A Single-Dose, Open-Label, Randomized, Parallel-Design Study of the Comparative Pharmacokinetics and Safety of TNX-102 2.4 mg SL Tablets (With Phosphate) at 2.4 mg and 4.8 mg, TNX-102-A 2.4 mg SL Tablets (Without Phosphate) at 2.4 mg and Cyclobenzaprine 5 mg Oral Tablets in Healthy Adults.
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 24
- 试验地点
- 1
- 主要终点
- Measured levels of cyclobenzaprine and norcyclobenzaprine in plasma and urine
研究概览
简要总结
Very low dose (VLD) cyclobenzaprine at bedtime has shown promise as a treatment for fibromyalgia, but the chemistry of cyclobenzaprine requires new formulation technology for bedtime use. The present trial is designed to assess the safety and tolerability of TNX-102 2.4 mg SL Tablets (a new formulation of cyclobenzaprine designed to result in increased dosage precision and decreased potential for morning grogginess) at 2.4 mg and 4.8 mg and to compare the bio-availability of TNX-102 2.4 mg SL Tablets at 2.4 mg and 4.8 mg to that of TNX-102-A 2.4 mg SL Tablets (without phosphate) at 2.4 mg and cyclobenzaprine (5 mg tablets).
研究设计
- 研究类型
- Interventional
- 分配方式
- 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
- •Healthy adults
- •Male or female
- •Non-smoker
- •18-65 years old
- •BMI > 18.5 and < 30.0
- •With medically acceptable form of contraception (female only)
- •With signed informed consent
排除标准
- •Any clinically significant abnormality including ECG abnormalities or vital sign abnormalities (systolic blood pressure < 90 or > 140 mmHg,
- •Diastolic blood pressure lower < 50 or > 90 mmHg, or heart rate < 50 or > 100 BPM)
- •Any abnormal laboratory test (including positivity for Hep B, Hep C, HIV, and
- •Hemoglobin < 128 g/L (males) or < 115 g/L (females) and hematocrit < 0.37 L/L (males) or < 0.32 L/L (females))
- •History of alcohol or drug abuse or dependence within 1 year and/or positive drug, cotinine, or alcohol tests
- •Use of any drug (within 30 days), supplement, or food (within 14 days) known to induce or inhibit hepatic drug metabolism prior to study medication
- •Positive pregnancy test, breastfeeding or lactating
- •Use of medication other than hormonal contraceptives or topical products, including OTC, natural health products, MAO inhibitors
- •Participation in an investigational study within 30 days prior to dosing
- •Donation of plasma (within 7 days), or donation or loss of blood of 50-499 mL (within 30 days), or of > 499 mL (within 56 days) prior to dosing.
研究组 & 干预措施
SL TNX-102 at 2.4 mg
1 x TNX-102 SL Tablets at 2.4 mg
干预措施: SL TNX-102 at 2.4 mg (Drug)
SL TNX-102 at 4.8 mg
2 x TNX-102 SL Tablets at 2.4 mg
干预措施: SL TNX-102 at 4.8 mg (Drug)
SL TNX-102-A at 2.4 mg
1 x TNX-102-A (without phosphate) SL Tablet at 2.4 mg
干预措施: SL TNX-102-A at 2.4 mg (Drug)
Cyclobenzaprine tablets
1 x 5 mg cyclobenzaprine oral tablet
干预措施: Cyclobenzaprine tablets (Drug)
结局指标
主要结局
Measured levels of cyclobenzaprine and norcyclobenzaprine in plasma and urine
时间窗: 27 time points per period for blood assessment ; 3 pooled analyses in urine.
Blood samples will be taken per period: within 30 minutes pre-dose and 2, 3.5, 5, 10, 20, 30, and 45 minutes and 1, 2, 2.5, 3, 3.33, 3.67, 4, 4.33, 4.67, 5, 5.5, 6, 8, 12, 16, 24, 36, 48, and 72 hours post-dose. A single urine sample will be collected within 30 minutes pre-dose (one sample), and urine will be pooled from 0-24, 24-48 and 48-72 hours post-dose.
Safety and tolerability of TNX-102 SL Tablets at 2.4 mg and 4.8 mg.
时间窗: Continuously until the end (day 4) of the study period + Telephone follow-up 7-13 days after dosing (total duration: about 1 month)
Every adverse events occurring during the study period will be reported.
次要结局
未报告次要终点