회원 학술보고 : 포스터 발표 / 18. 바이칼린 함유생약의 제제화 및 생체 이용률에 관한 연구 (2)

양재헌(Jae Heon Yang),김동수(Dong Su Kim),이남희(Nam Hee Lee),박현구(Hyun Goo Park) 한국약제학회 1993 한국약제학회 총회 및 학술대회 요지집 Vol.- No.23

황금 및 황련 공침물의 확인 및 물리화학적 성질

양재헌(Jae - Heon Yang),김동수(Dong - Su Kim),박현구(Hyun - Goo Park),이남희(Nam - Hee Lee) 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.

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.

황금 및 황련 공침물의 장내 흡수 및 항균 효과

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.

치자엑스 가수분해물 제제의 피부투과 및 생체 피부조직과의 교차결합에 관한 연구

양재헌,이남희 한국약제학회 2005 Journal of Pharmaceutical Investigation Vol.35 No.1

Gardeniae Fructus is consisted of geniposide and its derivatives. For the purpose of treatment of skin disease, geniposide and hydrolyzed products (HP) of Gardeniae Fructus were studied on skin permeation and crosslinking with biological tissue. The hydrolyzed products (HP) and active ingredients of Gardeniae Fructus were identified and investigated about skin permeability. Genipin has provided low cytotoxic crosslinking reagents and formed stable and biocompatible crosslinked products. The permeation enhancing effects of geniposide and genipin under the hydrolyzed products of cream and hydrogel preparations were tested using Franz type diffusion cell and the skin of hairless mouse. The remaining pro-portions of geniposide and genipin were measured in the hydrolyzed products of cream and hydrogel preparations. The crosslinking of epidermic and endodermic tissue with genipin under the hydrolyzed prodcuts of cream and hydrogel preparation was observed using light microscopy. Increased absorption ratio of the skin of hairless mouse about genipin was higher than that of geniposide. Loads at break, tensile strengths and skin permeation rate of the hydrolyzed products (HP) of cream and hydrogel preparations were higher than the nonhydrolyzed products (NHP). The hydrolyzed products (HP) of cream and hydrogel of Gardeniae Fructus Extracts were proper preparations and crosslinking agents to increase the trans-dermal absorption with epidermic and endodermic tissue.

치자 엑스의 가수분해에 의한 피부투과 및 항염효과

양재헌,이남희 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.2

Geniposide and its related iridoid compounds have been used in traditional herbal medicine for the treatment of Jaundice hepatic diseases and various inflammatorys. For the purpose to increase trandsdermal absorption, the hydrolyzed products of Gardeniae Furcuts were identified and assayed of active ingredients and investigated trandsdermal absorption and anti-inflammatory effects. Geniposide was hydrolyzed to genipin by β-glucosidase and it was suggested that genipin was more suitableform than geniposide for transdermal absorption by its lipophilic property. Using Franz type diffusion cell and the skin of hairless mouse, the permeation rate of hydrolyzed products and their emulsion preparation were determined. Genipin have more increased absorption ratio through the skin hairless mouse than geniposide. Also, the emulsion of hydrolyzed products of extracts showed higher permeability than that of nonhydrolyzed preparations. After 9 hours 280.85 ㎍/㎠ of genipin was absorbed and 193.52 ㎍/㎠ in case of geniposide. The Js of geniposide and genipin were 26.27±4.11 ㎍/㎠/hr and 40.35±5.04 ㎍/㎠/hr respectively. After carrageenan injection, the swelling was increased rapidly to 24 hr and maintained as a plateau. But emulsion group were reached about 2.5 mL and the swelling decreased successively from 24 hr to 72 hr. The anti-inflammation effects of extracts and hydrolyzed products emulsion were increased with significant difference with control group after 24 hr, 48 hr and 72 hr. In carrageenan induced edema, inhibition of swelling was increased in case of hydrolyzed product emulsion compare with nonhydrolyzed group at 24 hr, 48 hr and 72 hr after swelling. In histological study, the anti-inflammatory effects of hydrolyzed products were remarkable at 48 hr and 72 hr compare with nonhydrolyzed. Hydrolyzed products of Gardeniae Frucuts extract containing genipin would be a suitable preparation to increase the transdermal absorption and anti-inflammatory effects.

바이칼린 함유 생약의 제제화 및 생체 이용률 (제 2보) : 황금 및 황련 공침물의 장내 흡수 및 항균 효과 Gastro-Intestinal Absorption and Antibacterial Effect of Coprecipitated Product of Scutellariae Radix and Coptidis Rhizoma

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.