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目的:研究格列齐特缓释片的药动学及相对生物利用度,验证国产与进口格列齐特缓释片的生物等效性。方法:采用拉丁方试验设计,研究受试者在空腹条件下分别单剂量和多剂量口服格列齐特缓释片后,采用高效液相色谱法测定人血浆中格列齐特的浓度,计算其药动学参数和相对生物利用度,评价2制剂的生物等效性。结果:单剂量口服格列齐特缓释片受试制剂(国产)和参比制剂(进口)的主要药动学参数分别为:tma(x6.71±1.43)、(7.38±1.50)h,Cma(x0.813±0.178)、(0.782±0.129)μg.mL-1,AUC0～7(221.29±5.86)、(21.09±5.34)μg.h.mL-1,AUC0～∞(23.19±7.49)、(23.15±5.64)μg.h.mL-1,t1/2k(e18.79±5.24)、(20.03±5.67)h;多剂量口服格列齐特缓释片达稳态后2制剂主要药动学参数分别为:AUCs(s27.85±9.77)、(27.63±10.84)μg.h.mL-1,Cssmax(1.892±0.503)、(1.829±0.521)μg.mL-1,tssma(x5.33±1.24)、(6.13±1.42)h,Cssmi(n0.771±0.379)、(0.830±0.478)μg.mL-1,血药浓度波动度DF(103.8±40.0)%、(97.6±52.9)%。结论:2制剂具有生物等效性。
Objective: To study the pharmacokinetics and relative bioavailability of gliclazide sustained-release tablets and to verify the bioequivalence of domestic and imported gliclazide sustained-release tablets. Methods: The Latin square design was used to determine the concentration of gliclazide in human plasma after single and multiple doses of oral gliclazide sustained-release tablets under fasting conditions. The concentrations of gliclazide in human plasma were determined by HPLC Its pharmacokinetic parameters and relative bioavailability, to evaluate the bioequivalence of 2 preparations. Results: The main pharmacokinetic parameters of the single-dose oral gliclazide-treated tablets (domestic) and reference preparations (imported) were tma (x6.71 ± 1.43) and (7.38 ± 1.50) h, AUC0 ~ ∞ (23.19 ± 7.49) were significantly higher in Cma (x0.813 ± 0.178), (0.782 ± 0.129) μg.mL-1, AUC0 ~ 7 (221.29 ± 5.86), (21.09 ± 5.34) μg.h.mL- , (23.15 ± 5.64) μg.h.mL-1, t1 / 2k (e18.79 ± 5.24) and (20.03 ± 5.67) h, respectively. The multi-dose oral gliclazide sustained- The kinetic parameters were: AUCs (s27.85 ± 9.77), (27.63 ± 10.84) μg.h.mL-1, Cssmax (1.892 ± 0.503), (1.829 ± 0.521) μg.mL- (103.8 ± 40.0)%, (97.6 ± 52.9)%, respectively. The mean arterial blood concentration of the two groups were 33 ± 1.24, 6.13 ± 1.42 h, Cssmi n0.771 ± 0.379 and 0.830 ± 0.478 μg.mL- %. Conclusion: 2 formulations have bioequivalence.