Fischer L J, Weissinger J L, Rickert D E, Hintze K L
J Toxicol Environ Health. 1976 Mar;1(4):587-605. doi: 10.1080/15287397609529360.
Studies were conducted to elucidate the processes involved in the biological disposition of diethylstilbestrol (DES). The apparent biological half-life of [14C] DES decreased with increasing age in immature rats. The half-life of DES in adult rats (14 min) was reached between the 15th and 25th day after birth. Comparison of the intestinal absorption of [14C] DES and [14C]DES monoglucuronide showed the unconjugated drug to be absorbed much more rapidly. Hydrolysis of the conjugate took place in the lower intestine, and this permitted the drug to undergo enterohepatic cycling.
开展了多项研究以阐明己烯雌酚(DES)的生物处置过程。在未成熟大鼠中,[14C]DES的表观生物半衰期随年龄增长而缩短。DES在成年大鼠体内的半衰期(14分钟)在出生后第15天至第25天之间达到。对[14C]DES和[14C]DES单葡萄糖醛酸苷的肠道吸收情况进行比较,结果显示未结合的药物吸收速度要快得多。结合物在小肠下段发生水解,这使得药物能够进行肠肝循环。