FORMULATION AND EVALUATION OF SOLID DISPERSION FOR DISSOLUTION ENHANCEMENT OF KETOCONAZOLE

Paras Papneja*, Mahesh Kumar Kataria, Ajay Bilandi

ABSTRACT

Ketoconazole is one of the most commonly used anti-fungal drug. It is a member of imidazole containing compound that is used as a broad spectrum antifungal agent for the treatment or prevention of fungal infections especially against thrush, gastrointestinal infections, and infections of the skin, nails and scalp. Ketoconazole is available as oral tablet, cream and dandruff shampoo formulations. Ketoconazole has a high permeability and its solubility in aqueous media is not sufficient for the whole dose to be dissolved in the fluids under normal conditions. Formulation techniques that accelerate drug dissolution can guarantee a parallel improvement in bioavailability. Different techniques like co-solvent, solid dispersion, chemical modification of drug, liquid solid techniques etc. are available to enhance the solubility of drug. One of the favourable strategy to improve the solubility and hence bioavailability of poorly water soluble drugs is the formulation of solid dispersion. Solid dispersions and physical mixtures of ketoconazole were prepared by solvent evaporation method with different polymers viz. crosscarmellose sodium, sodium starch glycolate and Eudragit E100 in different ratio. Drug and excipients compatibilities were studied with FTIR method. The solid dispersion and physical mixtures were further studied for percentage practical yield, in vitro release of drug and solid dispersion with crosscarmellose in ration of 1:7 shows drug release of almost 3 times to the pure drug 20percentage increase with the marketed product. Further the optimised solid dispersion was used to formulate tablet.

Keywords: Biopharmaceutical Classification System, Ketoconazole Solubility, Solid dispersion.