Polymer Nanocoating of Amorphous Drugs for Improving Stability, Dissolution, Powder Flow, and Tabletability: The Case of Chitosan-Coated Indomethacin

无定形药物的聚合物纳米涂层可改善稳定性、溶解性、粉末流动性和可压片性:以壳聚糖包覆的吲哚美辛为例

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作者:Yuhui Li, Junguang Yu, Shenye Hu, Zhenxuan Chen, Mark Sacchetti, Changquan Calvin Sun, Lian Yu

Abstract

As a result of its higher molecular mobility, the surface of an amorphous drug can grow crystals much more rapidly than the bulk, causing poor stability and slow dissolution of drug products. We show that a nanocoating of chitosan (a pharmaceutically acceptable polymer) can be deposited on the surface of amorphous indomethacin by electrostatic deposition, leading to significant improvement of physical stability, wetting by aqueous media, dissolution rate, powder flow, and tabletability. The coating condition was chosen so that the positively charged polymer deposits on the negatively charged drug. Chitosan coating is superior to gelatin coating with respect to stability against crystallization and agglomeration of coated particles.

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