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Flavonoids의 약리작용(V) - 전기자극 및 과민반응으로 유발된 흰쥐 회장의 평활근수축에서 Flavones 및 Flavonols의 진경효과 -
안홍직,이지윤,김수정,김정민,박주현,박성훈,심상수,김창종,Ahn, Hong-Zick,Lee, Ji-Yun,Kim, Soo-Jeong,Kim, Jung-Min,Park, Ju-Hyun,Park, Sung-Hun,Sim, Sang-Soo,Kim, Chang-Jong 대한약학회 2007 약학회지 Vol.51 No.2
Some flavonoids have spasmolytic activities in various smooth muscles, but structure-activity relationships on their spasmolytic activity and its mechanism are unclear. In this study, effects of flavones (flavone and apigenin) and flavonols (quercetin and rutin) on the rat ileal smooth muscle contraction were studied in vitro and in vitro. In the electric stimulation-induced contraction, all of four flavonoids inhibited concentration-dependently the rat ileal smooth muscle contraction induced by electric stimulation (10 mV, 0.1 cps, 0.1 msec duration), IC$_{50}$ of quercetin, apigenin, flavone and rutin were 0.98${\times}$10$^{-5}$, 1.20${\times}$10$^{-5}$, 1.55${\times}$10$^{-5}$ and 1.85${\times}$10$^{-5}$ M, respectively. Flavonoids at a concentration of 2${\times}$10$^{-5}$ M also significantly inhibited the anaphylactic contraction and decreased concentration-dependently the mast cell degranulation by anaphylactic reaction, IC$_{50}$ of quercetin, apigenin, flavone and rutin were 4.0${\times}$10$^{-5}$, 7.5${\times}$10$^{-5}$, 8.0${\times}$10$^{-5}$ and 9.5${\times}$10$^{-5}$ M, respectively. These results indicated that flavones and flavonols inhibited the rat ileal smooth muscle contraction induced by electric stimulation because of their antagonism against acetylcholine and have spasmolytic activities on anaphylactic contraction which may be due to their mast cell-stabilizing activities. Furthermore, double bond of C$_{2,3}$ in benzene ring of flavonoids may be important in the their antispasmodic activities on the rat ileal smooth muscle contraction induced by electric stimulation and anaphylactic reaction.
시클로덱스트린과의 포접에 의한 케토고나졸의 비점막 흡수증가
박기배,이광표,노현구,안홍직,서보연,온윤성 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.2
Inclusion complexes of ketoconazole(KT) with α^-, β^- cyclodextrin(CD) and dimethyl-β-cyclodextrin (CD) and dimethyl-β-cyclodextrin(DMβCD) as nasal absorption enhancer were prepared in 1:2 molar ratios by freeze-drying and solvent evaporation methods. In order to compare with the intrinsic absorptivity of KT in the jejunum(J) and the nasal cavity(N), the in situ simultaneous perfusion method was employed. The in situ recirculation study revealed that KT-CD inclusion complexes with the greater stability constant and the faster dissolution rate proportionally increased the absorption of KT in the J and N of rats. The rank order of apparent KT permeability(P_(app) : ㎝/sec × 10^(-5)±S.E.), corrected by surface area of absorption, was 5.10±0.3(N, KT-DMβCD) >4.13±0.4(N, KT-β-CD) >3.52±0.2(N, KT-α-CD) >2.76±0.3(J, KT-DMβCD) >2.61±0.5(J, KT-β-CD) >2.42±0.4(J, KT-α-CD) at pH 4.0. The in crease in permeability of KT-DMβCD inclusion complex was 2.6 folds in the J and 4.5 folds in the N when the perfusing solution was changed from the buffer(pH 4.0) to saline. The absorption rate of KT-DMβCD inclusion complex after nasal administration was more rapid than those of ketoconazole alone and KT-DMβCD inclusion complex after oral administration to rats. In comparision with an oral administration of ketoconazole suspension in corn oil, the relative bioavailability was calculated 137.3% for the oral and 195.0% for nasal KT-DMβCD inclusion complex in rats. The present results suggest that KT-DMβCD inclusion complex may serve as a potential nasal absorption enhancer for the nasal delivery of ketoconazole.
시클로덱스트린과의 포접에 의한 케토코나졸의 용해성 및 용출 증가
장영수,박기배,이광표,안홍직,서보연 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.2
Inclusion complexes of ketoconazole (KT) with α-, β-cyclodextrin (CD) and dimethyl-β-cyclodextrin (DMβCD) in a molar ratio of 1:2 were prepared by freeze-drying and solvent evaporation methods. The interactions of KT with α-CD, β-CD and DMβCD in aqueous solution and in solid state were investigated by solubility study, infrared (IR) spectroscopy and differential scanning calorimetry (DSC). The stability constant of KT-DMβCD inclusion complex (IC) was found to be the largest among three inclusion complexes. Clear differences in IR spectra and DSC curves were observed between inclusion complexes and physical mixtures (PM) of KT-CDs. It was also shown by IR spectra and DSC curves that solvent evaporation method might be superior to the freeze-drying method in preparing the inclusion complexes of KT-CDs. The dissolution rate of KT was markedly increased by inclusion complex formation with CDs in the buffer solution at pH 4.0 and pH 6.8. The mean dissolution time (MDT, min), which represents the rapidity of dissolution, was in the order of KT-DMβCD IC (3.20) < KT-β-CD IC (4.36) < KT-α-CD IC (6.99) < KT-α-CD PM (17.46) < KT-β-CD PM (19.36) < KT-DMβCD PM (28.53). The dissolution rates of KT-CD ICsprepared by solvent evaporation method were faster than those of KT-CD ICs prepared by freeze-drying method.