Bioequivalence evaluation of acarbose tablet in healthy chinese volunteers with pharmacodynamic endpoints / 中国药学杂志

ABSTRACT

OBJECTIVE: To evaluate the bioequivalence of acarbose tablet in healthy Chinese volunteers through the use of pharmacodynamics endpoint parameters of serum glucose. METHODS: Following the Food and Drug Administration (FDA) guidance, a single oral dose of test and reference formulations was given to 32 healthy Chinese volunteers according to a randomized crossover design. Serum glucose concentrations after sucrose administration and co-administration of sucrose and acarbose on the following day were both determined. The reduction of serum glucose concentration were calculated following treatment with acarbose and sucrose together relative to the baseline serum glucose concentration observed. The parameters of Δcmax and AUEC0-4 h recommended by the FDA were used for bioequivalence evaluation. Four pharmacodynamics parameters of AUEC0-2 h,AUEC0-1.5 h, AUEC0-1.0 hand ΔGE were also tested in the evaluation. RESULTS: The main pharmacodynamics parameters of serum glucose in test and reference formulations were as followsΔcmax (1.169±0.719) and (0.878±0.571) mmol·L-1, AUEC0-2 h(46±25) and (50±21) mmol·min·L-1, AUEC0-1.5 h(62±42) and (70±29) mmol·min·L-1, AUEC0-1 h(59±52) and (73±32) mmol·min·L-1, ΔGE(1.829±0.952) and (1.656±0.764) mmol·L-1, respectively. The parameter AUEC0-4 h could not be evaluated due to the presence of negative values. CONCLUSION: Acarbose tablet is bioinequivalent to the reference tablet.This might be related to acarbose dose, the 50 mg dose of acarbose tablet is inadequate. Pharmacodynamics parameters which is suitable to demonstrate acarbose bioequivalence might also need to be optimized.