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The median C max (the maximum plasma drug concentration) following oral dosing with 50 mg of sumatriptan is 29 ng/mL and the t max (the time to reach maximum plasma concentration) generally ranges from 0.5 to 3 h after administration of 25-, 50-, and 100-mg oral doses. It is currently marketed as oral, subcutaneous, intranasal, and suppository (limited distribution) formulations.Īfter oral administration, sumatriptan is rapidly absorbed and eliminated with a half-life of about 2 h. Sumatriptan, a selective agonist acting on vascular 5-hydroxytryptamine (5-HT1B/1D) receptors, has been found to be a safe and effective treatment for migraine attacks. The final model was validated through a visual predictive check and bootstrapping with no serious model misspecification. The creatinine clearance as a covariate significantly ( P < 0.01) influenced the absorption fraction ( f ). A total of 364 concentrations of sumatriptan were captured by a one-compartment model with first-order elimination, and a combined transit compartment model and first-order absorption with lag time was successful in describing the PK with multiple peaks in the absorption phase of sumatriptan. Population PK analysis was performed using plasma concentration data for sumatriptan with NONMEM (ver. Plasma sumatriptan concentrations were analyzed using UPLC/MS/MS. Plasma data obtained after a single 50-mg oral dose of sumatriptan in 26 healthy Korean male subjects were used. Despite its relatively high between-subject variability, few reports have addressed PK modeling of sumatriptan. Sumatriptan, a selective agonist for the vascular serotonin (5-HT1) receptor that causes vasoconstriction of the cerebral arteries, is used for the acute treatment of migraine attack with or without aura. The objective of this study was to develop a population pharmacokinetic (PK) model for sumatriptan, which frequently shows an atypical absorption profile with multiple peaks.