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

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→24 h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。

Abstract: 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 ultracentrifugation. 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→24 h:( 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.