中国临床药理学杂志2024，Vol.40Issue(17)：2552-2556,5.DOI:10.13699/j.cnki.1001-6821.2024.17.020
达格列净片在中国健康受试者中的生物等效性研究
Bioequivalence study of dagliflozin tablets in Chinese healthy subjects
陈永兴 1刘剑锋 2温晓清2
作者信息
- 1. 厦门大学药学院,福建厦门 361102
- 2. 厦门大学附属第一医院BE/Ⅰ期临床试验研究中心,福建厦门 361003
- 折叠
摘要
Abstract
Objective To evaluate the bioequivalence and safety of the test formulation dapagliflozin tablets(10 mg)compared to the reference formulation in healthy adult subjects under fasting and fed conditions.Methods A single-center,randomized,open-label,two-period,two-sequence,crossover study design was employed.A total of 68 subjects were enrolled,with 32 subjects in the fasting group and 36 subjects in the fed group.Each subject received a single oral dose of either the test or reference formulation 10 mg.Plasma concentrations of dapagliflozin were measured using liquid chromatography-tandem mass spectrometry(LC-MS/MS).Pharmacokinetic parameters were calculated using Phoenix WinNonlin 8.2 to assess the bioequivalence of the two formulations and their safety.Results Key pharmacokinetic parameters of the test and reference formulations in the fasting group were as follows:Cmax were(195.08±58.24)and(200.22±45.20)ng·mL-1;tmax were 0.67 and 0.67 h;AUC0_t were(553.52±97.82)and(552.47±106.07)ng·h·mL-1;AUC0-∞ were(580.40±103.79)and(579.42±111.23)ng·h·mL-1.In the fed group,the parameters were:Cmax were(123.38±39.50)and(125.80±39.05)ng·mL-1;tmaxwere 2.00 and 2.50 h;AUC0-t were(606.05±129.44)and(596.73±131.97)ng·h·mL-1;AUC0-∞ were(637.12±138.77)and(629.38±136.81)ng·h·mL-1.The 90％confidence intervals for the geometric mean ratios of Cmax,AUC0-t and AUC0-∞ for the test and reference formulations were within the bioequivalence range of 80.00％to 125.00％.The incidence of adverse drug events was 3.23％in the fasting group and 5.56％in the fed group.Conclusion The test formulation of dapagliflozin tablets is bioequivalent to the reference formulation in healthy Chinese subjects and has a good safety profile.关键词
达格列净片/中国健康受试者/药代动力学/生物等效性/液相色谱-串联质谱法Key words
dagliflozin tablets/Chinese healthy subjects/pharmacokinetics/bioequivalence/liquid chromatography-tandem mass spectrometry分类
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陈永兴,刘剑锋,温晓清..达格列净片在中国健康受试者中的生物等效性研究[J].中国临床药理学杂志,2024,40(17):2552-2556,5.
