健康受试者单剂量口服头孢克洛干混悬剂的药动学及生物等效性(英文)  

Pharmacokinetics and bioequivalence of cefaclor for suspension after single dose administration in healthy volunteers

作　　者：薛洪源[1] 杨汉煜[2] 侯艳宁[1] 杨荣慧[1] 贾丽霞[1] 楚波[3] 

机构地区：[1]白求恩国际和平医院临床药理室,河北石家庄050082 [2]石药集团中奇制药技术有限公司,河北石家庄050011 [3]河北医科大学,河北石家庄050017

出　　处：《中国新药与临床杂志》2009年第11期841-845,共5页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的研究头孢克洛2种干混悬剂的药动学及生物等效性。方法采用随机交叉试验设计,20名健康男性志愿者单剂量口服2种头孢克洛干混悬剂各250mg,用液相色谱-串联质谱法测定血浆中头孢克洛的浓度,将20名受试者的经时血药浓度录入DAS(Ver1.0)程序,进行统计分析。结果单剂量口服试验与参比制剂后头孢克洛的ρmax分别为(9.0±s1.7)和(9.6±1.6)mg·L-1,tmax分别为(0.37±0.12)和(0.35±0.05)h,t1/2分别为(0.88±0.16)和(0.87±0.11)h,AUC0～5h分别为(7.9±1.0)和(7.9±1.1)mg·h·L-1,AUC0～∞分别为(8.0±1.0)和(8.0±1.1)mg·h·L-1。2种制剂的tmax、ρmax、AUC0～5h、AUC0～∞均无显著差异。试验制剂的相对生物利用度为(101±12)%。结论试验制剂与参比制剂具有生物等效性。AIM To study the pharmacokinetics and bioequivalence of two cefaclor for suspensions. METHODS A single oral administration of 250 mg test and reference of cefaclor for suspensions were given to 20 healthy male volunteers according to a randomized crossover design. The concentrations of cefaclor in plasma were determined by a HPLC-MS/MS method. The pharmacokinetic parameters were calculated and the bioequivalence were compared by DAS （Ver 1.0） program. RESULTS The pharmacokinetics parameters of test and reference preparations were as follows： pmax were （9.0 ± s 1.7） and （9.6 ± 1.6） mg·L^-1, tmax were （0.37 ± 0.12） and （0.35 ± 0.05） h, t1/2 were （0.88 ± 0.16） and （0.87 ± 0.11） h, AUC0-5h were （7.9 ± 1.0） and （7.9 ± 1.1） mg·h·L^-1, AUC0-∞ were （8.0 ±1.0） and （8.0 ± 1.1） mg·h·L^-1, respectively. There were no significant differences in tmax, pmax, AUC0-5 h, AUC0-∞, and t1/2 between the two preparations （P 〉 0.05）. The relative bioavailability of test suspensions was （101 ± 12）%. CONCLUSION The test and reference preparations were bioequivalence.

关 键 词：头孢克洛 药动学 色谱法 高压液相 光谱法 质量 电喷雾电离 生物等效性 干混悬利 

分 类 号：R978.11[医药卫生—药品] R969.1[医药卫生—药学]