Pharmacokinetics of Naltrexone Hydrochloride (HCl) Following Intravenous (i.v.) and Oral Routes of Administration in Healthy Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 18
- 主要终点
- Evaluate the pharmacokinetics of naltrexone following i.v. and oral routes of administration in healthy volunteers, and to assess the absolute bioavailability of naltrexone following oral administration.
研究概览
简要总结
The purpose of the study is to compare the pharmacokinetics of naltrexone following i.v. and oral administration in healthy volunteers, and to assess the bioavailability of naltrexone following oral administration. Moreover, safety is assessed.
详细描述
Naltrexone blocks the effects of opioid (morphine-like) drugs by competitive binding at the opioid receptors in the brain. Naltrexone does not possess morphine-like properties and exhibits minimal pharmacologic activity. Naltrexone is marketed as an oral tablet. A wide range of oral bioavailability values have been reported for naltrexone. The wide range in oral bioavailability of naltrexone appears to be due to differences in assay specificity and the method of estimation of bioavailability (use of total drug, free drug, or urinary excretion data rather than plasma level). This was a single-center, randomized (study drug assigned by chance), open-label, 2-treatment, 2-period crossover study in healthy volunteers. Healthy volunteers were randomly assigned to 1 of 2 treatment sequences (AB or BA) with a washout period of 6 to 14 days between treatments. The washout period commenced the day of dosing, after drug administration. Blood samples for determination of blood naltrexone levels were collected at scheduled time points from the arm opposite to the 1 selected for naltrexone i.v. administration. Pulse, blood pressure, breathing rate, body temperature were measured at the times listed in the study schema. Healthy volunteers remained at the research facility for blood sample collection periods and were monitored for adverse events throughout the treatment periods.
Treatment A: 1 mg naltrexone HCl administered i.v. over 15 minutes (naltrexone i.v.). Treatment B: 50 mg naltrexone HCl administered orally (naltrexone oral).
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 45 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Healthy, non smoker, men and nonpregnant nonlactating women
- •Weighing a minimum of 60 kg and were within 15% of ideal weight for height as described in the Metropolitan Life Insurance Height and Weight Standards
- •Who did not have a history or show presence of drug or alcohol dependence or abuse
排除标准
- •Known allergy or hypersensitivity to naltrexone
- •Usage of prescription medication including opioids (except for birth control medications, sex-hormone replacement, vitamins) within 14 days prior to Day 1, over-the-counter medication (except for vitamin supplements or acetaminophen [less than 2 g/day]) or herbal medication within 3 days prior to Day 1, alcohol, grapefruit juice, or caffeine within 48 hours before dosing
- •Consumption of more than 450 mg of caffeine per day (eg, approximately 5 cups of tea, 3 cups of regular coffee, or 8 cans of cola)
结局指标
主要结局
Evaluate the pharmacokinetics of naltrexone following i.v. and oral routes of administration in healthy volunteers, and to assess the absolute bioavailability of naltrexone following oral administration.
次要结局
- Assessment of safety. Vital signs, Physical examination, clinical laboratory tests, and electrocardiogram were performed at screening and study termination. Additionally, vital signs were recorded on Days 1 and 2 of both treatment periods.