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甘草次酸拼合物TOGA-X4微粒的制备工艺及其体外释药特性研究
引用本文:田娟,赵蕊,王鹏龙,范文硕,王之洋,马宏瑞,雷海民,蔡程科.甘草次酸拼合物TOGA-X4微粒的制备工艺及其体外释药特性研究[J].中草药,2018,49(8):1802-1808.
作者姓名:田娟  赵蕊  王鹏龙  范文硕  王之洋  马宏瑞  雷海民  蔡程科
作者单位:北京中医药大学中药学院
基金项目:国家自然科学基金面上项目(81173562)
摘    要:目的制备粒径均一、复水性良好的甘草次酸拼合物TOGA-X4微粒,得到稳定可靠的制剂工艺,评价其体外释药特性。方法以平均粒径、多分散指数和复水性为指标,通过单因素分析法对不锈钢膜乳化法制备抗肿瘤活性物质TOGA-X4微粒的工艺进行考察及优化,同时通过扫描电子显微镜观察微粒外观形态;采用直接释药法测定TOGA-X4微粒和原粉的累积释放率,并采用不同释放模型拟合体外释药曲线,对比评价其体外释药特性。结果优选的最佳制剂工艺为油相含TOGA-X4质量浓度5 mg/m L,水相PVA质量浓度30 mg/m L,油水比1∶1,过膜压力0.4 MPa,冻干保护剂为质量浓度50mg/m L蔗糖水溶液,固化温度为70℃。TOGA-X4微粒中TOGA-X4的释放曲线符合Logistic动力学方程,TOGA-X4原粉的释放曲线符合零级动力学方程。结论不锈钢膜乳化法制备微粒工艺简单、稳定、可靠,提高了难溶性药物的溶出速率,在难溶性药物微粒的制备中具有优越性。

关 键 词:不锈钢膜乳化法  甘草次酸  拼合物  微粒  体外释放  复水性  TOGA-X4  抗肿瘤  累积释放率  释药特性
收稿时间:2017/11/10 0:00:00

Preparation of microparticles of glycyrrhetinic acid complex TOGA-X4 and in vitro release characteristics
TIAN Juan,ZHAO Rui,WANG Peng-long,FAN Wen-shuo,WANG Zhi-yang,MA Hong-rui,LEI Hai-min and CAI Cheng-ke.Preparation of microparticles of glycyrrhetinic acid complex TOGA-X4 and in vitro release characteristics[J].Chinese Traditional and Herbal Drugs,2018,49(8):1802-1808.
Authors:TIAN Juan  ZHAO Rui  WANG Peng-long  FAN Wen-shuo  WANG Zhi-yang  MA Hong-rui  LEI Hai-min and CAI Cheng-ke
Institution:School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China,School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China,School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China,School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China,School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China,School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China,School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China and School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China
Abstract:
Keywords:stainless steel film emulsification method  glycyrrhetinic acid  complex  microparticles  in vitro release  rehydration property  TOGA-X4  antitumor  cumulative release rate  release characteristics
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