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JM216的水合反应及其稳定性影响因素

The Aquation Reactions of JM216 and the Effects of Acid and Light on Its Stability
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摘要 研究了JM2 1 6的水合反应动力学 ,并考察了光照、稀酸对其稳定性的影响。结果表明 ,JM2 1 6的水合反应为准一级反应 ,反应对JM2 1 6为一级 ,37°C时水合反应表观速率常数为kobs=5 0× 1 0 - 6 min- 1,半衰期t1 2 =96 2 5d。在光照下 ,JM2 1 6溶液稳定。而在稀HCl溶液中 ,随着酸浓度增加 ,JM2 1 6的稳定性降低 ,但在胃液酸度范围、口服用药时间内可保持稳定 ,因此口服用药过程不会影响JM2 1 6的稳定性。 The aquation of JM216 and the effects of acidity and light on the stability of JM216 were studied. The experimental results showed that the aquation of JM216 follows the pseudo-first-order- rate law, of which the observed-rate constant k_ obs is 5.0×1.0 -6 min -1 and the half life period t_ 1/2 is 96.25 days at 37℃. Upon irradiation with 4500±500 lx strong light, JM216 was unstable in aqueous solution .In 0.01~0.1mol/L HCl aqueous solution with the acidity of gastrointestinal environment, JM216 could keep stable for 5 hours. From these results, it can be seen that JM216 survives in gastric environment and may be applied orally.
出处 《贵金属》 CAS CSCD 2003年第3期41-44,共4页 Precious Metals
基金 云南省自然科学基金资助项目 (2 0 0 0B0 0 2 4Q)
关键词 铂族金属抗肿瘤药物 JM216 水合反应 动力学 稳定性 表观速率常数 medicine chemistry JM216 platinum(IV) anticancer drug aquation observed rate constant stability
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参考文献3

  • 1Roy Mason W. Platinum(II) -catalyzed substitutions of platinum (IV)complexes [J]. Cood Chem. Rev., 1972, 7 (3):241 - 255.
  • 2Hambley T W, Battle A R, Deacon G B, et al. Modifying the properties of platinum (IV)complexes in order to increase biological effectiveness [J]. J. Inor. Biochem., 1999, 77 (1): 3-12.
  • 3Neidle S, Snook C F, Murrer B A, et al. Bis(acetato)amminedichloro(cyclohexylamine)platinum(IV),an orally active anticancer drug[J]. Acta Cryst., 1995, C51: 822-824.

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