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

NCT01634412 Phase 1 COMPLETED

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).

Details

Lead sponsor	Tonix Pharmaceuticals, Inc.
Phase	Phase 1
Status	COMPLETED
Enrolment	24
Start date	2012-06
Completion	2014-01

Conditions

• Healthy Adults

Interventions

• SL TNX-102 2.4 mg at pH 3.5
• SL TNX-102 2.4 mg at pH 7.1
• Cyclobenzaprine Tablet
• Cyclobenzaprine IV

Primary outcomes

• • Measured levels of cyclobenzaprine and norcyclobenzaprine in plasma and urine — 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 sublingual TNX-102 2.4 mg at pH 3.5 and pH 7.1. — 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.

Countries

Canada