Single-dose and Steady-state Pharmacokinetics of BIA 2-093 and Its Metabolites in Healthy Elderly Subjects Compared With Those in Healthy Young Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 30
- 试验地点
- 1
- 主要终点
- Maximum Drug Concentration (Cmax)
研究概览
简要总结
The purpose of this study is to determine the effects of age on the pharmacokinetic profile of BIA 2-093 and its active metabolites.
详细描述
This was a single-centre, open-label, parallel group, non-randomised study with a single-dose phase (Phase A) followed by a multiple-dose phase (Phase B), in 12 healthy elderly and 12 healthy young subjects. During the whole study, subjects were to receive a single 600 mg dose of BIA 2-093 (Phase A) followed by 600 mg BIA 2-093 once daily for 8 days in Phase B. Phase B was to begun 96 hours post-Phase A dose.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 65 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Male or female subjects aged between 18 and 40 years, inclusive OR male or female subjects aged 65 years or more.
- •If young, subjects who were within 15% of ideal body weight OR, if elderly, subjects who were within 20% of ideal body weight according to the Metropolitan Life Insurance Table.
- •Subjects who were healthy as determined by pre-study medical history, physical examination, neurological examination, and 12-lead ECG.
- •Subjects who had clinical laboratory tests acceptable to the Investigator.
- •Subjects who were negative for HBsAg, HCVAb and HIV-1 and HIV-2 Ab tests at screening.
- •Subjects who were negative for alcohol and drugs of abuse at screening.
- •Subjects who were non-smokers or who smoked less than 10 cigarettes or equivalent per day.
- •Subjects who were able and willing to give written informed consent.
- •(If female) She was not of childbearing potential by reason of surgery or menopause or, if of childbearing potential, she used one of the following methods of contraception: double barrier or intrauterine.
- •(If female and with less than 40 years old) She had a negative pregnancy test at screening.
排除标准
- •Subjects who did not conform to the above inclusion criteria.
- •Subjects who had a clinically relevant history or presence of respiratory, gastrointestinal, renal, hepatic, haematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, connective tissue diseases or disorders.
- •Subjects who had a clinically relevant surgical history.
- •Subjects who had a clinically relevant family history.
- •Subjects who had a history of relevant atopy.
- •Subjects who had a history of relevant drug hypersensitivity.
- •Subjects who had a history of alcoholism or drug abuse.
- •Subjects who consumed more than 14 units of alcohol a week.
- •Subjects who had a significant infection or known inflammatory process on screening and/or admission.
- •Subjects who had acute gastrointestinal symptoms at the time of screening and/or admission (e.g., nausea, vomiting, diarrhoea, heartburn).
- •Subjects who had used drugs within 2 weeks of first dosing.
- •Subjects who had used any investigational drug and/or participated in any clinical trial within 3 months of their first admission to this study.
- •Subjects who had previously received BIA 2-
- •Subjects who had donated and/or received any blood or blood products within the previous 2 months prior to screening.
- •Subjects who were vegetarians, vegans and/or had medical dietary restrictions.
- •Subjects who could not communicate reliably with the investigator.
- •Subjects who were unlikely to co-operate with the requirements of the study.
- •Subjects who were unwilling or unable to give written informed consent.
- •(If female) She was pregnant or breast-feeding
- •(If female) She was of childbearing potential and she did not use an authorised effective contraceptive method.
研究组 & 干预措施
Elderly subjects
14 Elderly subjects aged 65 years or more; During the whole study, subjects were to receive a single 600 mg dose of BIA 2-093 (Phase A) followed by 600 mg BIA 2-093 once daily for 8 days in Phase B. Phase B was to begun 96 hours post-Phase A dose.
干预措施: BIA 2-093 (Drug)
Young subjects
16 young subjects aged between 18 and 40 years During the whole study, subjects were to receive a single 600 mg dose of BIA 2-093 (Phase A) followed by 600 mg BIA 2-093 once daily for 8 days in Phase B. Phase B was to begun 96 hours post-Phase A dose.
干预措施: BIA 2-093 (Drug)
结局指标
主要结局
Maximum Drug Concentration (Cmax)
时间窗: Day 1 at pre-dose, and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, and 96 hours post-dose From Day 5 to Day 11 inclusive, before the daily dose (for trough levels). On Day 12, pre-dose, and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours p
Single-dose period: Day 1 at pre-dose, and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, and 96 hours post-dose. Multiple-dose period: from Day 5 to Day 11 inclusive, early in the morning, before the daily dose (for trough levels). Day 12: pre-dose, and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours post-last dose. BIA 2-194, BIA 2-195, and oxcarbazepine are metabolites of BIA 2-093
次要结局
- Tmax - Time of Maximum Observed Concentration(Day 1 at pre-dose, and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, and 96 hours post-dose From Day 5 to Day 11 inclusive, before the daily dose (for trough levels). On Day 12, pre-dose, and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours p)
- AUC0-t - Area Under the Plasma Concentration-time Curve to Last Measurable Time Point(Day 1 at pre-dose, and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, and 96 hours post-dose From Day 5 to Day 11 inclusive, before the daily dose (for trough levels). On Day 12, pre-dose, and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours p)