摘要
目的:考察布洛芬包合物温敏凝胶在兔体内的药动学行为及其对注射部位的刺激性。方法:采用HPLC内标法测定了不同时间点的血药浓度,3P97软件进行房室模型的拟合和药动学参数的计算,光镜下观察对照组、空白凝胶组、凝胶低剂量组和高剂量组、水溶液组注射部位的病理切片。结果:布洛芬包合物温敏凝胶体内释放规律符合Weight为1/C2的二室模型,Cmax(5.81±0.65)μg·ml-1,Tpeak(101.77±2.59)h,AUC(0-t)(1 619.13±36.51)μg·min·ml-1。兔注射部位肌肉组织结构正常,横纹清晰,未见坏死肌细胞。结论:布洛芬包合物温敏凝胶能够延长达峰时间,显著提高生物利用度,且对注射部位无明显刺激性,生物相容性好。
OBJECTIVE To evaluate the pharmacokinetics and injection site irritation of ibuprofen inclusion complex thermo- sensitive in situ gel in New Zealand white rabbits. METHODS The ibuprofen concentrations in serum were determined by HPLC. The pharmacokinetic parameters of ibuprofen and the fitting of compartment model were analyzed using 3P97 program. The pathological sections in injection site of control group, blank gel group, low dose group, high dose group and ibuprofen a queous solution group were observed under the light microscope. RESULTS The drug release from ibuprofen inclusion complex thermosensitive in situ gel followed two-compartment model with 1/C2 as weight. The pharmacokinetic parameters were as fol lows： Cmax（5.81 ± 0. 65）/lg.mL 1;Tpeak（101.77±2.59）h;AUC（0-t）（1619. 13±36.51）μg.min.ml-1. CONCLUSION The ibu profen inclusion complex thermosensitive in situ gels significantly extended Tpeak and increased the bioavailability without notice able irritation to the injection site.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2014年第4期296-299,共4页
Chinese Journal of Hospital Pharmacy
关键词
包合物
温敏凝胶
药动学
刺激性
布洛芬
inclusion complex
thermosensitive in situ gel
pharmacokinetics
irritation
ibuprofen
