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Current Pharmaceutical Design

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ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

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General Review Article

Manipulation of Pharmaceutical Polymorphic Transformation Process Using Excipients

Author(s): Beiqian Tian, Zhiyong Ding, Shuyi Zong, Jinyue Yang, Na Wang, Ting Wang, Xin Huang and Hongxun Hao*

Volume 26, Issue 21, 2020

Page: [2553 - 2563] Pages: 11

DOI: 10.2174/1381612826666200213122302

Price: $65

Abstract

Background: In the pharmaceutical field, it is vital to ensure a consistent product containing a single solid-state form of the active pharmaceutical ingredient (API) in the drug product. However, some APIs are suffering from the risk of transformation of their target forms during processing, formulation and storage.

Methods: The purpose of this review is to summarize the relevant category of excipients and demonstrate the availability and importance of using excipients as a key strategy to manipulate pharmaceutical polymorphic transformation.

Results: The excipient effects on solvent-mediated phase transformations, solid-state transitions and amorphous crystallization are significant. Common pharmaceutical excipients including amino acids and derivatives, surfactants, and various polymers and their different manipulation effects were summarized and discussed.

Conclusion: Appropriate use of excipients plays a role in manipulating polymorphic transformation process of corresponding APIs, with a promising application of guaranteeing the stability and effectiveness of drug dosage forms.

Keywords: Manipulation, APIs, excipients, polymorphic transformation, amorphous, stability.

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