法罗培南钠片人体药动学研究

 目的研究中国健康受试者口服不同剂量法罗培南钠片的药动学。方法30名健康受试者(男性15名,女性15名)按性别随机分为3组,分别口服低、中、高(200,400,600mg)3个剂量的法罗培南钠片,于不同时间分别从受试者肘静脉取血4mL,离心分离血浆,对低浓度和高浓度样品分别处理后,高效液相色谱法测定血浆中法罗培南钠浓度。采用DASVer1.0药动学软件进行房室模型判断并计算药动学参数。结果法罗培南钠的体内经时过程符合有滞后时间的一室模型,口服低、中、高3个剂量组的t_max分别为(0.85±0.29),(0.73±0.34)和(0.88±0.29)h;ρ_max分别为(2.154±0.65),(4.425±2.403)和(8.126±2.635)mg·L^-1;AUC_0～t分别为(4.368±1.934),(9.273±7.817)和(18.431±9.167)mg·h·L^-1;t_1/2分别为(0.642±0.111),(0.769±0.217)和(0.702±0.120)h。结论健康人单剂量口服法罗培南钠片的体内药动学符合有滞后时间的一房室模型,ρ_max与AUC与服药剂量呈正相关。不同性别受试者单剂量口服法罗培南钠片后的药动学参数在男、女性受试者中无明显差异,表明男、女性受试者口服法罗培南钠片后的体内药动学过程基本相同。

Pharmacokinetics of a Single Dose Faropenem Sodium in Chinese Healthy Volunteers

OBJECTIVE To investigate the pharmacokinetics of Faropenem sodium in Chinese healthy volunteers. METHODS 30 Healthy volunteers (15 male, 15 female) were divided into three groups randomly,and were given a single oral dose (200, 400, 600 mg) of Faropenem sodium tablet.Blood samples were collected from elbow vein at certain sampling times. Faropenem in plasma was determined by HPLC method, and the pharmacokinetic parameters were calculated by DAS software.RESULTS The plasma concentration-time curves of Faropenem are fitted to an one-compartment model after an oral Faropenem sodium tablet in single dose(200, 400, 600 mg). The main pharmacokinetic parameters were as follows:t_max(0.85±0.29),(0.73±0.34) and (0.88±0.29)h;ρ_max (2.154±0.65),(4.425±2.403) and (8.126±2.635)mg·L^-1;AUC_0-t(4.368±1.934),(9.273±7.817) and (18.431±9.167) mg·h·L^-1;t_1/2(0.642±0.111),(0.769±0.217) and (0.702±0.120) h, respectively.CONCLUSION The plasma concentration-time curves of Faropenem are fitted to an one-compartment model in 30 healthy volunteers after an oral Faropenem sodium tablet in single dose (200, 400, 600 mg), and the ρ_max, AUC are increased with dose rising. There is no significant difference in the pharmacokinetic parameters between female and male.