Korst A E, Gall H E, Vermorken J B, van der Vijgh W J
University Hospital Vrije Universiteit, Clinical Research Laboratory of Oncology, Amsterdam, The Netherlands.
Cancer Chemother Pharmacol. 1996;39(1-2):162-6. doi: 10.1007/s002800050553.
The pharmacokinetics of amifostine, a protector against chemotherapy and radiation-induced toxicities, was investigated in the plasma and ascites of a cancer patient. A high-performance liquid chromatography (HPLC) procedure with electrochemical detection was used to measure amifostine, its active metabolite, WR 1065, and the disulfides (symmetrical plus mixed disulfides). Both amifostine and WR 1065 were rapidly cleared from the plasma (95% and 50% of the peak concentration within 1 h, respectively). The disulfides, which were rapidly formed from WR 1065, were cleared much more slowly (final half-life 13.6 h). Multiple dosing resulted in a tendency toward increasing peak levels of WR 1065 and decreasing peak levels of the disulfides. Only 1% of the delivered dose appeared in the ascites. Therefore, it is not plausible that the presence of ascites or other third spaces would have an impact on the pharmacokinetics of amifostine.
对一名癌症患者的血浆和腹水中用于预防化疗和放疗所致毒性的氨磷汀的药代动力学进行了研究。采用具有电化学检测的高效液相色谱（HPLC）方法来测定氨磷汀、其活性代谢产物WR 1065以及二硫化物（对称二硫化物和混合二硫化物）。氨磷汀和WR 1065均迅速从血浆中清除（分别在1小时内清除峰浓度的95%和50%）。由WR 1065迅速形成的二硫化物清除得要慢得多（终末半衰期为13.6小时）。多次给药导致WR 1065的峰浓度有升高趋势，而二硫化物的峰浓度有降低趋势。给药剂量中只有1%出现在腹水中。因此，腹水或其他第三间隙的存在会对氨磷汀的药代动力学产生影响这一说法是不合理的。
