D-最优混料设计制备川芎油微囊止痛凝胶膏剂及其药效学初步考察  

Pharmaceutical research of Ligusticum chuanxiong oil microcapsule analgesic gel patch by D-optimal mixture design

作　　者：周欣 康希 唐丽婧 曲彤 郝慧汇 穆成林 卢焘韬 王雪莲 杨荣平[1] ZHOU Xin;KANG Xi;TANG Li-jing;QU Tong;HAO Hui-hui;MU Cheng-lin;LU Tao-tao;WANGXue-lian;YANG Rong-ping(College of Pharmacy,Southwest University,Chongqing 400715,China;College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 610075,China;College of Pharmacy,Shanxi University of Chinese Medicine,Xianyang 712083,China)

机构地区：[1]西南大学药学院,重庆400715 [2]成都中医药大学药学院,四川成都610075 [3]陕西中医药大学药学院,陕西咸阳712083

出　　处：《中草药》2019年第22期5455-5461,共7页Chinese Traditional and Herbal Drugs

基　　金：重庆市科技局技术创新与应用示范(cstc2018jscx-msybX0179)

摘　　要：目的通过将川芎挥发油制成微囊中间体应用到凝胶膏剂,以解决川芎油不稳定特性,并优化处方及评价体外透皮速率,对药效学进行初步研究。方法采用D-最优混料设计,以初黏力、持黏力、剥离强度作为评价指标,优选出最佳制备工艺。通过Franz体外透皮试验仪,以藁本内酯为指标,研究凝胶膏剂的体外透皮行为。通过醋酸扭体实验初步评价药效。结果川芎油微囊止痛凝胶膏剂的最优处方为NP700、甘油、甘羟铝、高岭土、氮酮、酒石酸、PVPK30、0.5%卡波姆940分别为1.250、5.000、0.025、0.250、0.600、0.025、1.000、2.700 g。凝胶膏剂中藁本内酯透皮速率为5.1297μg/(cm2·h),高温、高湿、强光照射实验于第5、10天保留率分别为93.17%、91.21%,98.94%、92.36%,68.03%、60.78%;镇痛率为63.14%。结论最优处方凝胶膏剂具有良好的黏性,解决了川芎油不稳定的特性,为挥发油类应用到凝胶膏剂等新剂型提供参考。Objective The volatile oil of Ligusticum chuanxiong was made into microcapsule as intermediate and applied to gel paste to solve the instability characteristics of L.chuanxiong oil(LCO).The formulation and in vitro transdermal rate were optimized and the pharmacodynamics was preliminary studied.Methods D-optimal mixture design was adopted,and initial adhesion,adhesion holding and peeling strength were used as evaluation indexes to optimize the preparation process.The in vitro transdermal behavior of ligustilide was studied by Franz in vitro transdermal test instrument.The efficacy was evaluated by acetic acid writhing experiment.Results The optimal prescription of LCO microcapsule analgesic gel patch was as follow:NP700,glycerin,hydroxyaluminum,kaolin,azone,tartaric acid,microcapsule PVPK30,0.5%capom 940 was 1.250,5.000,0.025,0.250,0.600,0.025,1.000,and 2.700 g,respectively.Ligustilide transdermal rate in the gel patch was 5.1297μg/(cm2·h).The retention rate of high temperature,high humidity and strong light irradiation on the 5th and 10th day was 93.17%,91.21%,98.94%,92.36%,68.03%,and 60.78%,respectively,and the analgesic rate was 63.14%.Conclusion The optimal prescription of the gel patch had good viscosity,which solved the problem that ligustilide was difficult to be applied to the gel patches due to the instability of LCO and provided a reference for the application of volatile oil to new dosage forms such as gel patch.

关 键 词：川芎油 微囊 止痛 凝胶膏剂 D-最优混料设计 体外透皮 稳定性 醋酸扭体实验 药效学 初黏力 持黏力 剥离强度 藁本内酯 透皮速率 保留率 黏性 

分 类 号：R283.6[医药卫生—中药学]