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Evaluation of acarbose bioequivalence in healthy Chinese populations using novel pharmacodynamics endpoints
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  • Linling Que,
  • Zhenzhong Qian,
  • Xuemei Xiang,
  • Ying Ding,
  • Kai Huang,
  • Yichuan Bai,
  • Huanan Zhao,
  • Qing He
Linling Que
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Zhenzhong Qian
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Xuemei Xiang
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Yichuan Bai
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Huanan Zhao
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Qing He

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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.