透皮促渗剂对醋酸地塞米松壳聚糖凝胶透皮特性的影响

Effects of Transdermal Penetration Enhancers on the Permeation Properties of Dexamethasone Acetate Chitosan Gel

目的观察透皮促渗剂对醋酸地塞米松壳聚糖凝胶透皮特性的影响。方法实验分为无促渗剂组和促渗剂组。无促渗剂组为0.75%药物5%壳聚糖凝胶剂;促渗剂组根据含促渗剂不同又分为月桂氮酮+丙二醇、月桂氮酮、丙二醇+二甲亚砜、二甲亚砜+月桂氮酮组。以无毛大鼠皮肤为渗透屏障,进行体外渗透实验,分析该凝胶稳态透皮速率(Js)和Js提高率。结果无促渗剂组①Js为(3.75±0.56)μg.(cm2)-1.h-1。促渗剂组效果明显,其中二甲亚砜+月桂氮酮组②Js为(8.12±0.58)μg.(cm2)-1.h-1,月桂氮酮+丙二醇组③Js为(5.41±0.74)μg.(cm2)-1.h-1,丙二醇+二甲亚砜组④Js为(4.31±0.42)μg.(cm2)-1.-h1,月桂氮酮组⑤Js为(4.35±0.36)μg.(cm2)-1.h-1。与①比较,②的Js提高率为2.17%(P<0.01),与③④⑤比较,②的Js分别为1.51,1.89,1.87倍(P<0.05或P<0.01)。结论混合促渗剂具有比单一促渗剂更好的促渗效果。

Objective To study effects of penetration enhancers on the transdermal permeation of dexamethasone acetate chitosan gel. Methods The permeation enhancer-free group and enhancer added group were set up.There were 0.75% dexamethasone acetate and 5% chitosan gel in the permeation enhancer-free group.The permeation enhancer group was composed of 0.75% dexamethasone acetate and 5% chitosan gel,which subdivided into azone plus propylene glycol,azone,propylene glycol plus dimethyl sulfoxide,and dimethyl sulfoxide plus azone groups.Skin samples as permeability barriers were obtained from hairless rats for in vitro tests of the drug permeability.The permeation parameters,named as steady srate flux（Js）and Js enhancement ratio were evaluated. Results Js in the permeation enhancer-free group①was（3.75±0.56） μg·（cm2）-1·h-1,and that in the permeation enhancer group were（8.12±0.58） μg·（cm2）·h-1（dimethyl sulfoxide plus azone group②）（5.41±0.74） μg·（cm2）-1·h-1（Azone plus propylene glycol group③）,（4.31±0.42） μg·（cm2）-1·h-1（propylene glycol plus dimethyl sulfoxide group④）,（4.35±0.36） μg·（cm2）-1·h-1（azone group⑤,）respectively.Compared with ①,the Js enhancement ratio of ② was 2.17%（P0.01）,and the Js enhancement ratio were 1.51,1.89,1.87（P0.05 or P0.01）,respectively,compared with③,④,⑤,which all showed significant differences. Conclusion The mixed permeation enhancer has better permeation properties than the single enhancer.