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양재현,김동수,류희두,이남희 ( Jae Heon Yang,Dong Su Kim,Hee Doo Yoo,Nam Hee Lee ) 한국약제학회 1996 Journal of Pharmaceutical Investigation Vol.26 No.2
Precipitation was formed during the preparation of decoction from a mixure of Scutellariae Radix and Coptidis Rhizoma or Phellodendri Cortex according to the prescription of Hwang-ryean-hae-dog-tang. Baicalin and berberine, the active ingredients of the two herbal medicine were identified in coprecipitated product. Pills were prepared using the coprecipitated product and various binders. The dissolution rate of baicalin and berberine from pills was increased in at pH1.2 when acacia or tragacanth was used. The absorption rate of baicalin from the coprecipitated product was faster than that from Scutellaria extract, but the absorption of berberine from CPP was slower in stomach, duodenum and jejunum of rats compared with Coptis extract. The time required for the maximum serum concentration (Cmax) of baicalin and berberine from CPP in mice were 150 and 200 min after oral administration, respectively. The maximum serum concentration of baicalin from CPP in mice was higher than Scutellaria extract, but the concentration of berberine was lower compared with Coptis extract. The minimum inhibitory concentration of CPP was below 50 ㎍/㎖ against gram positive bacteria, and was higher than that against gram negative bacteria. The antibacterial activity of CPP was lower than that of berberine, but was more potent than Scutellaria extract. It was found that the inhibition rates of growth by CPP against S. epidermidis, K. pneumoniae, B. cereus and S. aureus were 60.0, 51.1, 45.4 and 39.9%, respectively.
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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.
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양재헌,김동수,류희두,이남희 우석대학교 의약품개발연구소 1996 藥學硏究誌 Vol.1 No.-
Precipitation was formed during the preparation of decoction from mixure of Scutellariae Radix and Coptidis Rhizoma or Phellodendri Cortex according to the prescription of Hwang-ryean-hae-dog-tang. Baicalin and berberine, the active ingredients of the two herbal medicine were identified in coprecipitated product. Pills were prepared using the coprecipitated product and various binders. The dissolution rate of baicalin and berberine from pills was increased in at pH1.2 when acacia or tragacanth was used. The absorption rate of baicalin from the coprecipitated product was raster than the from Scutellaria extract, but the absorption of berberine from CPP was slower in stomach, duodenum and jejunum of rats compared with Coptis expract. The time equired for the maximum serum concentration (Cmax) of baicalin and berberine from CPP in mice were 150 and 200 min after oral administration. respectively. The maximum serum concentration of baicalin from CPP in mice was higher than Scutellaria extract, but the concentration of berberine was lower compared with Coptis extract. The minimum inhibitory concentration of CPP was below 50 ug/ml against gram positive bacteria, and was higher than that against gram negative bacteria. The antibacterial activity of CPP was lower than the of berberine.but was more potent than Scutellaria extract. It was found that the ingibition rates of growth by CPP against S. cpidermidis, K. pneumoniae, B cereus and S. aureus were 60.1, 5.11, 45.4, and 39.9%. respectively.
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바이칼린 함유 생약의 제제화 및 생체이용률(제 3 보);황금 및 황련 공침물의 포접화합물 제조 및 생체이용률에 관한 연구
양재헌,신상철,류희두 전남대학교 약품개발연구소 1997 약품개발연구지 Vol.6 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-D) 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-D 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.
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