中国药房2012,Vol.23Issue(45):4269-4271,3.DOI:10.6039/j.issn.1001-0408.2012.45.17
甲睾酮聚乳酸缓释微球的制备
Preparation of Methyltestosterone Polylactic Acid Sustained-release Microspheres
吕竹芬 1黄思玉 1陈燕忠 1温玉琴 1林浩杰 1吴彩珍 1班俊峰 1孙美丽 1谢清春1
作者信息
- 1. 广东省药物新剂型重点实验室/广东药学院药物研究所,广州510006
- 折叠
摘要
Abstract
OBJECTIVE: To prepare Methyltestosterone polylactic acid sustained-release microspheres (MT-PLA-MS). METHODS: MT-PLA-MS was prepared by emulsification solvent evaporation method, and single factor test was conducted to select molecular weight and concentration of polylactic acids and ratio of drug to PLA. Orthogonal test was used to optimize temperature, rotation speed, concentration of polylactic acids and ratio of drug to PLA. The appearance, particle size, drug-loading amount, encapsulation coefficency and 168 h accumulative drug-releasing rate in vitro were investigated, and zero-order, first-order, Higuchi and two-phase dynamic equations of microspheres were fitted. RESULTS: The optimal condition was as follows: molecular weight of polylactic acids of 110 thousand, temperature of 30 ℃ , rotation speed of 500 r·min-1, concentration of polylactic acids of 0.1 g·mL-1 and ratio of drug to PLA of 1 : 5. Prepared microspheres were round with smooth surface. Mean particle size was (2.5 ± 0.2) μm, drug-loading amount was 6.18%~6.62% , encapsulation coefficency was 89.9% ~91.3% and 168 h accumulative drug-releasing rate was (41.8 ±0.1)%. Two-phase dynamic equation of microsphere was fitted for microspheres (r=0.994 5). CONCLUSION: The preparation technology is stable and microspheres exhibit good sustained-release capacity.关键词
甲睾酮/聚乳酸/缓释微球/制备/正交试验Key words
Methyltestosterone/ Polylactic acid/ Sustained-release microspheres/ Preparation/ Orthogonal test分类
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吕竹芬,黄思玉,陈燕忠,温玉琴,林浩杰,吴彩珍,班俊峰,孙美丽,谢清春..甲睾酮聚乳酸缓释微球的制备[J].中国药房,2012,23(45):4269-4271,3.