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给动物肠胃外注射顺式二氯二氨铂(II)后铂的处置与分布。

Disposition and distribution of platinum following parenteral administration of cis-dichlorodiammineplatinum(II) to animals.

作者信息

Litterst C L, LeRoy A F, Guarino A M

出版信息

Cancer Treat Rep. 1979 Sep-Oct;63(9-10):1485-92.

PMID:498147
Abstract

After iv administration of cis-dichlorodiammineplatinum(II) (cis-platinum) to animals, plasma levels of platinum decline in a biphasic manner, with a distribution phase (alpha) half-life of minutes and an elimination phase (beta) half-life of days. Urinary excretion of platinum is extensive on the first day after drug administration with a final urinary recovery of 70%--90% of the administered dose. Platinum is initially distributed to nearly all tissues with the highest levels appearing in kidney, liver, ovary, uterus, skin, and bone. There is no preferential uptake of platinum into tumor, although the presence of a tumor may alter the rate of platinum excretion and the extent of whole-body retention. No effect is seen on hepatic microsomal drug metabolism after ip administration of cis-platinum to rats. Platinum is excreted more rapidly from hydrated animals than from controls although total urinary recovery of platinum is nearly equal in both groups. Most analogs of cis-platinum appear to follow the same elimination and distribution patterns as cis-platinum itself.

摘要

给动物静脉注射顺二氯二氨铂(顺铂)后,血浆中铂的水平呈双相下降,分布相(α)半衰期为几分钟,消除相(β)半衰期为几天。给药后第一天铂的尿排泄量很大,最终尿中回收的铂占给药剂量的70% - 90%。铂最初分布到几乎所有组织,肾脏、肝脏、卵巢、子宫、皮肤和骨骼中的水平最高。虽然肿瘤的存在可能会改变铂的排泄速率和全身潴留程度,但铂在肿瘤中没有优先摄取。给大鼠腹腔注射顺铂后,对肝微粒体药物代谢没有影响。与对照组相比,水化动物体内的铂排泄更快,尽管两组铂的尿总回收量几乎相等。顺铂的大多数类似物似乎遵循与顺铂本身相同的消除和分布模式。

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