左炔诺孕酮-聚3-羟基丁酸酯缓释微球的研究  

STUDIES ON SUSTAINED RELEASE MICROSPHERES OF LEVONORGESTROL POLY 3 HYDROXYBUTYRATE

作　　者：王正容[1] 陆彬[1] 杨红[1] 

机构地区：[1]华西医科大学药学院

出　　处：《药学学报》1999年第1期54-57,共4页Acta Pharmaceutica Sinica

基　　金：国家计划生育委员会资助

摘　　要：目的：优化制备工艺，用可生物降解的成球材料制备缓释并有优良抗生育效果的左炔诺孕酮聚３羟基丁酸酯微球。方法：以均匀设计优化微球的液中干燥法制备工艺，用ＤＴＡ确证含药微球的形成，对微球的外观、粒径、载药量、体外释药、稳定性及小鼠体内抗生育等进行了研究。结果：微球平均粒径为６４μｍ，（２８７～８５８）μｍ的微球占总数９０％以上，微球中氯仿残留量低于０００１％，体外释药符合Ｈｉｇｕｃｈｉ方程，释药Ｔ１／２比原药延长约１８倍，４，２５及４０℃（ＲＨ７５％）放置３个月稳定。对小鼠具有抗生育效果。结论：微球的制备工艺满意，与原药相比，微球对小鼠有明显的缓释。AIM: To optimize the preparation with in liquid drying method of sustained release microspheres of levonorgestrol poly 3 hydroxybutyrate (LNG PHB) with good anticonceptive effect using PHB as the biodegradable material. METHODS: Uniformed design was used to optimize the technology of preparation with good reproducibility. The appearance, particle size, CHCl 3 residue, drug content, drug release in vitro , stability and anticonceptive effect on mice of the obtained microspheres were examined. The formation of the drug microspheres was confirmed with differential thermal analysis. RESULTS: The average particle size was 64 μm with over 90% of the microspheres being in the range of 28 7～85 8 μm. The CHCl 3 residue was lower than 0 001%, and the drug release behaviour in vitro could be descibed by Higuchi equation. The drug release T 1/2 was prolonged 1 8 times compared with the original drug LNG. The microspheres were stable in 3 months and showed significant sustained release and anticonceptive effect in mice and much lower toxicity compared with the original drug. CONCLUSION: The technology of preparation was successful and the anticonceptive effect in mice was satisfactory with much lower toxicity as desired.

关 键 词：左炔诺孕酮-聚3-羟基丁酸酯 缓释给药系统 微球 抗生育作用 避孕药 

分 类 号：R944[医药卫生—药剂学] R979.21[医药卫生—药学]