Abstract
Active pharmaceutical ingredients (APIs), frequently delivered to the patient in the solid-state as part of an approved dosage form, can exist in such diverse solid forms as polymorphs, pseudopolymorphs, salts, co-crystals and amorphous solids. Various solid forms often display different mechanical, thermal, physical and chemical properties that can remarkably influence the bioavailability, hygroscopicity, stability and other performance characteristics of the drug. Hence, a thorough understanding of the relationship between the particular solid form of an active pharmaceutical ingredient (API) and its functional properties is important in selecting the most suitable form of the API for development into a drug product. In past decades, there have been significant efforts on the discovery, selection and control of the solid forms of APIs and bulk drugs. This contribution discusses the thermodynamics and kinetics of polymorphic systems, the characterization of polymorphs, and the transformation between polymorphs. The major techniques for polymorph discovery and control developed in the past years are discussed as well.
Keywords: Crystallization, polymorphism, pseudopolymorphism, active pharmaceutical ingredients (APIs), discovery, control
Current Medicinal Chemistry
Title: Polymorphism and Crystallization of Active Pharmaceutical Ingredients (APIs)
Volume: 16 Issue: 7
Author(s): Jie Lu and Sohrab Rohani
Affiliation:
Keywords: Crystallization, polymorphism, pseudopolymorphism, active pharmaceutical ingredients (APIs), discovery, control
Abstract: Active pharmaceutical ingredients (APIs), frequently delivered to the patient in the solid-state as part of an approved dosage form, can exist in such diverse solid forms as polymorphs, pseudopolymorphs, salts, co-crystals and amorphous solids. Various solid forms often display different mechanical, thermal, physical and chemical properties that can remarkably influence the bioavailability, hygroscopicity, stability and other performance characteristics of the drug. Hence, a thorough understanding of the relationship between the particular solid form of an active pharmaceutical ingredient (API) and its functional properties is important in selecting the most suitable form of the API for development into a drug product. In past decades, there have been significant efforts on the discovery, selection and control of the solid forms of APIs and bulk drugs. This contribution discusses the thermodynamics and kinetics of polymorphic systems, the characterization of polymorphs, and the transformation between polymorphs. The major techniques for polymorph discovery and control developed in the past years are discussed as well.
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Cite this article as:
Lu Jie and Rohani Sohrab, Polymorphism and Crystallization of Active Pharmaceutical Ingredients (APIs), Current Medicinal Chemistry 2009; 16 (7) . https://dx.doi.org/10.2174/092986709787549299
DOI https://dx.doi.org/10.2174/092986709787549299 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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