퀘르세틴의 가용화, 퀘르세틴 및 루틴의 토끼 십이지장 점막 투과성

• 영문명: Solubilization of Quercetin, and Permeability Study of Quercetin and Rutin to Rabbit Duodenal Mucosa
• 발행기관: 대한약학회
• 저자명: 전인구(In Koo Chun) 서은하(Eun Ha Seo)
• 간행물 정보: 『약학회지』제42권 제1호 (1998년), 59~69쪽, 전체 11쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1998.01.31

영문 초록

To increase the solubility of quercetin, which is a practically insoluble flavonoid of Ginkgo biloba leaf, the effects of nonaqueous vehicles. Their cosolvents, water-soluble polymers and modified cyclodextrins (CDs) were observed. Polyethylene glycols, diethyleneglycol monoethyl ether, and their cosolvents with water showed a good solvency toward quercetin. Also the aqueous solutions of povidone, copolyvidone and Cremophor RH 40 was effective in solubilizing quercetin. Complex formation of quercetin with beta-cyclodextrin (beta-CD), dimethyl-beta-cyclodextiin (DMCD), 2-hydroxypropyl-beta-cyclodextrin (HPCD) and beta-cyclodextrin sulfobutyl ether (SBCD) in water was investigated by solubility method at 37oC. The addition of CDs in water markedly increased the solubility of quercetin with increasing the concentration. AL type phase solubility diagrams were obtained with CDs studied. Solubilizaton efficiency by CDs was in the order of SBCD >> DMCD > HPCD > beta-CD. The dissolution rates of quercetin from solid dispersions with copolyvidone, povidone and HPCD were much faster than those of drug alone and corresponding physical mixtures, and exceeded the equilibrium solubility (3.03+/-1.72mcg/ml). The permeation of quercetin through duodenal mucosa did not occur even in the presence of enhancers such as bile salts, but the permeation was observed when the mucus layer was scraped off. This was due to the fact that quercetin had a strong binding to mucin (58.5mcg/mg mucin). However rutin was permeable to the duodenal mucosa. The addition of enhancer significantly increased the permeation of rutin in the order of sodium glycocholate

키워드

Quercetin. rutin solubilization cosolvents cydodextrins duodenal permeation bile salts mucin binding.