Enhancement of methotrexate absorption by subdivision of dose.
A comparison was made in fasting patients between a single 100 mg oral dose of methotrexate formulated as its sodium salt in a palatable syrup and the same total quantity of drug administered in four divided doses of 25 mg taken at 2-h intervals. Allocation to the order of these treatment schedules was on a random basis. The area under the serum methotrexate concentration-time curve until 50 h was found to be considerably greater after the divided dose regimen, the mean ratio AUC 25 mg x 4/AUC 100 mg being 1.86 (+/- 0.90). There was no significant difference in peak serum methotrexate concentrations or methotrexate half-life estimates between the two regimens, however. The results of this study are consistent with saturation of an intestinal transport process when methotrexate is administered orally in a single large dose.
D006207:Half-Life; D006801:Humans; D007408:Intestinal Absorption; D008727:Methotrexate / Q000008:administration & dosage* / Q000378:metabolism / Q000627:therapeutic use; D009369:Neoplasms / Q000188:drug therapy; D013997:Time Factors
D008727:Methotrexate