Pharmacokinetics of benzophenone-3 after oral exposure in male rats.
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.
Kadry
A M
AM
Pharmacology and Toxicology Department, New Jersey Medical School, University of Medicine and Dentistry of New Jersey, Newark, USA.
Okereke
C S
CS
Abdel-Rahman
M S
MS
Friedman
M A
MA
Davis
R A
RA
D000284:Administration, Oral; D000818:Animals; D001577:Benzophenones / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D002851:Chromatography, High Pressure Liquid; D005243:Feces / Q000737:chemistry; D006207:Half-Life; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D011485:Protein Binding; D051381:Rats; D017207:Rats, Sprague-Dawley; D013473:Sunscreening Agents / Q000378:metabolism / Q000493:pharmacokinetics*; D013997:Time Factors; D014018:Tissue Distribution
D001577:Benzophenones; D013473:Sunscreening Agents; C005290:oxybenzone