白芷香豆素储库型贴剂的研制及其体外评价  

Development and in vitro evaluation of reservoir-type patch of coumarins in Angelicae Dahuricae Radix

作　　者：刘晓昱[1] 赖瑛[1] 

机构地区：[1]杭州市中医院临床药学室,浙江杭州310007

出　　处：《中草药》2018年第2期313-317,共5页Chinese Traditional and Herbal Drugs

基　　金：浙江省杭州市卫生科技计划项目(2013A47)

摘　　要：目的制备白芷香豆素储库型贴剂,考察其体外释药特性和离体皮肤渗透性,筛选有效的透皮吸收促进剂,提高白芷香豆素的透皮吸收速率。方法选取羟丙甲纤维素为储库介质,以乙烯-醋酸乙烯共聚物膜为控释膜,制备白芷香豆素储库型透皮贴剂。用Franz扩散池进行乳猪离体皮肤渗透实验,用HPLC测定欧前胡素量,考察凝胶用量、药物用量、促渗剂对药物透皮速率的影响,并对优选的贴剂进行体外释放研究。结果最佳处方为1%羟丙基甲基纤维素(HPMC)、1%白芷香豆素、3%肉豆蔻酸异丙酯、3%氮酮;由该处方制得的贴剂稳态透皮速率(Js)达到0.713μg/(cm2·h),体外释放速率接近零级。结论储库型白芷香豆素贴剂有较高的经皮渗透速率,体外释药完全,有望成为新型的透皮制剂。Objective To prepare the reservoir patch of coumarins in Angelicae Dahuricae Radix and investigate its release and transdermal absorption characteristics in vitro. The efficient enhancers were chosen to improve the drug＇s permeation rate. Methods The reservoir patch was prepared using hydroxypropyl methylcellulose （HPMC） as medium and ethylene vinyl acetate （EVA） membrane to control the release of drug. The Franz diffusion cells were used and HPLC was used to determine imperatorin content and permeation rate. The content ofimperatorin was determined by HPMC. The effect of the gel consumption, the content ofcoumarins and penetration enhancer on the transdermal flux were investigated by selecting porcine skin as model. The release of the selected patch in vitro was investigated. Results 1% HPMC, 1% coumarins in Angelicae Dahuricae Radix, 1% Isopropyl Myristate （IPM） and 3% Azone were the best permeation of the patch. The permeation rate reached 0.713 μg/（cm^2·h）. The release mechanisms of the patch in vitro coincided with zero-order kinetic. Conclusion The reservoir patch of coumarins in Angelicae Dahuricae Radix had high transdermal rate and complete in vitro release. It was indicated that the patch could be expected to be an effective transdermal drug delivery system.

关 键 词：白芷香豆素 经皮渗透 促渗剂 储库型 贴剂 释药特性 透皮吸收 欧前胡素 

分 类 号：R283.1[医药卫生—中药学]