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바이칼린 함유생약의 제제화 및 생체이용률 (제 1보): 황금 및 황련 공침물의 확인 및 물리화학적 성질
양재헌,김동수,박현구,이남희,Yang, Jae-Heon,Kim, Dong-Su,Park, Hyun-Goo,Lee, Nam-Hee 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.4
Precipitation was formed during the preparation of decoction from a mixture of Scutellariae Radix and Coptidis Rhizoma or Phellodendri Cortex according to the prescription of Hwang-ryean-hae-dog-tang. Baicalin and berberine were identified in coprecipitated product and these components were the active ingredients of two herbal medicine. The coprecipitated product was very slightly soluble in water and sparingly soluble in ethanol. The stoichiometric ratio of baicalin and berberine was found to be 1:1. The lipid-water partition coefficients of coprecipitated product were increased more than baicalin and berberine in chloroform, but were decreased in other organic solvents. The content of baicalin and berberine in coprecipitated product, determined by HPLC, were 23.08% and 26.75%, but the content of active ingredients in supernatant were 0.66% and 0.26%, respectively. The dissolution profile of baicalin of coprecipitated product was increased more than extract of Scutellariae Radix in artificial gastric juice, but was decreased in artificial intestinal juice. The dissolution rate of berberine of coprecipitated product was lower than extract of Coptidis Rhizoma in artificial gastric juice and intestinal juice commonly.
베르베린 제제의 생체이용율에 관한 연구 ( Ⅱ ) : 황련과 감초 공침물의 항균효과 및 생체이용율
양재헌,은재순,이남희 ( Jae Heon Yang,Jae Soon Eun,Nam Hee Lee ) 한국약제학회 1995 Journal of Pharmaceutical Investigation Vol.25 No.3
Precipitation reaction occurred between berberine in Coptidis Rhizoma and glycyrrhizin in Glycyrrhizae Radix when they were boiled together in aqueous solution and the supernatant solution thus obtained did not show any antibacterial activity which was derived from berberine. The content of berberine in BG and CGP by HPLC analysis were 41.1% 8.3% respectively. BG was occurred mostly at pH 5.0. The solubility of berberine was 0.15%, while that of BG and CGP was 0.07%. 0.12%. respectively. CGP shown more increased antibacterial activity to gram positive bacteria. S. dysenteriae and K. pneumoniae than berberine. The absorption rates of CGP in stomach, duodenum and jejunum of rats were compared with those of Coptidis Rhizoma water extracts (CR), which were increased more than CR. The time required for the maximum serum concentration of berberine from CGP in mice was 90 minutes after oral administration. The maximum serum concentration of berberine from CGP was higher than that from CR. The dissolution of CGP was increased more than berberine and BG in both artificial gastric and intestinal fluids. The dissolution of CGP pill made from gelatin was 63.4% in artificial gastric fluids and that made from CMC was 76.0% in artificial intestinal fluids.
양재헌,최철웅,김대근,이강노,지옥표,Yang, Jae-Heon,Choi, Cheol-Ung,Kim, Dae-Keun,Lee, Kang-Ro,Zee, Ok-Pyo 한국생약학회 1996 생약학회지 Vol.27 No.3
The studies were attempted to investigate the therapeutic effect of Solanum lyratum extract(SLE) on the liver damage induced by carbon tetrachloride in rats. Male rats (Sprangue-Dawley) were treated with subchronic concentration of $CCl_4$, which was 1 mg/kg of $CCl_4$ via per oral administration daily for three days. The level of serum cholesterol, transaminase, bilirubin and BSP were measured. Treatment of SLE significantly decreased the increment in serum transaminase activities, total cholesterol and enlargement of liver but serum bilirubin was not reduced. The protective effect was observed when SLE was given daily for 4 weeks after $CCl_4$ treated for 3 days. SLE administration to rats prevented the development of fatty change, necrosis, and fibrosis induced by $CCl_4$. The results suggest that SLE has appreciable therapeutic effect on $CCl_4$ induced hepatotoxicity.
황금 및 황련 공침물의 포접화합물 제조 및 생체이용률에 관한 연구
양재헌,신상철,류희두 ( Jae Heon Yang,Sang Chul Shin,Hee Doo Yoo ) 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.1
Precipitation was formed during the preparation of decoction from a mixture of Scutellariae Radix and Coptidis Rhizoma. Baicalin and berberine were identified in this coprecipitated product (CPP) and these components were the active ingredients of two herbal medicine. We extracted respectively crude baicalin and berberine in Scutellariae Radix and Coptidis Rhizoma and prepared coprecipitate of crude baicalin-berberine. To increase the stability and bioavailability of coprecipitate of crude baicalin-berberine(CBB), which is slightly soluble drug, its inclusion complex was prepared and studied in this experiment. Inclusion complex of CBB with β-cyclodextrin(CBB-β-CD) was prepared by freeze drying method and its characteristics were ascertained by means of solubility test, differential thermal analysis(DTA) and scanning electron microscope(SEM). The type of CBB-β-CD is classified as A_L-type on phase solubility diagram, and the stoichiometric ratio of CBB(baicalin in CBB) : β-CD complex is 1:1 and formation constant is 151 M^(-1). The solubility, dissolution, in situ absorption and serum concentration of CBB-β-CD were significantly increased when compared to CBB. Therefore enhanced bioavailability of CBB by inclusion complexation with β-cyclodextrin might be useful for dosage form design of active ingredients of two herbal medicine.
양재헌(Jae Heon Yang),김영일(Young Il Kim) 한국약제학회 1998 Journal of Pharmaceutical Investigation Vol.28 No.3
N/A The O/W and W/O emulsions containing Scutellariae Radix extract(SRE) which is very slightly soluble in oil phases and sparingly soluble in water phases, were prepared by homogenizing water and oil phases with emulsifier. The diameters of emulsion were ranged from 100 to 300 ㎛. The viscosity of W/O emulsion was higher than that of O/W emulsion. W/O emulsion was more stable than O/W emulsion which was gradually degraded when tested by centrifuge method and temperature tolerance method at 50℃. The antibacterial activity of two emulsions was not significantly different from that of aqueous solution of SRE, and showed similar MIC and bacterial growth inhibition rate.