乌拉草总黄酮脂质体凝胶剂的制备工艺研究  

Preparation of liposome Gel of Carex meyeriana Total Flavonoid

作　　者：苏婷[1] 赵燕 毕野 高羚毓 贾瑞欣 包正 李鹤 邱智东[1] SU Ting;ZHAO Yan;BI Ye;GAO Lingyu;JIA Ruixin;BAO Zheng;LI He;QIU Zhidong(College of Pharmacy,Changchun University of Chinese Medicine,Changchun 130117,China;Lanzhou Heshengtang Pharmaceutical Co.,Ltd,Lanzhou 730000,China)

机构地区：[1]长春中医药大学药学院,吉林长春130117 [2]兰州和盛堂制药股份有限公司,甘肃兰州730000

出　　处：《药物评价研究》2021年第5期990-996,共7页Drug Evaluation Research

基　　金：吉林省科技厅项目(20200602034ZP);吉林省发展和改革委员会项目(2020C007)。

摘　　要：目的优化乌拉草总黄酮脂质体凝胶剂的制备工艺,并进行质量评价。方法乙醇注入法制备乌拉草总黄酮(CMTF)脂质体,以包封率为指标,正交试验优化处方;以脂质体凝胶剂的外观、涂展性、均匀度、黏稠度等综合评分为指标,采用Box-Behnken响应面法优化CMTF脂质体凝胶的处方及制备工艺。通过观察性状、pH值、铺展性及可洗除性,以及离心试验、耐寒及耐热试验,考察CMTF脂质体凝胶稳定性;观察其对大鼠正常及破损皮肤的刺激性。结果CMTF脂质体的最佳制备工艺为:大豆磷脂与胆固醇的质量比为5∶3,大豆磷脂与CMTF的质量比为4∶1,注入体积比例1∶10;平均包封率为89.41%,粒径为(119.7±3.82)nm,Zeta电位为(-20.80±0.40)mV。CMTF脂质体凝胶剂的最佳处方为:1 g CMTF脂质体、2 g卡波姆940、20 g甘油、2 g三乙醇胺、10 mL水,该脂质体凝胶剂的稳定性良好,无皮肤刺激性。结论优化后的CMTF脂质体凝胶制备工艺简单,质量稳定,为CMTF经皮制剂的开发提供依据。Objective To optimize the formulation of of Carex meyeriana Total Flavonoid Liposome Gel and evaluate its quality.Methods The total flavonoid of Carex meyeriana Kunth(CMTF)liposomas was prepared by ethanol injection method,the encapsulation rate of CMTF was used as an index to optimize the formulation by orthogonal test.Based on the formation of appearance,malleability,uniformity and viscosity as the index,the Box-Behnken response surface method was used to optimize the formulation and preparation process of the CMTF liposome gel.The stability of CMTF liposome gel was investigated by observing its properties,pH value,spreading property,washable property,and centrifugal test,cold resistance test and heat resistance test.The irritation to normal and damaged skin of rats was observed.Results The optimum technological conditions of CMTF liposome gel was:soybean lecithin to cholesterol ratio of 5:3,soybean lecithin to CMTF ratio of 4:1,the injection volume ratio of 1:10;average encapsulation efficiency of 89.41%,the particle size was(119.7±3.82)nm and the Zeta was(-20.80±0.40)mV.The best formulation of CMTF liposome gel was:1 g of CMTF liposome freeze-dried powder,2 g of carbomer 940,20 g of glycerol,2 g of triethanolamine,10 mL of water.The liposome gel has good stability and no skin irritation.Conclusion The optimized liposome gel was simple in preparation and stable in quality,which provided a basis for the development of transdermal preparations of CMTF.

关 键 词：乌拉草总黄酮 脂质体 凝胶 Box-Behnken响应面法 稳定性 刺激性 

分 类 号：R943[医药卫生—药剂学]