This is a pilot, open label, single center study in 40 subjects undergoing bunionectomy. The study will assess and collect information on pharmacokinetics, pharmacodynamics, safety and efficacy of EXPAREL administered as a sciatic nerve block (in popliteal fossa). A total of 10 subjects will be enrolled in each of the 4 cohorts.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
45
bupivacaine liposome injectable suspension
1.3%, 13.3 mg/mL
First Surgical Hospital
Bellaire, Texas, United States
Pharmacokinetic 1 (Area under the plasma concentration)
Area under the plasma concentration-versus-time curve (AUC).
Time frame: predose (up to 15 min before block), 30 min(±5min), 45 min(±5min), and 60 min (±15min) and 30 min(±5min), 45 min(±5min), 1(±15min), 2(±30min), 12(±30min), 24(±1), 60(±2), 72(±2), 84(±2), 96(±3), 120(±3), 144(±3), and 168(±3) hours following block
Pharmacokinetic 2 (Cmax)
Maximum plasma concentration (Cmax)
Time frame: predose (up to 15 min before block), 30 min(±5min), 45 min(±5min), and 60 min (±15min) and 30 min(±5min), 45 min(±5min), 1(±15min), 2(±30min), 12(±30min), 24(±1h), 60(±2h), 72(±2h), 84(±2h), 96(±3h), 120(±3h), 144(±3h), and 168(±3h) hours following block
Pharmacokinetic 3 (half-life )
The apparent terminal elimination half-life (t1/2el).
Time frame: predose (up to 15 min before block), 30 min(±5min), 45 min(±5min), and 60 min (±15min) and 30 min(±5min), 45 min(±5min), 1(±15min), 2(±30min), 12(±30min), 24(±1h), 60(±2h), 72(±2h), 84(±2h), 96(±3h), 120(±3h), 144(±3h), and 168(±3h) hours following block
Pharmacokinetic 4 (Apparent clearance)
Apparent clearance (CL/F).
Time frame: predose (up to 15 min before block), 30 min(±5min), 45 min(±5min), and 60 min (±15min) and 30 min(±5min), 45 min(±5min), 1(±15min), 2(±30min), 12(±30min), 24(±1h), 60(±2h), 72(±2h), 84(±2h), 96(±3h), 120(±3h), 144(±3h), and 168(±3h) hours following block
Pharmacokinetic 5 (volume of distribution)
Apparent volume of distribution (Vd).
Time frame: predose (up to 15 min before block), 30 min(±5min), 45 min(±5min), and 60 min (±15min) and 30 min(±5min), 45 min(±5min), 1(±15min), 2(±30min), 12(±30min), 24(±1h), 60(±2h), 72(±2h), 84(±2h), 96(±3h), 120(±3h), 144(±3h), and 168(±3h) hours following block
Pharmacokinetic 6 (Tmax)
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Time of Cmax (Tmax)
Time frame: predose (up to 15 min before block), 30 min(±5min), 45 min(±5min), and 60 min (±15min) and 30 min(±5min), 45 min(±5min), 1(±15min), 2(±30min), 12(±30min), 24(±1h), 60(±2h), 72(±2h), 84(±2h), 96(±3h), 120(±3h), 144(±3h), and 168(±3h) hours following block
Pharmacodynamic 1 (duration of sensory and motor block)
Average duration of sensory block and motor block
Time frame: up to 15 min before block, 15 min(±5 min), 30 min(±5min), 45 min(±5min), and 60 min (±15min) and 30 min(±5min), 45 min(±5min), 1(±15min), 2(±30min), 12(±30min), 24(±1), 60(±2), 72(±2), 84(±2), 96(±3), 120(±3), 144(±3), and 168(±3) hours following block
Pharmacodynamic 2 (duration of sensory and motor block)
Average duration of sensory block and motor block
Time frame: up to 15 min before block, 15 min(±5min), 30 min(±5min), 45 min(±5min), and 60 min (±15min) and 30 min(±5min), 45 min(±5min), 1(±15min), 2(±30min), 12(±30min), 24(±1), 60(±2), 72(±2), 84(±2), 96(±3), 120(±3), 144(±3), and 168(±3) hours following block