タイトル無し

概要

論文の詳細を見る
Blood and urine levels of malotilate (NKK-105) (unchanged) and its metabolites after single oral administration of malotilate 100 mg, 200 mg and 400 mg or repeated administration in a single dose of 200 mg three times daily for seven days.were determined for the purpose of elucidating the in vivo behavior of malotilate in normal adults. After administration, malotilate was absorbed rapidly and well, but its in vivo metabolism was rapid and the blood malotilate level was very low. In blood, malotilate was mostly present as hydrolyzed metabolites (isopropyl hydrogen 1, 3-dithiol-2-ylidenemalonate: M-1) but it cleared up rapidly.In urine, it was excreted as glucuronic acid conjugate of M-1 (M-3). The blood levels of unchanged malotilate and M-1 was increased along with the doses from 100mg to 400mg. The rate of excretion of M-3 and isopropyl hydrogen malonate (M-6) into urine remained almost constant irrespective of the doses. With the two metabolites put together, the rate of urinary excretion was between 37%and 48%. As to the influence of meal on absorption, the maximum blood level of malotilate and M-1 was slightly higher and the half-life was shorter on postprandial administration than fasting administration, but there was no significant difference in the area under the curve of blood concentration (AUC). Where malotilate was administered repeatedly three times daily for seven days, changes in the levels showed the same pattern daily, there being no chronological accumulation of blood concentrations of malotilate and M-1. Chronological changes in the urinary excretion of M-3 and M-6 were hardly observed in both cases. That is, there is no difference in vivo behavior of malotilate between single administration and repeated administrations. These results suggest that malotilate is almost devoid of the tendency to accumulate in the body.
一般社団法人日本臨床薬理学会の論文

タイトル無し

スポンサーリンク

概要

著者

関連論文

スポンサーリンク