Pharmacokinetic study of meptazinol hydrochloride capsule in Chinese healthy volunteers
- VernacularTitle:盐酸美普他酚胶囊在中国健康受试者中的药代动力学研究
- Author:
Chang-Cheng YANG
1
;
Xin GUO
;
Tao SU
;
Zhi LIU
;
Li-Ling RAN
;
Ren GUO
Author Information
1. 解放军第163 医院 药剂科
- Keywords:
meptazinol hydrochloride;
pharmacokinetic;
HPLC-MS/MS
- From:
The Chinese Journal of Clinical Pharmacology
2014;(8):685-688
- CountryChina
- Language:Chinese
-
Abstract:
Objective To study the pharmacokinetic characteristics of meptazinol after single oral dose and multiple doses of meptazinol hydro-chloride capsule in Chinese healthy volunteers.Methods A random-ized, open, 3 ×3 Latin square design was adopted.Twelve healthy vol-unteers were divided into six groups , two people ( one male and one fe-male) per group.The dosages are 100 mg, 200 mg and 400 mg in single dosage study , and 200 mg every 6 hours for 5 times in multiple dosage study.The concentrations of meptazinol in plasma were determined by HPLC -MS/MS.The pharmacokinetic parameters were calculated by WinNonlin 6.1 software.Results The main pharmacokinetics parame-ters of meptazinol in three single dose were as follow: Cmax were (22.21 ±12.74), (55.01 ±36.38) and (97.80 ±64.23) μg· L-1;tmax were (1.00 ±0.54),(1.04 ±0.61) and (1.54 ±0.91) h; t1/2 were (2.31 ±0.24), (2.31 ±0.24 ) and (2.46 ±0.59 ) h; AUCinf were ( 50.78 ±13.14 ) , ( 134.06 ±56.90 ) and ( 281.34 ±135.34 )μg· h· L-1.The main pharmacokinetic parameters of meptazinol under multiple dose were as follow:Cssmin was ( 6.01 ±2.03 ) μg · L-1 , Cmax was ( 54.30 ±27.10 ) μg · L-1 , Cavg was (20.13 ±6.82) μg· L-1, tmax was(1.06 ±0.51) h, t1/2 was (2.62 ±0.24) h, and AUCinf was (149.63 ±50.49)μg · h· L-1.Conclusion The plasma concentrations of meptazinolin in Chinese healthy volunteers were proceeded in an apparently mono-exponential fashion after a single oral dose from 100 mg to 400 mg meptazinol hydrochloride cap-sula.Meptazinol has no accumulation in the human body , after multiple doses of 200 mg every 6 hours for 5 times.The accumulation of meptazinol is consistent with linear pharmacokinetic process.
