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考察了3种促透剂(油酸、1,2-丙二醇和月桂氮?酮)在浓度为3%和5%时对罗格列酮透过小鼠离体皮肤的影响。结果显示,5%月桂氮?酮对罗格列酮的促透效果最佳。以贴剂黏性和透皮速率(J_s)为主要指标,通过正交设计优化了罗格列酮透皮贴剂的处方基质。结果所得优化处方中压敏胶(聚丙烯酸酯Eudragit E100)∶增塑剂(琥珀酸)∶交联剂(癸二酸二丁酯)的质量比为8∶3∶1,增黏剂聚乙二醇400含量为20%。3批优化贴剂的黏性和经皮渗透性均无显著性差异,J_s分别为26.38、25.73和25.23mg·cm~(-2)·h~(-1)。
The effects of rosiglitazone on skin exudation of mice were examined at 3% and 5% of three flux enhancers (oleic acid, 1,2-propanediol and lauropenthrone). The results showed that 5% laurocapram was the best propolis to rosiglitazone. Taking adhesive and transdermal rate (J_s) as the main indexes, the prescription matrix of rosiglitazone transdermal patch was optimized by orthogonal design. Results Optimized prescription pressure sensitive adhesive (polyacrylate Eudragit E100): plasticizer (succinic acid): cross-linking agent (dibutyl sebacate) mass ratio of 8: 3: 1, tackifier Polyethylene Diol 400 content of 20%. There was no significant difference in the adhesiveness and transdermal permeability between the three batches of optimized patches, with J_s of 26.38, 25.73 and 25.23 mg · cm -2 · h -1, respectively.