Relative Bioavailability of Crushed Apixaban Tablets Administered With Water or Apple Sauce Compared With Intact Tablet in Healthy Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 69
- 主要终点
- Adjusted Geometric Mean of Maximum Observed Plasma Concentration (Cmax) of Apixaban
研究概览
简要总结
The purpose of this study is to determine whether the bioavailability of apixaban crushed tablets suspended in water or mixed with applesauce is similar to the bioavailability of apixaban whole tablets administered orally.
详细描述
This study will investigate the bioavailability of apixaban administered as crushed tablets suspended in water and as crushed tablets mixed with applesauce compared with that of whole tablets. The study results may allow enhancement of the apixaban label to include alternative methods of apixaban administration, which may be of benefit to patients who have difficulty swallowing.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 45 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Healthy participants as determined by no clinically significant deviation from normal in findings of medical history, physical examination, electrocardiograms, vital signs, and clinical laboratory tests.
- •Women of childbearing potential allowed. Must be following highly effective methods of contraception
排除标准
- •Any significant acute or chronic medical illness
- •History of significant head injury within the last 2 years, including individuals with base of skull fractures
- •Any major surgery within 4 weeks of study drug administration or anticipated within 2 weeks after completion of the study
- •Any gastrointestinal (GI) surgery or GI disease that could impact absorption of study drug
- •History of Gilbert's Syndrome
- •Inability to tolerate oral medication
- •Inability to be venipunctured and/or tolerate venous access
- •Use of tobacco- or nicotine-containing products (including, but not limited to, cigarettes, pipes, cigars, chewing tobacco, nicotine patches, nicotine lozenges, or nicotine gum) within 6 months prior to study drug administration
- •Any laboratory test results outside of the range of normal, confirmed by repeat results of:
- •Platelet count <150,000 cells/µL
- •Activated partial thromboplastin time >upper limit of normal (ULN)
- •International normalized ratio >ULN
- •Alanine aminotransferase >ULN
- •Aspartate aminotransferase >ULN
- •Total bilirubin >ULN
- •Serum creatinine ≥1.5 mg/dL
- •Hemoglobin <lower limit of normal (LLN)
- •Hematocrit <LLN
研究组 & 干预措施
Apixaban, 10 mg (whole tablets)
Participants received a single dose of apixaban, 10 mg, given orally as 2 5-mg whole commercial tablets (reference)
干预措施: Apixaban (Drug)
Apixaban, 10 mg (crushed and suspended in water)
Participants received a single dose of apixaban, 10 mg, given by mouth as 2 5-mg whole commercial tablets crushed and suspended in 30 mL of water
干预措施: Apixaban (Drug)
Apixaban, 10 mg (crushed and mixed with applesauce)
Participants received a single dose of 10 mg, given by mouth as 2 5-mg apixaban commercial tablets crushed and mixed with 30 g of applesauce
干预措施: Apixaban (Drug)
结局指标
主要结局
Adjusted Geometric Mean of Maximum Observed Plasma Concentration (Cmax) of Apixaban
时间窗: Days 1, 5, and 9 predose and 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 24, 36, 48, 60 and 72 hours post dose
Maximum observed plasma concentration (Cmax) measured in nanograms per milliliter (ng/mL)
Adjusted Geometric Mean of Area Under the Plasma Concentration-time Curve (AUC) From Time Zero Extrapolated to Infinite Time [AUC(INF)] of Apixaban
时间窗: Days 1, 5, and 9 predose and 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 24, 36, 48, 60, and 72 hours post dose
Area Under the Plasma Concentration-time Curve (AUC) From Time of Zero Extrapolated to Infinite Time (INF) \[AUC (INF)\] is measured as nanograms multiplied by hours per milliliter (ng\*h/mL)
Adjusted Geometric Mean of Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to the Time of the Last Quantifiable Concentration [AUC(0-T)] of Apixaban
时间窗: Days 1, 5, and 9 predose and 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 24, 36, 48, 60, and 72 hours post dose
Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to the Last Quantifiable Concentration \[AUC (0-T)\] is measured as nanograms multiplied by hours per milliliter (ng\*h/mL)
次要结局
- Number of Participants With Serious Adverse Events, Death, or Discontinuation Due to Adverse Events by Study Completion(Randomization to May 2014; approximately 6 weeks)
- Time of Maximum Observed Plasma Concentration (Tmax) of Apixaban(Days 1, 5 and 9 pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12 24, 36, 48, 60 and 72 hrs post dose)
- Terminal Plasma Half-life (T-HALF) of Apixaban(Days 1, 5 and 9 pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12 24, 36, 48, 60 and 72 hrs post dose)
- Relative Bioavailability (Frel) of Apixaban(Days 1, 5 and 9 pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12 24, 36, 48, 60 and 72 hrs post dose)