吡喹酮长循环纳米粒在家兔体内的药动学

Pharmacokinetics of Long-circulating Nanoparticles Containing Praziquantel in Rabbits

健康成年家兔18只,随机分为3组,分别静注吡喹酮溶液、吡喹酮纳米粒和吡喹酮长循环纳米粒(10 mg/kg)。以地西泮为内标,采用HPLC法测定家兔血浆中的吡喹酮。吡喹酮注射液和吡喹酮纳米粒的体内过程符合二房室模型,吡喹酮长循环纳米粒的体内过程符合三房室模型,3种制剂的主要药动学参数分别为:t1/2(1.27±1.56)、(1.13±0.66)和(23.82±8.94)h,CL(5.29±0.78)、(2.38±1.00)和(1.16±0.16)L.h-1.kg-1,AUC0→t(1.48±0.27)、(3.52±1.79)和(4.93±1.27)mg.h.ml-1,MRT(0.44±0.30)、(0.41±0.10)和(16.12±1.38)h。

Eighteen rabbits were randomly praziquantel solution, praziquantel nanoparticles and divided into three groups and intravenous administration of praziquantel long-circulating nanoparticles, respectively. The concentration of praziquantel in rabbit plasma were determined by HPLC. The pharmacokinetics of praziquantel solution and praziquantel nanoparticles was fitted into a two-compartment open model, and praziquantel long-circulating nanoparticles was fitted into a three-compartment open model. The main pharmacokinetic parameters were as follows： t1/2 （1.27±1.56）, （1.13±0.66） and （23.82±8.94）h, CL （5.29±0.78）, （2.38±1.00） and （1.16±0.16）L.h^-1 ·kg^-1, AUCo→t （1.48± 0.27）, （3.52±1.79） and （4.93±1.27） mg.h.ml^- 1, MRT （0.44±0.30）, （0.41±0.10） and （16.12±1.38） h.