1-Hexylcarbamoyl-5-fluorouracil (HCFU) の体内分布と活性化
1981 年 12 巻 2 号 p. 233-243
詳細
1981 年 12 巻 2 号 p. 233-243
In vivo distribution and the activation of HCFU were studied by using rabbitsand mice bearing Sarcoma 180 following oral administration, and the phamacokineticbehaviours were compared with other masked type derivatives of 5-FU.
HCFU was absorbed gradually from gastrointestinal tracts, and HCFU and theoxidation products (CPEFU, CPRFU, etc.), (HCFU fraction) persisted for severalhours in the tissues and they were successively converted to 5-FU.
HCFU fraction and 5-FU distributed highly in the stomach, kidney and urinebladderand slightly in the brain and spleen. A relative high concentration of 5-FUwas detected in the tumor tissues and lung, lip, rectum, skin, etc.
5-FU level in the tumors was elevated by co-administration of HCFU withthymine, thymidine or uracil. Among them, thymine had the strongest effects toincrease 5-FU level and anticancer activities to Sarcoma 180.
The production of 5-FU from HCFU was not influenced by pre-treatments ofphenobarbital and glutathione, or CCl4. This indicates that the activation of HCFU is not mainly depend to the liver.
