Fabrication of micro spherulitic particles of carbamazepine-hesperetin cocrystal via QESD with enhanced manufacturability and dissolution  

作　　者：Jinbo Ouyang Lishan Liu Zichen Ning Zhuoshan Gong Limin Zhou Feiqiang He Zhi Gao Li Xu Shichao Du Huaiyu Yang 

机构地区：[1]Jiangxi Province Key Laboratory of Functional Organic Polymers,East China University of Technology,Nanchang,330013,China [2]School of Pharmaceutical Science,Qilu University of Technology,Jinan,250353,China [3]Department of Chemical Engineering,Loughborough University,Leicestershire,LE113TU,UK

出　　处：《Particuology》2024年第10期11-21,共11页颗粒学报（英文版）

基　　金：supported by National Natural Science Foundation of China(grant Nos.22068002 and 22178054);Jiangxi ProvincialNatural Science Foundation(grant Nos.20224ACB213007_and 20232BBH80015);Jiangxi Province Key Laboratory of Synthetic Chemistry(grant No.JXSC202209).

摘　　要：Granulation is an effective method for improving the flowability of drugs, particularly when they are in needle form. Carbamazepine-hesperetin (CBZ-HPE) cocrystal is a needle-like crystal with low solubility and poor flowability, which limits its application. To address this issue, this study aimed to obtain CBZ-HPE microspheres using the quasi-emulsion solvent diffusion (QESD) technique. The preparation process was monitored using polarized light microscopy, and the formation mechanism was elucidated using the radial distribution function (RDF). The microspheres were extensively characterized using PXRD, DSC, TGA, and SEM. Furthermore, the effects of surfactants, contents, and rotational speeds on the morphology and particle size distribution of microspheres were analyzed to determine the optimal experimental conditions. Based on these findings, naringenin and quercetin, the active ingredients of traditional Chinese medicine, were chosen to successfully prepare CBZ-HPE multicomponent microspheres. This research provides a foundation for increasing drug powder properties and drug conjugation through the preparation of microspheres.

关 键 词：Carbamazepine-hesperetin cocrystal Quasi-emulsion solventdiffusion(QESD) technique Microspheres FLOWABILITY Dissolution rate 

分 类 号：R318[医药卫生—生物医学工程]