Regulating Drug Release Via Non-Uniform Distribution of Coating Composition in Multilayer Drug-Coated Granules

Abstract

Multilayer drug-coated granules with a non-uniform distribution of the coating composition specifically the drug loading and the polymer viscosity, across the thickness of the film matrix were prepared by the fluidized bed coating process. The rate and duration of diphenhydramine hydrochloride release from the coated granules can be modified through control of the gradient change in the coating composition across the thickness of the methylcellulose (MC) film matrix. A steeper gradient change across the film matrix resulted in a slower overall release rate. Formulations with gradient drug loading distribution exhibited an extended release time that can be twice as long as that for the control formulation. Gradient layered matrices obtained by sequentially depositing different viscosity grades of MC produced release profiles that differed from film matrices prepared using MC blends.