氯雷他定片人体生物利用度研究

Bioavailability of loratadine tablet in healthy subjects

目的:研究氯雷他定片在正常人体内药代动力学与相对生物利用度。方法:利用HPLC法测定20名志愿受试者随机交叉口服单剂量重庆或上海氯雷他定片(LORAL或LORAS)20mg后的血药浓度,用3p97软件包计算两者的药代动力学参数与相对生物利用度。结果:测试药物与对照药的药鄄时曲线均符合口服吸收一室模型。Tmax分别为(0.99±0.48)h和(0.95±0.54)h;Cmax分别为(13.11±9.15)ng/ml和(12.18±7.04)ng/ml;AUC0鄄T分别为(30.21±17.69)ng·h/ml与(30.96±18.27)ng·h/ml;t1/2Ke分别为(1.66±0.63)h和(1.64±0.54)h;经配对t检验,两制剂药代动力学参数无显著性差异(P>0.05)。结论:重庆氯雷他定片相对于上海片剂的生物利用度为97.58﹪,经方差分析、双单测t检验及1鄄2α置信区间法统计分析,两种片剂具有生物等效性。

Objective: To study the relative bioavailability and pharmacokinetics of loratadine tablet in healthy subjects. Methods: A single oral dose of 20 mg of loratadine tablet made in Chongqing or Shanghai (LORAL or LORAS) was given to 20 healthy volunteers in a randomized crossover study. Drug concentrations in plasma were determined by HPLC. The pharmacokinetics parameter were calculated with 3p97 pharmacokinetic program and the bioequivalency was evaluated. Results: The results showed that the plasma concentration-time curve of the two preparations were all fitted to a one-compartment model. The peak plasma levels (Cmax) of LORAL or LORAS were (13.11±9.15)ng/ml or (12.18±7.04)ng/ml; the peak time (Tmax) were (0.99±0.48)h or (0.95±0.54)h; AUC0-T were (30.21±17.69)ng·h/ml or (30.96±18.27)ng·h/ml, respectively. The relative bioavailability of LORAL was 97.58%. Conclusion: The result of two one-sided tests suggest that the LORAL is bioequivalence with the LORAS.