绿原酸溶液、微乳和凝胶的透皮特性与皮肤刺激性研究  

Study on in vitro transdermal permeability and skin irritation of chlorogenic acid in solution,microemulsion and carbomer hydrogel

作　　者：陈莉[1] 侯成贤 杨燕飞[1] 

机构地区：[1]遵义医学院药学院药剂学教研室,贵州遵义563099

出　　处：《遵义医学院学报》2017年第2期119-123,共5页Journal of Zunyi Medical University

基　　金：贵州省联合基金资助项目(NO:黔科合J字LKZ[2013]26)

摘　　要：目的对绿原酸溶液、微乳和凝胶的体外透皮特性和皮肤刺激性进行对比研究,为绿原酸外用制剂的开发提供实验依据。方法以雄性大鼠背部皮肤为渗透屏障,采用Franz扩散池比较不同制剂中绿原酸的透皮特性,并采用大鼠自身对照考察绿原酸不同制剂对大鼠皮肤的刺激性。结果绿原酸3种制剂的累积渗透量Qn与时间t有较好线性关系。微乳及凝胶组24 h的累积渗透量Q_(24h)分别为溶液组的7.71倍和7.49倍,其透皮速率常数J分别为7.98倍和7.50倍,且累积透过百分率分别为2.63倍和2.16倍。绿原酸凝胶组的体外透皮释放过程符合Higuchi模型。绿原酸制剂对大鼠皮肤均无刺激性。结论绿原酸微乳及凝胶能够促进绿原酸经皮渗透,有望开发成为新的绿原酸外用制剂。Objective To investigate the differences in transdermal permeability and skin irritation of chlorogenic acid in three different formulations based on solution, microemulsion and carbomer hydrogel.Methods Franz diffusion cells were used for the transdermal permeation study using male rats dorsal skin.Irritation effects on rats intact or damaged skin were studied by self control.Results The accumulative amount of the permeated chlorogenic acid （Qn） increased linearly with time （t）.Within 24 hours, the Q24h of chlorogenic acid in microemulsion and gel groups were 7.71 times and 7.49 times than that in solution group, respectively.The permeation rate （J） was 7.98 times and 7.50 times, meanwhile the accumulative permeation percent ratio was 2.63 times and 2.16 times.The in vitro transdermal delivery ability of chlorogenic acid in gel group conformed to Higuchi equation.The skin irritation test indicated that chlorogenic acid formulations did not cause irritation on the intact or damaged skin.Conclusion Chlorogenic acid formulations have no stimulation to rat skin.Compared with the solution group, microemulsion and gel groups can promote transdermal permeability, suggesting that microemulsion and gel may be promising new transdermal formulations of chlorogenic acid.

关 键 词：绿原酸 微乳 凝胶 体外经皮渗透 皮肤刺激性 

分 类 号：R943[医药卫生—药剂学]