Pharmacokinetics

Absorption Distribution Metabolism Excretion Special Population (N/A) Other Details

Absorption

Plasma Concentration

(5 healthy adults under fasting conditions, single administration of 5 mg of mosapride citrate)

Tmax (h) Cmax (ng/mL) T1/2 (h) AUC0-∞ (ngh/mL)
0.8±0.1 30.7±2.7 2.0±0.2 67±8

 

Distribution

Plasma Protein Binding Rate

99.0% [in vitro, human serum, at a concentration of 1 μg/mL, methods of ultrafiltration or equilibrium dialysis]


 

Metabolism

Metabolic Enzyme: Cytochrome P-450 sub-family: mainly CYP3A4.

Main metabolite: Des-4-fluorobenzyl-mosapride

Metabolic pathway: Mosapride citrate is metabolized mainly in the liver, where the 4-fluorobenzyl group is removed, followed by oxidation of the morpholine ring at position 5, and hydroxylation of the benzene ring at position 3.


 

Excretion

Excretion route: In urine and feces

Excretion rate: In urine collected for 48 hours after administration, 0.1% was excreted as unchanged compound and 7.0% was excreted as the main metabolite (des-4-fluorobenzyl mosapride). (Healthy adults, single administration of 5 mg of mosapride citrate under fasting conditions)


 

Special Population

N/A


 

Other details

Drug interactions

When erythromycin at 1,200 mg/day was concomitantly administered with this drug at 15 mg/day, in comparison with a single administration of mosapride, maximum blood concentration of mosapride increased from 42.1 ng/mL to 65. 7 ng/mL, the half-life was prolonged from 1 .6 hours to 2.4 hours and AUC0-4 increased from 62 ng•hr/mL to 114 ng•hr/mL. (Healthy adult).