栀子苷乳剂的制备工艺及质量评价.PDFVIP

中草药 Chinese Traditional and Herbal Drugs 第50 卷 第2 期 2019 年1 月 ·375 · 栀子苷乳剂的制备工艺及质量评价 1 1 1 2 3* 王金悦 ，叶青卓 ，武琰琛 ，刘 玲 ，张向荣 1. 沈阳药科大学中药学院，辽宁 沈阳 110016 2. 辽宁海思科制药有限公司，辽宁 葫芦岛 125000 3. 沈阳药科大学药学院，辽宁 沈阳 110016 摘 要：目的 制备油包水型栀子苷乳剂，对处方工艺进行优化并进行质量评价。方法 通过单因素考察和混料设计，以乳 化时间、析油时间和静置分层时间为指标，研究处方对乳剂性质的影响，并筛选出最佳的制备工艺，得到最优的栀子苷乳剂。 并对乳剂的性质、稳定性、含量和体外释放进一步考察。结果 栀子苷乳剂的平均粒径为（5.48±0.02 ）μm ，PDI 值为0.125± 0.096 ；离心加速实验4 000 r/min 离心15 min 未见分层；栀子苷乳剂的平均质量分数为92.14%，RSD 为1.86% （n ＝3 ）；6 h 内栀子苷乳剂在pH 4.5 、6.8、7.4 的环境下体外释放分别最高达105.32%、98.41%、98.70%，而在pH 1.2 的环境下体外释放 最高为 63.45%；最后通过拟合方程来解释释药规律。结论 高速剪切机械法可用于栀子苷乳剂的制备，优化后处方的质量 评价符合要求。 关键词：栀子苷；油包水型乳剂；混料设计；稳定性；体外释放 中图分类号：R283.6 文献标志码：A 文章编号：0253 - 2670(2019)02 - 0375 - 07 DOI: 10.7501/j.issn.0253-2670.2019.02.015 Preparation and quality evaluation of gardenoside emulsion 1 1 1 2 3 WANG Jin-yue , YE Qing-zhuo , WU Yan-chen , LIU Ling , ZHANG Xiang-rong 1. Traditional Chinese Medicine College, Shenyang Pharmaceutical University, Shenyang 110016, China 2. Liaoning Haisike Pharmaceutical Co., Ltd., Huludao 125000, China 3. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China Abstract: Objective To prepare water-in-oil gardenoside emulsion, optimize its formulation process, and evaluate the quality. Methods The formulation was optimized based on emulsification time, oil floating time and phase separation time, and investigated the optimal gardenoside emulsion by the single factor investigation and mixture design. The properties, stability, content, and in vitro release of the emulsion were also studied. Results The mean particle size of gardenoside emulsion was (5.48 ±0.02) μm and the value of PDI was 0. 125 ±0.096; Centrifugation accelerated test was perfor