 78.32±1.84% after 7h and tablets showed a neutral surface pH. Ex-vivo residence time was long enough for more than 10h. Ex-vivo bioadhesion force was 0.38±0.01N. Drug release was 57.64±3.43% after 8h following zero order kinetics with a steady state permeation flux of 0.959mg/cm2h. Tablets were physically stable in human saliva.
Conclusion: These formulae improved, controlled and prolonged the release of losartan potassium from a buccal bioadhesive system for at least 8h in a simple way which can achieve a high patient compliance.

Open Access Original Research Article

Acute and Sub-acute Toxicity Studies of Ethanol Seed Extract of Raphia hookeri on Swiss Albino Rats

G. O. Mbaka, S. O. Ogbonnia, F. O. Awoyemi

Journal of Pharmaceutical Research International, Page 1196-1208
DOI: 10.9734/BJPR/2014/9330

Aim: To evaluate the acute and sub-acute toxicities of Raphia hookeri (Rh) seed hydroethanolic extract on experimental animals.
Materials and Methods: Acute toxicity study was evaluated on Swiss albino mice of both sexes. Administration of a single dose of 4000mg/kg of Rh seed extract by gavages to five mice showed no mortality, hence, its 1/20th dose was used as the highest therapeutic dose. The intra-peritoneal administration produced dose dependent mortality with median lethal dose (LD50) of approximately 323.6mg/kg body weight (bwt). In sub-acute toxicity study, Wistar rats received daily administration of the extract in the dose range of 50 to 200mg/kgbwt for 30 days. The effects on biochemical, histological and haematological parameters were evaluated.
Results: The animals exhibited dose dependent body weight changes. There were some organs weight gains with the exception of the liver and testes which showed comparably lower weight compared to the control. There was a significant (p<0.05) increase in total protein, aspartate aminotransferase (AST) and albumin levels compared to the control while bilirubin and alanine aminotransferase (ALT) levels decreased appreciably at the highest extract dose. The urea level decreased while the creatinine level increased in dose dependent manner. In lipid profile study, total cholesterol, triglycerides and low density lipoprotein cholesterol (LDL-cholesterol) levels showed significant (p<0.05) decrease in value. There was significant (p<0.05) increase in high density lipoprotein cholesterol (HDL-cholesterol). Marked decrease in red blood cells, haemoglobin and haematocrit occurred. The white blood cells also decreased while neutrophil and lymphocytes increased appreciably. The extract caused marked deleterious effect on the testes leading to drastic reduction in sperm cells.
Conclusion: The extract caused undesirable effect on the male reproductive organ of the animals making it unsafe for consumption by males of reproductive age.

Open Access Original Research Article

Assessment of Antimicrobial Utilization and Prescribing Pattern among the Health Care Professionals at a Tertiary Care Rural Teaching Hospital in Southern India

Pitchaipillai Revathi, Thalaimalai Senthinath Jeyaseelan, Madhavan Vigneshwari, Nagarajan Prabhu, Mayilsamy Nithya, Subramaniya Pillai Manickavasagam, Alagappan Uma, Ponniah Thirumalaikolundusubramanian

Journal of Pharmaceutical Research International, Page 1209-1216
DOI: 10.9734/BJPR/2014/9961

Aims: To monitor the antimicrobial utilization; identify the preferred group of antibiotics in outpatient services, determine the prescribing pattern of antibiotics by consultants in a rural teaching hospital, evaluate the inappropriate usage of antibiotics among population and evaluate the patients knowledge about use of antimicrobials taken for their illness.
Methodology: A period of 24 months of investigation is carried out towards prescribing antibiotics and the inappropriate usage of antibiotics among rural population who attended outpatient departments were elicited by Questionnaires survey method and analysed in relation to rational use of antibiotics. The patients were also interviewed for their knowledge regarding drugs, sources, dose, duration and frequency of the drugs.
Results: The percentage of distribution of various group of antibiotics in the years of 2009-2010 and 2010-2011 were Sulphonamide (SULP) (4.42%, 1.1%), Penicillin (Pn) (52.4%, 9%), Fluroquinolones (FQs) (24.9%, 44%), Cephalosporins (CPs) (1.2%, 5.2%), Broad spectrum antibiotics (BSA) (3.4%, 3.6%), Macrolide (Mac) (1.3%, 5.2%), Antiprotozoal drug (APD)-metronidazole (12.3%, 12.7%) and fixed dose combination (FDC) (0.2%, 3.6%) respectively. Many practitioners were not aware of Multidrug Resistance (MDR) (50.5%) nor the type of infections (52.6%) or the group of antibiotics (57.9%) exhibiting resistance.
Conclusion: Antibiotics are considered as the second most prescribed drugs in the world. In our study, 76.2% were prescribed with antibiotics in their prescription. Analysis of utilization of antibiotics in pharmacy during the year of 2010-2011 revealed a reduction in antibiotic use compared to 2009–2010. Further awareness required to the prescribers and beneficiaries regarding antimicrobial resistance.

