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二苯甲酮-3在雄性大鼠口服暴露后的药代动力学

Pharmacokinetics of benzophenone-3 after oral exposure in male rats.

作者信息

Kadry A M, Okereke C S, Abdel-Rahman M S, Friedman M A, Davis R A

机构信息

Pharmacology and Toxicology Department, New Jersey Medical School, University of Medicine and Dentistry of New Jersey, Newark, USA.

出版信息

J Appl Toxicol. 1995 Mar-Apr;15(2):97-102. doi: 10.1002/jat.2550150207.

Abstract

Benzophenone-3 (BZ-3) is one of the UV-absorbing agents that has been used in industry and medicine for more than 30 years. Millions of consumers are exposed to benzophenones on a daily basis owing to the widespread use of these compounds in many of the products on the market, such as lipsticks, hair sprays, hair dyes, shampoo and detergent bars and sunscreen lotions. This study was performed to investigate the pharmacokinetics of BZ-3 after oral administration at 100 mg kg-1 body weight in male Sprague-Dawley rats. Absorption from the gastrointestinal tract was rapid because BZ-3 was detected in blood 5 min after administration. The peak plasma concentration (Cmax) was 25.6 +/- 4.6 micrograms ml-1 and the time of occurrence (tmax) was 3.0 +/- 0.4 h. The half-life of absorption of BZ-3 was 0.71 h. The elimination pattern was biphasic with alpha and beta half-lives of elimination of 0.88 and 15.90 h, respectively. The results of this study indicate the presence of strong binding between the plasma protein and BZ-3. Tissue distribution studies at 6 h indicate that the liver contained the highest concentration of free (58.9 +/- 23.8 micrograms) and total (free+bound or conjugated) BZ-3 (2087 +/- 60.1 micrograms), followed by kidney and testes, respectively. Urine and feces analysis indicate that urine was the major route of excretion, followed by feces. Further analysis of urine samples also indicates that conjugation of BZ-3 with glucuronic acid was the major systemic elimination route for the compound.

摘要

二苯甲酮 - 3(BZ - 3)是一种紫外线吸收剂,已在工业和医学领域使用了30多年。由于这些化合物在市场上的许多产品中广泛使用,数百万消费者每天都接触到二苯甲酮,如口红、发胶、染发剂、洗发水、洗衣皂和防晒霜。本研究旨在调查雄性Sprague - Dawley大鼠口服100 mg kg-1体重的BZ - 3后的药代动力学。胃肠道吸收迅速,给药后5分钟即可在血液中检测到BZ - 3。血浆峰浓度(Cmax)为25.6±4.6微克/毫升,出现时间(tmax)为3.0±0.4小时。BZ - 3的吸收半衰期为0.71小时。消除模式为双相,α和β消除半衰期分别为0.88和15.90小时。本研究结果表明血浆蛋白与BZ - 3之间存在强结合。6小时的组织分布研究表明,肝脏中游离(58.9±23.8微克)和总(游离+结合或共轭)BZ - 3浓度最高(2087±60.1微克),其次是肾脏和睾丸。尿液和粪便分析表明,尿液是主要排泄途径,其次是粪便。对尿液样本的进一步分析还表明,BZ - 3与葡萄糖醛酸的结合是该化合物的主要全身消除途径。

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