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无味核壳型克拉霉素微胶囊的制备与表征

The preparation and characterisation of tasteless core-shell clarithromycin microcapsules.

作者信息

Fu Yu, Zhu Yunjing, Liang Xue, Kong Yihan, Wang Xiaolin, Zhang Anan, Zhao Zhiqing, Gou Jingxin, Wang Yanjiao, Yin Tian, Zhang Yu, He Haibing, Tang Xing

机构信息

Department of Pharmaceutics, College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.

School of Functional food and Wine, Shenyang Pharmaceutical University, Shenyang, China.

出版信息

J Microencapsul. 2022 Nov-Dec;39(7-8):654-667. doi: 10.1080/02652048.2022.2146221. Epub 2022 Dec 15.

Abstract

This study aims to fabricate core-shell clarithromycin (CAM) microcapsules to cover up the bitter taste of CAM by spray drying with aqueous polymer dispersion. Water dispersion of Eudragit EPO and Surelease were innovatively used to encapsulate CAM into microcapsules via a one-step spray-drying method. The inlet air temperature, airflow rate, CAM-polymer ratio, and particle size of CAM were optimised based on drug content and T (the time taken for the drug to release equal to 6% /). The powder properties were assessed by measuring particle size and microstructure using SEM, FT-IR, and PXRD. Furthermore, selected batch was assessed for their drug content, encapsulation efficiency, in vitro release, bitterness, and stability studies. EPO-Surelease (1: 4) microcapsules had an average diameter (D50) of 37.69 ± 3.61 μm with a span of 2.395. The drug contents and encapsulation efficiency of EPO-Surelease(1:4) were 10.89% and 63.7%, respectively. EPO-Surelease (1:4) microcapsules prepared by spray drying with aqueous polymer dispersion can effectively mask the bitter taste of CAM.

摘要

本研究旨在通过用聚合物水分散体喷雾干燥制备核壳型克拉霉素(CAM)微胶囊,以掩盖CAM的苦味。创新性地使用了丙烯酸树脂EPO和Surelease的水分散体,通过一步喷雾干燥法将CAM包封入微胶囊中。基于药物含量和T(药物释放量达到6%所需的时间),对进风温度、气流速率、CAM与聚合物的比例以及CAM的粒径进行了优化。通过扫描电子显微镜(SEM)、傅里叶变换红外光谱(FT-IR)和粉末X射线衍射(PXRD)测量粒径和微观结构,对粉末特性进行了评估。此外,对选定批次进行了药物含量、包封效率、体外释放、苦味和稳定性研究。EPO-Surelease(1:4)微胶囊的平均直径(D50)为37.69±3.61μm,跨度为2.395。EPO-Surelease(1:4)的药物含量和包封效率分别为10.89%和63.7%。通过用聚合物水分散体喷雾干燥制备的EPO-Surelease(1:4)微胶囊能够有效掩盖CAM的苦味。

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