十一酸睾酮外用微乳巴布剂的质量控制和体外透皮效果

Quality Control and in vitro Transdermal Effects of Testosterone Undecanoate Microemulsion Cataplasm

目的:制备十一酸睾酮微乳,并以水溶性高分子材料为辅料制备外用微乳巴布剂。方法:选用肉豆蔻酸异丙酯(IPM)为油相,Cremophor EL为表面活性剂,Larbrasol为辅助表面活性剂,制备微乳。使用聚乙烯吡咯烷酮(K-90)、聚丙烯酸钠(NP-700)等为基质,制备巴布剂。对制备的巴布剂进行了质量考察,采用体外扩散池法测定了巴布剂中十一酸睾酮的透皮渗透率。结果:最终制备得到的微乳巴布剂中十一酸睾酮载药量400μg.cm-2,经皮渗透速率3.822μg.cm-2.h-1。结论:所选择的微乳处方黏度小、粒径细腻、质量稳定,制备得到的巴布剂具有良好的涂展性、保湿性,且黏着力适中。微乳巴布剂具有明显的控释效果。

Objective：To prepare testosterone undecanoate（TU） microemulsion,and microemulsion cataplasm was prepared with water-soluble polymer materials as accessories.Method：Isopropyl myristate was chosen for oil phase,Cremophor EL was selected as surfactants,Larbrasol was used as auxiliary surfactants to prepare microemulsion.PVP K-90 and NP-700 were used as matrix to prepare cataplasm.Quality of prepared cataplasm was investigated,transdermal penetration of TU was determined by in vitro diffusion cell method.Result：TU loading ability of prepared microemulsion cataplasm was 400 μg·cm-2.Percutaneous penetration of TU was 3.822 μg·cm-2·h-1.Conclusion：This selected microemulsion prescription had low viscosity,fine particle and stable quality.TU microemulsion cataplasma had good extension,moisture,viscosity,and obviously drug control-release ability.