Pharmacokinetics of a New Antigastritic Agent, Eupatilin, an Active Component of StillenE, in Rats

Jang, Ji-Myun; Park, Kyung-Jin; Kim, Dong-Goo; Shim, Hyun-Joo; Ahn, Byung-Ok; Kim, Soon-Hoe; Kim, Won-Bae

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자료유형: 학술저널

저자정보: Jang, Ji-Myun (Research Laboratory, Dong-A Pharmaceutical Company Ltd) Park, Kyung-Jin (Research Laboratory, Dong-A Pharmaceutical Company Ltd) Kim, Dong-Goo (Research Laboratory, Dong-A Pharmaceutical Company Ltd) Shim, Hyun-Joo (Research Laboratory, Dong-A Pharmaceutical Company Ltd) Ahn, Byung-Ok (Research Laboratory, Dong-A Pharmaceutical Company Ltd) Kim, Soon-Hoe (Research Laboratory, Dong-A Pharmaceutical Company Ltd) Kim, Won-Bae (Research Laboratory, Dong-A Pharmaceutical Company Ltd)

저널정보: 한국응용약물학회 The journal of applied pharmacology : the official journal of the Korean Society of Applied Pharmacology The journal of applied pharmacology : the official journal of the Korean Society of Applied Pharmacology 제11권 제3호

발행연도: 2003.1

수록면: 163 - 168 (6page)

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Pharmacokinetics of eupatilin (an active components of $Stillen^{\circledR}$, a new antigastritic agent) were investigated after both intravenous and oral administration at a dose of 30mg/kg to rats. After intravenous administration, the plasma concentrations of unchanged eupatilin declined rapidly with a mean terminal half-life of 0.101 h. Eupatilin was eliminated fast in rats; the total body clearance was 121 mL/min/kg. Eupatilin was mainly metabolized in rats; the percentage of intravenous dose of eupatilin excreted in 24 h urine and feces as unchanged eupatilin was only 2.5 and 0.919％, respectively. Eupatilin was mainly metabolized to form its glucuronide conjugate; after intravenous administration, 15.9 and 51.7％ of intravenous dose was excreted in 24 h urine and feces, respectively, as eupatilin plus its glucuronide. After oral administration, the absolute bioavailability was only 3.86％ based on $AUC_{0-24h}$ of eupatilin plus its glucuronide. Approximately 68.5％ of oral dose was not absorbed from the entire gastrointestinal tract. Therefore, it could be concluded that the superior effect of eupatilin in experimental animal models of gastric ulcer and inflammatory bowel disease after oral administration could be due to the local action of eupatilin. Further pharmacokinetic studies to elucidate the local action of eupatilin are required.

#eupatilin #Stillen $textregistered$ #pharmacokinetics #glucuronide conjugation #biliary excretion #rat

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