两种扑热息痛薄膜包衣异型片的药代动力学比较及生物利用度初步研究

目的 研究单剂量口服两种扑热息痛异型片500mg的药代动力学和相对生物利用度。方法 10名男性健康志愿者按照随机、交叉试验设计,采集服药后0.5,1,1.5,2,3,4,6,8,10h的血样本。用HPLC方法测定扑热息痛的血药浓度。结果 两种制剂的药-时曲线符合口服吸收有滞后时间的一级动力学一室模型。受试制剂扑热息痛薄膜包衣异型片(康司达)的主要药代动力学参数:C_max=5.51±1.24mg/L,T_peak=1.03±0.43h,T_1/2ka=0.27±0.16h,T_1/2ke=2.60±0.51h,AUC_0~t=23.69±4.08mg/h·L^-1,MRT=3.65±0.22h。结论 受试制剂相对于参比制剂的生物利用度为102.5±13.3%,受试制剂(康司达)与参比制剂扑热息痛片生物等效。

Evaluation of bioavailability and pharmacokinetics of film-coating special shaped tablet of acetaminophen in health volunteers

Aim The pharmaco kinetics and relative bioavailability of domestic film-coating special shaped tablet of acetaminophen were studied.Methods A single oral dose of 500 mg of the two formations (test and reference preparation)was given to 10 healthy male volunteers according to randomized 2-w ay cross-over design,blood sample was with drawn 10 hours after administ ration,and plasma concent rations of acetaminophen were assayed by a high performance liquid chromtography (HPLC)method.Results The concentration-time curves of the two preparations fitted to a one-compartment model with first order absorption and lag time.The main pharmacokinetic parameters of the tested preparation were as follows:C_max=5.51±1.24 mg/L,T_peak=1.03±0.43h,T_{1/2k a}=0.27±0.16h,T_1/2ke =2.60±0.51h,AUC_0~t =23.69±4.08 mg·h·L^-1,MRT=3.65±0.22 h.Conclusion The relative bioavailability of the test preparation is 102.5±13.3% to the reference preparation.The bioavailabity of the two kinds of acetaminophen is equal,showing that the two kinds of preparations are bioequivalent preparations.