通过 QESD 制备卡马西平-阿司佩林共晶体的微球状颗粒,提高其可制造性和溶解性

IF 4.1 2区 材料科学 Q2 ENGINEERING, CHEMICAL Particuology Pub Date : 2024-06-04 DOI:10.1016/j.partic.2024.06.001
Jinbo Ouyang , Lishan Liu , Zichen Ning , Zhuoshan Gong , Limin Zhou , Feiqiang He , Zhi Gao , Li Xu , Shichao Du , Huaiyu Yang
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引用次数: 0

摘要

制粒是改善药物流动性的一种有效方法,尤其是当药物呈针状时。卡马西平-紫杉醇(CBZ-HPE)共晶体是一种针状晶体,溶解度低,流动性差,限制了其应用。针对这一问题,本研究旨在利用准乳液溶剂扩散(QESD)技术获得 CBZ-HPE 微球。利用偏光显微镜对制备过程进行了监控,并利用径向分布函数(RDF)阐明了其形成机理。利用 PXRD、DSC、TGA 和 SEM 对微球进行了广泛表征。此外,还分析了表面活性剂、含量和转速对微球形态和粒度分布的影响,以确定最佳实验条件。基于这些发现,研究人员选择中药有效成分柚皮苷和槲皮素成功制备了 CBZ-HPE 多组分微球。该研究为通过制备微球提高药物粉末性能和药物共轭奠定了基础。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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

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.

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来源期刊
Particuology
Particuology 工程技术-材料科学:综合
CiteScore
6.70
自引率
2.90%
发文量
1730
审稿时长
32 days
期刊介绍: The word ‘particuology’ was coined to parallel the discipline for the science and technology of particles. Particuology is an interdisciplinary journal that publishes frontier research articles and critical reviews on the discovery, formulation and engineering of particulate materials, processes and systems. It especially welcomes contributions utilising advanced theoretical, modelling and measurement methods to enable the discovery and creation of new particulate materials, and the manufacturing of functional particulate-based products, such as sensors. Papers are handled by Thematic Editors who oversee contributions from specific subject fields. These fields are classified into: Particle Synthesis and Modification; Particle Characterization and Measurement; Granular Systems and Bulk Solids Technology; Fluidization and Particle-Fluid Systems; Aerosols; and Applications of Particle Technology. Key topics concerning the creation and processing of particulates include: -Modelling and simulation of particle formation, collective behaviour of particles and systems for particle production over a broad spectrum of length scales -Mining of experimental data for particle synthesis and surface properties to facilitate the creation of new materials and processes -Particle design and preparation including controlled response and sensing functionalities in formation, delivery systems and biological systems, etc. -Experimental and computational methods for visualization and analysis of particulate system. These topics are broadly relevant to the production of materials, pharmaceuticals and food, and to the conversion of energy resources to fuels and protection of the environment.
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