文献类型：期刊文献

英文题名：Development of a reservoir-type transdermal delivery system containing eucalyptus oil for tetramethylpyrazine

作者：Shen, Teng[1,2];Xu, Huinan[1,2];Weng, Weiyu[3];Zhang, Jianfeng[1,2]

机构：[1]Fudan Univ, Sch Pharm, Minist Educ, Dept Pharmaceut,Key Lab Smart Drug Delivery, Shanghai 201203, Peoples R China;[2]Fudan Univ, Sch Pharm, PLA, Shanghai 201203, Peoples R China;[3]E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

年份：2013

卷号：20

期号：1

起止页码：19

外文期刊名：DRUG DELIVERY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000313670400003)】；

基金：This work was supported by the National Natural Science Foundation of China (81072594). The authors report no declarations of interest.

语种：英文

外文关键词：Human skin; patch; penetration enhancer; permeation study; pharmacokinetic

摘要：The purpose of this study was to formulate a reservoir-type transdermal delivery system (TDS) for 2,3,5,6-tetramethylpyrazine (TMP) to enable the delivery of a sufficient dose through human skin to achieve an effective therapeutic plasma concentration. To improve the penetration of TMP in the reservoir-type TDS, several chemical penetration enhancers were investigated using in vitro rat dorsal skin permeation studies. Eucalyptus oil was found to enhance the permeation of TMP to the greatest extent, with the optimal concentration being 5% and the flux being 542.6 +/- 49.7 mu g/cm(2)/h, which was 4.5-fold greater than control with no enhancer (p<0.01). The flux of the optimized reservoir-type TDS permeated through the human epidermis was 346.0 +/- 27.7 mu g/cm(2)/h. Based on the in vitro human skin permeation flux and the pharmacokinetics parameters observed, the clinical surface area of the TDS patch was predicted to be 20 cm(2). The in vivo study conducted in rabbits showed that the TMP TDS patch containing 5% eucalyptus oil had a more favorable pharmacokinetic profile, with a lower C-max and prolonged T-max and mean residence time than that observed with the oral administration of TMP. The TMP reservoir-type TDS was shown to be a promising alternative route to oral administration or intravenous infusion of TMP.