尼索地平片在健康人体的药动学

Pharmacokinetics of nisoldipine in healthy volunteers

目的 :研究 10例健康男性单剂量口服尼索地平片 2 0mg的药动学。方法 :用HPLC测定尼索地平血药浓度 ,采用 3P87药动学程序对血药浓度 时间数据进行线性拟合 ,计算药动学参数。色谱柱为C18柱 ( 2 5 0mm× 4 6mm ,10 μm) ,流动相 :甲醇 水 磷酸 ( 70∶3 0∶1,V/V) ,检测波长为 2 3 6nm。结果 :本实验建立的HPLC线性关系、回收率、日内及日间RSD均能满足药动学研究的要求 ,口服尼索地平后血药浓度 时间数据符合二室模型 ,主要的药动学参数tmax为 ( 0 9± 0 2 )h ,cmax为 ( 8 0± 3 0 )ng·mL-1,T1/ 2 为 ( 9 5± 3 4)h ,AUC0→t为 ( 60 2± 3 0 8)ng·h·mL-1。结论

AIM: To study its pharmacokinetics in 10 healthy volunteers after an oral administration of 20 mg nisoldipine. METHODS: The concentration of nisoldipine in serum were measured by HPLC. The pharmacokinetic parameters were fitted by 3P87. The C 18 column (250 mm×4.6 mm, 10 μm) was used. The mobile phase consisted of a mixture of methanol -H 2O-phosph=(70∶30∶1, V/V) and the wavelength of UV detector was 236 nm. RESULTS: The RSD of intra-day and inter-day were less than 10%. The serum concentration-time curves fitted the two-compartment model. The main parameters were as follows: t max=(0.9±0.2) h, c max=(8.0±3.0) ng·mL -1, T 1/2=(9.5±3.4) h. AUC 0→t=(60.2±30.8) ng·h·mL -1. CONCLUSION: The variation of the pharmacokinetic parameters of nisodipine is large for individuals. Being a basic drug for hypertension, nisodipine should be monitored for its safety and effectiveness. Our method is practical for popular use.