胸腺肽聚乳酸微球的制备和体外释药研究(英文)

Preparation and in vitro release studies of thymosin-loaded PLA microspheres

为了寻找适于多肽分子吸收,免疫学上“有效”、“安全”,且服用方便的口服制剂,用W/O/W型乳化挥发法制备胸腺肽聚乳酸微球,正交实验方法优化了制备工艺.通过差热分析证明载药微球已较好形成,Lowry法测定药物的含量,计算微球的载药量、包封率及体外释药量.结果表明,所得微球平均粒径为13.8μm,平均包封率为80.7%,前12h的体外释药符合Higuchi方程,T1/2=295min,在25℃和40℃分别放置90d,微球的粒径分布和剩余药量无显著变化.微球的载药量和包封率符合要求,释药半衰期长,具有良好的应用前景.

To obtain a kind of convenient oral dosage form of protein, which can be fully absorbed and is efficient and safe, the thymosin-loaded PLA（polylactic acid） microspheres are prepared by the emulsification- solvent evaporation method and the orthogonal design is used to optimize the technology of preparation. The form of the medicament microspheres of thymosin are proved by differential thermal analysis （DTA）. The drug content is determined by the Lowry method, and the package ratio of medicament microspheres of thymosin and drug release in vitro are calculated. The results show that the average diameter and encapsulation efficiency of the product prepared according to the optimized formulation are 13. 8 μm and 80. 7%, respectively. The in vitro release behavior within 12 h can be described by the Higuchi equation with T1/2 = 295 rain. There are no significant changes in size distribution and residual drug contents after being stored at 25℃ and 40 ℃ for 90 d, respectively. Due to the fact that its thymosin content and package ratio meet the requirement, and its releasing half life is long, the thymosin-loaded PLA microsohere has a favorable application future.