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目的：评价盐酸美普他酚胶囊在中国健康受试者中的单次及连续多次给药后的体内药代动力学特征。方法用随机、开放、拉丁方试验设计，12例健康受试者分为6组，每组2人，男女各1人。单次口服给药剂量分别为100，200，400 mg；连续多次口服给药剂量为200 mg，q6 h，共给药5次，用HPLC-MS/MS法测定不同时间点血浆中美普他酚的浓度，用WinNonlin 6.1软件计算美普他酚的药代动力学参数。结果单次口服给药3个剂量组美普他酚的药代动力学参数如下：Cmax分别为（22.21±12.74），（55.01±36.38）和（97.80±64.23）μg· L-1；tmax分别为（1.00±0.54），（1.04±0.61）和（1.54±0.91）h；t1/2分别为（2.31±0.24），（2.34±0.21）和（2.46±0.59）h；AUCinf分别为（50.78±13.14），（134.06±56.90）和（281.34±135.34）μg· h· L-1。连续多次给药药代动力学参数Cssmin为（6.01±2.03）μg · L-1， Cmax为（54.30±27.10）μg · L-1， Cavg为（20.13±6.82）μg· L-1，tmax为（1.06±0.51）h，t1/2为（2.62±0.24）h，AUCinf为（149.6±50.5）μg· h· L-1。结论单次口服盐酸美普他酚胶囊100～400 mg后，体内过程符合1级速率线性动力学过程；每次200 mg，q6 h，连续给药5次后，在人体内无蓄积，其累加过程符合线性动力学。“,”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 undermultiple 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.