药剂与工艺β-细辛醚微乳的制备及其性质考察.PDFVIP

中草药 Chinese Traditional and Herbal Drugs 第 44 卷 第 1 期 2013 年 1 月 ·31· ? 药剂与工艺 ? β-细辛醚微乳的制备及其性质考察 许日鑫，石添香，廖 娴，林华燕，林微微，欧斯健，魏 刚* 广州中医药大学 新药开发研究中心，广东 广州 510006 摘 要：目的 制备 β-细辛醚微乳，并对其性质进行考察。方法 根据 β-细辛醚在各溶媒中的溶解度初步确定处方组成， 通过绘制伪三元相图对处方进行优化；采用 HPLC 法测定微乳中 β-细辛醚的质量分数；以外观、粒径及其分布、多分散指 数（PI）、pH 值、黏度和 β-细辛醚的质量分数为指标考察所制备微乳的初步稳定性。结果 优化的处方组合为 β-细辛醚-肉 豆蔻酸异丙酯-聚氧乙烯蓖麻油-丙三醇的质量比为 1∶2∶8∶2。制备的微乳澄清透明，有蓝色乳光，平均粒径为（18.2±0.2） nm，PI 为 0.222±0.005，pH 值为 6.50±0.01，10 000 r/min 离心 10 min 后和高温灭菌后均无分层现象，平均载药量为 （21.5±0.48）mg/mL。结论 所制备的微乳理化性质较稳定，符合鼻腔给药制剂的标准。 关键词：β-细辛醚；微乳；伪三元相图；鼻腔给药；理化性质 中图分类号：R283.6 文献标志码：A 文章编号：0253 - 2670(2013)01 - 0031 - 05 DOI: 10.7501/j.issn.0253-2670.2013.01.007 Preparation and quality investigation of β-asarone microemulsion XU Ri-xin, SHI Tian-xiang, LIAO Xian, LIN Hua-yan, LIN Wei-wei, OU Si-jian, WEI Gang Research Center of New Drug Development, Guangzhou University of Chinese Medicine, Guangzhou 510006, China Abstract: Objective To prepare β-asarone microemulsion (β-AME) and to investigate its physicochemical properties. Methods The formulation was investigated by solubility experiment and optimized by pseudoternary phase diagram; The content of β-asarone was determined by HPLC method. Physical appearance, particle size and its distribution, polydispersity index (PI), pH value, viscosity, and content of β-asarone were used as indexes to evaluate the stability of β-AME. Results The optimized formulation was as follows: The proportion of β-asarone-isopropyl myristate-Cremophor EL-glycerol was 1∶2∶8∶2. The emulsion was transparent liquid with blue opalescence; The average particle size of β-AME was (18.2