摘要
目的:制备青藤碱微乳,研究青藤碱微乳及透皮吸收促进剂对体外透皮吸收的影响。方法:Zetasize多功能电位/粒度分析仪测定青藤碱微乳的粒度及其分布。用稳定性实验考察青藤碱微乳的稳定性。用Valia-Chien扩散池,研究青藤碱微乳的透皮速率以及薄荷脑、冰片、肉豆蔻酸异丙酯(IPM)等透皮促进剂对青藤碱微乳吸收的影响。结果:青藤碱微乳液滴的平均粒径均为31.3 nm。青藤碱微乳具有很好的稳定性。青藤碱微乳的平均透皮速率为(32.238±1.13)μg/cm2.h,几种促进剂对青藤碱微乳经皮渗透都有显著的促进作用(P<0.05)。以含2%冰片组促渗效果最好。结论:所制备的微乳具有很好的透皮速率,有望成为青藤碱的新型经皮给药制剂,薄荷脑、冰片和肉豆蔻酸异丙酯可以作为促渗剂用于青藤碱经皮吸收制剂。
AIM: To prepare O/W microemulsion formulation containing sinomenine and investigate the effect of different penetration enhancers on transermal delivery character of microemulsion in vitro. METHODS: The microemulsions were prepared and characterized using Zetasize potential/particle size analysis instrument. The stability tests were performed to evaluate the sinomenine microemulsions. Franz diffusion cell was adopted as the apparatus for in vitro transdermal test. Excised Wistar-rat abdomen skin was pretreated with penetration enhancers, such as menthol, borneol and isopropyl myristate. RESULTS: The average droplet size of the microemulsion was about 31.3 nm. A high permeation rate of (32. 238 ± 1.13 ) μg/cm^2 · h was showed in vitro. All the enhancers showed significant enhancement effect on the transdermal behavior of sinomenine microemulsion. 2% borneol had the strongest effect in all. CONCLUSION: These results indicate that the studied microemulsion system with high permeation rate may be a promising vehicle for the transdermal delivery of sinomenine. Menthol, borneol and isopropyl myristate were found to be the proper penetration enhancers in the transdermal preparation.
出处
《中成药》
CAS
CSCD
北大核心
2008年第8期1119-1122,共4页
Chinese Traditional Patent Medicine
关键词
青藤碱
微乳
经皮给药
促进剂
sinomenine
microemulsion
transdermal delivery
enhancer