Evaluation of acarbose bioequivalence in healthy Chinese populations
using novel pharmacodynamics endpoints
Abstract
Background and Objective Acarbose is a widely used α-glucosidase
inhibitor to control postprandial hyperglycemia in type 2 diabetes
mellitus patients. Recently, quite a few pilot studies on acarbose
bioequivalence (BE) in Asian populations have defined new
pharmacodynamic (PD) parameters as reliable endpoints. However, pivotal
studies utilizing these new PD parameters were rarely reported. The
study aims to explore acarbose BE using the new PD parameters and
compare their applicability and sensitivity. Methods The study was
conducted with an open, randomized, two-period crossover design using
the test (T) or reference (R) drug at the dose of 2*50 mg. 64 subjects
were recruited, with a one-week washout period. Serum glucose and
insulin concentrations were determined after sucrose administration
(baseline) and sucrose/acarbose co-administration. Results Using the
parameters of rectifying method, which conducts pre-dose value
deduction, the geometric mean ratios of Cmax,r and AUC0-2h,r were
102.91% and 105.29%, respectively. The 90% CIs of Cmax,r and
AUC0-2h,r were all within acceptance limits (80.00-125.00%). The new
parameters exhibited superior applicability and sensitivity in the
evaluation of acarbose BE in healthy subjects. The incidence of AEs
after the T drug or R drug was comparable, and healthy subjects were
well tolerated. Conclusions The results from our study manifested that
the PD parameters of the rectifying method demonstrate superior
applicability and sensitivity in the evaluation of acarbose BE in
healthy subjects. The T and R drug were bioequivalent using the novel PD
parameters as primary endpoints, and both drugs demonstrated good safety
and tolerability.