Disposition of 2‐hydroxy‐4‐methoxybenzophenone in rats dosed orally, intravenously, or topically

Abstract

Administration to rats of oral doses of [ ¹⁴ C]‐2‐hydroxy‐4‐methoxybenzophenone (HMB) in the range of 3.01–2570 mg/kg revealed that a dose‐dependent elimination process was operative at the highest dose. Urinary excretion (63.9–72.9% of the dose in 72 h) was the major route for elimination of radioactivity. An intravenous dose (4.63 mg/kg) distributed rapidly throughout the body of rats and appeared in the urine in an amount (67.4%) similar to those for the oral doses. Rats absorbed large portions of doses of [ ¹⁴ C]HMB administered topically, either as an ethanolic solution (50, 200, or 800 μg/rat) or formulated in a lotion (50 μg/rat). For rats with biliary cannulas, 36.6% of the radioactivity of an intravenous dose (4.46 mg/kg) appeared in the bile in 4 h; the initial half‐life for biliary elimination was 40 min. In the bile, at least five radioactive components, none of which was intact HMB, were present. The two major components were glucuronides of HMB and demethylated HMB, and a third was probably a sulfate ester of hydroxylated HMB. In urine, there were nine radioactive components, two of which were unchanged HMB and its glucuronide.