Open Access Short Research Article

Primary Unresponsiveness to Pioglitazone is not Related to PPAR-ϒ and Its Co-activator Gene Exon SNP Markers

Prashant Mathur, Poonam Punjabi, Soiya Lalwani, M. Krishna Mohan, Mukul Mathur, Sandeep K. Mathur

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/25480

The objective of this prospective observational study was to assess inter-individual variations in lipid and glycemic response to pioglitazone (30 mg OD) and their predictors in newly diagnosed T2DM patients. Out of 104 patients recruited, 88 completed 12 weeks follow up and were included in the final analysis. The patient characterstics studied were: BMI, W: H ratio, HbA1c, fasting and post meal glucose, lipid profile, HOMA-R, HOMA- beta and high resolution melting curve analysis (HRM) of PCR amplified DNA fragments flanking SNP markers of PPAR- γ and its co-activator gene. The mean decrease in HbA1c observed was 2.61% with wide inter-individual variation (coefficient of variance 66.44%, 95.75%, and 75.22% respectively for FPG, 2 hours PPG and HbA1c). Positive association between decrease in glycemic parameters and baseline HOMA- β, FPG, PPG HbA1c1 was observed. This finding suggest better glycemic response could be expected in those with higher beta cell function and severe hyperglycemia. Though lipid parameters improved significantly, they did not show any association with baseline characteristics studied as well as change in glycemic parameters. Eighteen (20.45%) patients were primary non-responder for glycemic, lipid and weight changes. This unresponsive could not be predicted on the basis of clinical and genetic parameters studied.

Open Access Original Research Article

Diclofenac-induced Gastric Ulceration in Rats: Protective Roles of Pantoprazole and Misoprostol

E. E. Zien El-Deen, N. A. El-Mahdy, M. A. El Rashidy, M. M. Ghorab, Shadeed Gad, H. A. Yassin

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/BJPR/2016/24636

Gastrointestinal damage caused by diclofenac remains a significant clinical problem. Pantoprazole provides potent and long-lasting inhibition of gastric acid secretion and has proven efficacy in healing diclofenac-associated ulcers, including those with continued exposure to diclofenac. The objective of this study was to prepare and evaluate microbeads of diclofenac sodium coated with sodium alginate and Hydroxypropylmethylcellulose (HPMC) in order to obtain controlled release drug delivery system. The ulcerogenic activity and histopathological effects of the prepared formulation were compared with a marked formula containing the drug with misoprostol which orally administered to male Wistar rats. Ionotropic gelation technique was the technique of choice to encapsulate the drug. IR spectral analysis indicated no interaction between the drug and polymers used. Microbeads which showed a significant reduction in the release of diclofenac at acidic pH of the stomach as well as maximal release at alkaline pH of the intestine were selected to conduct further in vivo evaluation. The beads were administered to rats in combination with pantoprazole. The obtained ulcer index as well as the histopathological effects of the proposed formulations was compared to marketed formula containing the drug combined with misoprostol. The obtained In vivo results indicate that administration of pantoprazole and diclofenac microbeads has shown efficacy in reducing the risk of GIT ulcerations compared with administration of misoprostol and diclofenac or diclofenac separately.

Open Access Original Research Article

Square Wave Voltammetric Determination of Ropinirole HCl in Bulk, Dosage Forms and Biological Samples on Carbon Paste Electrode

Ibrahim H. I. Habib, Mohamed Rizk, Dalia Mohamed, Shereen Mowaka, Rasha Th. El-Eryan

Journal of Pharmaceutical Research International, Page 1-13
DOI: 10.9734/BJPR/2016/25506

Aim: Voltammetric determination for of Ropinirole HCl.

Study: We will study the behaviour of Ropinirole HCl on the carbon paste electrode.  So several factors such as pH, type of pasting oil, pulse amplitude and scan rate were studied to optimize the condition for  voltammetric determination of drug.

