Bioequivalence of metformin/vigagliptin fixed-dose combination tablets in Chinese healthy volunteers
Objective:To evaluate the bioequivalence of metformin/vigagliptin fixed-dose combination tablets under fasting and fed conditions in Chinese healthy volunteers.Methods:A randomized,open,double-cycle,double-crossover design was adopted.Twenty-four volunteers were randomly divided into two groups to participate in fasting or fed trial and received a single dose of test tablets or reference tablets,respectively.The plasma concen-trations of metformin and vigagliptin were detected by LC-MS/MS.The pharmacokinetic parameters were calculated and the bioequivalence was evaluated with Phoenix WinNonlin 8.0 software.Results:The pharmacokinetic parameters of the test formulation and reference formulation under fasting condition were as follows:metformin:Cmax(2 439.6±375.82)and(2 429.2±443.76)ng·mL-1,AUC0-t(16 432.84±3 131.070)and(16 112.18±3 043.149)ng·h·mL-1,AUC0-∞(16651.43±3 128.196)and(16 329.73±3 032.013)ng·h·mL-1,respectively;vigagliptin:Cmax(293.8±53.60)and(284.3±57.90)ng·mL-1,AUC0-t(1309.60±255.478)and(1 258.79±273.810)ng·h·mL-1,AUC0-∞(1 329.82±259.085)and(1 277.78±281.023)ng·h·mL-1,respectively.The pharmacokinetic parameters of the test formulation and reference formulation under fed condition were as follows:metformin:Cmax(1502.5±298.17)and(1 432.1±318.79)ng·mL-1,AUC0-t(12 461.28±2 353.450)and(12 326.72±2 582.538)ng·h·mL-1,AUC0-∞(12 672.87±2 349.686)and(12 562.70±2 546.608)ng·h·mL-1,respectively;vigagliptin:Cmax(235.5±57.99)and(224.8±62.42)ng·mL-1,AUC0-t(1 101.25±193.069)and(1 034.83±187.020)ng·h·mL-1,AUC0-∞(1 132.03±203.630)and(1 066.49±191.585)ng·h·mL-1,respectively.The 90%confidence intervals for the geometric mean ratio(T/R)of Cmax,AUC0-t,AUC0-∞ under fasting and fed conditions were within the bioequivalence acceptance range of 80.00%～125.00%.Conclusion:The test formulation was bioequivalent to the reference in Chinese healthy volunteers under fasting and fed conditions.Both formulations were safe and well tolerated.
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