氯雷他定片的人体相对生物利用度

Relative bioavailability of loratadine tablets in healthy volunteers

目的 :研究氯雷他定片在健康人体内的相对生物利用度。方法 :18名健康男性志愿者按随机交叉试验设计口服单剂量受试制剂和参比制剂 4 0mg ,用高效液相色谱 质谱 (HPLC MS)法测定血药浓度 ,NDST程序作统计学处理。结果 :受试制剂和参比制剂在血浆中的cmax分别为 (5 1 0 5± 2 3 16 ) ,(4 7 5 5± 2 0 2 2 ) μg·L-1;tmax分别为 (1 35± 0 35 ) ,(1 4 4± 0 5 3)h ;T1/ 2 分别为(13 16± 5 2 0 ) ,(13 2 5± 4 0 8)h ;AUC0→ 3 6h分别为 (135 2 7± 6 2 82 ) ,(130 5 9± 5 5 5 8) μg·h·L-1。主要药动学参数AUC0→ 3 6h,tmax,cmax经方差分析均无显著性差异。以AUC0→ 3 6h计算 ,受试制剂的相对生物利用度为 (10 3 5± 2 4 7) %。结论

AIM:To study the relative bioavailability of loratadine tablets in healthy volunteers. METHODS:Eighteen healthy male volunteers administered a single oral dose of 40 mg tested and reference tablets according to a random cross-over design. The concentrations of loratadine in plasma were determined by HPLC-MS and the pharmacokinetic parameters were analysed by NDST program. RESULTS:For tested and reference tablets,c max were (51.05±23.16) and (47.55±20.22) μg·L -1;t max were (1.35±0.35) and (1.44±0.53)h;T 1/2 were (13.16±5.20) and (13.25±4.08)h;AUC 0→36h were (135.27±62.82) and (130.59±55.58)μg·h·L -1,respectively. The main pharmacokinetic parameters AUC 0→36h,t max and c max had no significant difference between 2 preparations by variance analysis. Calculated on AUC 0→36h,the relative bioavailability of tested tablets was (103.5±24.7)%. CONCLUSION:The 2 preparations are bioequivalent.