BILIARY EXCRETION AND ENTEROHEPATIC RECIRCULATION OF METHAQUALONE IN THE RAT

Autor: POLK, ANDREW, DELONG, ALLYN F., SMYTH, ROBERT D., HERCZEG, TIHAMER, BURNS, BERNARD J., KLUNK, LEWIS J., REAVEY-CANTWELL, NELSON H.
Zdroj: Drug Metabolism and Disposition; July 1974, Vol. 2 Issue: 4 p365-369, 5p
Abstrakt: Biliary excretion of methaqualone metabolites was demonstrated after oral administration of 2-14C-methaqualone to bile-cannulated rats. Over 5- and 24-hr collection periods, 29 and 77% of the 14C-methaqualone dose appeared in the bile, respectively. Enterohepatic recirculation of the bile metabolites was demonstrated after intraduodenal administration of the bile-derived metabolites to bile-cannulated rats; 18 and 52% of the 14C metabolite dose appeared in the bile at the 5- and 24-hr collection periods. After the intraduodenal administration of the bile-derived metabolites to noncannulated rats, 21 and 37% appeared in the urine at the 24- and 72-hr collection periods. Elucidation of the structure of the biliary metabolites showed that 95% appeared as the O-glucuronide conjugate of 2-methyl-3-(2'-hydroxymethylphenyl)-4(3H)-quinazolinone metabolite and the remaining 5% consisted of two unidentified metabolites.
Databáze: Supplemental Index