el Dareer S M, Kalin J R, Tillery K F, Hill D L
J Toxicol Environ Health. 1986;19(4):491-502. doi: 10.1080/15287398609530947.
Administration to rats of oral doses of [14C]-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 [14C]HMB administered topically, either as an ethanolic solution (50, 200, or 800 micrograms/rat) or formulated in a lotion (50 micrograms/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.
给大鼠口服剂量范围为3.01 - 2570毫克/千克的[14C]-2-羟基-4-甲氧基二苯甲酮（HMB），结果显示在最高剂量时存在剂量依赖性消除过程。尿排泄（72小时内剂量的63.9 - 72.9%）是放射性消除的主要途径。静脉注射剂量（4.63毫克/千克）在大鼠体内迅速分布，并以与口服剂量相似的量（67.4%）出现在尿液中。大鼠局部给予[14C]HMB剂量时，无论是乙醇溶液（50、200或800微克/只大鼠）还是配制成洗剂（50微克/只大鼠），都能吸收大部分剂量。对于有胆管插管的大鼠，静脉注射剂量（4.46毫克/千克）的36.6%放射性在4小时内出现在胆汁中；胆汁消除的初始半衰期为40分钟。胆汁中至少存在五种放射性成分，其中没有一种是完整的HMB。两种主要成分是HMB的葡糖醛酸苷和去甲基化HMB，第三种可能是羟基化HMB的硫酸酯。尿液中有九种放射性成分，其中两种是未变化的HMB及其葡糖醛酸苷。