Place and Duration of Study: Microanalytical Chemistry Laboratory, Applied Organic Chemistry Department, National Research Centre, Dokki, Giza, Egypt, between August 2015 and December 2015.

Methodology: Square wave voltammetry (SWV) was employed in order to determine Ropinirole in bulk powder and plasma in a voltammetric cell containing 10 mL of 0.1 mole L-1 sulphuric acid as supporting electrolyte. After every aliquot addition, the solution was  stirred for 30 s at 2000 rpm, rested for 10 s then SWV mode was ramped from +300 to +1600 mV with scan rate 100 mV s-1 and pulse amplitude 50 mV. The experiment was triplicated for every standard solution addition.

Results: A good linearity was obtained over a range of (4.96x10-6 to 3.90x10-5 mol L-1) with mean recovery and relative standard deviation (RSD) values of 99.15% and 3.7%, respectively. The lower detection (LOD) and quantification (LOQ) limits were found to be (1.48x10-6 and 4.96x10-6 mol L-1) respectively at Square wave (SWV) mode. The accuracy and precision of the method were presented with inter and intra days determinations which were within acceptable limits. The method was applied successfully for determining the active ingredients in pharmaceutical preparations with mean percentage recoveries ± RSD of 98.38±3.1 and in spiked human plasma with the mean of recoveries ± RSD, 99.56±3.63%.

Conclusion: An economic, accurate and precise electrochemical method has been developed and validated for the determination of Ropinirole HCl in bulk, dosage form and human plasma.

Open Access Original Research Article

Application of Response Surface Methodology and Central Composite Design for the Optimization of Metformin Microsphere Formulation using Tangerine (Citrus tangerina) Pectin as Copolymer

Adenike Okunlola, Olawunmi Lateefat Akindele

Journal of Pharmaceutical Research International, Page 1-14
DOI: 10.9734/BJPR/2016/25095

Aims: To prepare metformin microspheres by ionic gelation using novel pectin from the peel of tangerine, Citrus tangerina (Rutaceae), as a copolymer with sodium alginate.

Study Design: Central composite design and response surface methodology.

Place and Duration of Study: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria, between September 2015 and February 2016.

Methodology: Central composite design and response surface methodology were applied to evaluate the interactive effects of three variables: Percent of pectin in polymer blend, X1, (50 to 75% w/w), curing time, X2, (10 to 30 min) and concentration of chelating agent (calcium chloride), X3, (5 to 10% w/v) on entrapment and dissolution time (t90).

Results: Entrapment efficiency was 59.10 to 94.90% and t90 was 6.52 to 10.50 h.  X1 and X3 had significant effects on entrapment and t90 (p < 0.0001). The interactions between X2 and X3 was significant at p = 0.033 for entrapment. The correlation coefficients (R2 = 0.9557 and R2(Adj) = 0.9158 for entrapment; R2 = 0.9677 and R2 (Adj) = 0.9387 for t90) showed that the regression model represented the experimental data well. The optimization of the analyzed responses demonstrated that peak conditions for obtaining desired maximum responses, entrapment (102.66%) and t90 (12.27 h), were 82.91% w/w pectin; 36.33 min curing time and 7.50% w/w of calcium chloride.

Conclusion: Tangerine pectin could serve as a cheaper alternative polymer for the formulation of microspheres.

Open Access Original Research Article

Effect of Sub acute Exposure to Telfairia occidentalis Root, Pod and Stem Extracts on Some Liver and Renal Function Parameters in Rats

Enyinnaya A. Ogbonnaya, Patrick O. Uadia

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/25038

Aim: This study assessed the effect of twenty eight (28)-day exposure to aqueous extract of Telfairia occidentalis root, pod and stem on the liver and kidney of Wistar rats.

Methodology: Sixty eight (68) wistar rats were distributed into 17 groups of 4 animals per group and administered, per os (p.o), distilled water, root, pod, and stem extracts each at 250, 750, 1500, 2250, and 3000 mg/kg body weight (bw). All animals were treated for 27 days, followed by sacrificing under chloroform anesthesia on the 28th day.

