1. Pharmacokinetic interaction between linagliptin and tadalafil in healthy Egyptian males using a novel LC-MS method.
- Author
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Mourad SS, El-Kimary EI, Barary MA, and Hamdy DA
- Subjects
- Adult, Analytic Sample Preparation Methods, Drug Interactions, Egypt, Humans, Limit of Detection, Linagliptin blood, Male, Middle Aged, Reproducibility of Results, Tadalafil blood, Blood Chemical Analysis methods, Chromatography, Liquid methods, Healthy Volunteers, Linagliptin pharmacokinetics, Mass Spectrometry methods, Tadalafil pharmacokinetics
- Abstract
Aim: Assessment of pharmacokinetic interaction between linagliptin (LNG) and tadalafil (TDL) in healthy males. Methods: First, a novel LC-MS method was developed; second, a Phase IV, open-label, cross-over study was performed. Volunteers took single 20-mg TDL dose on day 1 followed by wash out period of 2 weeks then multiple oral dosing of 5-mg/day LNG for 13 days. On day 13, volunteers were co-administered 20-mg TDL. Results: LNG and TDL single doses did not affect QTc interval. Smoking did not alter pharmacokinetics/pharmacodynamics of LNG and TDL. Co-administration of LNG with TDL resulted in TDL longer time to reach maximum plasma concentration (T
max ), decreased oral clearance (Cl/F) and oral volume of distribution (Vd/F), increased its maximum plasma concentration (Cmax ), area under concentration-time curve (AUC), muscle pain and QTc prolongation. Conclusion: LNG and TDL co-administration warrants monitoring and/or TDL dose adjustment.- Published
- 2019
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