LC/MS/MS法测定法罗培南血尿药浓度及药动学研究

目的研究法罗培南钠片在健康人体内的药动学及饮食对药动学的影响。方法药动学试验：采用低、中、高三个剂量组的平行试验设计；饮食对人体药动学的影响试验：采用自身对照的双周期交叉试验设计。血浆样品处理后采用LC／MS／MS测定血药浓度。结果空腹po100、200、400mg法罗培南片，主要药动学参数AUC和Cmax随剂量呈线性相关。进餐后影响药物的Tmax和Cmax，其他药动学参数无变化。给予法罗培南在100、200、400mg的剂量，受试者尿中0～24h原形药物的平均累积排泄率分别为4．52％、7．73％和3．28％。结论LC／MS／MS方法操作简单，结果准确，专属性强，灵敏度高，适用于法罗培南人体药动学研究。

Determination of Faropenem in Human Plasma and Urine by LC/MS/MS and Study of Pharmacokinetics

AimTo study the endosomatic pharmacokinetics of faropenem tablets in healthy adults and assess the effect of food on pharmacokinetics. Methods The single dose study was a parallel design with three groups receiving different doses. The study of food effect on pharmacokinetics was conducted according to an open, randomized, 2 - period crossover design. The blood samples were determined by LC/MS/MS after pretreatment. Results Linear pharmacokinetics of faropenem in healthy Chinese volunteers was observed when administered of 100 - 400mg faropenem. Food affects Tmax and Cmax of faropenem but there are no significant differences between other pharmacoki netic parameters. The average cumulative excretory rates of original drug were 4.52%,7.73% and 3.28% respectively from Oh to 24h under the administration of 100 mg,200 mg and 400 mg. Conclusion The reliable, simple and sensitive LC/MS/MS method was ideal for evaluating the pharmacokinetics of faropenem.