The present study was carried out to assess the pharmacokinetic drug interaction between nebivolol and lansoprazole following single oral dose administration in hypertensive patients. Therapeutic dose of nebivolol alone and combination with lansoprazole were administered to a separate group of hypertensive patients. Serial blood samples were collected at pre-dose (0.0) to 36 h post-dose following each treatment to characterize the pharmacokinetic parameters. The plasma nebivolol concentrations were estimated by a sensitive liquid chromatographic mass spectrometry (LC-MS) method. Mean (SD) of AUC0-t (ng.h/mL) and AUC0–∞ (ng.h/mL) for nebivolol given as a combination versus nebivolol alone is 34.08 (6.67) vs. 17.29 (4.60) and 43.36 (10.61) vs. 24.42 (5.08) respectively. Corresponding values for Cmax (ng/mL) is 6.37 (0.89) vs. 3.09 (0.37). Lansoprazole significantly increased the peak and extent of exposure of nebivolol when used in combination. There was minor change in the elimination parameters. The results indicate that there observed to be a pharmacokinetic interaction when nebivolol is administered in combination with lansoprazole. Hence, the combination is contraindicated or used with caution in a clinical situation
