Sulfamethoxazoleと Trimethoprimの研究 ラットにおける吸収, 分布, 排泄, 代謝に関する検討 : Trimethoprimについて
1973 年 21 巻 2 号 p. 229-231
詳細
1973 年 21 巻 2 号 p. 229-231
Absorption, distribution, excretion and metabolism of trimethoprim were studied in rats. Trimethoprim was absorbed rapidly and almost completely from the digestive tract, the half-life for absorption being 18 minutes.
The concentration of the drug in blood and tissues attained maximum at 20 minutes after oral administration, and thereafter decreased rapidly. The highest concentration was found in the kidney. Appreciable levels were found in the bone marrow, thyroid, liver and lung. The lowest drug concentration was noted in the brain.
Approximately 95 % of the radioactivity after oral administration of 14C-trimethoprim was recovered from the urine and feces within 72 hours. The urinary excretion is the major excretory route since more than 85 % of the total radioactivity recovered appeared in the 72 hour urine.
Metabolic pathways of trimethoprim consisted of O-demethylation, ring N-oxidation, α-hydroxylation and glucuronic acid conjugation. Intact trimethoprim accounted for about 30% of the radioactivity excreted in 8 hour urine.
The simultaneous administration of sulfamethoxazole did not influence the absorption, distribution, excretion and metabolism of trimethoprim in rat.
