Abramson F P, Miller H C
J Urol. 1982 Dec;128(6):1336-9. doi: 10.1016/s0022-5347(17)53502-8.
The kinetic behavior of diethylstilbestrol (DES) produced from stilphostrol has been studied in man, dog and rat. A sensitive and selective assay for DES in plasma and tissues has been developed with the use of gas chromatographic separation and mass spectrometric detection. In patients with prostate cancer, the plasma concentrations of DES produced by 1,000-mg. infusions of stilphostrol are 1,500 times the DES concentrations produced by conventional oral DES doses. The pharmacokinetics of DES show 2 separate phases; 1 with a t1/2 of approximately 1 hour, another with a t1/2 of approximately a day. In rats, stilphostrol does not selectively liberate DES in the prostate compared to dosing with DES itself. In dogs, a 50-mg. tablet of stilphostrol was bioequivalent to 40 mg. of DES taken orally. Some of these data support the idea that the high DES concentrations produced by stilphostrol infusions underlie in its ability to produce objective responses in patients refractory to conventional oral DES therapy.
已在人、狗和大鼠中研究了己烯雌酚从己烯雌酚双磷酸酯产生的动力学行为。利用气相色谱分离和质谱检测开发了一种灵敏且选择性的血浆和组织中己烯雌酚检测方法。在前列腺癌患者中，静脉输注1000毫克己烯雌酚双磷酸酯产生的血浆己烯雌酚浓度是常规口服己烯雌酚剂量产生的己烯雌酚浓度的1500倍。己烯雌酚的药代动力学表现出两个不同阶段；一个阶段的半衰期约为1小时，另一个阶段的半衰期约为一天。在大鼠中，与直接给予己烯雌酚相比，己烯雌酚双磷酸酯在前列腺中不会选择性地释放己烯雌酚。在狗中，一片50毫克的己烯雌酚双磷酸酯片剂与口服40毫克己烯雌酚具有生物等效性。这些数据中的一些支持这样的观点，即己烯雌酚双磷酸酯输注产生的高己烯雌酚浓度是其在对常规口服己烯雌酚治疗难治的患者中产生客观反应的能力的基础。
