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首页> 外文期刊>Crystal growth & design >New Approach to Reduce the Overhigh Plasma Concentration of Captopril by the Formation of Zinc Coordination Polymer
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New Approach to Reduce the Overhigh Plasma Concentration of Captopril by the Formation of Zinc Coordination Polymer

机译：通过形成锌配位聚合物降低卡托普利血浆过高浓度的新方法

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Captopril is an antihypertension drug, it has side effects of vertigo, headache, and functional gastrointestinal disorders due to its overhigh plasma concentration. In addition, captopril undergoes oxidation at its thiol to yield captopril disulfide. In order to reduce its release rate and increase its oxidation stability, coordination polymer of captopril with zinc ion was prepared and its structure was determined by single crystal X-ray diffraction. The results of solubility measurements indicate that the apparent solubility and intrinsic dissolution rate of captopril can be dramatically decreased after the formation of coordination polymer. Pharmacokinetic studies in rats reveal that the plasma concentration of captopril can be reduced by the formation of zinc coordination polymer, with maximum plasma concentration reduced from 2.53 μg/mL for captopril to 0.99 μg/mL for the zinc coordination polymer. Moreover, the oxidation stability of captopril is simultaneously improved by the formation of zinc coordination polymer.
机译：卡托普利是一种抗高血压药，由于其血浆浓度过高，因此具有眩晕，头痛和胃肠功能紊乱的副作用。此外，卡托普利在其硫醇上发生氧化，生成卡托普利二硫化物。为了降低其释放速率并提高其氧化稳定性，制备了卡托普利与锌离子的配位聚合物，并通过单晶X射线衍射确定其结构。溶解度测量的结果表明，形成配位聚合物后，卡托普利的表观溶解度和固有溶解速率可以大大降低。大鼠的药代动力学研究表明，卡托普利的血浆浓度可通过形成锌配位聚合物而降低，最大血浆浓度从卡托普利的2.53μg/ mL降至锌配位聚合物的0.99μg/ mL。此外，通过形成锌配位聚合物同时改善了卡托普利的氧化稳定性。

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