Superior Dissolution Behavior and Bioavailability of Pharmaceutical Cocrystals and Recent Regulatory Issues

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2022 Jan 21

PMID 35059121

Authors

Meng Y Xia

Bing Q Zhu

Jian-R Wang

Ze E Yang

Xue F Mei

Affiliations

Soon will be listed here.

Abstract

Cocrystallization has been used extensively to optimize the physicochemical properties of active pharmaceutical ingredients (APIs), such as stability, dissolution, and bioavailability. This review summarizes the history and development of cocrystals, the differences between pharmaceutical cocrystals and salts, and the mechanism underlying the improvement of dissolution through cocrystallization. The correlation of dissolution and absorption data (IVIVC) of cocrystals has been discussed as well. Subsequently, guidelines for regulatory classification of cocrystals by the U.S. Food and Drug Administration (FDA) and European Medicines Agency (EMA) are introduced. Finally, d-α-tocopherol is used as an example to demonstrate the potential of cocrystals in patent generation.

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