Pharmacokinetic studies of Aloin and Isobarbaloin in Rabbits

• Main Authors: CHIA-HUI tsao, 曹嘉蕙
• Other Authors: 劉正雄
• Format: Others
• Language: zh-TW
• Published: 2006
• Online Access: http://ndltd.ncl.edu.tw/handle/06855234970416687491

碩士 === 中國醫藥大學 === 藥物化學研究所碩士班 === 94 === ABSTRACT Aloin and Isobarbaloin are major activity for anthraquinone derivative in Aloe. It’s hydrolysis to aloe-emodin-9-anthrone, and oxidant to aloe-emodin at intestine bacteria. They are widely used in the treatment of constipation and rectal operation. In clinic study, they have purgative、 anti-tumor、tissue healing、regular immune function、anti-dyslipidemia. In this study, we investigate pharmacokinetic relative studies of Aloin and Isobarbalon in Aloe’s target component. The high-performace liquid chromatographic method was developed for determination of Aloin and Isobarbaloin in rabbit blood. A HPLC system equipment, a Merk LiChrospher 100 RP-18e column with the mobile phase consisted of methanol-water (50:50) and UV detection wavelength at 359nm. The internal standard was 7-hydroxycoumarin and follow rate was 1.0ml/min. After IV administration of Aloin and Isobarbaloin mixture solution to six rabbits, the plasma level-time profiles of Aloin and Isobarbaloin were adequately described by an open two-compartment model. At the IV dose of 20 and 30 mg/kg, Aloin and Isobarbaloin result appear the mean terminal eliminate half-life（T1/2 β）were 54.1±28.4； 28.7±18.3 and 36.9±21.9；49.7±17.1 min, respectively. The mean area under the serum concentration curve（AUC0-∞）were about 411.655± 13.027；318.213±19.924 and 701.336±116.631；573.278± 86.870μg• min/mL, respectively. The mean drug clearance（CL）were 0.165±0.011；0.214±0.016 and 0.149±0.030；0.182±0.035 L/min, respectively. The result may be useful in support of the dosage forms design and clinic pharmacokinetic and provide study based for clinic trail and bioavailability in future.