DESIGN AND DEVELOPMENT OF HYDROXYZINE HYDROCHLORIDE CONTROLLED RELEASE TABLETS BASED ON MICROSPONGE TECNOLOGY

Abstract

The purpose of the present study aims to design novel drug delivery system containing hydroxyzine hydrochloride microsponges and to prepare controlled release microsponge tablets. Hydroxyzine hydrochloride is an anti-histaminic drug used in the treatment of urticaria and pruritus. It has a half-life of about 3-4hrs. The Microsponge Delivery System is a unique technology for the controlled release of active agents, and it consists of porous polymeric microspheres, typically 10–50 μm in diameter. Microsponges of the drug were prepared by using polymer Methocel 10000cps and in combination with Eudragit –S 100, Eudragit-L 100, Eudragit-RL 100 and Eudragit-RS 100. These are prepared by oil in oil emulsion solvent diffusion method using acetone as dispersing solvent and liquid paraffin as the continuous medium. Magnesium stearate was added to the dispersed phase to prevent flocculation of polymeric microsponges. Compatibility of the drug with adjuncts was studied by FT-IR. Production yield, loading efficiency, particle size analysis, surface morphology and invitro release studies were carried out. The microsponge formulation (F8) was found to be stable at 40ᴼC and 75% relative humidity with respect to particle size, loading efficiency and invitro drug release. The optimized microsponge formulation F8 was compressed into tablets by using different diluents (Microcrystalline cellulose, directly compressible lactose and directly compressible dicalcium phosphate dihydrate). Mechanically strong tablets were obtained owing to plastic deformation of sponge like structure of microsponges. Thickness, hardness, friability, % drug content and invitro release studies were done on microsponge tablets. The results were kinetically evaluated and the release rate of hydroxyzine hydrochloride was found to be zero order. The microsponge tablet formulation, F11 showed controlled release of hydroxyzine hydrochloride for 12hrs.