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베타-글루쿠로니다제에 의한 황련.황금 공침물의 가수분해 및 생체이용률 증가
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  • 베타-글루쿠로니다제에 의한 황련.황금 공침물의 가수분해 및 생체이용률 증가
저자명
김미정,김남순,김영일,김대근,양재헌,Kim. Mi-Jeong,Kim. Nam-Soon,Kim. Young-Il,Kim. Dae-Keun,Yang. Jae-Heon
간행물명
藥劑學會誌
권/호정보
2003년|33권 2호|pp.91-97 (7 pages)
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한국약제학회
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

During the preparation of decoction from the mixture of Coptidis Rhizoma and Scutellariae Radix, insoluble copreciptate was formed. The coprecipitated product (COP) was composed of berberine and baicalin which was the active ingredient of Coptidis Rhizoma and Scutellariae Radix, respectively. COP was slightly soluble in water and could not be well absorbed after oral administration. This poor bioavailibility might be associated with its poor aqueous solubility. With the purpose of increasing the solubility and bioavailibility of COP, hydrolysis of COP by ${eta}-glucuronidase$ was carried out. Hydrolyzed products (HOP) of COP were identified and assayed for active ingredients. The partition coefficient study, in situ absorption test, and pharmacokinetic study after oral administration were also performed. COP was found to be consisted of berberine and baicalin with molecular ratio of 1 to 1. This compound was hydrolyzed to berberine and baicalin by ${eta}-glucuronidase$. The rate of hydrolysis was higher at higher temperature up to $50^{circ}C$ and higher concentration of ${eta}-glucuronidase$ up to 2500 unit under our experimental conditions. Baicalein, which is more liphophilic than baicalin, showed greater absorption in small intestine than baicalin did. The plasma concentrations of berberine and baicalein after oral administration of HOP were significantly higer than those of COP. The possible mechanism of increased bioavailibility of berberine and baicalein could be the hydrolysis of COP by ${eta}-glucuronidase$. On the basis of the above results, it might be said that HOP should be a suitable preparation for increasing the bioavailibility of Coptidis Rhizoma and Scutellariae Radix.