PROTEIN-BINDING OF 5 PLATINUM COMPOUNDS - COMPARISON OF 2 ULTRAFILTRATION SYSTEMS
PROTEIN-BINDING OF 5 PLATINUM COMPOUNDS - COMPARISON OF 2 ULTRAFILTRATION SYSTEMS
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DOI：
10.1007/bf00262281
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发表时间：
1986-01-01
影响因子：
3
通讯作者：
KLEIN, I
中科院分区：
文献类型：
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作者：
VANDERVIJGH, WJF;KLEIN, I
比较了Amicon Centriflo CF 50 A锥和Amicon MPS-1微分配系统（带YMT过滤器）制备含顺铂、螺铂、JM-40、卡铂或异丙铂血浆样品的超滤。配备YMT膜的MPS-1系统对铂化合物的吸附比CF 50 A锥管少，可以更快速地处理较小的血浆体积。孵育24 h后，使用YMT滤膜测量的顺铂、螺铂、JM-40、卡铂和异丙铂与人血浆蛋白的体外结合率分别为94%、89%、83%、31%和0。这些值对应于血浆中的初始半衰期和通过HPLC测量的血浆超滤液中完整药物的分解半衰期。这表明蛋白质结合的程度与离去基团的稳定性有关。
Amicon Centriflo CF50A cones and Amicon MPS-1 micropartition systems with YMT filters were compared for the preparation of ultrafiltrates of plasma samples containing cisplatin, spiroplatin, JM-40, carboplatin or iproplatin. The MPS-1 system equipped with YMT membranes showed less adsorption of the platinum compounds than CF50A cones and allowed more rapid processing of smaller plasma volumes. In vitro binding to human plasma proteins measured with YMT filters after 24 h of incubation was 94%, 89%, 83%, 31% and 0 for cisplatin, spiroplatin, JM-40, carboplatin and iproplatin, respectively. These values corresponded with the initial half-lives in plasma and the decomposition half-lives of intact drug in plasma ultrafiltrate as measured by HPLC. It is suggested that the degree of protein binding is related to the stability of the leaving groups.