Evaluation of Lipophilic Properties of Thermoplastic Granule in Formulation of Sustained Release Matrix in Solid Dosage Forms

Abstract

This study was aimed at developing a new, technically simple method for the preparation of a once-daily sustained release matrix formulations, which would enable reproducible release of the active ingredient. Thermoplastic granulation is a new technique in pharmaceutical formulation. Coated particles of an active pharmaceutical ingredient (API) in sustained release matrix are prepared by thermoplastic granulation technique via heating (50 – 75°C) in fluid-bed dryer (FBD) granulator. The FBD creates ideal conditions for the most intense heat and mass transfer by spraying melted liquids onto the granular API. A variety of innovative processes such as granulation, agglomeration, coating and microencapsulation can be realized. Melted mixture of cetyl alcohol, glyceryl monostearate, and polyethylene glycol 4000 (PEG 4000) was used for fluid-bed coating. The present article deals with assessing the influence of rheological properties and hydrophile-lipophile balance (HLB) parameter of thermoplastic granules on the mechanism of drug delivery from sustained release matrix in solid dosage forms. The drug release kinetics model is affected by rheology, HLB of cetyl alcohol, and physicochemical properties of API granules.