新型睡眠促进剂褪黑激素 (Melatonin)的药代动力学研究(英文)

测定新型睡眠促进剂 Melatonin的药代动力学参数的方法是以咖啡因为内标、以 GC/ MS的SIM(选择性离子监测 )为检测手段 ,定量测定家兔体内 Melatonin的含量及药代动力学参数。其结果为家兔灌胃给予 Melatonin3 0 mg· kg- 1后 ,Melatonin在家兔体内呈二室分布 ,药代动力学参数为t1/ 2α=0 .3 1 h,t1/ 2β=8.58h,t1/ 2 Ka=0 .3 4h,Tmax=0 .6 3± 0 .47h,Cm ax=3 2 2 .2 3± 2 55.40 ng/ m L,K12= 0 .81 h- 1,K2 1=2 .80 h- 1,K10 =2 .1 0 h- 1,AUC=6 97.49(ng/ m L) * h,CL(s) =0 .0 97± 0 .0 54 (mg/kg) / h/ (ng/ m L) .这种测量方法灵敏度高、特异性强、准确性好 ,为测定 Melatonin药代动力学参数提供了有效实用的分析方法。 Melatonin在家兔体内分布及消除都很快 ,不会在体内蓄积

Pharmacokinetic Study of A Sleep-Promoting Agent Melatonin

The plasma concentration of melatonin in rabbits are measured by GC/MS with selected ion (m/z 173) and caffeine(m/z 194) as internal standard to determine the pharmacokinetic of melatonin. The concentrtion-time profile of melatonin is abtained after melatonin 30 mg*kg-1 administered for a two-compartment open model in rabbits. The pharmacokinetic parameters are t1/2α=0.31 h, t1/2β=8.58 h, t1/2Ka=0.34 h, Tmax=0.63±0.47 h, Cmax=322.23±255.40 ng/mL, K12=0.81 h-1, K21=2.80 h-1, K10=2.10 h-1, AUC=697.49(ng/mL)*h,CL(s)=0.097±0.054(mg/kg)/h(ng/mL). The method is stable, sensitive and accurate. It is a useful method for the determination of pharmacokinetics of melatonin which is important for clinic.