An Open-Label, Phase I Study of the Pharmacokinetics and Bioavailability of Single, Ascending Subcutaneous Doses of Methylnaltrexone Versus Intravenous Dose in Normal, Healthy Male Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 6
- 试验地点
- 1
- 主要终点
- Peak Plasma Concentration of MNTX
研究概览
简要总结
This is an open-label, Phase I study. Study treatments will entail a four-way crossover among three single, ascending, subcutaneous doses and one intravenous dose of MNTX in six healthy normal male volunteers. Blood samples will be obtained to determine plasma pharmacokinetics, dose proportionality for subcutaneous doses, and absolute bioavailability versus an intravenous dose.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non 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 45 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Subject weight between 60 and 80 kg
- •Subject a non-smoker
- •Subject in good physical health, based on history, physical exam, appropriate laboratory and diagnostics tests at screening with no evidence of clinically significant chronic medical condition.
排除标准
- •Subject with known hypersensitivity to methylnaltrexone, naltrexon or other opioids
- •Subject consuming any prescription medication within the past two weeks, over-the-counter (OTC) products within seven days, any experimental medication within 30 days prior to study screening, or of any drug with a half-life longer then three days within 10 half-lives (>30 days) of screening
- •Subject consuming barbiturates or other inducers or inhibitors of CYP450 within 3 months of screening
- •Subject with history or evidence of cardiovascular, gastrointestinal, hepatic, neurological, pulmonary, and renal or other significant chronic illness.
研究组 & 干预措施
Arm 1
干预措施: SC Methylnaltrexone (MNTX) (Drug)
Arm 2
干预措施: SC Methylnaltrexone (MNTX) (Drug)
Arm 3
干预措施: SC Methylnaltrexone (MNTX) (Drug)
Arm 4
干预措施: IV Methylnaltrexone (MNTX) (Drug)
结局指标
主要结局
Peak Plasma Concentration of MNTX
时间窗: 32 days
The objective of this study is to determine the plasma pharmacokinetic of single, ascending, subcutaneous doses and a single intravenous dose of methylnaltrexone (MNTX) in normal healthy male subjects.
次要结局
- Half-live of MNTX(32 days)
- Volume of Distribution of MNTX(32 days)
- Time to Maximum Plasma Concentration (Tmax) of MNTX(32 days)
- Clearance of MNTX(32 days)
- Area Under the Plasma Concentration versus Time Curve (AUC) of MNTX(32 days)
- Urinary Clearance of MNTX(32 days)
- Percentage of MNTX Excreted in Urine(32 days)