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目的评价格列齐特缓释片试验制剂和市售参比制剂的人体生物等效性。方法采用高效液相色谱-质谱联用技术,以内标法测定20名男性健康受试者单次和多次交叉给予格列齐特缓释片后的血药浓度经时过程,估算药代动力学参数。结果口服格列齐特缓释试验片(30mg)和参比片(30mg)后,受试及参比制剂中药物主要药代动力学参数如下:单次给药时达峰浓度(Cmax)分别为1.21±0.26μg/ml和1.09±0.24μg/ml,达峰时间(Tmax)分别为7.4±1.8h和7.0±1.6h,消除半衰期t1/2(Kel)分别为14.82±4.10h和13.57±4.16h,AUC0～72分别为26.23±8.65μg·h·ml-1和25.88±8.87μg·h·ml-1,AUC0～∞分别为27.65±9.80μg·h·ml-1和27.12±9.90μg·h·ml-1;多次给药时Cmax分别为1.37±0.49μg/ml和1.31±0.41μg/ml;谷浓度(Cmin)分别为0.069±0.075μg/ml和0.060±0.066μg/ml;平均稳态血药浓度(Cav)分别为0.41±0.20μg/ml和0.42±0.19μg/ml;Tmax分别为6.0±1.7h和6.6±2.6h;波动系数(DF)分别为3.46±0.99和3.29±1.06;稳态药时曲线下面积(AUCss)别为29.66±14.10μg·h·ml-1和29.95±13.40μg·h·ml-1。AUC和AUCss经对数转换后方差分析检验,差异无统计学意义。结论试验制剂和参比制剂生物等效。
OBJECTIVE To evaluate the bioequivalence of human glicachet sustained-release tablets and commercially available reference preparations. Methods The pharmacokinetic parameters of 20 male healthy subjects were determined by internal standard method after single or multiple crossover administration of gliclazide sustained-release tablets Learning parameters. Results The main pharmacokinetic parameters of the drugs in the test and reference preparations after oral administration of Glicachet (30 mg) and reference tablets (30 mg) were as follows: Cmax (Tmax) were 1.21 ± 0.26μg / ml and 1.09 ± 0.24μg / ml respectively, the peak time (Tmax) were 7.4 ± 1.8h and 7.0 ± 1.6h, and the elimination half-life t1 / 2 was 14.82 ± 4.10h and 13.57 ± 4.16h, AUC0 ~ 72 were 26.23 ± 8.65μg · h · ml-1 and 25.88 ± 8.87μg · h · ml-1, AUC0 ~ ∞ were 27.65 ± 9.80μg · h · ml-1 and 27.12 ± 9.90μg · H · ml-1; Cmax were 1.37 ± 0.49μg / ml and 1.31 ± 0.41μg / ml for multiple administrations; Cmax were 0.069 ± 0.075μg / ml and 0.060 ± 0.066μg / ml respectively; The mean steady-state plasma concentrations (Cav) were 0.41 ± 0.20 μg / ml and 0.42 ± 0.19 μg / ml respectively; the Tmax were 6.0 ± 1.7 h and 6.6 ± 2.6 h, respectively; the coefficient of variation (DF) were 3.46 ± 0.99 and 3.29 ± 1.06. The area under the curve of steady state drug (AUCss) was 29.66 ± 14.10μg · h · ml-1 and 29.95 ± 13.40μg · h · ml-1, respectively. AUC and AUCss logarithmic conversion analysis of variance, the difference was not statistically significant. Conclusions The test and reference formulations are bioequivalent.