氮酮对丙酸氯倍他索乳膏经皮渗透和吸收的影响  

Effect of azone in vitro on percutaneous penetration and absorption of clobetasol propionate cream

作　　者：李中东[1] 王宏图[1] 施孝金[1] 陈妙英[1] 印绮平 

机构地区：[1]上海医科大学华山医院临床药学研究室,上海200040

出　　处：《中国临床药学杂志》2000年第1期40-43,共4页Chinese Journal of Clinical Pharmacy

摘　　要：目的 :考察氮酮对丙酸氯倍他索乳膏经皮渗透的作用 ,通过比较累积透过量和皮层中量 ,分析在该制剂中使用氮酮的利弊。方法 :采用直立式扩散池 ,考察氮酮在 0 .5 %、1.0 %、2 .0 %和 5 .0 %浓度下 0 .0 5 %丙酸氯倍他索乳膏经皮渗透 2、4、6、8、10、2 4h后累积透过量 Q(μg/ cm2 )和稳态流量 J(μg· cm- 2 · h- 1 ) ;分别测定了经皮渗透 2 4h后每克皮肤组织中氯倍他索的量 D(μg/ g)。结果 :4个浓度氮酮均极显著促进 CBT乳膏经皮渗透 (P<0 .0 1) ,Q2 4分别是 4.817、7.32 7、4.34 1、4.783,对照组的 Q2 4为 2 .391μg/ g;J值分别是对照组的 1.90 1、2 .892、1.72 9、1.92 1倍。其中在 1.0 %时 ,J值 (0 .2 979)最大 (P<0 .0 1) ;0 .5 %、1.0 %、2 .0 %、5 .0 %氮酮浓度时 ,其 2 4h时皮层量平均为 42 .92、35 .40、2 0 .5 1、2 2 .0 9μg/ g,而对照组为 (37.71±7.92 6 ) μg/ g,随氮酮浓度增加 ,皮层量 D并不随之相应增加 (P<0 .0 1)。结论 :氮酮可加快氯倍他索经皮渗透的速度 ,Q值和 J值增大 ,但并不能使皮层中氯倍他索量明显增加。为谨慎起见 ,氯倍他索乳膏以不加氮酮为好。AIM:To evaluate the effect of azone on the percutaneous penetration and absorption of clobetasol propionate (CBT) cream.METHODS: With vertical perfusion cell, in vitro penetration of CBT through excised mouse abdominal skin in the presence of 0 5%, 1 0%, 2 0%, 5 0%. Azone was conduc ted with CBT cream. The cumulative amount ( Q , μg/cm 2) at 2, 4, 6, 8, 10, 24 h was caculated from the CBT concentrations in receptor fluid and the steady state flux ( J , μg·cm -2 ·h -1 ) was determined from slope of the linear portion of Q versus time plot. The analysis of variance and Student Newman Keuls test were used for analysis of Q at each hours points. Differences were considered significant at P <0 01. The quantities of CBT within the whole strata of skin after 24 h in vitro treatment was investigated. RESULTS: Azone as enhancer can not highly obviously increase the quantities of CBT within skin, but increase the cumulative amount and steady state flux of CBT. CONCLUTION: On the basis of data presen ted herein, we can suggest that it's better for CBT cream, not to use penetration enhancers as azone, because azone would increase corticosteroids percutaneous absorption which might lead to unwanted systemic effects.

关 键 词：丙酸氯倍他索 乳膏 氮酮 透皮促进剂 

分 类 号：R944[医药卫生—药剂学]