Dissolution Improvment of a Poorly Soluble Drug Using Hot Melt Extrusion Technique

Abstract

The aim of the present study was dissolution improvement of poorly soluble drug using hot melt extrusion technique. Hot melt extrusion (HME) involves the compaction and conversion of blends from a powder or a granular mix into a product of uniform shape. HME is a widely used process in the preparation of solid dispersion (SD) in a single step to enhance solubility of poorly water soluble drugs. Hydrochlorothiazide (HCTZ) is a BCS class-IV having low solubility and low permeability. It is a diuretic used in the treatment of hypertension where rapid onset of action is required. This strongly indicates need to improve its solubility. various techniques were used to improve release like Melt agglomeration, bead formulations and solvent evaporation etc. but HME was feasible because of facilitate better control over process variables such as temperature, shearing rate and time required for preparation. The solid dispersion was prepared using different concentration ratio of drug to polymer by two methods initially, i.e. Fusion method and Hot melt extrusion method. Poloxamer 188, having higher solubility, was selected after solubility studies. The drug release from SD prepared HME exhibited higher drug release compared to SD prepared by fusion method. The process parameter i.e. drug: polymer ratio, temperature and shearing rate were optimized to improve drug release. Thus, it was concluded that HME technique was found promising in improving drug released compared to fusion method. Moreover, the HME method is industrial applicable and scalable.