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出 处:《中国药物应用与监测》2016年第1期17-20,共4页Chinese Journal of Drug Application and Monitoring
基 金:军队十二五面上项目(CWS11J114)
摘 要:目的:探讨卢立康唑醇质体的透皮性,为其新制剂开发提供理论参考。方法:通过检测卢立康唑醇质体、脂质体、软膏、45%水醇溶液经大鼠皮肤的48 h药物渗透累积量、药物滞留量及透皮速率,比较不同制剂的透皮性差异。结果:卢立康唑24 h单位面积累积透皮量醇质体优于其他剂型(P<0.05),卢立康唑48 h单位面积累积透皮量:醇质体/软膏>脂质体/45%水醇溶液(P>0.05)。透皮速率大小顺序为:醇质体>软膏>45%水醇溶液>脂质体(P<0.05)。卢立康唑药物滞留量顺序为:醇质体/软膏>脂质体>45%水醇溶液(P<0.05),但醇质体与软膏在全层皮肤中滞留量差异无统计学意义(P>0.05)。结论:卢立康唑醇质体透皮性优于脂质体、软膏、45%水醇溶液,有良好的体外透皮性,可作为药物载体。Objective: To investigate the transdermal difference of luliconazole ethosomes, and provide references for the development of new dosages. Methods: 48 h cumulative transdermal amount, retention of the drug and permeation rate were analyzed about luliconazole ethosomes, lipidosome, ointment and 45% hydroalcoholic solution. Results: The cumulative transdermal amount of luliconazole ethosomes at 24 h was superior to others (P 〈 0.05). The transdermal amount of luliconazole at 48 h were as follows: ethosomes/ointment 〉 lipidosome/45% hydroalcoholic solution (P 〉 0.05). The permeation rate of luliconazole were as follows: ethosomes 〉 ointment 〉 45% hydroalcoholic solution 〉 lipidosome (P 〈 0.05). The retention of luliconazole were as follows: ethosomes/ointment 〉 lipidosome 〉 45% hydroalcoholic solution (P 〈 0.05), while the retention in full-thickness skin showed no significant difference between luliconazole ethosomes and ointment (P 〉 0.05). Conclusion: The transdermal ability of luliconazole ethosomes is better than lipidosome, ointment and hydroalcoholic solution, which could be used as drug carrier.
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