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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。
OBJECTIVE: To investigate the effect of Azone on the transdermal permeation of clobetasol propionate cream, and to compare the pros and cons of Azone in this formulation by comparing the cumulative permeation and the amount of cortisol. Methods: The upright diffusion cell was used to investigate the effects of Azone on the permeation of 0.5, 5%, 1.0%, 2.0% and 5.0% concentrations of clobetasol propionate cream , The cumulative permeation Q (μg / cm2) and the steady state flow J (μg · cm-2 · h-1) after 6, 8, 10 and 24 h; the percutaneous permeation Clobetasol dose D (μg / g). Results: The average concentrations of azone at 4 concentrations significantly promoted the transdermal permeation of CBT cream (P <0.01), the values of Q2 4 were 4.817, 7.32 7, 4.344 and 1.4783, respectively. The control group’s Q2 4 was 2.391 μg / g; J values were 1.90 1,2 .892,1.72 9,1.92 1 times the control group. When 1.0%, the value of J (0.2979) was the highest (P <0.01); when the concentration was 0.5%, 1.0%, 2.0%, 5.0% The average amount of cortical layer was 42.92, 35.040, 20.51, 22.09μg / g, while the control group was (37.71 ± 7.92 6) μg / g. Do not increase accordingly (P <0.01). Conclusion: Azone accelerates transdermal permeation of clobetasol, and the Q and J values increase, but it does not increase the amount of clobetasol in the cortex. For the sake of caution, clobetasol creams are better with no azone.