摘要
目的:制备银杏内酯B自微乳化制剂,并对其质量进行评价。方法:通过高效液相-电喷雾-质谱(HPLC-ESI-MS)方法测定银杏内酯B在不同油相、表面活性剂、助表面活性剂中的溶解度,结合伪三元相图,筛选银杏内酯B自微乳化制剂的处方。考察药物含量和分散介质对制剂稳定性的影响以及经0.1 mol.L-1HCl稀释后形成微乳的形态、粒径和成乳稳定性。结果:自微乳化介质处方为油酸乙酯-(cremophor EL-大豆磷脂-无水乙醇,40∶60),其中cremophor EL-大豆磷脂-无水乙醇(4∶1∶2),GB的载药量为2.5%。乳化介质(H2O和0.1 mol.L-1HCl)对制剂自微乳化效率影响不大。银杏内酯B自微乳制剂经0.1 mol.L-1HCl稀释100倍后透射电镜下呈圆球形,分布均匀,粒径(41.6±1.11)nm,自微乳化时间大约在2 min。8 h内制剂稳定,粒径变化不大,无药物析出。结论:银杏内酯B自微乳化制剂制备简单,质量稳定,可以显著提高药物的溶解度。
Objective： To prepare ginkgolide B-loaded self microemulsifying drug delivery system（SMEDDS） and evaluate its quality.Method： The solubility of ginkgolide B in different oil,surfactant and co-surfactant were measured by HPLC-ESI-MS.The GB-SMEDDS formulation was optimized by the self emulsifying efficiency of various combinations of oil and mix-surfactant evaluated by using pseudo-temary phase diagram.The preliminary stability of GB-SEMEDDS was evaluated by the variety of loading rate of GB and dispersed medium.The morphology,the particle size and the formulation stability were evaluated after diluting by 0.1 mol·L-1 HCl.Result： The blank self microemulsified system was composed of ethyl oleate-（cremophor EL-lecithin-ethanol,4∶1∶2）（40∶60）,the loading dosage was 2.5%.Little influence of GB and emulsified medium was observed on the stability of GB-SEMDDS.After diluted with 0.1 mol·L-1 HCl,the morphology of the microemulsion was homogeneous small spherical drops observed under electro-microscope.The particle size was（41.6±1.11） nm,the self microemulsifing time was around 2 min.The formulation was stable within 8 h,without significant changes in particle size and separation of drugs.Conclusion： GB-SMEDDS is easy to prepare and its quality is stable.The solubility of GB was significantly improved by SMEDDS.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2010年第22期2967-2971,共5页
China Journal of Chinese Materia Medica
基金
广东省建设中医药强省专项基金项目(2008087)
关键词
银杏内酯B
自微乳化
伪三元相图
ginkgolide B； self-emulsified； pseudo-temary phase diagram
