Enhancement of Bioavailability of Clopidogrel Using Different Solubility Enhancement Techniques

Abstract

Bioavailability is the key determinant of a drug for its therapeutic effectiveness, which in turn depends upon the solubility of that drug in gastro intestinal fluid. Clopidogrel is a BCS class II drug. Drugs of this category have low solubility and high permeability, so their bioavailability is less. This can be overcome by doing pharmaceutic modifications on it. In the present study, three different modifications, namely, complexation, solvent deposition and surface solid dispersion were utilized to improve the solubility. Preformulation studies included solubility, melting point determination and compatibility studies. FTIR, solubility analysis, in vitro drug release study and kinetic studies were done for all the formulations. Solubility study results showed better solubility of formulations. The mechanism of drug release from formulations was found to be super case 2 transport. From all these evaluations, the F_3Sol.D was taken as better formulation. The F_3Sol.D was subjected to further evaluation before formulating it into capsule form. The values of angle of repose and Carrs index show that the powder is having good flow properties. F_3Sol.D was formulated into capsule. Capsules were evaluated for properties like content uniformity, weight uniformity and disintegration. In vitro dissolution studies showed 96% release at 60th min. Clopidogrel capsules were found to pass one month stability studies as per ICH guidelines.

Keywords: Clopidogrel, solubility enhancement techniques, encapsulation complex, solvent deposition, surface solid dispersion

Cite this Article

Arun Raj R, Nadiya KK, Jyoti Harindran. Enhancement of Bioavailability of Clopidogrel Using Different Solubility Enhancement Techniques. Research and Reviews: A Journal of Pharmaceutical Science. 2016; 7(2): 25–39p.