卡铂的临床药物动力学。

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清水Oguri年代,神T,激射微波H, T,石川K,木村K,史密斯RD

卡铂的临床药物动力学。

中国新药杂志。1988年3月,28(3):208 - 15所示。doi: 10.1002 / j.1552-4604.1988.tb03134.x。

PubMed ID

3283185 (在PubMed

]

文摘

卡铂的药物动力学是研究癌症患者单后,静脉输注剂量的75年,150年,247.5,300,375,450 mg / m2。总血浆和尿液铂和等离子体ultrafilterable铂原子吸收光谱法测定浓度。卡铂分析等离子体的一个特定的高效液相色谱法(HPLC)过程。总等离子体铂,代表自由卡铂,蛋白结合的铂和代谢物,拒绝triexponentially;血浆半衰期(t1/2λ1,0.2到0.4人力资源;t1/2λ2、1.3到1.7小时;t1/2λ3,22至40人力资源)和全身间隙(CLTB 2.8 + / - 0.5 L / m2 /小时)剂量无关。最大血浆浓度(Cmax)和血浆浓度时间曲线下面积(AUC)与剂量成比例地增加。等离子体ultrafilterable铂和卡铂浓度剂量的375和450 mg / m2拒绝两相的方式。等离子体卡铂消除(t1/2λ1,0.50人力资源; t1/2 lambda 2, 2.2 hr) and CLTB (4.4 to 5.6 L/m2/hr) were also independent of dose; AUC and Cmax increased proportionally to dose. Plasma free platinum was essentially all carboplatin for 8 or 12 hours after administration. Carboplatin did not bind to plasma protein in vitro but did degrade (t1/2-26 hours) to yield a reactive intermediate that bound rapidly and irreversibly to protein. The long terminal elimination half-life of plasma platinum was associated with irreversible binding of a platinum metabonate to plasma protein. The urinary excretion of platinum (0 to 24 hours) accounted for 58 to 72% of doses in 12 to 24 hours. The remainder of the dose is slowly excreted. The pharmacokinetics, in vivo stability, protein binding, and elimination of carboplatin are distinct from the first-generation analog cisplatin.

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药物

卡铂