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目的:筛选用于痤疮等局部皮肤疾病治疗的隐丹参酮凝胶处方。方法:以卡波姆934L为基质,制备含不同种类和浓度促渗剂的隐丹参酮凝胶。以离体大鼠腹部皮肤为模型,采用单室透皮扩散池,40%聚乙二醇-400的生理盐水作为接受液,考察不同处方隐丹参酮凝胶的稳态经皮渗透速率和皮肤内药物滞留量,以皮肤内滞留量/经皮渗透速率比为指标,筛选最佳处方。结果:不同浓度的薄荷醇(MEN)对隐丹参酮经皮渗透速率促进效果为5%>3%>1%,对皮肤内滞留量的促进效果为5%≈3%>1%;不同浓度的月桂氮酮(AZO)对隐丹参酮的促渗透效果为5%≈3%>1%,对皮肤内滞留量的促进效果为5%>3%≈1%;促渗剂混合使用与单独使用相比,在经皮渗透速率和皮肤内滞留量方面均未提高;5%AZO具有最大的皮肤内滞留量/经皮渗透速率比。结论:最佳处方为含5%AZO作为促渗剂的隐丹参酮凝胶处方。
Objective: To screen cryptotanshinone gel for the treatment of local skin diseases such as acne. METHODS: Cryptotanshinone gel with different kinds and concentrations of penetration enhancers was prepared with carbomer 934L as substrate. Using isolated rat peritoneal skin as a model, single compartment transdermal diffusion cells and 40% polyethylene glycol-400 saline were used as receiving fluids to investigate the steady-state transdermal permeation rate and intradermal Drug retention, skin retention / transdermal penetration rate as an index, screening the best prescription. Results: The effects of different concentrations of menthol (MEN) on the transdermal permeation rate of cryptotanshinone were 5%> 3%> 1% and 5% ≈3%> 1% The promoting effect of Azone (AZO) on Cryptotanshinone was 5% ≈3%> 1%, and the promoting effect on the retention of skin was 5%> 3% ≈1% No increase in transdermal permeation rate and intradermal retention; 5% AZO had the largest intradermal instillation / transdermal permeation rate ratio. Conclusion: The best prescription is cryptotanshinone gel with 5% AZO as penetration enhancer.