NCT02171559已完成1 期
Relative Bioavailability and Pharmacodynamics of Dabigatran After a Single Dose of 220 mg Dabigatran Etexilate and After 40 mg Enoxaparin s.c. for 3 Days Followed by a Single Dose of 220 mg Dabigatran Etexilate in Healthy Male and Female Volunteers (an Open-label, Randomised, Single and Multiple Dose, Two Way Crossover Phase I Study)
适应症
干预措施
相关药物
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 29
- 主要终点
- Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞) of dabigatran
研究概览
简要总结
To investigate the relative bioavailability and the pharmacodynamics of dabigatran after switching from enoxaparin to dabigatran etexilate as compared to dabigatran etexilate alone
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 55 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Subjects were healthy males and females based upon a complete medical history, including a physical examination, vital signs (blood pressure, pulse rate), 12-lead ECG, and clinical laboratory tests
- •Age ≥18 to ≤55 years
- •Body mass index (BMI) ≥18.5 to ≤29.9 kg/m2
- •Signed and dated written informed consent prior to admission to the study in accordance with GCP and the local legislation
排除标准
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological, or hormonal disorders
- •Relevant surgery of gastrointestinal tract
- •History of any bleeding disorder or acute blood coagulation defect
- •Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
- •History of relevant orthostatic hypotension, fainting spells or blackouts
- •Chronic or relevant acute infections
- •History of allergy/hypersensitivity (including drug allergy) which was deemed relevant to the trial as judged by the investigator
- •Intake of any medication within 2 weeks of first dosing, especially intake of medication, which influences blood clotting, i.e. acetylsalicylic acid, cumarin etc.
- •Use of drugs which might reasonably influence the results of the trial based on the knowledge at the time of protocol preparation within 4 weeks prior to administration or during the trial
- •Alcohol abuse (more than 60 g/day for males and more than 20 g/day for females)
- •Intake of grapefruit, grapefruit juice, or products containing grapefruit juice, Seville oranges, garlic supplements, or St. John's wort within 5 days of first dosing
- •Participation in another trial with an investigational drug within 2 months prior to trial drug administration or during the trial
- •Blood donation (more than 100 mL within 4 weeks prior to trial drug administration or during the trial)
- •Excessive physical activities (within 1 week prior to trial drug administration or during the trial)
- •Any laboratory value outside the reference range that was of clinical relevance
- •Inability to comply with dietary regimen of study centre
- •Smoker (>10 cigarettes or >3 cigars or >3 pipes/day)
- •Inability to refrain from smoking on trial days
- •For female subjects:
- •Pregnancy / positive pregnancy test, or planning to become pregnant during the study or within 1 month after study completion
- •No adequate contraception during the study and within 1 month after study completion such as implants, injectables, combined oral contraceptives, intrauterine device, sexual abstinence (for at least 1 month prior to enrolment), vasectomised partner (vasectomy performed at least 1 year prior to enrolment), or surgical sterilisation (including hysterectomy). Females, who did not have a vasectomised partner, were not sexually abstinent or surgically sterile, were asked to additionally use a barrier contraception method (e.g. condom, diaphragm with spermicide)
- •Lactation period
研究组 & 干预措施
Dabigatran etexilate capsules after enoxaparin ampoules
Experimental
干预措施: Enoxaparin prefilled syringes (Drug)
Dabigatran etexilate capsules after enoxaparin ampoules
Experimental
干预措施: Dabigatran etexilate capsules (Drug)
Dabigatran etexilate capsules without enoxaparin
Active Comparator
干预措施: Dabigatran etexilate capsules (Drug)
结局指标
主要结局
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞) of dabigatran
时间窗: Up to 48 hours after drug administration
Maximum measured concentration of the analyte in plasma (Cmax ) of dabigatran
时间窗: Up to 48 hours after drug administration
Area under the effect-time curve of the analyte in plasma over the time interval from 0 to 48 h after administration (AUEC0-48) after dabigatran alone and after dabigatran following enoxaparin administration
时间窗: Up to 48 hours after drug administration
Maximum effect ratio to baseline (ERmax) after dabigatran alone and after dabigatran following enoxaparin administration
时间窗: Baseline and up to 48 hours after drug administration
次要结局
- Change in clinical laboratory tests(up to day 61)
- Occurrence of adverse events(Up to day 61)
- Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) of dabigatran(Up to 48 hours after drug administration)
- Time from dosing to the maximum concentration of the analyte in plasma (tmax) of dabigatran(Up to 48 hours after drug administration)
- Terminal rate constant in plasma (λz) of dabigatran(Up to 48 hours after drug administration)
- Terminal half-life of the analyte in plasma (t1/2) of dabigatran(Up to 48 hours after drug administration)
- Mean residence time of the analyte in the body after oral administration (MRTpo) of dabigatran(Up to 48 hours after drug administration)
- Apparent clearance of the analyte in plasma after extravascular administration (CL/F) of dabigatran(Up to 48 hours after drug administration)
- Apparent volume of distribution during the terminal phase λz following an extravascular administration (Vz/F) of dabigatran(Up to 48 hours after drug administration)
- Anti-FIIa activity for Dabigatran etexilate(Up to 48 hours after drug administration)
- Anti-FXa/anti-FIIa activity for Enoxaparin(Up to 48 hours after drug administration)
- Activated partial thromboplastin time (aPTT) for Dabigatran etexilate(Up to 48 hours after drug administration)
- Ecarin clotting time (ECT) for Dabigatran etexilate(Up to 48 hours after drug administration)
- Thrombin time (TT) for Dabigatran etexilate(Up to 48 hours after drug administration)
- Change in vital signs (blood pressure, pulse rate)(up to day 61)
- Change in 12-lead electrocardiogram (ECG)(up to day 61)
- Assessment of global tolerability by investigator on a four point scale (good, satisfactory, not satisfactory, bad)(Day 61)
- Assessment of local tolerability by investigator on a four point scale (good, satisfactory, not satisfactory, bad)(day 3 of enoxaparin administration)
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