YH1885의 체내동태(제1보) : 흰쥐에서 14C-YH1885의 단회투여시 흡수, 조직분포 및 배설

• 영문명: Pharmacokinetic Study of YH1885 (I) : Absorption, Distribution and Excretion of 14C-YH1885 in Rats
• 발행기관: 대한약학회
• 저자명: 안병락(Byung Nak Ahn) Naoki Fujio Naotoshi Kusumoto Yoshifumi Abe Masaaki Odomi 이종욱(Jong Wook Lee)
• 간행물 정보: 『약학회지』제41권 제3호 (1997년), 335~344쪽, 전체 10쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1997.06.30

영문 초록

The absorption, distribution and excretion of 14C labeled YH1885 {5,6-Dimethyl-2(4-fluorophenylamino)-4-(1-methyl-1,2,3,4-tetrahydroisoquinolin-2-yl)pyrimidine hydrochloride), a new proton pumpinhibitor, were investigated in rats after a single administration of 14C-YH1885. 1. After intravenous administration of 5mg/kg, the blood level of radioactivity declined in a biphasic fashion with the mean terminal elimination half-life of 12.4hr. 2. After oral administration of 20mg/kg, the maximum blood level of radioactirity was reached at 4.0hr in female rats. The blood level of radioactivity-time profiles in male and female rats were similar, and the absorptionof 14C-YH1885 was not affected by food. 3. Appproximately 89% and 1% of radioactivity of the total dose were excreted in feces and urine, respectively. 4. Biliary excretion of radioactivity was 47.9% of the dose. Enterohepatic circulation of radioactivity was 49.6%. 5. Radioactivity was excreted maily into feces via bile. 6. The concentration of radioactivity in most tissues reached the peak level at 4.0hr after dosing, and then declined. Autoradiograms of male rats showed that the radioactivity levlels in the fat, harder's gland, liver and G-Itract were higher than those in the other tissues and the elimination of radioactivity from fat and liver was slow. 7. Autoradiograms of a pregnant rat showed that radioactivity was transferred to mammary gland, placenta and fetus. The radioactivity level in the mammary gland was higher than that in the blood.

키워드

5.6-Dimethyl-2-{4-fluorophenylamino)-4-(l-methyl-l,2.3,4-tetxahydroisoquinolin-2-yl)pyrimidine hydrochloride YH1885 Blood concentration Distribution Excretion Pregnant rat Autoradiogram Rat.