Study on the bioequivalence of gliclazide sustained released tablet in healthy volunteers / 中国药理学通报

ABSTRACT

Aim To evaluate the bioequivalence of two preparations of gliclazide in healthy volunteers.Methods The concentration of gliclazide was measured by high performance liquid chromatography(HPLC) after a single or multiple dosage of gliclazide sustained released tablet in healthy volunteers.The pharmacokinetic parameters of the two preparations were calculated by 3P97 program.LnAUC0~∞,lnAUC0~72 and lnAUC0~? were used to evaluate the bioequivalence of the two preparations with analysis of variance and two one-side t-test.Results Both the gliclazide extended action tablet were best fitted to one-compartment model.The main parameters of the tested and reference gliclazide after a single dose were as followsCmax(2.07?0.61) and(2.26?0.61)mg?L-1;Tmax(5.10?0.55)h and(5.05?0.51)h;T12Ka(1.50?0.26)h and(1.52?0.27)h;T12Ke(8.89?1.56)h and(8.68?1.72)h;MRT(22.63?1.01)h and(22.38?0.93)h;AUC0~72(39.19?8.03)mg?h-1?L-1 and(39.26?8.37)mg?h-1?L-1;AUC0~∞(45.80?9.51)mg?h-1?L-1 and(45.57?9.76)mg?h-1?L-1;F0~72 and F0~∞(100.19?6.22)% and(100.85?5.88)%,respectively.The main parameters of the tested and reference gliclazide after multiple dose were as followsCmax(4.83?0.86)mg?L-1 and(4.69?0.64)mg?L-1;Cmin(0.68?0.14) mg?L-1 and(0.66?0.12)mg?L-1;Tmax(4.10?0.45) h and(4.10?0.55)h;T12Ka(2.03?0.53)h and(2.04?0.40)h;T12Ke(7.24?0.87)h and(7.09?1.14)h;MRT(9.17?0.30)h and(9.19?0.37)h;AUCSS(41.62?6.48) mg?h-1?L-1 and(42.18?6.03)mg?h-1?L-1;Cav(1.73?0.27)mg?L-1 and(1.76?0.25)mg?L-1;DF(240.85%?34.07)and(230.23%?24.80%) respectively.The relative bioavailability was(98.60?4.60)%.The AUC0~T,AUC0~∞ or AUCSS,Cmax and Tmax were bioequivalent between the two preparations.Conclusion The tested and reference gliclazide sustained released tablet are bioequivalent.