Pharmacokinetics and relative bioavailability of gliclazide sustained-release tablet in healthy volunteers

Objective: To establish a LC/MS/MS method for determination of gliclazide in human plasma,and to investigate pharmacokinetics and relative bioavailability of gliclazide sustained-release tablet in healthy male volunteers.Methods: In 18 healthy volunteers,single and multiple oral doses of gliclazide sustained-release tablet were administrated in a randomized cross-over design.Plasma concentration of glaclizide was determined by LC/MS/MS method,and pharmacokinetics and relative bioavailability were evaluated.Results: Main pharmacokinetic parameters for single dose were as follows: the values of Tmax were(6.44±1.42) and(6.44±1.15)h;Cmax were(730±136) and(735±155)ng·mL-1;t1/2 were(15.4±4.48) and(14.5±1.91)h;Cl were(2.12±0.60) and(2.11±0.70) L·h-1;Vd were(45.0±10.2) and(44.5±15.4) L for the test and reference drugs,respectively.Main pharmacokinetic parameters for multiple doses were as follows: the values of Tmax were(6.11±0.83) and(6.06±0.73) h;Cmax were(1354±420) and(1324±430) ng·mL-1;Cmin were(244±63.2) and(254±59.6) ng·mL-1;Cav were(496±182) and(505±218) ng·mL-1,respectively.Conclusion: The relative bioavailability of the test drug for single dose and multiple doses are(98.3±14.3)% and(99.8±8.4)%,respectively.The test and reference tablets of gliclazide are bioequivalent.