Two-way Crossover Bioequivalence Study of Alendronate Sodium Tablets in Healthy, Non-smoking Male Volunteers under Fasted Conditions

Abstract

This study was conducted in order to assess the bioequivalence of two different formulations containing 70 mg alendronate sodium (CAS 121268-17-5) under fasted conditions. One hundred twenty-two healthy male volunteers were enrolled in an open label, randomized, crossover design with a wash-out period of 20 days in one study center. Urine samples were collected up to 36 h post-dose, and the concentrations of alendronic acid were determined using a high performance liquid chromatographic method with pre-derivatization and fluorescence detection (HPLC/FL) method. The mean Ae_0–t were 604.24 ± 348.73 µg and 627.36 ± 327.99 µg, while the mean R_max were 193.87 ± 114.68 µg/h and 202.00 ± 107.83 µg/h for the test and reference formulations, respectively. The T_max of the test and reference tablets were 1.26 ± 0.58 h and 1.26 ± 0.51 h, respectively. No significant differences of pharmacokinetic parameters between the two studied formulations were found. The 90% confidence intervals for the primary target parameters, intra-individual ratios for Ae_0–t and R_max of alendronic acid, were between 0.86–1.00 and 0.85–1.01, respectively, and thus within the acceptance range for bioequivalence criteria. In the light of the present study it can be concluded that the test formulation is bioequivalent to the reference formulation.

Key words

Alendronate sodium, bioequivalence, pharmacokinetics, urine - Alendronic acid - Aminobisphosphonate - CAS 121268-17-5

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