This study aims to determine the relative bioavailability of two candidate formulations of mosapride citrate 5mg tablets compared the reference product GASMOTIN (mosapride citrate 5mg) from Dainippon Pharmaceutical Company in healthy adult subjects. This will be an open-label, randomised, single dose, three-way crossover, six sequence study. Subjects will receive a single oral dose separated by at least 7 days and no greater than 14 days washout period. This study is required to select a candidate mosapride citrate (GR107719B) formulation for further development and provide data to allow the design of a future pivotal bioequivalence study. The candidate formulations will be compared with the innovator GASMOTIN. GASMOTIN is a trademark of Dainippon Sumitomo Pharmaceutical Company.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
18
Reference mosapride citrate (GASMOTIN) 5mg will be supplied as caplet shaped tablet embossed with P218 and film-coated; administer orally with approximately 240 mL of water.
GR107719B (Formulation 1) 5 mg will be supplied as L-HPC disintegrant caplet shaped tablet, embossed and film-coated; administer orally with approximately 240 mL of water.
GR107719B (Formulation 2) 5 mg will be supplied as caplet shaped tablet, embossed and film-coated; administer orally with approximately 240 mL of water.
GSK Investigational Site
Hyderabad, India
Composite of pharmacokinetics (PK) parameters of mosapride following administration of two candidate tablet formulations of mosapride citrate (GR107719B) relative to reference mosapride citrate (GASMOTIN)
PK parameters include: area under the concentration-time curve from time zero (pre-dose) extrapolated to infinite time \[AUC(0-infinity)\] and area under the concentration-time curve from time zero (pre-dose) to last time of quantifiable concentration \[AUC(0-t)\]
Time frame: Day 1 of each treatrment period (Pre dose and 0.25 hour (h), 0.5 h, 0.75 h, 1 h, 1.33 h, 1.67 h, 2 h, 2.5 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, 24 h post dose)
PK parameters of two candidate tablet formulations of mosapride citrate (GR107719B) relative to reference mosapride citrate tablets (GASMOTIN)
PK parameters include: Percentage of AUC (0-∞) obtained by extrapolation (%AUCex) time of occurrence of Cmax (tmax), terminal phase half-life (t1/2).
Time frame: Day 1 of each treatrment period (Pre dose and 0.25 hour (h), 0.5 h, 0.75 h, 1 h, 1.33 h, 1.67 h, 2 h, 2.5 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, 24 h post dose)
Safety and tolerability assessment as assessed by review of adverse events (AEs)
Time frame: Up to 51 days
Safety and tolerability assessment as assessed by vital signs
Vital sign measurements will include systolic and diastolic blood pressure, and pulse rate.
Time frame: Up to 51 days
Safety and tolerability assessment as assessed by clinical laboratory values
Clinical laboratory assessments will include hematology, clinical chemistry, routine urinalysis and additional parameters.
Time frame: Up to 51 days
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