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盐酸川芎嗪羧甲基壳聚糖与胶原蛋白微球的研制:处方优化、表征及体外释放

Development of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres: Formulation optimization, characterization, and vitro release.

作者信息

Lin Qiang, Huo Qing, Qin Yingzhe, Zhao Zhuo, Tao Fengyun

机构信息

a The College of Art and Science , Beijing Union University , Beijing , P.R. China.

b Biochemical Engineering College , Beijing Union University , Beijing , P.R. China.

出版信息

Bioengineered. 2017 Jan 2;8(1):55-60. doi: 10.1080/21655979.2016.1227584. Epub 2016 Sep 30.

DOI:10.1080/21655979.2016.1227584
PMID:27689792
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5172495/
Abstract

This study investigates the preparation of ligustrazine hydrochloride carboxymethyl chitosan and collagen microspheres. This experiment investigates effects of the ratio of carboxymethyl chitosan and collagen blend, water to oil ratio, stirring speed, and other factors on the microsphere properties. The experiment had the following conditions: a 1:2 proportion of carboxymethyl chitosan and collagen, a 1:2 proportion of drugs and materials, a 5:1 proportion of oil phase and water phase, 0.5% of span80, a 600r/min stirring speed, 3 ml of a cross-linking agent, 3 h of cross-linking curing, 1.25 ± 0.05 mm diameter LTH microcapsules, a 54.08% envelop rate, and a 14.16% carrier rate. The microspheres release rate reached 66% within 1 h, then steadily released within 5 h in vitro. The experimental results showed that the ligustrazine hydrochloride microsphere production process was stable and exhibited a good release effect compared with other ligustrazine hydrochloride tablets and pills.

摘要

本研究探讨盐酸川芎嗪羧甲基壳聚糖与胶原微球的制备。本实验研究羧甲基壳聚糖与胶原的混合比例、水油比、搅拌速度等因素对微球性能的影响。实验条件如下:羧甲基壳聚糖与胶原比例为1:2,药物与材料比例为1:2,油相与水相比例为5:1,司盘80含量为0.5%,搅拌速度为600r/min,交联剂用量为3ml,交联固化时间为3h,LTH微胶囊直径为1.25±0.05mm,包封率为54.08%,载药量为14.16%。微球在1h内释放率达66%,然后在体外5h内稳定释放。实验结果表明,盐酸川芎嗪微球生产工艺稳定,与其他盐酸川芎嗪片剂和丸剂相比,具有良好的释放效果。

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