G. Shu
2009
Citations
0
Influential Citations
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Citations
Quality indicators
Journal
Anhui Medical and Pharmaceutical Journal
Abstract
Aim To investigate the pharmacokinetics of mitiglinide calcium tablets with a single and multi-dose p.o.administration in Chinese healthy volunteers.Methods 40 healthy volunteers were randomly divided into four groups with 5 male and 5 females in each group.The volunteers in three groups were administrated with single dose of mitiglinide calcium tablets 5,10,20 mg.respectively.The last group was administrated with the dose of mitiglinide calcuim tablets 10 mg,tid,till the seventh day.Blood samples were collected according to the protocol and plasma concentration of mitiglinide were measured by validated LC-MS/MS.DAS2.0 software was performed for calculating pharmacokinetic parameters.Results The main pharmacokinetics parameters of mitiglinide in volunteers who were administrated with a single dose of 5,10,20 mg were as follows:tmax(0.27±0.10),(0.39±0.39)and(0.34±0.16)h;Cmax(697.11±168.83),(1293.56±293.59)and(1716.43±276.29)μg·h-1·L-1;t1/2β(2.44±2.32),(1.32±0.45)and(2.38±2.22)h;AUC0-t(797.8±149.0),(1545.1±240.5)and(2474.7±624.6)μg·h-1·L-1,respectively.The main pharmacokinetics parameters of mitiglinide after multi-dose(10 mg)administration were as follows:tmax(0.27±0.07),Cmax(1149.99±297.61)μg·h-1·L-1,t1/2β(1.40±0.33)h,AUC0-t(1236.8±327.6)μg·h-1·L-1,Cmin(5.68±2.32)μg·h-1·L-1,AUCss(1236.78±327.64)μg·h-1·L-1,Cav(154.60±40.96)μg·h-1·L-1,DF(7.45±0.68),R(0.93±0.30).Conclusion After administration of mult-dose mitiglinide calium tablets(10 mg tid p.o.),plasma concentrations of mitiglinide have been in steady state till fourth day and have no obvious accumulation in vivo.Increase of mitiglinide calcium tablets dosage(5~20 mg)is positively calculated with increase of Cmax and AUC0-t and simultaneously with no significant difference of physiological disposition between the male and female.