Comparative Pharmacodynamic Bioequivalence Study of Enoxaparin Sodium 100 mg/1 mL Solution for Injection in Prefilled Syringe in Healthy Volunteers Under Fasting Conditions.

Abstract

This study evaluated the bioequivalence of enoxaparin sodium 100 mg/1 mL solution for injection in a prefilled syringe manufactured by a generic company was compared with the reference product of the same dosage form, in healthy adult volunteers under fasting conditions. The comparison focused on pharmacodynamic (PD) parameters. This open-label, randomized, balanced, 2-treatment, 2-period, single-dose, crossover study involved 60 healthy volunteers. No serious adverse events were reported. Chromogenic assay techniques were used for sample analysis. The linearity range for PD parameters was from 0.100 to 0.800 IU/mL for anti-factor IIa activity, from 0.100 to 0.800 IU/mL for anti-factor Xa activity, and from 750.000 to 10,000.000 pg/mL for tissue factor pathway inhibitor quantification. Statistical analysis was conducted using SAS software Version 9.4. The PD parameters evaluated included maximum observed activity concentration, area under the effect curve from time 0 to time t, median time to maximum concentration, and terminal elimination half-life for anti-factor Xa and anti-factor IIa activity. The 95% confidence intervals for the geometric mean ratio of log-transformed PD parameters between the test and reference products for anti-factor Xa and anti-factor IIa activities were within the range of 80%-125%. It was concluded that the test formulation is bioequivalent to the reference formulation of 100 mg/1 mL solution for injection in a prefilled syringe, under fasting conditions.