摘要
目的:研究辛伐他汀咀嚼片在20名健康志愿者体内的药动学特征及相对生物利用度。方法:20名健康男性志愿者采用随机交叉给药方案,分别单剂量口服的40mg辛伐他汀咀嚼片和参比片,采用液-液相萃取后、HPLC-ESI-MS分析方法对血药浓度进行测定,计算两者的药代动力学参数及相对生物利用度。结果:试验片和参比片的血药浓度水平一致。其主要药代动力学参数t1/2分别为3.46±0.61和3.53±0.85h;tmax分别为1.2±0.5h和1.4±0.6h,Cmax分别为7.03±3.33μg·L-1和7.04±3.78μg·L-1,AUC0-14分别为23.22±9.96μg·h·L-1和23.57±9.41μg·h·L-1,两制剂的药代动力学参数相近。用面积估算的辛伐他汀咀嚼片的相对生物利用度F0-14为97.9%±11.1%,F0-∞为97.6%±11.4%。结论:辛伐他汀咀嚼片和参比片的AUC、Cmax经方差分析和双单侧t-检验表明:两制剂生物等效;tmax经非参数法检验,表明两种制剂无显著性差别(>0.05)。
OBJECTIVE:To study the pharmacokinetics and relative bioavailability of simvastatin in 20 healthy volunteers. METHODS:A single oral dose 40mg simvastatin of reference or test drugs was given to each volunteer according to an open randomized crossover study. The concentrations in plasma were determined by HPLC-ESI-MS method after liquid-liquid extraction methods. RESULT:The main pharmacokinetics parameters of simvastatin were as follows:t1/2 were 3.46±0.61 and 3.53 ± 0.85h, tmax were 1.2 ± 0.5h and 1.4 ± 0.6h,C were 7.03 ± 3.33 μ g·L-1 and 7.04 ± 3.78μ g·L-1, AUC0-14 were 23.22 ?9.96 μg·h-L-1 and 23.57 ±9.41 μ g·h·L-1for test and reference tablet respectively. The relative bioavailability of F0-14 and F0-∞ were 97.9% ± 11.1% and 97.6% ± 11.4% respectively. CONCLUSION:The result of statistical analysis showed that two formulations were bioequivalent.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2002年第6期441-444,共4页
The Chinese Journal of Clinical Pharmacology