Supersaturation-driven self-assembly formation of ceftriaxone sodium spherulites:From amorphous form to spherulites  

作　　者：Shankun Liang Yuchao Niu Xueyan Hu Wu Xiao Xuehua Ruan Gaohong He Xiaobin Jiang 

机构地区：[1]State Key Laboratory of Fine Chemicals,Frontiers Science Center for Smart Materials,School of Chemical Engineering,Dalian University of Technology,Dalian,116024,China [2]School of Chemical Engineering at Panjin,Dalian University of Technology,Panjin,124221,China

出　　处：《Particuology》2024年第7期10-19,共10页颗粒学报（英文版）

基　　金：the financial contribution from Central Guidance on Local Science and Technology Development Fund of Liaoning Province(grant No.2023JH6/100100004);National Key Research and Development Program of China(grant No.2021YFC2901300);National Natural Science Foundation of China(grant No.22021005,22378041);Fundamental Research Funds for the Central Universities(grant No.DUT22YG208,DUT22LAB603);Key Research and Development Projects in Shandong Province(grant No.2022CXGC010303);acknowledge the assistance of Dalian University of Technology Instrumental Analysis Center.

摘　　要：Drug particles with spherical morphology possess amazing advantages in terms of particle flowability,mechanical properties,drug solubility,and bioavailability.The growth mechanism of drug spherulite is of great importance for the preparation and regulation of spherulites.Herein,ceftriaxone sodium spherulites were fabricated by the antisolvent crystallization method using dropwise addition of ceftriaxone sodium solution to acetone.Online observation of the whole crystallization process combined with electron microscopy technique revealed the spherical growth process from amorphous form to spherulites.As the supersaturation of the crystallization system was adjusted,the ceftriaxone sodium crystals transformed from amorphous form to spherulites.In the process of antisolvent crystallization with acetone as antisolvent,when the theoretical supersaturation degree S was higher than 2.62,the crystallization system tended to appear amorphous form;when S was between 2.57 and 2.62,the amorphous form transformed into clustered spherulites;when S was less than 2.57,the surface of spherulites will be covered with flaky crystal,which transformed into urchin-like type.With the understanding of the spherical growth mechanism,the ceftriaxone sodium spherulites prepared in this research with modified supersaturation control had a low residue of antisolvent acetone,and the flowability was significantly improved.

关 键 词：SPHERULITE Ceftriaxone sodium Antisolvent crystallization SUPERSATURATION Online observation 

分 类 号：TQ317[化学工程—高聚物工业]