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

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

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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 spher-ulites 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 spher-ulites.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 crys-tallization 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 modi-fied supersaturation control had a low residue of antisolvent acetone,and the flowability was signifi-cantly improved.

SpheruliteCeftriaxone sodiumAntisolvent crystallizationSupersaturationOnline observation

Shankun Liang、Yuchao Niu、Xueyan Hu、Wu Xiao、Xuehua Ruan、Gaohong He、Xiaobin Jiang

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State Key Laboratory of Fine Chemicals,Frontiers Science Center for Smart Materials,School of Chemical Engineering,Dalian University of Technology,Dalian,116024,China

School of Chemical Engineering at Panjin,Dalian University of Technology,Panjin,124221,China

financial contribution from Central Guidance on Local Science and Technology Development Fund of Liaoning ProvinceNational Key Research and Development Program of ChinaNational Natural Science Foundation of ChinaNational Natural Science Foundation of ChinaFundamental Research Funds for the Central UniversitiesFundamental Research Funds for the Central UniversitiesKey Research and Development Projects in Shandong Provinceassistance of Dalian University of Technology Instrumental Analysis Center

2023JH6/1001000042021YFC29013002202100522378041DUT22YG208DUT22LAB6032022CXGC010303

2024

10.1016/j.partic.2023.11.018

颗粒学报(英文版)
中国颗粒学会　中国科学院过程工程研究所

颗粒学报(英文版)

CSTPCD
影响因子：0.632
ISSN：1674-2001
年,卷(期)：2024.90(7)
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