Fed and fasted bioequivalence assessment of two formulations of extended-release fixed-dose combination dapagliflozin/metformin (10/1,000 mg) tablets in healthy subjects

被引:1
|
作者
Lee, Hae Won [1 ,2 ]
Kang, Woo Youl [3 ]
Park, Ji Seo [1 ,2 ]
Lee, Jae Hwa [1 ,2 ]
Gwon, Mi-Ri [1 ,2 ]
Yang, Dong Heon [4 ]
Kim, Eun Hee [5 ]
Park, Soo-Jin [6 ]
Yoon, Young-Ran [1 ,2 ,7 ]
Seong, Sook Jin [1 ,2 ]
机构
[1] Kyungpook Natl Univ, Sch Med, Daegu 41944, South Korea
[2] Kyungpook Natl Univ Hosp, Dept Clin Pharmacol, 130 Dongdeok Ro, Daegu 41944, South Korea
[3] Natl Inst Food & Drug Safety Evaluat, Dept Innovat Prod Support, Clin Trial Dossier Evaluat Team, Cheongju 28159, South Korea
[4] Kyungpook Natl Univ Hosp, Dept Internal Med, Div Cardiol, Daegu 41944, South Korea
[5] Catholic Univ Daegu, Coll Nursing, Gyongsan 38430, South Korea
[6] Daegu Haany Univ, Coll Korean Med, Daegu 38610, South Korea
[7] Kyungpook Natl Univ, Sch Med, Dept Mol Med, 130 Dongdeok Ro, Daegu 41944, South Korea
关键词
Bioequivalence; Fixed-Dose Combination; Dapagliflozin; Metformin Extended Release; Type; 2; Diabetes; TYPE-2; DIABETES-MELLITUS; SINGLE-COMPONENT DAPAGLIFLOZIN; GLYCEMIC CONTROL; METFORMIN; INHIBITION; MANAGEMENT;
D O I
10.12793/tcp.2023.31.e10
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Two open-label, randomized, two-period crossover studies were conducted to investigate the pharmacokinetic (PK) properties, safety, and bioequivalence of the test formulation (KD4004), a new fixed-dose combination (FDC) formulation of dapagliflozin and metformin extended release (XR) tablets, relative to the reference formulation (10 mg dapagliflozin/1,000 mg metformin XR FDC tablet) in healthy subjects under fasting (Part A) and fed (Part B) conditions. After giving the dose, serial blood samples were collected for a period of 48 hours. Primary PK parameters (AUC0-t and Cmax) were used to assess bioequivalence between two dapagliflozin/metformin XR (10/1,000 mg) FDC formulations under fed and fasting conditions. Safety and tolerability were also evaluated. Part A and Part B were completed by 32 and 37 subjects, respectively. Bioequivalence of the two FDC formulations of dapagliflozin and metformin XR tablets was established in both the fasted and the fed conditions as the 90% confidence interval of the ratios of adjusted geometric means for AUC0-t and Cmax were contained within the predefined range of 0.800-1.250 bioequivalence criteria. Single-dose administration of dapagliflozin and metformin XR was safe and well tolerated as the two FDC formulations. In conclusion, both FDC formulations of dapagliflozin and metformin XR tablets were bioequivalent in fed and fasted subjects. All treatments were well tolerated.Trial Registration: Clinical Research Information Service Identifier: KCT0004026
引用
收藏
页码:105 / 113
页数:9
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