리포좀에 봉입된 5-플루오로우라실 프로드럭의 약물 동태 및 장기 분포

• 영문명: Pharmacokinetics and Tissue Distribution of 5-Fluorouracil Prodrugs Entrapped in Liposome
• 발행기관: 대한약학회
• 저자명: 이계원(Gye Won Lee) 지웅길(Ung Kil Jee)
• 간행물 정보: 『약학회지』제40권 제5호 (1996년), 532~538쪽, 전체 7쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1996.10.31

영문 초록

In cancer chemotherapy, it is necessary to control the phamacokinetic behavior of an antitumor drug for effective treatment. Therefore, two 5-fluorouracil derivatives synthesized with N-a-cyloxycarbonyl derivatives {1-(N-t-butyloxycarbonyl)leucyloxymethyl-5-FU(BLFU) and 1-(N-t-carbobenzyloxymethyl)leucyloxymethyl-5-FU(CLFU)}. prodrugs of 5-fluorouracil, antitumor agent, were loaded into liposome of different lipid compositions. After liposomal drugs were injected intramuscularly, their pharmacokinetics and tissue distribution were assessed. The AUC0->infinity values were 1.29, 72.50, 85.57, 66.40 and 103.60mcg.hr/ml for 5-FU, BLFU, CLFU, BLFU- and CLFU-loaded liposome, respectively. 5-FU was distributed to spleen and liver with a maximal concentration after 1 hr and eliminated after 24 hr. But both prodrugs and dimyristoylphosphatidylcholine liposome entrapped prodrugs were distributed to spleen and liver at a lower concentration but maintained for a long time with a relatively high concentration in lung. Especially, liposome-entrapped CLFU was distributed to lung with a maximal concentration after 1 hr and redistributed to spleen increasingly, while the concentration of liposome-entrapped BLFU in lung reached a maximal level after 12 hr.

키워드

5-FU prodrugs of 5-FU liposome pharmacokinetics tissue distribution.