H. Emori et al., EFFECT OF DISSOLUTION RATE AND FOOD ON ORAL BIOAVAILABILITY OF BROPIRIMINE TABLETS IN DOGS, Drug development and industrial pharmacy, 22(9-10), 1996, pp. 1041-1046
Three different tablet formulations of bropirimine were evaluated in a
n in vitro dissolution study. Further, the effect of dissolution rate
of bropirimine and food on the bioavailability after oral administrati
on of the tablets was investigated in dogs. A tablet formulation with
lower bropirimine content percent and smaller tablet size showed faste
r in vitro dissolution rate due to the larger tablet surface area per
unit mass of bropirimine and the higher ratio of hydrophilic excipient
s in a tablet. In the fasted state, the bioavailability of bropirimine
after oral administration of tablets tended to reflect the in vitro d
issolution characteristics. The bioavailability after administration o
f tablets with slow in vitro dissolution rate was increased by food in
take due to the in vivo dissolution increased in the fed state, while
the postprandial effect on the bioavailability of tablets with fast in
vitro dissolution rate was not clearly observed. In the fed state, th
ere were no differences in the plasma concentration profile and pharma
cokinetic parameters of bropirimine between the tablets with a slow an
d a fast in vitro dissolution rate. This suggests that the postprandia
l administration of bropirimine tablets may maximize the bioavailabili
ty without distinction of the in vitro dissolution rate.