桉油对丙酸氯倍他索乳膏经皮渗透和吸收的作用

Effect of eucalyptus oil on the percutaneous penetration and absorption of clobetasol propionate cream

目的 :考察促进剂桉油对丙酸氯倍他索 (CBT)乳膏经皮渗透的促进作用 ,通过比较透过量和皮层中量 ,分析在该制剂中是否适合使用桉油。方法 :采用直立式扩散池 ,考察了桉油在 0 .5 % ,1.0 % ,2 .0 % ,5 .0 %浓度下 0 .0 5 %CBT乳膏经皮渗透2 ,4 ,6,8,10 ,2 4h后单位面积累积透过量Q( μg·cm-2 )和稳态透皮流量J( μg·cm-2 ·h-1) ;HPLC法测定经皮渗透 2 4h后每克皮肤组织中CBT的量D( μg·g-1)。结果 :4种浓度的桉油均显著促进CBT乳膏透皮吸收 (P <0 .0 1) ,其J值约是对照组的 3～ 5倍 (P <0 .0 1) ;随浓度增加 ,皮层量D并不随之相应增加。结论 :桉油可加快CBT经皮渗透速度 ;也能增加皮层中CBT量 ,但有饱和性。建议CBT乳膏以少加 ( <0 .5 % )或不加桉油为好。

OBJECTIVE:To evaluate the effect of eucalyptus oil on percutaneous penetration and absorption of clobetasol propionate (CBT) cream.METHODS:With vertical permusion cell,in vitro penetration of CBT through excised mouse abdominal skin in the present of eucalyptus oil at its four concentrations was conducted with 0.05% CBT cream.The cumulative amount (Q,μg·cm -2 ) of this study at 2,4,6,8,10,24 h was got and the steady-state flux (J,μg·cm -2 ·h -1 ) was determined.The quantities of CBT (D,μg·g -1 ) within the whole strata of skin after 24 hours in vitro treatment were investigated.RESULTS:Eucalyptus oil as an enhancer could highly increase,Q and J of CBT within skin,but D was not proportional to the concentrations of eucalyptus oil.CONCLUSIONS:On the basis of data presented herein,we can suggest that it's better for CBT cream,eucalyptus oil not use/or less use (0.5%),because eucalyptus oil would increase CBT percutaneous absorption which might lead to unwanted systemic effects.