Foth H, Kahl R, Kahl G F
Department of Pharmacology and Toxicology, University of Göttingen, Federal Republic of Germany.
Food Chem Toxicol. 1988 Jan;26(1):45-51. doi: 10.1016/0278-6915(88)90040-3.
Intestinal absorption, bioavailability, hepatic and pulmonary extraction and elimination of low doses of benzo[a]pyrene (BP; 0.7-4.4 nmol) were studied in the rat using [G-3H]BP. The hepatic extraction ratio was 0.4 both in a liver perfusion model and in vivo as determined by comparison of intravenous and intraportal infusion experiments in anaesthetized rats. The pulmonary extraction ratio in vivo was 0.11 in control rats and 0.16 in rats pretreated with an inducer of cytochrome P-448. Analysis of BP concentrations in atrial blood and in the bile after continuous BP infusion into the duodenum of anaesthetized rats indicated that at least 30% of the dose must have been absorbed from the gut. Studies have also been performed in conscious rats given BP either as an intravenous bolus or by gavage. The bioavailability was determined to be about 10% in these experiments. Elimination proceeded in a triphasic manner with a half-life of 16.6 hr for the terminal phase.
使用[G-3H]苯并[a]芘（BP；0.7 - 4.4纳摩尔）在大鼠中研究了低剂量BP的肠道吸收、生物利用度、肝脏和肺的摄取及消除情况。通过比较麻醉大鼠的静脉注射和门静脉注射实验确定，在肝脏灌注模型和体内，肝脏摄取率均为0.4。对照大鼠体内肺摄取率为0.11，用细胞色素P - 448诱导剂预处理的大鼠体内肺摄取率为0.16。对麻醉大鼠十二指肠持续输注BP后心房血和胆汁中BP浓度的分析表明，至少30%的剂量必定已从肠道吸收。也对清醒大鼠进行了研究，通过静脉推注或灌胃给予BP。在这些实验中，生物利用度确定为约10%。消除过程呈三相，终末相半衰期为16.6小时。
