Okereke C S, Kadry A M, Abdel-Rahman M S, Davis R A, Friedman M A
Department of Pharmacology/Toxicology, New Jersey Medical School.
Drug Metab Dispos. 1993 Sep-Oct;21(5):788-91.
Benzophenone-3 [2-hydroxy-4-methoxybenzophenone (HMB), oxybenzone, Spectra-Sorb UV-9 light absorber] is used in many cosmetics and sunscreens as a UV absorber. This study was conducted to investigate the metabolism of HMB (100 mg/kg body weight administered orally). 2,4-Dihydroxybenzophenone (DHB), 2,2'-dihydroxy-4-methoxybenzophenone (DHMB), and 2,3,4-trihydroxy-benzophenone (THB) metabolites were identified as free and conjugated forms by HPLC analysis. HMB was rapidly absorbed, metabolized, and detected in plasma (as free and protein bound) at 5 min postadministration. The parent compound and metabolites (free and conjugated) were detected at 6 hr in most tissues. DHB was present in most tissues with the highest concentration in the liver. DHMB was only detected as the conjugated form in liver, spleen, and heart. Trace amounts of THB were also detected in biological samples. Urine was the primary route, whereas feces was the secondary route of elimination of HMB and its metabolites. This study revealed O-dealkylation as the major pathway of HMB metabolism.
二苯甲酮-3[2-羟基-4-甲氧基二苯甲酮（HMB）、二苯甲酰甲烷、Spectra-Sorb UV-9光吸收剂]在许多化妆品和防晒剂中用作紫外线吸收剂。本研究旨在调查HMB（口服给药100mg/kg体重）的代谢情况。通过高效液相色谱分析，将2,4-二羟基二苯甲酮（DHB）、2,2'-二羟基-4-甲氧基二苯甲酮（DHMB）和2,3,4-三羟基二苯甲酮（THB）代谢物鉴定为游离和结合形式。HMB给药后5分钟在血浆中（以游离和蛋白结合形式）被快速吸收、代谢并检测到。在大多数组织中6小时时检测到母体化合物和代谢物（游离和结合形式）。DHB存在于大多数组织中，在肝脏中浓度最高。DHMB仅在肝脏、脾脏和心脏中以结合形式被检测到。在生物样品中也检测到痕量的THB。尿液是主要排泄途径，而粪便则是HMB及其代谢物的次要排泄途径。本研究揭示O-去烷基化是HMB代谢的主要途径。
