Bioavailability and mammary excretion of bisphenol a in Sprague-Dawley rats.
This study reports the absolute oral bioavailability and mammary excretion of bisphenol A in rats. The oral bioavailability was determined after administration of relatively low iv (0.1 mg/kg) and oral (10 mg/kg) doses of bisphenol A to rats. After iv injection, serum levels of bisphenol A declined biexponentially, with the mean initial distribution and terminal elimination half-lives being 6.1 +/- 1.3 min and 52.5 +/- 2.4 min, respectively. The systemic clearance (Cls) and the steady-state volume of distribution (Vss) averaged 107.9 +/- 28.7 m/min/kg and 5.6 +/- 2.4 L/kg, respectively. Upon oral administration, the maximum serum concentration (Cmax) and the time to reach the maximum concentration (Tmax) were 14.7 +/- 10.9 ng/ml and 0.2 +/- 0.2 h, respectively. The apparent terminal elimination half-life of bisphenol A (21.3 +/- 7.4 h) after oral administration was significantly longer than that after iv injection, indicating the flip-flop of the absorption and elimination rates. The absolute oral bioavailability of bisphenol A was low (5.3 +/- 2.1%). To determine the extent of mammary excretion, bisphenol A was given by simultaneous iv bolus injection plus infusion to steady state at low, medium, and high doses. The steady-state serum levels of bisphenol A were linearly increased with higher dosing rates. The systemic clearance (mean range, 119.2-154.1 ml/min/kg) remained unaltered over the dosing rate studied. The levels of bisphenol A in milk exceeded those in serum, with the steady-state milk to serum concentration ratio being 2.4-2.7.
Yoo
S D
SD
College of Pharmacy, Sungkyunkwan University, Suwon, Kyonggi-do, Korea. sdyoo@skku.ac.kr
Shin
B S
BS
Lee
B M
BM
Lee
K C
KC
Han
S Y
SY
Kim
H S
HS
Kwack
S J
SJ
Park
K L
KL
D000284:Administration, Oral; D000395:Air Pollutants, Occupational / Q000493:pharmacokinetics*; D000818:Animals; D019540:Area Under Curve; D001559:Benzhydryl Compounds; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D005260:Female; D007262:Infusions, Intravenous; D007774:Lactation / Q000502:physiology; D008321:Mammary Glands, Animal / Q000378:metabolism*; D010636:Phenols / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D000098826:Bisphenol A Compounds
D000395:Air Pollutants, Occupational; D001559:Benzhydryl Compounds; D010636:Phenols; C006780:bisphenol A; D000098826:Bisphenol A Compounds