Evaluation of Pharmacokinetic Interactions Between Vildagliptin and Digoxin in Healthy Volunteers
Evaluation of Pharmacokinetic Interactions Between Vildagliptin and Digoxin in Healthy Volunteers
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健康志愿者中维格列汀和地高辛药代动力学相互作用的评价
DOI：
10.1177/0091270007301802
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发表时间：
2007
期刊：
影响因子：
--
通讯作者：
D. Howard
中科院分区：
文献类型：
--
作者：
Yan;R. Sabo;G. Sunkara;M. Bizot;G. Rivière;S. Leon;M. Ligueros‐Saylan;W. Dole;D. Howard
维达列汀是一种新型抗糖尿病药物，是一种口服活性、强效且选择性的二肽基肽酶IV抑制剂，该酶负责肠促胰岛素激素的降解。这项开放标签、随机化、3阶段交叉研究在18例健康受试者中研究了维达鲁肽和地高辛联合给药期间药代动力学相互作用的可能性。受试者随机接受3种治疗：维达鲁肽100 mg qd、地高辛（0.5 mg，然后0.25 mg qd，第2-7天）和维达鲁肽/地高辛联合治疗7天。地高辛与维达鲁普联合给药对维达鲁普（几何均值比[90%置信区间]：AUC 0 - 24 h，0.99 [0.95-1.03]; Cmax，0.95 [0.85-1.06]）或地高辛（AUC 0 - 24 h，1.02 [0.94-1.12]; Cmax，1.08 [0.97-1.20]）的暴露量无影响。此外，两种药物的tmax、t1/2和CL/F均未观察到变化。这些结果表明，当维格鲁肽和地高辛联合给药时，无需调整剂量。
Vildagliptin is a novel antidiabetic agent that is an orally active, potent, and selective inhibitor of dipeptidyl peptidase IV, the enzyme responsible for degradation of the incretin hormones. This open‐label, randomized, 3‐period crossover study investigated the potential for pharmacokinetic interactions in 18 healthy subjects during coadministration of vildagliptin and digoxin. Subjects were randomized to receive each of 3 treatments: vildagliptin 100 mg qd, digoxin (0.5 mg, then 0.25 mg qd on days 2–7), and the combination vildagliptin/digoxin for 7 days. Coadministration of digoxin with vildagliptin had no effect on exposure to vildagliptin (geometric mean ratios [90% confidence interval]: AUC0‐24h, 0.99 [0.95–1.03]; Cmax, 0.95 [0.85–1.06]) or to digoxin (AUC0‐24h, 1.02 [0.94–1.12]; Cmax, 1.08 [0.97–1.20]). In addition, no changes in tmax, t1/2, and CL/F were observed for either drug. These results indicate that no dose adjustment is necessary when vildagliptin and digoxin are coadministered.