Objective To evaluate the pharmacokinetics of dexmedetomidine hydrochloride injection in Chinese healthy volunteers. Methods 30 healthy volunteers were divided into three groups: intravenous administration of dexmedetomidine at 0.5, 1. 0 and 1. 5 (xg ' kg"1. Concentrations of dexmedetomidine in plasma were determined by HPLC/MS/MS. The pharmacokinetics parameters were calculated with DAS 2. 0 software. Results The main pharmacokinetic parameters for three groups were as follows: AUC^, were ( 902. 51 ±264. 18 ),( 1 828. 68±643.71 )and ( 2 462. 55±492. 97 ) pg ? H ? Ml/1 ^UC^were( 1 068.87±505. 46 ),( 2 027. 72±816. 93 ) and (2 597. 89±463. 06 ) pg ? H ? Ml/1 ; C._ were ( 569. 90±155. 87 ), ( 1 042.80±330.77) and ( 1 682. 00±639.67 ) pg ■ ml/1 ;lmi were ( 0. 13+0. 03 ),( 0. 08±0. 00 )and( 0. 11 ±0.04 ) h;lw were (2.69±1.38),(2.59±1.12) and ( 2. 62±0. 87 ) h, respectively. There were no significant differences in AUC^,, , AUQ,_. , Cmax,tw2 ,2mai ,CLz, Fz among three groups by variance analysis( P>Q. 05 ). Conclusion The pharmacokinetic parameters of dexmedetomidine hydrochloride such as AUC0_12 , AUQ,_U , CmaI increased in a dose-dependent manner in healthy human,which is consistent with linear kinetic process.%目的 在中国健康志愿者中进行盐酸右美托咪定注射液的药动学研究.方法 健康志愿者30例,分为3个剂量组:分别静脉推注盐酸右美托咪定0.5,1.0和1.5 μg ·kg-1.采用高效液相色谱-质谱联用(HPLC/MS/MS)法测定血浆中右美托咪定浓度变化.以DAS2.0软件进行数据处理,计算药动学参数[血药浓度-时间曲线下面积(AUC),血药峰浓度(Cmax),半衰期(t1/2),清除率(CLz),表观分布容积(Vz),达峰时间(tmax)].结果 盐酸右美托咪定注射剂3个剂量组的AUC0→12分别为(902.51±264.18),(1 828.68±643.71)和(2 462.55±492.97) pg·h·mL-1;AUC0→∞分别为(1 068.87±505.46),(2 027.72±816.93)和(2 597.89±463.06) pg·h·mL-1;Cmax分别为(569.90±155.87),(1 042.80±330.77)和(1 682.00±639.67) pg·mL-1;tmax分别为(0.13±0.03),(0.08±0.00)和(0.11±0.04) h;t1/2分别为(2.69±1.38),(2.59±1.12)和(2.62±0.87) h;3个剂量组间药动学参数AUC0→12,AUC0→∞,Cmax,t1/2,tmax,CLz,Vz均差异无统计学意义(均P＞0.05).结论 静脉给予盐酸右美托咪定注射剂在健康受试者体内呈现随着剂量增加,AUC0→12,AUC0→∞,Cmax增大的代谢规律,其代谢呈线性动力学特征.
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