利福平微球-原位凝胶复合给药系统的研究

 目的 制备利福平聚乳酸-羟基乙酸共聚物（PLGA微球-原位凝胶复合给药系统用于结核病局部给药,以达到局部滞留、缓慢释放的作用。方法 采用液中干燥法制备微球,用海藻酸钠制成离子敏感型原位凝胶,考察微球以及复合给药系统的体外药物释放情况,初步考察复合给药系统在大鼠肺部的胶凝时间。结果 微球平均粒径为149.569 μm,包封率（n=3为（69.43±3.53%,载药量(n=3为（26.43±3.10%,体外释放实验表明,微球-原位凝胶复合给药系统有抑制药物突释的作用,且药物在30 d内释放25%,大鼠肺部胶凝实验表明,离子敏感型原位凝胶在大鼠肺部可滞留6 h。结论 利福平PLGA微球-原位凝胶复合给药系统达到了局部滞留、缓慢释放药物的目的。

Study on Rifampicin Microspheres-In Situ Gel Complex Drug Delivery System

OBJECTIVE To prepare RFP-microspheres-in situ gel complex drug delivery system(CDDSfor topical administration, achieve the local retention and sustained release function. METHODS The RFP-loaded microspheres were fabricated by a modified emulsification/solvent diffusion method, sodium alginate for in situ gel .The drug release from microspheres and CDDS were investigated. Gelatinization time of CDDS were studied preliminarily in lung of SD rats. RESULTS Average particle size of MS was 149.569 μm,entrapment rate and drug-loading rate(n=3were（ 69.43±3.53% and（26.43±3.10%.The study shows that CDDS may reduce dumping in vitro and drug release 25% for 30 d.CONCLUSION RFP microspheres-in situ gel complex drug delivery system can local retention and sustained release.