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[通过仪器中子活化分析法对单剂量口服金诺芬后金在胆汁、肾脏及粪便中的排泄与分布进行定量分析]

[Biliary, renal and fecal elimination and distribution of gold after a single oral administration of auranofin, quantified by the instrumental neutron activation analysis method].

作者信息

Benn H P, Schnier C, Bauer E, Seiler K U, Elhöft H, Löffler H

机构信息

II. Medizinische Klinik und Poliklinik, Christian-Albrechts-Universität, Kiel.

出版信息

Z Rheumatol. 1991 Jan-Feb;50(1):32-8.

PMID:2058320
Abstract

Three days after cholecystectomy, seven patients received a single dose of auranofin (5 tablets Ridaura = 4.35 mg gold). At defined time points thereafter the gold content in samples of blood, plasma, urine, bile, and feces was determined by instrumental neutron activation analysis (INAA). Maxima of the mean gold concentrations in blood (140 +/- 42 ng/ml) and plasma (173 +/- 54 ng/ml) are found 2 h after oral administration of the antirheumatic agent, after 16 h in urine (43 +/- 28 ng/ml) and bile (65 +/- 50 ng/ml), and after 24 h in erythrocytes (greater than 200 ng/ml). The mean terminal half-lives are 7.6 days (blood), 15 days (plasma), 5 days (erythrocytes), and 6.5 days (bile). The cumulative biliary gold excretion within 8 days after the administration of auranofin was 1.6%, compared with 4% and 40% for renal and fecal elimination, respectively. The gold concentration in plasma is always higher than that in bile. There is a close correlation between the areas under the concentration curves (AUC) in bile and plasma (r = 0.864).

摘要

胆囊切除术后三天,七名患者接受了单剂量的金诺芬(5片瑞得 = 4.35毫克金)。此后在特定时间点,通过仪器中子活化分析(INAA)测定血液、血浆、尿液、胆汁和粪便样本中的金含量。口服抗风湿药后2小时,血液(140±42纳克/毫升)和血浆(173±54纳克/毫升)中的平均金浓度达到最大值,尿液(43±28纳克/毫升)和胆汁(65±50纳克/毫升)中的平均金浓度在16小时后达到最大值,红细胞中的平均金浓度在24小时后达到最大值(大于200纳克/毫升)。平均终末半衰期分别为血液7.6天、血浆15天、红细胞5天和胆汁6.5天。金诺芬给药后8天内,胆汁中金的累积排泄率为1.6%,而肾脏和粪便排泄率分别为4%和40%。血浆中的金浓度始终高于胆汁中的金浓度。胆汁和血浆中浓度曲线下面积(AUC)之间存在密切相关性(r = 0.864)。

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