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Superior Dissolution Behavior and Bioavailability of Pharmaceutical Cocrystals and Recent Regulatory Issues
Meng Y Xia1,2, Bing Q Zhu1, Jian-R Wang1
1Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
ACS Medicinal Chemistry Letters
|January 21, 2022
Summary
Pharmaceutical cocrystals enhance active pharmaceutical ingredient (API) properties like solubility. This review covers cocrystal development, regulatory guidelines, and their patent potential, using d-α-tocopherol as an example.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Drug Delivery
Background:
- Cocrystallization is a key strategy for improving the physicochemical properties of active pharmaceutical ingredients (APIs).
- Optimized properties include enhanced stability, dissolution rates, and bioavailability.
- Understanding cocrystal formation is crucial for drug development.
Purpose of the Study:
- To review the history and development of pharmaceutical cocrystals.
- To differentiate pharmaceutical cocrystals from salts and explain dissolution enhancement mechanisms.
- To discuss regulatory guidelines and patent generation potential.
Main Methods:
- Literature review of cocrystallization techniques and applications.
- Analysis of mechanisms for improved dissolution.
- Examination of regulatory frameworks (FDA, EMA) and patent strategies.
- Case study using d-α-tocopherol.
Main Results:
- Cocrystallization significantly improves API physicochemical properties.
- Clear distinctions exist between cocrystals and pharmaceutical salts.
- In vitro dissolution and in vivo absorption data correlation (IVIVC) is established for cocrystals.
- Regulatory guidelines for cocrystals are emerging.
- Cocrystals offer opportunities for novel patent generation.
Conclusions:
- Cocrystallization is a valuable technique for optimizing drug properties.
- Further research into cocrystal mechanisms and regulatory aspects is warranted.
- Cocrystals, exemplified by d-α-tocopherol, hold significant potential for intellectual property development.
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