Bioequivalence and Pharmacokinetic Study of Ranazoline in Healthy Male Volunteers: An Open label, Randomized, Single-Dose, Two-Way Crossover Study
Abstract
The present study was to assess the relative bioavailability and pharmacokinetic properties of extended release formulations of Ranolazine 1000 mg in healthy male volunteers using a randomized, open-label, balanced, twotreatment, two-period, two sequence, single dose, crossover, bioequivalence study under fasting conditions. Bioavailability of the test product of Ranolazine extended release tablets 1000 mg was compared with that of the reference product of Ranexa® (Ranolazine extended release tablets 1000mg) of CV Therapeutics Inc., California. The plasma samples were collected at 0.50, 1.00, 1.50, 2.00, 2.50, 3.00, 3.50, 4.00, 4.50, 5.00, 5.50, 6.00, 6.50, 7.00, 8.00, 10.00, 12.00, 16.00, 24.00 and 48.00 hours post dose after single administration of Ranolazine 1000mg. The plasma Ranolazine concentrations were estimated by using a validated bioanalytical method by LC-MS/MS. A ten day washout period is followed between two treatments. The formulations were considered to be bioequivalent if the 90% CIs for the log-transformed values were within the predetermined equivalence range 80%–125% for AUC and Cmax. For Ranolazine, at 90% confidence intervals Cmax, AUC0-t and AUC0-∞ were 83.43-113.29, 82.10-102.87 and 80.94-101.85 for log-transformed data respectively. The present results show that the formulation of Ranolazine was bioequivalent to the reference in fasting, healthy, male volunteers.
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