摘要
以天然可生物降解的明胶为载体材料,液体石蜡为油相,Span80为乳化剂,采用正交试验优化空白明胶微球的乳化法制备工艺,并在此基础上制备了恩诺沙星明胶微球。结果显示,含药微球平均粒径为12.35μm,粒径7～30μm的微球占总数的92.3%,符合肺靶向的要求。恩诺沙星明胶微球载药量为20.67%、包封率为43.62%,动态透析法研究体外释放特性,符合Higuchi规律,释药t1/2比原药延长了约6倍,表明有明显的缓释功能。在37℃、相对湿度值(RH)75%考察3月,几乎无变化。兔体内分布试验表明具有明显的肺靶向性,肺中药代动力学行为符合三室开放模型。
Biodegradable gelatin was used as a carder material,liquid paraffin as the oil phase,Span80 as the emuLsifier.The preparation condition of the blank gelatin microspheres （GMS） was optimized by an orthogonal test design. Furthermore, en-rofloxacin lung targeting gelatin microspheres （ENR-GMS） were prepared based on the method of emulsion. Results indicated that arithmetic mean diameter of ENR-GMS was 12.35 μm with 92.3% of the microspheres ranging from 7 to 30 μm.The average quantity of load-drug was 20.67% and average ENR drug entrapment efficiency was 43.62% .Release of the drug from the ENR-GMS in vitro became much slower with its tl/2 of about 6 times longer than that of original ENR.The release profiles of the micro- spheres followed Higuchi kinetic equation.It showed that the ENR-GMS had obviously sustained-release effect.AImest no change was observed after the ENR-GMS were stored for 3 months at 37℃ （relative humidity 75%） .The distribution test in vivo in rabbit indicated that the lung targeting effect of the ENR-GMS was obvious and kinetic bahavior of the drug in rabbit lung could be de-scribed by the three open compartment model.
出处
《中国兽医学报》
CAS
CSCD
北大核心
2008年第1期79-83,共5页
Chinese Journal of Veterinary Science
关键词
恩诺沙星
明胶微球
乳化法
肺靶向给药系统
enrofloxacin
gelatin microsphere
emulsification
lung targeting drug delivery system
