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沙格列汀联合达格列净治疗 2 型糖尿病的药代动力学药物评价。

Pharmacokinetic drug evaluation of saxagliptin plus dapagliflozin for the treatment of type 2 diabetes.

机构信息

a Department of Medicine , Division of Diabetes, Nutrition and Metabolic Disorders , CHU Liège, Liège , Belgium.

b Division of Clinical Pharmacology , Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Liège , Belgium.

出版信息

Expert Opin Drug Metab Toxicol. 2017 May;13(5):583-592. doi: 10.1080/17425255.2017.1315102. Epub 2017 Apr 11.

Abstract

Combining a dipeptidyl peptidase-4 inhibitor and a sodium-glucose cotransporter type 2 inhibitor is an attractive option to treat hyperglycaemia in type 2 diabetes. Areas covered: The saxagliptin plus dapagliflozin combination is carefully analysed, focusing on: 1) pharmacokinetic properties, 2) pharmacodynamics data, and 3) results of randomised controlled trials (dual combination versus either monotherapy, sequential therapy saxagliptin added to dapagliflozin or dapagliflozin added to saxagliptin). Expert opinion: Pharmacokinetic findings demonstrate the absence of drug-drug interaction and the bioequivalence of the FDC compared with separated tablets. Pharmacodynamic observations confirm a complementary mode of action of the two agents. Dual saxagliptin-dapagliflozin therapy is more potent than either monotherapy. It may be used as an initial combination, although this approach remains debatable and should probably be reserved in case of high glycated hemoglobin, or a stepwise strategy, according to a personalized approach. The developed saxagliptin-dapagliflozin FDC may simplify anti-hyperglycemic therapy and improve drug compliance.

摘要

将二肽基肽酶-4 抑制剂和钠-葡萄糖共转运蛋白 2 抑制剂联合使用是治疗 2 型糖尿病高血糖的一种有吸引力的选择。

涵盖领域

对沙格列汀加达格列净联合用药进行了仔细分析,重点关注:1)药代动力学特性,2)药效学数据,和 3)随机对照试验的结果(双联治疗与任一单药治疗、沙格列汀序贯加用达格列净或达格列净序贯加用沙格列汀)。

专家意见

药代动力学研究结果表明,与分开服用片剂相比,药物之间不存在药物相互作用,且固定剂量复方与分开片剂具有生物等效性。药效学观察结果证实了两种药物的互补作用模式。双联沙格列汀-达格列净治疗比任一单药治疗更有效。它可以作为初始联合治疗方案使用,尽管这种方法仍存在争议,并且可能应该保留在糖化血红蛋白较高的情况下,或者根据个性化方法采用逐步治疗策略。已开发的沙格列汀-达格列净固定剂量复方可能会简化抗高血糖治疗并提高药物依从性。

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