醋氯芬酸醇质体的制备及体外经皮渗透考察  

Preparation of aceclofenac ethosomes in vitro and their transdermal penetration

作　　者：赖超[1] 黄华[1] 张涛[2,3] 沈丹丹[1] 

机构地区：[1]重庆医科大学药学院,重庆400016 [2]重庆医药工业研究院有限责公司,重庆400061 [3]重庆市化学制药工程技术研究中心,重庆400061

出　　处：《中国医院药学杂志》2012年第6期427-431,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:制备醋氯芬酸(ACF)醇质体并考察其对离体大鼠的透皮能力。方法:采用乙醇注入均质法制备醋氯芬酸醇质体,利用正交试验优化处方;对其粒径、包封率、形态及大鼠离体皮肤经皮渗透量进行考察。结果:优选处方为乙醇用量45%,大豆磷脂用量3%,醋氯芬酸用量0.35%。制备的醇质体平均粒径为102 nm,包封率为48%。醋氯芬酸醇质体的24 h经皮渗透量为821.8μg.cm-2是其45%乙醇溶液的6.36倍。结论:醇质体能显著提高醋氯芬酸经皮渗透量,是经皮给药的优良载体。OBJECTIVE To prepare aeeclofenac ethosomes and evaluate their transdermal penetration in vitro. METHODS The ethosomes were prepared by ethanol infusion and homogenization method. The optimal formation and preparation were selected by an orthogonal design test. The size, entrapment efficacy, the shape of ethosomes and in vitro transdermal flux was investigated. RESULTS The appropriate formulation consisted of 45% ethanol, 3% phospholipids, 0. 35% aceclofenac. The average particle size of acecolfenac ethosomes was 102 nm, the encapsulation efficiency of the ethosomes was 48%. The cumulative penetration during 24 h of ethosomes was 821.8 ug. cm-2, which was 6. 36 times higher than that form 45% ethanol solution. CONCLUSION Ethosomes was effective for transdermal penetration, it could be an ideal carrier in aceclofenac transdermal delivery.

关 键 词：醋氯芬酸 醇质体 包封率 经皮渗透量 

分 类 号：R943[医药卫生—药剂学]