青藤碱微乳凝胶的制备及体外透皮特性研究  

Preparation and In-vitro Transdermal Properties of Sinomenine Microemulsion-based Gel

作　　者：王利胜[1] 张升[1] 刘丽萍[1] 赖宝林[1] 夏祖猛[1] 吴阳[1] 程龙[1] 田瑶[1] 

机构地区：[1]广州中医药大学药剂学教研室,广州510006

出　　处：《中药新药与临床药理》2011年第1期21-24,共4页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：国家自然基金资助(30873443);广州中医药大学本科创新基金资助(201038)

摘　　要：目的制备青藤碱微乳凝胶,并对其进行质量评价和体外透皮扩散特性进行考察。方法以卡波姆940为基质,采用直接溶胀法制备青藤碱微乳凝胶。采用Zetasizer1000-HAS激光粒度测定仪测定微乳凝胶的粒度分布。采用NDJ-7旋转黏度计和pH计分别测定微乳凝胶的黏度和pH。采用改良的Franz扩散池,比较青藤碱微乳、微乳凝胶及亲水凝胶中青藤碱的透皮特性。结果青藤碱微乳凝胶外观为透明金黄色溶液,粒度分布在4～15nm范围内,pH 6.5左右,黏度为2.0 pa.s,稳定性良好。青藤碱对照水溶液、微乳、微乳凝胶、亲水凝胶的稳态渗透速率分别为3.328,42.861,17.244,12.185μg.cm-2.h-1,12 h的累积渗透量分别为41.104±1.219,505.198±176.964,211.373±24.856,145.391±24.392μg.cm-2。结论青藤碱微乳、微乳凝胶的12 h累积渗透量和渗透速率均优于青藤碱对照水溶液和亲水凝胶,可为青藤碱经皮给药剂型选择提供参考。Objective To prepare the microemulsion-based gel of sinomenine, and to study its quality evaluation and transdermal diffusion characteristics in vitro. Methods With Carbopol 940 as a substrate, we prepared mieroemulsion-based gel of sinomenine by direct swelling method. The particle size distribution of microemulsionbased gel was detected with Zetasizer1000-HAS particle size laser analyzer. The viscosity of microemulsion- based gel was measured with NDJ-7 rotating viscometer, and the pH value was detected with pH meter. We compared the transdermal characteristics of sinomenine in mieroemulsion, microemulsion-based gel and hydrophilic gel by modified Franz diffusion cell. Results With good stability, the appearance of microcmulsionbased gel of sinomenine was transparent yellow solution. The distribution of its particle size was 4-15 nm, pH was about 6.5, and viscosity was 2.0 pa ·s The steady-state infiltration rates of Sinomenine control solution, microemulsion, microemulsion-based gel, hydrogel were 3.328, 42.861, 17.244, 12.185 μg·cm^-2·h^-1, and their 12 h cumulative permeation amountwcre 41.104 ~ 1.219,505.198 ± 176.964,211.373 ± 24.856,145.391 ± 24.392 μg·cm^-2. Conclusion The infiltration rate and 12-h cumulative permeation amount of sinomenine in microemulsion, microemulsion-based gel are superior to those in the control water solution and the hydrophilic gel, which will supply evidence for the selection for the transdermal formulations of sinomenine.

关 键 词：青藤碱 微乳凝胶 体外透皮 

分 类 号：R285.5[医药卫生—中药学]