盐酸万乃洛韦人血浆浓度的HPLC-荧光法测定及其药物动力学

Determination and Pharmacokinetics of Valaciclovir Hydrochloride in Human Plasma by HPLC with Fluorescence Detection

建立了盐酸万乃洛韦 (1)体内活性代谢物阿昔洛韦 (2 )浓度的蛋白沉淀 -荧光检测 HPL C法。采用 Genesis C1 8柱 (10 0× 3mm ,3μm ) ,流动相为 0 .1m ol/ L磷酸 (0 .6 m l/ m in,恒流速 )和乙腈 (0 .0 0 5～ 0 .1m l/ m in,变速 ) ;柱温35°C;荧光激发波长 2 85 nm,发射波长 370 nm。最低检测浓度 10 ng/ ml,最低定量浓度 (L OQ) 2 0 ng/ m l,2 0～ 15 0 0ng/ m l浓度范围线性良好。 8名志愿者口服 30 0 m g 1片后 ,t1 /2 为 3.19± 0 .36 h,AUC为 95 73.37± 16 40 .0 9h· ng· m l- 1 ,Cmax为 2 5 87.0 4± 710 .16 ng/ ml,Tmax为 1.2 5± 0 .46

A highly sensitive and selective HPLC method for the determination of aciclovir (2), active metabolite of valaciclovir hydrochloride (1) in human plasma was established. The method involved HPLC with fluorescence detection, using salbutamol as the internal standard. The mobile phase consisted of 0.1 mol/L phosphoric acid (with flow rate 0.6 ml/min) and acetonitrile (with flow rate 0.005~ 0.1 ml/min). The analysis column was C 18(Genesis, 100×3 mm,3 μm) and set at 35°C. The fluorescence detection excitation wavelength and emission wavelength were set at 285 nm and 370 nm, respectively. The lim-it of quantification was 20.0 ng/ml. The linear range of 2 was 20~1500 ng/ml. Eight volunteers orally taken 300 mg of 1 tablet, the pharmacokinetics parameters were t 1/2 3.19±0.36 h, AUC 9573.37±1640.09 h·ng·ml -1, C max 2587.04±710.16 ng/ml, T max 1.25±0.46 h.