Ｕｌｉｎａｓｔａｔｉｎの生体内動態　（１）：　ラット，マウスおよびウサギにおける静脈内投与後の生体内動態

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  • Studies on the metabolic fate of ulinastatin (1): Pharmacokinetics in rats, mice and rabbits following a single intravenous dose.

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Blood or plasma concentration, distribution, metabolism and excretion of ulinastatin were investigated in rats, mice and rabbits after single intravenous administration of 125I-ulinastatin.<BR>1. After administration of 125I-ulinastatin to rats, mice and rabbits, blood or plasma levels of the radioactivity and that of the high molecular weight fraction decreased rapidly in biphasic manner. The half-lives of radioactivity in α and β phase were 4.2 ?? 9.5 min and 88 ?? 225 min, respectively. The half-lives of radioactivity of the high molecular weight fraction in α and β phase were 5.1 ?? 8.0 min and 32 ?? 80 min, respectively.<BR>2. At 2.5 min after administration of 125I-ulinastatin to male rats, high radioactivities were observed in the kidney, decreased rapidly like in case of the plasma.<BR>3. Within 168hr after administration of 125I-ulinastatin to rats, mice and rabbits, urinary and fecal excretion of radioactivity were 90.0 ?? 96.5% and 2.2 ?? 5.6% of the dose, respectively. Within 24hr after administration to male rats, biliary excretion of radioactivity was 2.9% of the dose.<BR>4. At 1 and 10 min after administration of 125I-ulinastatin to male rats, the radioactivity in the plasma was detected at the peak(67K peak) as a moiety with a molecular weight of ca. 67000 as same as that of ulinastatin determined by gel filtration chromatography. At 120 min after administration, the radioactivity in the plasma was detected at the peak (LMW peak) represented a compounds of a molecular weight less than 10000. Most of the radioactivity in the urine collected within 24hr after administration was detected at LMW peak on gel filtration chromatography, but the radioactivity was detected at 67K peak also.<BR>5. At 168hr after administration of 125I-ulinastatin to male rabbits, the radioactivity in the supernatant of centrifuged thyroid homogenate was detected at the peak with a molecular weight of ca. 670000 as same as that of thyroglobulin on the gel filtration high performance liquid chromatography.

収録刊行物

  • 薬物動態

    薬物動態 5 (5), 739-753, 1990

    日本薬物動態学会

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