A Single-Dose, Open-Label, Randomized Study of the Comparative Pharmacokinetics of Sublingual TNX-102 2.4 mg at pH 3.5 and 7.1, Oral Cyclobenzaprine 5 mg Tablets, and Intravenous Cyclobenzaprine 2.4 mg 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
- Safety and tolerability of sublingual TNX-102 2.4 mg at pH 3.5 and pH 7.1.
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 sublingual TNX-102 2.4 mg (a new formulation of cyclobenzaprine designed to result in increased dosage precision and decreased potential for morning grogginess) at pH 3.5 and 7.1 and to compare the bio-availability of sublingual TNX-102 2.4 mg at pH 3.5 and 7.1 and cyclobenzaprine (5 mg tablets, or 2.4 mg iv).
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 (within30 days), or of > 499 mL (within 56 days) prior to dosing.
研究组 & 干预措施
SL TNX-102 at pH 3.5
2.4 mg TNX-102 sublingual solution (2.4 mg/mL) in PBS at pH 3.5
干预措施: SL TNX-102 2.4 mg at pH 3.5 (Drug)
SL TNX-102 at pH 7.1
2.4 mg TNX-102 sublingual solution (2.4 mg/mL) in PBS at pH 7.1
干预措施: SL TNX-102 2.4 mg at pH 7.1 (Drug)
Cyclobenzaprine tablets
5 mg cyclobenzaprine tablet once
干预措施: Cyclobenzaprine Tablet (Drug)
Cyclobenzaprine IV
2.4 mg cyclobenzaprine USP in PBS (0.6 mg/mL) at pH 7.4
干预措施: Cyclobenzaprine IV (Drug)
结局指标
主要结局
Safety and tolerability of sublingual TNX-102 2.4 mg at pH 3.5 and pH 7.1.
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.
• 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.
次要结局
未报告次要终点