国产格列齐特片(Ⅱ)在健康人体内的药动学研究

Pharmacokinetics of domestic and imported gliclazide tablets(Ⅱ) in healthy volunteers

目的 :研究国产格列齐特片 (Ⅱ )和进口片的药动学。方法 :10名健康男性受试者单剂量随机交叉口服格列齐特片(Ⅱ )受试制剂或参比制剂各 80mg ,采用HPLC法测定血药浓度 ,用 3P87程序对试验数据进行处理。结果 :受试制剂和参比制剂主要药动学参数 :cmax分别为 (5 .78± 1.90 ) ,(5 .93± 1.18)mg·L-1;tmax分别为 (5 .12± 1.6 0 ) ,(5 .2 2± 1.14 )h ;T1/ 2 分别为(11.19± 2 .6 7) ,(10 .94± 2 .6 3)h ;Ka分别为 (1.17± 0 .4 4 ) ,(1.18± 0 .4 3)h-1;Ke分别为 (0 .0 6 5 1± 0 .0 15 ) ,(0 .0 6 70± 0 .0 17)h-1;AUC0→∞ 分别为 (10 0 .85± 16 .87) ,(97.87± 17.81)mg·h·L-1;受试制剂的相对生物利用度为 (10 4 .5 1± 18.86 ) %。AUC经对数转换后的双单侧t检验结果表明无显著差别。结论

AIM:To study the pharmacokinetics of domestic and imported gliclazide tablets(Ⅱ). METHODS:Ten healthy male volunteers were treated with a single does of 80 mg trial tablets and contrast tablets in cross over order,then their serum drug levels were determined by HPLC and data obtained were analyzed by 3P87 program. RESULTS:The pharmacokinetic parameters for trial and contrast tablets were as follows: c max ( 5.78±1.90) mg·L -1 and (5.93±1.18)mg·L -1; t max(5.12±1.60) h and (5.22±1.14) h;T 1/2(11.19±2.67) h and (10.94±2.63) h;Ka( 1.17±0.44) h -1 and (1.18±0.43) h -1;Ke(0.065 1±0.015) h -1 and (0.067 0±0.017) h -1; AUC 0→∞( 100.85± 16.87)mg·h·L -1 and ( 97.87 ±17.81)mg·h·L -1. The relative bioavailability of domestic tablets was(104.51± 18.86)%. CONCLUSION:The trial and contrast gliclazide tablets(Ⅱ) are bioequivalent.