Pharmacokinetics/pharmacodynamics evaluation of two injection formulations of propofol in healthy Chinese volunteers
- VernacularTitle:丙泊酚注射液在中国健康受试者的药代动力学和药效学
- Author:
Wan-Wen CAO
1
;
Zhong-Yuan XU
;
Peng-Xiang HUANG
;
Yuan-Cheng CHEN
;
Ping ZHENG
;
Miao-Ning GU
;
Jin-Fang XIAO
;
Hang ZHENG
;
An-De MA
Author Information
1. 南方医科大学 南方医院
- Keywords:
propofol injection;
pharmacokinetic;
pharmacodynamic;
bioequivalence
- From:
The Chinese Journal of Clinical Pharmacology
2014;(5):421-424,435
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the pharmacokinetics and pharmaco-dynamics and to assess the therapeutic equivalence between two injection formulations of propofol medium and long chain fat emulsion injection in healthy male Chinese volunteers.Methods Twenty healthy male Chi-nese volunteers were enrolled in a randomized , double -blinded , and crossover study.Each subject was intravenously injected a single dose of 2 mg · kg-1 test or reference formulation.The plasma concentration of propofol was determined by a validated HPLC -MS/MS method.Phar-macodynamics (PD) parameters, and bispectral index (BIS) were recor-ded by EEG monitor.In addition,the onset time of emergences from hyp-nosis were observed.Results Twenty subjects accomplished the trial.The propofol belonged to three -compartment model in vivo.After a sin-gle dose of propofol or reference formulation , the pharmacokinetics pa-rameters of propofol were as follows:tmax were (2.25 ±0.44), (2.25 ± 0.44) min; t1/2 were ( 1.94 ±0.45 ), ( 1.89 ±0.36 ) h; cmax were (6.53 ±1.91), (6.41 ±1.77) μg· mL-1; AUC0-t were (1.534 ± 0.242 ) , ( 1.571 ±0.259 ) μg · mL-1 · h.The relative bioavailability of test to reference formulation was (101.10 ±12.06 )%.The appearing time of minimum BIS value were as follows: tmin-BIS were (2.90 ±0.79 ), (2.95 ±0.69 ) min, BISAUC(0-25 min) were 1904.2 ±129.9 , 1914.1 ±170.7.No serious adverse events occurred in the trial.Conclusion The elimination of propofol in healthy male Chinese volunteers is quick.There are rapid changes in BIS value after injection and a good correlation is maintained with plasma concentration changes.
