In vitro and in vivo Studies of Repaglinide Fast Dissolving Tablet Utilizing Solid Dispersion Techniques
Journal Title: Journal of Pharmaceutical Research International - Year 2015, Vol 5, Issue 4
Abstract
Repaglinide according to the biopharmaceutics classification system is considered as class II drug, which suffers from low aqueous solubility and hence, low bioavailability. The current study concerned with improvement of the aqueous solubility and dissolution rate of repaglinide by using solid dispersion techniques with different polymers. Moreover, fast-dissolving tablets of repaglinide solid dispersion with superdisintegrant were formulated to enhance the repaglinide bioavailability. In the present study, solid dispersion formulae of repaglinide were prepared by utilizing different polymers namely polyethylene glycol 6000, mannitol and urea in various drug: polymer ratio (1:1, 1:3, 1:5, 1:10) by using melting and solvent evaporation methods. The solubility of repaglinide in different carriers was estimated, and solid dispersions were prepared and characterized. The drug release profile was carried out in phosphate buffer 6.8 using USP type I dissolution apparatus. From the above studies, it was found that the fusion method shows the better enhancement of dissolution in comparison to the solvent evaporation method. Among carriers used and based on the in vitro release study, the faster drug release appeared from solid dispersion prepared with urea in ratio 1:10. The increase in dissolution rate of repaglinide was confirmed by X-ray diffraction spectral studies of its solid dispersion which showed a significant decrease in drug crystallinity. The absence of interactions between drug and polymer was confirmed by differential scanning calorimetry and Fourier transform infrared spectroscopy studies. In addition, formula repaglinide solid dispersion FU10 was selected to develop a fast dissolving tablet that disintegrates rapidly and releases the maximum amount of repaglinide using Ac-Di-Sol as superdisintegrant. The prepared batches of tablets were tested for mechanical strength properties (hardness and friability), weight variation, disintegration, drug content and in vitro dissolution studies. Furthermore, pharmacokinetic studies with the selected fast dissolving tablet of repaglinide in solid dispersion were conducted on human volunteers. The fast dissolving tablet is a promising formulation for repaglinide that results in higher solubility, a rapid onset of action, and enhanced systemic bioavailability.
Authors and Affiliations
Dalia Abdel-Rhman Attia
Keywords
Related Articles
- EP ID EP344773
- DOI 10.9734/BJPR/2015/14739
- Views 117
- Downloads 0
The Effects of Kolaviron on the Atherogenic Propensity of Nigeria Local Edible Oils in Male Wistar Rats
Background: Dyslipidemia is partly dependent on consumption of edible oils. We set out to determine the atherogenic effects of commonedible oils in Nigeria, in male Wistar rats and to find out if administration of oral k...
In vitro Efficacies of Some Nigerian Medicinal Plant Extracts against Toxigenic Aspergillus flavus, A. parasiticus and A. ochraceus
The aim of this work was to find an alternative to chemical fungicides currently used in the control and prevention of activities of toxigenic Aspergillus flavus, A. parasiticus and A. ochraceus in food and feed. The anti...
Hepatoprotective Effect of Crocus sativus on Amiodarone-Induced Liver Toxicity
Aims: The purpose of this study was to investigate the hepatoprotective effect of aqueous and ethanolic extract of Crocus sativus in amiodarone-induced hepatotoxicity in rabbits. Methods: Study was divided into 2 major g...
A Demographical Assessment of Different Insulin Regimens in Non-insulin Dependent Diabetics
A Demographical Assessment of Different Insulin Regimens in Non-insulin Dependent Diabetics Sajjad Ali1*, Syed Atif Raza2, Humayun Riaz1, Mobasher Ahmad Butt2, Hamid Saeed2, Zikria Saleem2, Tanveer Ahmed Khan1, and Mu...
Effect of Levetiracetam in the Treatment of Refractory Seizure in Infants through EEG: The Case of the Neonatal Intensive Care Unit of Tehran’s Children’s Medical Center
Objective: Phenobarbital, phenytoin and Benzodiazepins are the most common treatments for resistant neonatal seizure [1]. Drug of choice in the treatment of neonatal seizure should be more effective and have fewer side e...