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喷雾干燥无定形药物的综述:合成、分析和应用。

A critical review of spray-dried amorphous pharmaceuticals: Synthesis, analysis and application.

机构信息

Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, Hunan 410013, China.

School of Materials Science and Engineering, Central South University, Changsha, Hunan 410013, China.

出版信息

Int J Pharm. 2021 Feb 1;594:120165. doi: 10.1016/j.ijpharm.2020.120165. Epub 2020 Dec 10.


DOI:10.1016/j.ijpharm.2020.120165
PMID:33309835
Abstract

New drugs are frequently found with poor water-solubility in recent pharmaceutical projects, which brings difficulties of bioavailability for the clinical development of new drugs. When these drug compounds in a crystalline state are absorbed by gastrointestinal tract, their dissolution rates and absorption rates are very limited. Nowadays, various methods have been developed to improve the solubility, dissolution and bioavailability of drugs. According to the characteristics of drugs, this work suggests the use of spray drying technology to amorphize APIs (active pharmaceutical ingredients) to improve their bioavailability. This work reviews the properties of the spray-dried amorphous drugs, the progress made in drug synthesis and application, and the existing problems.

摘要

近年来,新药研发中常发现一些水溶性较差的药物,这给新药的临床开发带来了生物利用度的难题。当这些处于结晶状态的药物化合物被胃肠道吸收时,其溶解速率和吸收速率非常有限。目前,已经开发出各种方法来提高药物的溶解度、溶解速率和生物利用度。根据药物的特点,本工作建议使用喷雾干燥技术使原料药(API)非晶化以提高其生物利用度。本工作综述了喷雾干燥无定形药物的性质、药物合成和应用方面的进展以及存在的问题。

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