摘要
目的:研究复方雷公藤微乳凝胶体外释放度及其体外透皮特性,为复方雷公藤处方开发成经皮给药制剂的微乳凝胶提供实验依据.方法:采用改良Franz扩散池方法,分别以半透膜和小鼠离体腹部皮肤为屏障,利用高效液相色谱法测定接收液中雷公藤甲素的含量,释放度试验以12 h的累积释放量对时间以零级方程、一级方程和Higuich方程进行回归,求得最佳拟合方程并计算累积释放率;透皮试验以24 h的累积透皮量对时间进行回归,计算透皮速率方程,并通过透皮速率比较复方雷公藤微乳凝胶、复方雷公藤凝胶和复方雷公藤巴布剂的体外透皮特性.结果:复方雷公藤微乳凝胶12 h内的释药特性符合零级释药方程:Q=1.25 t+2.67,释放速率为1.25μg/(cm^2·h),累积释放率达91%;复方雷公藤微乳凝胶24 h的体外透皮速率为0.419μg/(cm^2·h),大于复方雷公藤凝胶[0.205μg/(cm^2·h)]和复方雷公藤巴布剂[0.253μg/(cm^2·h)]的透皮速率.结论:复方雷公藤微乳凝胶释放速率远大于透皮速率,其透皮速率不受释放速率的影响,具有良好的透皮特性,适合开发成经皮给药制剂.
Objective: To study the releasing and in vitro transdermal permeation of Fufang Leigongteng micro. emulsion gel and to provide experimental evidence for preparation of transdermal delivery system. Methods: The modi. fied Franz diffusion pool method was used. Semipermeable membrane and the excised mouse abdominal skin were used as barrier respectively in release and permeation experiment in vitro. The concentration of triptolide that was used as an index ingredient in receiving pool was determined by high performance liquid chromatography(HPLC)method. For re. lease experiment,the cumulative release amount of triptolide to time was regressed in zero-order equation,first-order equation and Higuich equation and the optimal fitting equation was chosen according to regression coefficient r. In ad. dition the accumulative released rate was calculated. For the permeation study in vitro,the accumulative amount of trip. tolide in 24 h to time was regressed and the trasndermal properties of Fufang Leigongteng microemulsion gel,Fufang Leigongteng gel and Fufang Leigongteng gel paste was compared by permeation rate. Results: The release characteris. tic of triptolide in Fufang Leigongteng microemulsion gel comply to zero-order equation Q=1.25t+2.67. The release rate and accumulative release rate were 1.25 μg(/ cm^2 · h)and 91% respectively. The permeation rate of Fufang Leigongteng microemulsion gel was 0.419 μg(/ cm^2·h)for 24 hours,it is higher than that of Fufang Leigongteng gel [0.205 μg(/ cm^2·h)] and that of Fufang Leigongteng gel paste [0.253 μg(/ cm^2·h)]. Conclusion: The release rate of Fu. fang Leigongteng microemulsion gel was far greater than the transdermal rate,So the transdermal rate is not affected by the release rate. Fufang Leigongteng microemulsion gel has good transdermal characteristics which is suitable for devel. oping into a transdermal drug delivery preparation.
作者
王晓娟
李娟
李周
Wang Xiaojuan;Li Juan;Li Zhou(Luoyang second hospital of Traditional Chinese Medicine,Luoyang 471003;Guangzhou University of Chinese Medicine,Guangzhou,Guangdong,510006)
出处
《广西中医药》
2019年第4期60-64,共5页
Guangxi Journal of Traditional Chinese Medicine
基金
广东省教育部产学研结合项目（编号：2012B091100486）
