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首页> 外文期刊>American Journal of Drug Discovery and Development >In vitro Binding Chemistry of Amlodipine Besylate (Calcium Channel Blocker) and Atorvastatin Calcium (HMG-CoA Reductase Inhibitor) to Serum Albumin and their Mutual Effect to Displace Each Other from the Binding Site
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In vitro Binding Chemistry of Amlodipine Besylate (Calcium Channel Blocker) and Atorvastatin Calcium (HMG-CoA Reductase Inhibitor) to Serum Albumin and their Mutual Effect to Displace Each Other from the Binding Site

机译：苯磺酸氨氯地平（钙通道阻滞剂）和阿托伐他汀钙（HMG-CoA还原酶抑制剂）与血清白蛋白的体外结合化学及其从结合位点相互置换的相互作用

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Combination therapy is now very common for the effective management of cardiovascular problems. The aim of the present study was to evaluate how clinically two important drugs, Amlodipine Besylate and Atorvastatin Calcium, bind with serum protein and the effect of drug-protein binding when they administered concomitantly. In this study the binding chemistry of Amlodipine and Atorvastatin to Bovine Serum Albumin (BSA) was evaluated by Equilibrium dialysis method utilizing Warfarin Sodium (site-I specific probe) and Diazepam (site-II specific probe). Association constant and number of binding sites of the experimental drugs were carried out at pH values of 6.4 and 7.4. The non-liner curve of the plot suggests the presence of at least two classes of binding site (low affinity binding site and high affinity binding site) of experimental drugs to BSA. In both cases of high affinity binding site and low affinity binding, value of association constants of experimental drugs were found higher at pH 7.4. Both of the experimental drugs found to bind site-I preferentially as both of drugs displaced Warfarin Sodium more from the binding site on BSA than that of Diazepam. During concurrent administration of Amlodipine Besylate and Atorvastatin Calcium in presence or absence of diazepam, it was found that the ability of Atorvastatin Calcium to displace Amlodipine Besylate is more than the ability of Amlodipine Besylate to displace Atorvastatin Calcium from the binding site on BSA. The ability of experimental drugs to displace each other is found more in presence of Diazepam. As both drugs compete for the same binding site care should be given during concurrent administration of these two drugs.
机译：对于有效解决心血管问题，联合疗法现在非常普遍。本研究的目的是评估临床上两种重要药物苯磺酸氨氯地平和阿托伐他汀钙如何与血清蛋白结合以及同时给药时药物-蛋白结合的作用。在这项研究中，氨苯地平和阿托伐他汀与牛血清白蛋白（BSA）的结合化学是通过使用华法林钠（I位特异性探针）和地西am（II位特异性探针）的平衡透析方法评估的。在6.4和7.4的pH值下进行实验药物的缔合常数和结合位点数。该图的非线性曲线表明存在至少两类实验药物与BSA的结合位点（低亲和力结合位点和高亲和力结合位点）。在高亲和力结合位点和低亲和力结合两种情况下，发现实验药物的缔合常数值在pH 7.4时较高。发现这两种实验药物都优先结合I位，因为这两种药物都比Biazepam从BSA的结合位点上将华法林钠置换得更多。在存在或不存在地西epa的同时施用苯磺酸氨氯地平和阿托伐他汀钙的过程中，发现阿托伐他汀钙取代苯磺酸氨氯地平的能力比苯磺酸氨氯地平从BSA结合位点取代阿托伐他汀钙的能力强。在地西p存在下，更多地发现了实验药物彼此置换的能力。由于两种药物都竞争相同的结合位点，因此在同时使用这两种药物时应注意。

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