文献类型：期刊文献

英文题名：Continuous Antisolvent Crystallization of Dolutegravir Sodium Using Microfluidics

作者：Liu, Fen[1,2];Luo, Wei[1,2];Qiu, Junjie[1,2];Guo, Yaohao[1,2];Zhao, Shuangliang[1,2,3,4];Bao, Bo[1,2]

机构：[1]East China Univ Sci & Technol, State Key Lab Chem Engn, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Chem Engn, Shanghai 200237, Peoples R China;[3]Guangxi Univ, Guangxi Key Lab Petrochem Resource Proc & Proc In, Nanning 530004, Peoples R China;[4]Guangxi Univ, Sch Chem & Chem Engn, Nanning 530004, Peoples R China

年份：2022

卷号：61

期号：19

起止页码：6693

外文期刊名：INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH

收录：;EI(收录号：20222112146897);WOS:【SCI-EXPANDED(收录号:WOS:000812202700001)】；

基金：This work is supported by Science and Technology Commission of Shanghai Municipality: Natural Science Foundation of Shanghai (No. 19ZR1472200) .

语种：英文

外文关键词：Biochemistry - Crystallizers - Drug delivery - Particle size - Sodium

摘要：Continuous antisolvent crystallization of Dolutegravir Sodium was studied using a novel device integrating the microfluidic continuous crystallizer and the agitated crystallizer. This study successfully minimized the risks of channel blockage during continuous crystallization by innovating an approach to isolate crystal nucleation from subsequent crystal growth. We systematically investigated the effects of the antisolvent content, channel width, and stirring speed on the particle size, the crystal size distribution (CSD), and the morphology of the crystals. By optimization of experimental parameters, crystals can be continuously obtained with small particle sizes (D-50 values of 5-10 mu m), narrow CSDs (widths of 4-7 mu m), and prismatic morphologies by this apparatus and approach. The particle sizes D-50 and CSDs of crystals are reduced by 30% and 60% at least, respectively, compared with values of the commercial sample. Small and uniform crystals are particularly desirable in the pharmaceutical industry, which can significantly improve drug solubility, bioavailability, corresponding pharmacokinetic performance, and the properties of the tablet.