STUDY ON THE RELATIVE BIOAVAILABILITY OF RACECADOTRIL DISPERSED TABLET IN HEALTHY VOLUNTEERS

[Objective]To study the pharmacokinetics and relative bioavailability of racecadotril dispersed tablet.[Methods]A single oral 400 mg dose of racecadotril was given to 24 healthy male volunteers according to a randomized cross-over design.The Thiophine,a active metabolity of racecadotril,concentration in plasma was determined by HPLC-MS/MS method.The pharmacokinetics and bioavailability of the test tablet were compared with the reference granules.[Results]The main pharmacokiletic parameters as follow:AUC0～11 were(2 132.8±439.6)h.μg.L-1,(2 384.7±615.3)h.μg.L-1,Cmax were(661.6±158.4)μg.L-1,(763.8±268.3)μg.L-1,Tmax were(1.65±0.91)h,(1.83±0.91)h.[Conclusion]Through the one two-sided test and the analysis of covariance,no significant difference between the AUC0～11,Cmax and Tmax of the two formu-lations is fount.The relative bioavailability of the test racecadotril tablet was(92.7±23.2)%of the reference granules.The two formulations are bioequivalent..