摘要
目的探讨超顺磁性异烟肼(Isoniazide,INH)聚乳酸-聚乙二醇共聚物(Polylactide-polyethylene glycol copolymers,PELA)微球(Superparamagnetic isoniazide PELA microspheres,SPIPM)在振荡磁场作用下体内异烟肼的释放规律,并建立异烟肼HPLC检测方法。方法采用化学共沉淀法制备超顺磁性Fe3O4纳米粒,复乳化(W/O/W)溶剂蒸发法制备SPIPM,离心,洗涤,HPLC法检测洗涤液中异烟肼的含量,计算载药量和包封率;并检测SPIPM的表征;选取18只新西兰大白兔,随机分为SPIPM外加振荡磁场干预组,SPIPM组和异烟肼组,给药后每隔15 min取静脉血,采用HPLC法测定异烟肼的血药浓度。结果 SPIPM的载药量为(7.5±0.5)%,包封率为(50±1.5)%;微球表明光滑,形态圆整,分散性良好,粒度分布基本呈正态分布,粒径分布范围窄。与单纯注射异烟肼相比,SPIPM能延缓异烟肼释放,外加振荡磁场时,可重复提高动物体内SPIPM中异烟肼的释放量。结论超顺磁性异烟肼PELA微球具有缓释性,振荡磁场可明显促进超顺磁性异烟肼PELA微球中异烟肼的释放。
Objective To investigate the principle of in vivo release of isoniazide（INH） from superparamagnetic isoniazide polylactide-polyethylene glycol copolymers（PELA） microspheres（SPIPM） under oscillating magnetic field and develop a HPLC method for INH.Methods Superparamagnetic Fe3O4 nanoparticles were prepared by chemical coprecipitation,based on which SPIPMs were prepared by solvent evaporation with complex emulsification,then centrifuged,washed,determined for INH content by HPLC to calculate drug load and envelopment rate,and observed for surface characters.Eighteen New Zealand white rabbits were randomly divided into three groups.The rabbits in groups A and B were injected i.m.with SPIPM,while those in group C with INH.However,the rabbits in group A were injected under oscillating magnetic field.Venous blood was collected every 15 min after injection and determined for INH concentration by HPLC.Results The load and envelopment rate of SPIPM were（7.5 ± 0.5）% and（50 ± 1.5）% respectively.The microspheres showed smooth surface,round and intact morphology,and good dispersiveness.The granularities were basically in normal distribution,and the particle sizes were distributed in a narrow range.Compared with that in group C,the release of INH was slowly in group B,and was further increased in group A.Conclusion Superparamagnetic isoniazide PELA microspheres were controlled-released,in which the release of INH was promoted significantly by oscillating magnetic field.
出处
《中国生物制品学杂志》
CAS
CSCD
2011年第12期1433-1436,共4页
Chinese Journal of Biologicals
基金
中国博士后科学基金(20080430754)
重庆市卫生局重点课题(渝卫科教[2007]1号)
重庆市卫生局课题(2009-2-246)
关键词
超顺磁性微球
异烟肼
聚乳酸-聚乙二醇共聚物
色谱法
高压液相
振荡磁场
Superparamagnetic microspheres
Isoniazide（INH）
Polylactide-polyethylene glycol copolymers（PELA）
Chromatography
high performance liquid
Oscillating magnetic field
