Pharmacokinetic behavior of docetaxel lipid emulsion injection in rats
10.11665/j.issn.1000-5048.20160515
- VernacularTitle:多西他赛脂肪乳注射液在大鼠体内的药代动力学研究
- Author:
Xiaofei ZHANG
1
;
Qiuting GUO
;
Jing SUN
Author Information
1. 陕西中医药大学 陕西省中药制药重点学科
- Publication Type:Journal Article
- Keywords:
docetaxel;
lipid emulsion;
high pressure homogenization method;
pharmacokinetics;
two-compartment model
- From:
Journal of China Pharmaceutical University
2016;47(5):595-598
- CountryChina
- Language:Chinese
-
Abstract:
The aim of this study was to prepare and characterise docetaxel lipid emulsion injection and to conduct the characterization of its pharmacokinetics in rats after tail-vein injection. High pressure homogenization method was used to prepare docetaxel lipid emulsion. 12 Wistar rats were randomly divided into docetaxel lipid emulsion injection group and docetaxel injection group, and dosed at 6 mg/kg through tail-vein injection. Docetaxel concentration in plasma was determined by HPLC. The pharmacokinetic parameters of docetaxel in rats were obtained using the 3P97 program. Particle size, polydispersion index, Zeta potential of docetaxel lipid emulsion were found to be(221. 6±13. 4)nm, (0. 092±0. 003)and -30. 3 mV, respectively. t1/2(α) of docetaxel lipid emulsion injection and docetaxel injection were(0. 072±0. 014)and(0. 066±0. 015)h; t1/2(β) were(0. 573±0. 253)and(0. 432±0. 184)h; AUC0-12 h were(7. 98±1. 25)and(6. 26±1. 83)μg ·h/mL, respectively. Docetaxel lipid emulsion injection had similar pharmacokinetic characteristics to docetaxel injection. The pharmacokinetic data obtained for both preparations fitted a two-compartment model.
