摘要
目的:研究不同透皮促进剂对环孢素A纳米粒丝素蛋白膜剂(简称环孢素A膜剂)经皮渗透的影响,并优选出其最佳透皮促进剂。方法:以不同浓度的氮酮、油酸、月桂醇、丙二醇、尿素单用及氮酮与其他辅料联用作为透皮促进剂,制备环孢素A膜剂;采用药物透皮扩散试验仪,以离体大鼠腹部皮肤为渗透屏障,40%乙醇-生理盐水为接收介质,高效液相色谱法为接收介质中药物含量的测定方法,比较不同透皮促进剂作用下环孢素A累积透皮量(Q)、稳态透皮速率(Js)、增渗倍数(ER)等。结果:氮酮、月桂醇、丙二醇、尿素对环孢素A膜剂均有透皮促进作用,其中以1%氮酮+2%丙二醇的透皮促进效果最好,令24h内Q提高至2.81倍、Js为6.59μg·cm-2·h-1、ER为2.59。结论:1%氮酮+2%丙二醇更适合作为环孢素A膜剂的透皮促进剂。
OBJECTIVE： To study the effects of different penetration enhancers on transdermal penetration of silk fibroin membrane of cyclosporine A nanoparticles （CyA-NP） in vitro, and to select optimal penetration enhancers. METHODS： The membrane of CyA-NP was prepared with different concentrations of ozone, oleic acid, lauryl alcohol, propylene glycol, urea alone and combi- nation of ozone with other excipients as penetration enhancers. Using modified Franz diffusion cell, isolated rat abdominal skin as transdermal barrier in vitro, 40% ethanol-normal saline as reception fluid, the concentration of CyA in reception fluid was deter- mined by HPLC. The cumulative permeation quantity （Q）, steady-state penetrating rate （Js） and enchancement ratio （ER） of CyA were compared in different penetration enhancers. RESULTS：Azone, lauryl alcohol, propylene glycol, urea enhanced the transdermal penetration of the membrane of CyA-NP. The highest permeation rate was obtained in mixture of 1% azone and 2% propylene glycol. The cumulative permeation quantity in 24 h was 2.81 times compared with the membrane without penetration enhancer. The steady-state penetrating rate （Js） was about 6.59 μg·cm^-2·h^-1 and enchancement ratio （ER） was 2.59. CONCLUSION： Combination of 1% azone with 2 % propylene glycol is suitable penetration enhancer for the silk fibroin membrane of CyA-NP.
出处
《中国药房》
CAS
CSCD
北大核心
2011年第9期801-803,共3页
China Pharmacy
基金
科技型中小企业技术创新基金资助项目(07C26223201333)
江苏省"六大人才高峰"资助项目(094110)
2009年国家大学生创新性实验计划资助项目(57315924)
关键词
环孢素A
体外透皮
膜剂
透皮促进剂
单用
联用
Cyclosporine A
Transdermal penetration
Membrane
Penetration enhancer
Alone
Combination
