摘要
目的制备雌三醇微球,考察其外观形态、粒径、载药量、包封率及体外释放度,为萎缩性阴道炎治疗提供一种新制剂。方法用可生物降解的聚乳酸-羟基乙酸为微球材料,采用O/W单乳法制备雌三醇微球。分别用光学显微镜、扫描电镜观察外观形态,用激光粒度仪测定粒径。用无水乙醇溶解微球后,涡旋破碎,提取雌三醇,用紫外分光光度法测定药物含量,计算载药量、包封率。测定雌三醇微球体外释放率,评价其缓释效果。结果雌三醇微球呈圆整的球形粒子,粒径约3μm。载药量为19.1%,包封率为95.5%,在体外主要以扩散机制释药。结论将雌三醇制备成微球后,能实现缓释、降低给药频率,可应用于治疗萎缩性阴道炎。
Objective To prepare estriol microspheres and evaluate their morphology,size,drug loading, encapsulation efficiency and release in vitro.Methods Biodegradable poly (lactic-co-glycolic acid)(PLGA) was used to prepare microspheres and estrioI microspheres were prepared with O/W single emulsion method. The morphology was observed by optical microscope and scanning electron microscope (SEM),and the size was determined by dynamic laser scanning method.Estriol was extracted from the vortexed and disrupted microspheres with ethanol and determined by ultraviolet spectrophotometry.Drug loading,encapsulation efficiency and release in vitro were evaluated.Results Estriol microspheres were smooth spheres with diameter at about 3μm.The drug loading was 19.1%and the encapsulation efficiency was 95.5%.The drug was mainly released by diffusion in vitro.Conclusion Estriol microspheres may decrease the administration frequency and are convenient for atrophic vaginitis.
作者
张丽花
郝文艳
朱思庆
杜丽娜
ZHANG Li-hua;HAO Wen-yan;ZHU Si-qing;DU Li-na(Shandong University of Traditional Chinese Medicine,Jinan 250355;Beijing Institute of Radiation Medicine,Millitacy Medical Academy,Beijing 100850;Weifang Medical University,Weifang Anhui 261021;Anhui Medical University,Hefei 230032)
出处
《中南药学》
CAS
2018年第12期1709-1712,共4页
Central South Pharmacy
关键词
雌三醇
单乳法
缓释
聚乳酸-羟基乙酸
微球
estriol
single emulsion method
sustained release
poly (lactic-co-glycolic acid)
microsphere
作者简介
张丽花,女,硕士研究生,主要从事新型药物递送系统研究,E-mail:13051908662@163.com;通讯作者:杜丽娜,女,博士,副研究员,硕士研究生导师,主要从事经皮肤、黏膜给药制剂研究,E-mail:dulina@188.com