Determine bioequivalence, safety and tolerability of guaifenesin extended-release 600 mg (Mucinex® SE) compared to an immediate-release syrup reference product in normal healthy subjects.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
30
Single dose of Mucinex® SE extended-release 600 mg bi-layer tablet
Vicks Cough Syrup for Chesty Coughs 15 mL (200 mg guaifenesin q4h) immediate release (IR) syrup
Maximum Observed Plasma Concentration (Cmax) of Guaifenesin
Pharmacokinetic Parameter (Cmax) Maximum observed plasma concentration.
Time frame: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2
Area Under Plasma Concentration-time Curve From Time 0 to the Last Measurable Concentration (AUC(0-t)) of Guaifenesin
Area under the plasma concentration versus time curve from time 0 to the time of the last measurable concentration, as calculated by the linear trapezoidal method.
Time frame: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2
Area Under Plasma Concentration-time Curve From Time 0 to Infinity (AUC(0-inf)) of Guaifenesin
Area under the plasma concentration versus time curve from time 0 to infinity, calculated as AUC 0-t + C last/kel, where C last is the last measurable concentration and kel is the apparent first-order terminal elimination rate constant.
Time frame: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2
Time to Maximum Observed Concentration (Tmax) of Guaifenesin
Pharmacokinetic Parameter (Tmax) Time of the maximum observed plasma concentration.
Time frame: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2
Area Under Plasma Concentration Curve Ratio (AUCR) of Guaifenesin
Pharmacokinetic Parameter AUCR is the ratio of AUC(0-t) to AUC(0-inf). AUCR = AUC(0-t) / AUC(0-inf)
Time frame: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2
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Apparent Terminal Elimination Rate Constant (Kel) of Guaifenesin
Apparent first-order terminal elimination rate constant calculated from a semi-log plot of the plasma concentration versus time curve. The parameter was calculated by linear least-squares (LS) regression analysis using the maximum number of points (e.g. 3 or more non-zero plasma concentrations) in the terminal log-linear phase.
Time frame: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2
Apparent Terminal Elimination Half-life (t1/2) of Guaifenesin
Apparent first-order terminal elimination half-life, calculated as ln(2)/kel.
Time frame: 0 (pre-dose), 0.5, 0.75, 1, 1.5, 2, 3, 4, 4.5, 4.75, 5, 5.5, 6, 7, 8, 8.5, 8.75, 9, 9.5, 10, 11, 12, 14, 16 and 24 hours (post-dose) on Day 1 and 2
Number of Adverse Events (AE) of Participants
Mild = AE does not limit usual activities;subject may experience slight discomfort; Moderate = AE results in some limitation of usual activities; subject may experience significant discomfort; Severe = AE results in an inability to carry out usual activities; Probable = Most likely that the AE was caused by study drug; Possible = Reasonable suspicion that the AE was caused by the study drug; Unlikely = Slight but remote chance that the AE was caused by study drug but the balance of judgment is that it was most likely not due to the study drug.
Time frame: Upto Day 2