In vivo and in vitro binding of (-)-hydroxyhexamide, a major metabolite of acetohexamide, to rabbit serum.
The in vivo and in vitro bindings of (-)-hydroxyhexamide, a major metabolite of acetohexamide, to rabbit serum were examined by using an ultrafiltration method. The in vivo serum protein binding of (-)-hydroxyhexamide was much lower than the in vitro serum protein binding. The in vitro serum protein binding of (-)-hydroxyhexamide was strongly displaced by the addition of acetohexamide. Furthermore, the in vitro serum protein binding of (-)-hydroxyhexamide in the presence of acetohexamide and (-)-hydroxyhexamide at the same concentrations as those found 1.0 h after acetohexamide administration was approximately similar to the in vivo serum protein binding of (-)-hydroxyhexamide. These results lead us to conclude that acetohexamide, the parent drug of (-)-hydroxyhexamide, plays an important role in the in vivo serum protein binding of (-)-hydroxyhexamide.
Imamura
Y
Y
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Abe
H
H
Kojima
Y
Y
Otagiri
M
M
D000092:Acetohexamide / Q000031:analogs & derivatives* / Q000097:blood / Q000302:isolation & purification / Q000378:metabolism* / Q000493:pharmacokinetics; D000818:Animals; D001667:Binding, Competitive; D001798:Blood Proteins / Q000378:metabolism*; D066298:In Vitro Techniques; D008297:Male; D011485:Protein Binding; D011817:Rabbits; D000096926:Benzenesulfonamides
D000092:Acetohexamide; D001798:Blood Proteins; C020362:hydroxyhexamide; D000096926:Benzenesulfonamides