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 3 different formulations of TNX-102 2.8 mg SL Tablets (a new formulation of cyclobenzaprine designed to result in increased dosage precision and decreased potential for morning grogginess) and to compare the bio-availability of 3 different formulations of TNX-102 2.8 mg SL Tablets (TNX-102 with potassium phosphate, TNX-102-B with sodium phosphate, and TNX-102-C with trisodium citrate) to that of cyclobenzaprine (5 mg tablets).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
24
1 x TNX-102 SL Tablet (with potassium phosphate) at 2.8 mg held under the tongue until dissolution, without swallowing or chewing it.
1 x TNX-102-B SL Tablet (with sodium phosphate) at 2.8 mg held under the tongue until dissolution, without swallowing or chewing it.
1 x TNX-102-C SL Tablet (with trisodium citrate) at 2.8 mg held under the tongue until dissolution, without swallowing or chewing it.
1 x 5 mg cyclobenzaprine tablet, swallowed with 240 mL of room-temperature water
PharmaNet, Inc.
Québec, Quebec, Canada
Measured levels of cyclobenzaprine and norcyclobenzaprine in plasma and 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, and 48 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 and 24-48 hours post-dose.
Time frame: 26 time points per period for blood assessment ; 2 pooled analyses in urine.
Safety and tolerability of the 3 formulations of TNX-102 SL Tablets at 2.8 mg
Every adverse events occurring during the study period will be reported.
Time frame: Continuously until the end (day 3) of the study period + Telephone follow-up 7-13 days after dosing (total duration: about 1 month)
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