Release of medroxyprogesterone acetate from a silicone polymer.

TLDR: In this paper, the physicochemical factors involved in the in vitro release of medroxyprogesterone acetate (MPA) a water-insoluble steroid embedded in a silicone rubber matrix was based upon a model system which considered the matric boundary diffusion layer.

Abstract: A study of the physicochemical factors involved in the in vitro release of medroxyprogesterone acetate (MPA) a water-insoluble steroid embedded in a silicone rubber matrix was based upon a model system which considered the matric boundary diffusion layer; extensive mathematical equations for the model are presented for planar and cylindrical cases. Initial and long-time release rates were obtained. Zones of MPA depletion were measured microscopically as a function of time and the partition coefficient of MPA was determined. Following relatively constant initial release rates a nonlinear dependence of release rates upon MPA concentration (3% 12% 24%) was found. As MPA diffused from the matrix well-defined zones of depletion developed and were photographed. Comparison of the present model to the T. Higuchi model of drug release (based on a purely matrix-controlled system) indicated that when boundary layer was considered a better fit of experimental data to theory was found. Findings suggest that the partition coefficient diffusion coefficients medroxyprogesterone acetate concentration within the polymer and agitation conditions play important roles in the release process. The applicability of the model to an in vivo system (in which slower release of MPA has been observed) is evaluated.