Results: Biochemical assay results showed that the extracts had varying effects on the liver and kidney and these effects do not correlate directly with dose administered. The root extract showed some degrees of hepatotoxicity and nephrotoxicity at half the maximum dose, and no toxicity observed at maximum dose. The pod extract caused disruption in liver membrane integrity and hyperalbuminemia, while the stem extract caused no necrotic injury but hypoalbuminemia. Both extracts showed mild to significant renal toxicity.

Conclusion: The non correlation of dose and effect was suggested to be due to different concentrations of the inherent bioactive principles which may be cumulative; exhibiting some synergistic and /or antagonistic tendencies, either which is achievable with varying dose and duration.

Open Access Original Research Article

Antimicrobial Resistance Profile of Urinary Isolates from Patients with Indwelling Urinary Catheter Diagnosed of Benign Prostate Hyperplasia in Bida, Niger State, Nigeria

O. A. Akobi, H. E. Inyinbor, E. C. Akobi, E. G. Emumwen, S. O. Ogedengbe, E. O. Uzoigwe, R. O. Abayomi, E. F. Emumwen, O. V. Nwala, Y. A. Abaukaka

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/25109

Antimicrobial resistance is increasing daily and a cause of major challenges in many countries.

Indiscriminate antibiotic prescription is associated to a higher prevalence of antibiotic resistant bacteria. The incidence of antimicrobial resistance among urinary pathogens is also increasing and its treatment has become more complicated due to increasing resistance.

Aims: The present study investigated the pattern of uropathogens and their antimicrobial resistance pattern among the clinical isolates to commercially available antibiotics that are often prescribed in UTI treatment.

Materials and Methods: The research was a retrospective study carried out on January 2009 through November 2013 and was exempted from ethical approval. Three hundred and thirty one (331) bacterial pathogens were selected for this study as isolated at the Medical Microbiology Laboratory, Federal Medical Centre, Bida, Niger State.

Data was coded, computed and analyzed using SPSS version 16.0.

Results: Out of (331) isolates, the most prevalent isolate is Escherichia coli 247(74.6%) followed by Staphylococcus aureus 34(10.3%), Pseudomonas aeruginosa 29(8.8%), Klebsiella species 10(3.0%), Proteus species 10(3.0%) and least uropathogen Staphylococcus albus 1(0.3%). Mean resistance of isolated uropathogen to Augmentin (94.0%), followed by Ampicillin (93.4%), Gentamycin (90.0%), while least resistance are Nitrofurantoin (36.3%) and Levofloxacin (56.2%).

Conclusion: It is quite alarming to note that almost all of the isolates included in this study were found resistant to multiple drugs (four or more antibiotics).

Open Access Review Article

“The Nutraceutical Amino Acids”- Nature’s Fortification for Robust Health

Vijay Sharma, Lalit Singh, Navneet Verma, Garima Kalra

Journal of Pharmaceutical Research International, Page 1-20
DOI: 10.9734/BJPR/2016/24415

Nutraceuticals i.e. the product positioned at the interface between food and drugs, are an increasing group of products gaining importance; patients/consumers of drug always have a wish to have no or less side/ toxic effect and also complementary or alternative benefit of the drug products and that’s why nowadays they are using nutraceuticals. In recent years, because of health benefits and an alternative to modern medicine, there is a growing interest in nutraceuticals. Nutrients, functional foods, medicinal food, herbals and dietary supplements are major constituents of nutraceuticals these play an artistic instrumental role in health maintenance, they also show various acts against various disease conditions and thus promote and sustain the quality of life. The article aims to explore and discuss the ability of nutraceuticals to treat or prevent underlying causes of disease; the article outlines nutraceuticals with their therapeutic applications, adverse effects and interaction. Various researches on nutraceutical product are under process which will be integrating and assessing information further.