Open Access Original Research Article

Determination of Survival Rates of Bacteria in Contaminated Fresh Fruit Juice Samples

Olufunmiso O. Olajuyigbe, Olujimi M. Akinwande, Otunola Adedayo

Journal of Pharmaceutical Research International, Page 1217-1227
DOI: 10.9734/BJPR/2014/7384

Aims: To determine the survival rates of bacteria in contaminated fresh fruit juice samples
Place and Duration of Study: Biosciences and Biotechnology Department, Babcock University, Ilisan Remo, Ogun State, Nigeria, between November, 2012 and May, 2013.
Methodology: Freshly extracted juice samples were obtained from intact pineapple (Ananas comosus Merr.) and watermelon (Citrillus lanatus Thunb.) were pasteurized before being contaminated with Escherichia coli ATCC 25922 and Lactobacillus acidophilus. While the pH and the sugar contents were determined at interval after being contaminated with the bacterial strains, the contaminated juice samples were sampled for 150 min to determine colony forming unit per milliliter (cfu/ml) at different sampling time.
Results: In pineapple juice, the log of concentration of E. coli was reduced from 6.452 at 0 min to 5.079 at 150min. In watermelon, the log of concentration of E. coli was reduced from 6.301 at 0min to 5.954 at 150min. While the log of concentration of L. acidophilus in pineapple juice was between 6.204 at 0 min and 6.262 at 150min, its log of concentration in watermelon juice ranged between 6.228 at 0 min and 6.291 at 150min. The pH was reduced to 2.9 and 3.7 by E. coli while L. acidophilus reduced the pH to 2.5 and 3.0 for pineapple and watermelon juices respectively. After 150min, the sugar contents of pineapple and watermelon juices decreased from 1.181 and 1.060mg/ml to 0.011 and 0.004mg/ml by the E. coli while L. acidophilus reduced the sugar contents to 0.003mg/ml for pineapple juice and 0.018mg/ml for watermelon juice. The reduction in the pH values of each of the fruit juices showed that the activities of each bacterial strain resulted in increase in the production of acid in the growth medium.
Conclusion: The inability of coli form (E. coli) to survive in the fruit juices suggested that the fruit juices may not harbor and/or disseminate enteric pathogens if allowed to stay for a while before packaging.

Open Access Original Research Article

Pharmacological Effect of Panax ginseng Extract Standardized with Ginsenoside Rg3 on Mating Behavior of Male Rats Treated with Dopamine Antagonists

Mosaad A. Abdel-Wahhab, Ahmed A. El-Kady, Olivier Joubert, Aziza A. El-Nekeety, Yong T. Kim, Won J. Yoon, Myung H. Park, Bertrand H. Rihn

Journal of Pharmaceutical Research International, Page 1228-1241
DOI: 10.9734/BJPR/2014/9673

Aim: The aim of this study was to evaluate the effects of Panax ginseng extract standardized with ginsenoside Rg3 (PGRg3) on the mating behavior of sexually active or inactive male rats treated with dopamine antagonists.
Methodology: Animals were treated with PGRg3 (50,150 and 450mg/kgb.w) with or without dopamine antagonists. The penile erection, motor activity and stretching-yawning episode were evaluated in animals treated with PGRg3 alone or in combination with lisurode or SND 919. Testosterone and sperm counts were also evaluated in different treatment groups.
Results: The results showed that (-) Eticlopride counteracted PGRg3-induced penile erection but not motor hyperactivity. PGRg3 treatment enhanced lisuride-induced behavioral effects. Moreover, PGRg3 plus SND 919 showed a marked stretching-yawning behavior compared to the animals received SND 919 alone. PGRg3 also succeeded to increase testosterone level and sperm count in a dose dependent fashion.
Conclusion: It could be concluded that DAD2 receptors are involved in PGRg3-induced mating behavior and testicular function improvement. PGRg3 could be used to improve sexual function and mating behavior in people suffering from erectile dysfunction.

