期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 13, 期 1, 页码 29-37出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.1c00478
关键词
Pharmaceutical cocrystals; solubility; dissolution; bioavailability; IVIVC; patentability
资金
- Shanghai Science and Technology Innovation Action Plan [20142201800]
This article provides an overview of cocrystals in terms of their history, development, differences with salts, mechanisms for improved dissolution, as well as regulatory guidelines from FDA and EMA. It also discusses the correlation between cocrystals and IVIVC data, and highlights the potential of cocrystals in patent generation using D-alpha-tocopherol as an example.
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 in vitro dissolution and in vivo 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-alpha-tocopherol is used as an example to demonstrate the potential of cocrystals in patent generation.
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