Bioequivalence Of Vildagliptin Tablets In Healthy Volunteers

Objective:To evaluate the bioequivalence and safety of two kinds of Vildagliptin tablets in healthy Chinese volunteers.Methods:A randomized,single-dosed,open label,two way crossover study was designed?cleanse time is seven days?.Thirty-six healthy adult volunteers were randomly divided into two groups and administered with single dose of test or reference preparation of Vildagliptin tablets?50 mg?respectively under the condition of fasting.Twenty-four healthy adult volunteers were randomly divided into two groups and administered with single dose of test or reference preparation of Vildagliptin tablets?50 mg?respectively under the condition of a high-fat diet.Blood samples were collected at due time.Plasma was then obtained and stored at-70?refrigerator after centrifugation.HPLC-MS/MS was applied to determine the concentration of Vildagliptin in plasma,and the drug and time curve was drew to calculate the pharmacokinetic parameters and to evaluate the bioequivalence.All subjects were housed in Phase I wards and were monitored intensively by doctors or nurses.Vital signs and adverse events after medication were recorded,And physical examination and laboratory tests were performed before and after the completion of the trial.Results:Thirty-six subjects were enrolled in the fating study with one subject withdrawn from the trial by adverse events?AEs?before treatment.The remaining thirty-five subjects completed the fating trial.The 90%confidential intervals?CIs?for the ratios of C_max,AUC_0-t-t and AUC_0-?were 95.15%¹10.60%?100.71%¹06.14%and75%¹06.14%,respectively,which all met the predetermined criteria for assuming bioequivalence?80.00%¹25.00%?.Seven subjects reported mild AEs;No serious adverse events?SAEs?were observed.Twenty-four subjects were enrolled in the after high fat diet study,and all subjects were completed.The 90%confidential intervals?CIs?for the ratios of C_max,AUC_0-t-t and AUC_0-?were 94.32%¹08.68%,99.13%¹03.72%and 99.38%¹04.06%,respectively,which all met the predetermined criteria for assuming bioequivalence?80.00%¹25.00%?.Two subjects reported mild AEs;No serious adverse events?SAEs?were observed.Conclusion:Both the test and reference preparations of Vildagliptin tablets are safe and tolerated,which met the regulatory definition for assuming bioequivalence in Chinese healthy adult volunteers.The domestic preparation is generally well tolerated in the test population.