當歸有效成分阿魏酸（Ferulic acid）在家兔之藥物動力學及生體可用率研究; Pharmacokinetics and Bioavailability Studies of Ferulic Acid in Rabbits

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Title:	當歸有效成分阿魏酸（Ferulic acid）在家兔之藥物動力學及生體可用率研究;Pharmacokinetics and Bioavailability Studies of Ferulic Acid in Rabbits
Authors:	陳照賢;Chen Chao-hsien
Contributors:	中國醫藥學院中國藥學研究所
Keywords:	阿魏酸;藥物動力學;生體可用率;高效液相層析;兔子;Ferulic acid;Pharmacokinetics;Bioavailability;HPLC;Rabbit
Date:	1990
Issue Date:	2009-12-02 11:53:38 (UTC+8)
Abstract:	中文摘要阿魏酸是中藥當歸、川芎等有效成分之一，具有抗氧化及抗發炎增強巨噬細胞吞噬作用，抑制血小板凝集等藥理活性。本研究中對於阿魏酸在家兔體內之藥物動力學與生體可用率進行評估。阿魏酸之血漿檢品經除蛋白後，利用Merck LiChrospher® 100 RP-18 （(125 ´ 4 mm) ，5mm ）層析管，移動相為氰甲烷：水=13:87（pH=3.45），流速1.0 ml/min，以3-hydroxybenzaldehyde溶液為內標準品，偵測UV波長為322nm，最低偵測濃度為0.05 mg/ml，回收率為95﹪以上，同日及間日之精確度試驗其變異係數(C.V.%)均在10﹪以下，故本法足以應用於阿魏酸之定量分析。家兔在注射阿魏酸（2、10、50 mg/Kg）後，藥物動力學的研究結果顯示，可以二室體模式描述。平均曲線下面積分別為63.9、333.3、1569.6 µg.min/ml；呈線性關係。平均半衰期分別為31.8、35.4、40.2分鐘。在肌肉注射（50 mg/Kg）後，血中濃度以二室體模式。生體可用率約為61﹪。家兔口服阿魏酸液後，血中濃度以二室體模式配適。口服之生體可用率約為29﹪。; ABSTRACT Ferulic acid, an active constituent found in the root or rhizoma of Angelica sinensis DIELS. and Ligusticum wallichii FRANCH. possesses antioxidative, antiinflammatory and anticoagulant effects. In this study, the pharmacokinetics and bioavailability of ferulic acid in rabbits were evaluated. A simple high performance liquid chromatographic method involving UV detection was modified for determination of ferulic acid in rabbits plasma. A Lichrospher 100 RP-18 column （125 mm×4 mm, 5 mm）was used as the stationary phase and mobile phase consisted of acetonitrile and phosphoric acid solution （13：87,pH＝3.45）with flow rate at 1.0 ml/min. and 3-hydroxybenzaldehyde solution as the internal standard.The UV absorbance monitored 322 nm . After analysis limit of quantitation was 0.05 mg/ml , recovery was 95﹪.The coeffcient for within-run and between-run precison and accuracy was less 10﹪.There date inducates this modified method was enough for a quantitative analysis of ferulic acid. The pharmacokinetics of ferulic acid in the rabbit after intravenous bolus administration of various doses (2, 10 and 50 mg/kg) were well described by a two compartment model. The elimination half-lives were 31.8, 35.4 and 40.2 minutes；the mean AUCs were 63.9, 333.3 and 1569.6 µg.min/ml respectively.The results indicated that the pharmacokinetics of ferulic acid after I.V. administration are linear over the 2-50 mg/kg dose range. The bioavailability of ferulic acid in rabbits after I.M. administered of 50 mg/kg dose was 61%. However, after oral administration of 100 mg/kg dose of the same preparation, the bioavailability was only about 29%.
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