Formulating buffered dissolution media for sparingly soluble weak acid and weak base drug compounds based on microenvironmental pHo considerations

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Abstract

The theoretical framework for dissolution of weak acid and weak base drug compounds in buffered media is well established. Therefore, this article is intended to provide a review of this framework and apply it to formulate buffered dissolution media based on ionic equilibrium conditions within the diffusion layer at the solid-liquid interface. The pHo in the microenvironment is identified as a singularly important parameter that reflects ionic interactions between dissolving drug and buffer at the solid-liquid interface. This article is focused on (1) formulating buffered dissolution media based on ionic equilibrium conditions at the solid-liquid interface, (2) identifying key physicochemical parameters for both drug and buffer that are relevant to buffer formulation, and (3) providing experimental and calculation-based methods to estimate the pHo at the solid-liquid interface. A shift in emphasis from relying solely on bulk buffer pH properties forms a basis for formulating buffered dissolution media and also provides insight into the physicochemical factors that affect the dissolution rate of the drug compound.

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CITATION STYLE

APA

Stippler, E. S., Romero, N. E., & Mauger, J. W. (2014). Formulating buffered dissolution media for sparingly soluble weak acid and weak base drug compounds based on microenvironmental pHo considerations. Dissolution Technologies, 21(4), 20–25. https://doi.org/10.14227/DT210414P20

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