【摘要】 采用改良Franz扩散池,以离体大鼠皮肤为透皮屏障,考察促进剂氮酮、桉叶油、冰片等以及助溶促渗剂二甲基亚砜、丙二醇、异丙醇对伊维菌素体外透皮吸收促进效果,并正交筛选促进剂及助溶剂的最佳组合,探讨伊维菌素体外经皮渗透的影响。结果表明:单独使用二甲基亚砜、冰片、桉叶油促渗效果较好,增渗倍数分为4.99、4.60、4.00;复合促进剂以桉叶油4%+氮酮1.5%+冰片3.5%组合促透性最好,增渗倍数达到24.62倍;在最佳复合促进剂基础上,丙二醇15%+二甲基亚砜35%+异丙醇15%组合助溶促渗效果最佳,增渗倍数达29.48倍;重复5次,增渗倍数达(28.01±4.02)%。证明以桉叶油4%+氮酮1.5%+冰片3.5%+丙二醇15%+二甲基亚砜35%+异丙醇15%组合制备的1%伊维菌素透皮剂,体外透皮性能最好。更多还原

【Abstract】 The permeation experiments were conducted through excised rats skin by modified Franz diffusion cell to study the enhancing effect of penetration enhancers such as azone,eucalyptus oil,borneol and solution adjuvants and also their optimized combination through orthogonal experiments Results showed that when the penetration enhancers were applied alone,dimethyl sulfoxide,borneol and eucalyptus oil achieved better penetration rate,with the rates of 4.99,4.60,4.00respectively.Eucalyptus oil 4%+azone 1.5%+borneol 3.5% showed the best enhancement effect of all the combined transdermal enhancers and the enhancing rate was 24.62;propylene glycol 15%+dimethyl sulfoxide 35%+ isopropyl alcohol 15% behaved the best enhancement effect of all the solution adjuvants and the enhancing rate was 29.48 based on the best enhancer combination.As the Optimal group of combined transdermal enhancers with solution adjuvants was repeated 5batches,the average enhancing rate was(27.39+2.29)%.Conclusion:eucalyptus oil 4% +azone 1.5%+borneol 3.5% +propylene glycol 15% +dimethyl sulfoxide 35% +isopropyl alcohol 15% was the optimum promoting group in vitro transdermal permeation of 1%Ivermectin.更多还原