氟比洛芬酯脂微球的制备及其在兔体内的药物动力学评价  

Preparation of Flurbiprofen Axetil Lipid Microspheres and Their Pharmacokinetics in Rabbits

作　　者：屠祎惺 方源[1] 黄小音 付爱玲[2] 高峰[1,3,4] 

机构地区：[1]华东理工大学药学院药剂教研组,上海200237 [2]上海景峰制药股份有限公司,上海201908 [3]华东理工大学上海市功能性材料化学重点实验室,上海200237 [4]华东理工大学上海市新药设计重点实验室,上海200237

出　　处：《华东理工大学学报（自然科学版）》2013年第6期681-684,共4页Journal of East China University of Science and Technology

基　　金：上海市科学技术委员会项目资助(11DZ2260600;10DZ2220500);上海市宝山区科学技术委员会产学研合作项目(Y100-81110)

摘　　要：以两步乳匀法制备氟比洛芬酯(FA)脂微球,采用动态光散射法、超速离心法测得FA脂微球粒径为(168.6±9.3)nm,Zeta电位为(-34.8±1.4)mV,包封率为(99.4±0.9)%;用高效液相色谱法检测兔体内FA代谢产物氟比洛芬(FP),FA脂微球静脉给药后,FP主要药物动力学参数分别如下:t1/2β为(0.83±0.13)h,AUC0→24h为(16.10±1.56)μg·h/mL,CL为(0.41±0.02)L/(h·kg)。制得的FA脂微球包封率高,稳定性好,在兔体内的FP药物动力学过程符合二室模型。Flurbiprofen axetil （FA） loaded lipid microspheres （LM） were prepared by two-step emulsification method. Their mean size was （168.6 ± 9.3） nm as determined by dynamic light scattering and uhracentrifugation. The zeta potential was （--34. 8± 1. 4） mV, and entrapment efficiency was （99.4±0.9）%. A high-performance liquid chromatography （HPLC） method was established to detect flurbiprofen （FP） concentration of the FA loaded LM in rabbits after intravenous injection. Pharmacokinetic parameters were t1/2β： （0.83 ± 0.13） h, AUC0-24h：（ 16. 10 ± 1.56） μg·h/mL, CL： （0.41± 0.02） L/（h ·kg）, respectively. The obtained LM showed high entrapment efficiency of FA with high stability. The plasma concentration of FP showed that the pharmacokinetics of FA loaded LM was well fitted by two-compartments model.

关 键 词：脂微球 药物动力学 氟比洛芬酯 氟比洛芬 

分 类 号：R94[医药卫生—药剂学]