Open Access Original Research Article

Improve Markers of Oxidative Stress and Coagulation Parameters in Response to Atorvastatin Therapy

Bassim I. Mohammad, Najah R. Hadi, Haider M. Jawad, Dina A. Jamil, Hayder A. Al-Aubaidy

Journal of Pharmaceutical Research International, Page 1242-1252
DOI: 10.9734/BJPR/2014/10140

Aims: This study was undertaken to investigate the antioxidant effects of atorvastatin in treating cases of atherosclerosis associated with hyperlipidemia.
Methodology: Forty local domestic rabbits were assigned to five groups (eight rabbits in each group): After two weeks acclimatization period, a group of 8 rabbits (Group I) were used as the baseline values of the study parameters. Another 8 rabbits were selected and maintained on standard chow diet (4% fat, 18% protein, 60% carbohydrate, and 4% fibers) throughout the experiment (12 weeks) and served as a normal diet control (Group II). The rest 24 rabbits were fed on an atherogenic diet for 8 weeks to induce atherogenesis. At the end of 8th week, a group of 8 atherogenic rabbits (Group III) were separated and sacrificed and served as an atherogenic-baseline group. The remaining 16 atherogenic rabbits were randomly allocated into two groups; first group received atherogenic diet only for the next four weeks and served as an atherogenic control (Group IV). The other group received atorvastatin (Group V).
Results: Blood samples were collected for serum lipids, coagulation parameters and oxidation parameters. Results showed a significant improvement in the coagulation parameters and oxidation parameters in the atorvastatin treated group compared to the atherogenic control group (P= .01).
Conclusion: This study illustrated the beneficial anti-oxidant effects of atorvastatin in treating atherosclerosis associated with hyperlipidemia.

Open Access Original Research Article

Anti-inflammatory and Antinociceptive Effects of the Aqueous Extract of the Bark of Chrysobalanus icaco Linnaeus

Tatiane Bezerra de Oliveira, Carlson Helder Reis de Carvalho Júnior, Fernanda Virgínia Barreto Mota, Larissa Cardoso Corrêa de Araújo, Maria Bernadete Sousa Maia, Karina Perrelli Randau, Silene Carneiro do Nascimento, Teresinha Gonçalves da Silva

Journal of Pharmaceutical Research International, Page 1253-1268
DOI: 10.9734/BJPR/2014/8742

Aims: This paper describes the anti-inflammatory and antinociceptive effects of the aqueous extract of Chrysobalanus icaco.
Study Design: Study the anti-inflammatory and antinociceptive activity of the aqueous extract of C. icaco using in vivo models.
Place and Duration of Study: Department of Antibiotics and Department of Pharmaceutical Science, Federal University of Pernambuco, Recife, Pernambuco, Brazil, between March 2010 and March 2012.
Methodology: The anti-inflammatory activity was evaluated by carrageenan/dextran-induced paw edema, vascular permeability induced by acetic acid and subcutaneous air pouch models, with measurements of cell migration, nitric oxide and cytokines TNF-α and IL-6. Acetic acid-induced abdominal writhing, formalin and hot plate tests were performed to investigate the antinociceptive effects.
Results: The aqueous extract of C. icaco (100, 200 and 400 mg/kg) reduced dextran/carrageenan-induced rat paw edema, the vascular permeability, cell migration, and nitric oxide concentration. However, it did not affect the levels of TNF-α and IL-6 produced in the pouch. The aqueous extract also demonstrated antinociceptive activity by acetic acid-induced abdominal writhing and formalin test, and was able to prolong the reaction time in the hot plate model in the first hour with activity similar to morphine (2.5 mg/kg, s.c.). There was no acute toxicity in mice after oral administration of the aqueous extract at doses of 2 g/kg.
Conclusion: Our results indicate that the aqueous extract of C. icaco demonstrated anti-inflammatory activity through the reduction of vascular permeability, inhibition of cellular migration and nitric oxide production and that the antinociceptive activity seems to be mediated by central mechanisms.

Open Access Original Research Article

Amlodipine Abridged Calcium Associated Complex-I Inhibition in 6-OHDA Lesioned Parkinson’s Rat

A. Shanish Antony, P. Vijayan

Journal of Pharmaceutical Research International, Page 1269-1275
DOI: 10.9734/BJPR/2014/6613

Aims: The present study was carried out to evaluate Amlodipine, a L-type calcium channel blocker for alleviating or reducing the neurodegeneration in 6-OHDA lesioned rat models.
Place and Duration of Study: Department of Pharmacology, JSS College of Pharmacy, Rocklands, Ooty, India between October 2011 and may 2012.
Methodology: Male adult Wistar rats were given with intra-cerebroventricular injection of 6-hydroxydopamine (6-OHDA) into the median forebrain bundle and treated post 48 hours with Amlodipine (10 mg/kg and 20 mg/kg) per oral for 30 days. Motor coordination, striatal dopamine, mid brain calcium and complex-I activity were estimated. Data were statistically analyzed and p<0.05 was considered significant.
Results: Amlodipine regained motor coordination, mid-brain dopamine content, and prevented calcium overload and complex I activity at both dose levels when compared with 6-OHDA control group. Alleviation of calcium overload and complex I inhibition with subsequent increase in dopamine level in Parkinson’s rats were observed at the end of treatment period.
Conclusion: The experimental study gave light to a new therapeutic intervention of Amlodipine in preventing neuronal morbidity in Parkinson’s disease (PD). So, further neuro-molecular study with Amlodipine in experimental PD is warranted in future.