Form Conversion and Solvent Entrapment during API Drying
Form Conversion and Solvent Entrapment during API Drying
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DOI：
10.1021/acs.oprd.7b00270
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发表时间：
2017-11-01
影响因子：
3.4
通讯作者：
Zhou, George
中科院分区：
文献类型：
--
作者：
Lamberto, David J.;Diaz-Santana, Anthony;Zhou, George
活性药物成分（API）作为结晶水合物从溶液中分离，然后在干燥过程中转化为所需的弱结晶形式。在工厂规模下观察到溶剂去除不完全。怀疑加工设备和干燥条件的差异导致固体中的水分快速损失、早期形式转化以及随后工艺溶剂的截留超过质量标准水平。进行了实验，以获得更好地了解干燥过程和测试理论的溶剂捕获。本文描述的实用方法和技术被认为广泛适用于API干燥工艺开发;与溶剂截留相关的发现可能在干燥过程中经历形式转变的化合物中很常见。本文介绍了实验结果，这些结果有助于加深对API成功干燥的工艺理解和条件识别。
An active pharmaceutical ingredient (API) was isolated from solution as a crystalline hydrate and then converted to the desired weakly crystalline form during drying. Incomplete solvent removal was observed at the factory scale. It was suspected that differences in the processing equipment and drying conditions led to the rapid loss of water from the solids, early form conversion, and subsequent trapping of the process solvent above specification levels. Experiments were conducted to gain a better understanding of the drying process and test theories for solvent trapping. The practical methods and techniques described here are considered broadly applicable to API drying process development; findings associated with solvent entrapment may be common across compounds undergoing a form transition during drying. This article presents experimental results that led to an increased process understanding and identification of conditions for successful drying of the API.