十一酸睾酮自微乳化制剂的处方研究

Study on Formulation of Testosterone Undecanoate Self-emulsifying Drug Delivery Systems

关键词:  十一酸睾酮  自乳化  处方

Key words:  testosterone undecanoate  self-microemulsifying drug delivery systems  formulation

摘要:

目的 制备十一酸睾酮(TU)自微乳化制剂。方法 通过伪三元相图绘制和自乳化效率的评价筛选TU自微乳化制剂处方，用HPLC测定药物的含量，考察制剂经高温和光照的影响因素试验后的质量。结果 以辛癸酸甘油酯为油相、Cremophor EL /Tween 85(1∶4)为混合乳化剂、油相与乳化剂重量比1∶1作为TU自乳化制剂介质的处方，在不同介质能迅速形成自微乳液。经高温10 d放置，TU自乳化制剂的质量未发生变化，光照10 d后药物含量略有下降。结论 制备了不含助乳化剂的TU自微乳化制剂，适合于进一步制成软胶囊。

Abstract:

OBJECTIVE To preparation testosterone undecanoate self-microemulsifying drug delivery systems (TU SMEDDS). METHOD The formulation of TU SMEDDS was obtained by pseudo-ternary phase diagram and the determination of self-microemulsifying efficiency. RP-HPLC was used to assay the contents of TU. The quality of TU SMEDDS was evaluated under the conditions of severe temperature and light test. RESULTS The medium of TU SMEEDS was composed of equi-weight of octyl decyl glycerate (ODO) as oil phase and two nonionic surfactants, Cremophor EL and Tween85, with the weight ratio of 1∶4 as emulsifying agents. This formulation can be rapidly emulsified in different aqueous. The TU content gave slight decrease under the 10 day severe light test while represented stability under temperature test. CONCLUSION The emulsifying agent of TU-SEDDS is using two mixture nonionic surfactants while no co-surfactants included, which is suitable to prepare soft capsules.