ABSTRACT
OBJECTIVE:To compare benproperine sustained-release tablet(BP)with cofrel tablet(CF)in respect to the bioequivalence,release characteristics and correlation between in vitro dissolubility and in vivo absorption METHODS:A HPLC method was used to determine the serum benproperine concentration after single and multiple oral administration of 80mg BP and CF in a two-period cross-over test RESULTS:The T1/2(?),Tpeak,Cmax,AUC0～36,AUC0～∞ of BP after single and multiple oral administration were (11 99?1 15)h and (11 91?1 41)h,(3 80?0 42)h and (2 25?0 26)h,(0 2 787?0 03)?g/ml and (0 4 507?0 07)?g/ml,(4 1 445?0 48)?g/(ml?h)and (3 8 981?0 54)?g/(ml?h),(4 7 908?0 42)?g/(ml?h) and (4 3 278?0 55)?g/(ml?h),and those of CF were (11 68?1 24)h and (10 83?1 01)h,(3 10?0 26)h and (1 95?0 16)h,(0 4 737?0 32)?g/ml and (0 6 163?0 42)?g/ml,(9 3 954?0 80)?g/(ml?h) and (8 5 223?0 76)?g/(ml?h),(10 1 336?0 87)?g/(ml?h) and (8 8 821?0 77)?g/(ml?h),respectively The relative bioavailability of BP versus CF was(112 40?0 06)% CONCLUSION:The results show that the benproperine sustained-release tablet and cofrel are bioequivalent