目的制备水包油型秋水仙碱微乳,并对其理化性质及体外经皮渗透性能进行考察。方法以秋水仙碱、聚山梨醇酯、异丙醇、油酸和蒸馏水为主要成分,制备秋水仙碱微乳,考察其外观形态、粒径大小及分布。采用改良的Franz扩散池考察秋水仙碱微乳的体外透皮过程,HPLC法测定秋水仙碱。结果制得的秋水仙碱微乳为淡黄色透明液体,平均粒径60.2 nm,外观圆整均匀,渗透效果依次为水溶液<微乳<促渗剂氮酮,其中氮酮7 h即达到释药平台期,微乳在12 h才接近平台期。结论制备的水包油型秋水仙碱微乳具有良好的透皮效果,且较透皮促渗剂氮酮来说能够缓释药物,为秋水仙碱的新型透皮给药系统提供前期研究基础。

Objective To prepare oil in water (O/W) microemulsion and investigate its in vitro transdermal permeation ability. Methods The O/W microemulsion was prepared with the formulation containing colchicine, polysorbate, isopropyl alcohol, oleic acid, and deionized water. The morphology and grain size distribution of microemulsion were studied. Using Franz cell to investigate the transdermal process of colchicine microemulsion. The content of colchicine was measured by HPLC. Results The microemulsion was transparent liquid in light yellow and its grains were round with mean grain size at 60.2 nm in diameter. Permeation sequence was aqueous solution < microemulsion < penetration enhancers, azone. Azone reached the drug delivery level in 7 h and microemulsion was in 12 h. Conclusion Microemulsion has good transdermal penetration which could release drugs slower than transdermal penetration enhancers, azone. This could provide the basis for preliminary studies of a new transdermal delivery system of colchicine.

江苏省中医药领军人才项目(LJ200913)