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Release of medroxyprogesterone acetate from a silicone polymer.

T. J. Roseman, +1 more
- 01 Mar 1970 - 
- Vol. 59, Iss: 3
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.

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Citations
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Studies of diffusional release of a dispersed solute from polymeric matrixes by finite element method.

TL;DR: The method presented here can describe the entire process of diffusional release before and after the dispersed solute has been dissolved without the pseudo steady-state assumption and it is applicable to both small and large ratio of initial solute loading to the solute solubility in the matrix.
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Theoretical analyses of dispersed-drug release from planar matrices with a boundary layer in a finite medium.

TL;DR: The formulas, with explicit expressions, can be readily applied to analyze determinants of release kinetics, including volume of external medium, initial drug loading, and boundary layer thickness, and the criterion established for finding the conditions of drug saturation in a medium can be determined.
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Drug release from non-disintegrating hydrophilic matrices: sodium salicylate as a model drug

TL;DR: In this paper, the authors showed that the rate constants observed a semi-logarithmic relation to polymer content and extrapolated to give reasonable diffusion coefficient values for hypothetical low and high polymer content matrices.
References
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Mechanism of sustained‐action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices

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A simple equation for description of solute release I. Fickian and non-fickian release from non-swellable devices in the form of slabs, spheres, cylinders or discs

TL;DR: In this paper, a simple exponential relation Mt/M∞ = ktn is introduced to describe the general solute release behavior of controlled release polymeric devices, where Mt is the fractional release, t is the release time, k is a constant, and n is the diffusional exponent characteristic of the release mechanism.
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Diffusion in polymers

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