| 草酸铂与Cl-的取代反应动力学 |
| Kinetics of the Substitution Reactions of Oxaliplatin and Cl- |
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| 摘要: 采用高效液相色谱研究了新型铂类抗癌药草酸铂与Cl-的取代反应动力学,并讨论了酸性条件下H+对取代反应的影响。结果表明,Cl-大量存在时,体系中草酸铂与Cl-的取代反应为优势反应,反应对草酸铂和Cl-均为一级。根据动力学数据提出了可能的反应机理,并由此推导出反应速率r=(KClk5′+K1′k3)[L-OHP][Cl-],与实验结果相吻合;当H+也大量存在时,取代反应被加速,此时表观速率常数kobs与[H+]、[Cl-]之间呈非线性递增,但反应对草酸铂仍为一级。在生理盐水中,反应的准一级速率常数kobs=3.6×10-4min-1,1%～2%的草酸铂发生反应所需时间不足1h,因此临床使用草酸铂时要避免与Cl-配伍。 |
| 关键词: 草酸铂 取代反应 准一级反应 表观速率常数 |
| 基金项目: |
| Abstract: The substitution reactions of oxaliplatin with Cl- have been studied by high performance liquid chromatograph in neutral and acid aqueous solution. The experimental results show that under the condition of [Cl-]0》[L- OHP]0 the reactions of oxaliplatin with Cl- are first order in both oxaliplatin and Cl-, which have advantage over other reactions. In this paper, the possible mechanism has been proposed. From it, the rate law r=(KClk5′+K1′k3)[Cl-][L-OHP] is deduced, which is in perfect agreement with the experiment results. When excess acid is added to the systems, the reactions of oxaliplatin with Cl- are accelerated by H+ and the observed rate constants kobs are nonlinearly increased with the improvement of [H+] or [Cl-]. However, the rates of the reactions still follow to the first order dependence on L-OHP. In 0.9% NaCl solution, the pseudo-first-order rate constant kobs is 3.6×10-4min-1, which determines that it takes less one hour for 1%～2% of oxaliplatin reacting with Cl-. As a result, the physiological saline solution should not be used to dissolve or dilute the complex in clinical. |
| Keywords: oxaliplatin substitution reaction pseudo-first-order reaction observed rate constant |
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| 高文桂,普绍平,刘伟平,刘祝东,杨一昆.草酸铂与Cl-的取代反应动力学[J].无机化学学报,2002,18(7):679-682. |
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