• Journal of Pharmaceutical Investigation
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• 제21권4호
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• pp.223-230
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• 1991

The structural specificity and the chemical dynamics between ${\beta}-cyclodextrin$ and aspirin were studied by FT-IR UN, $^1H$ NMR. $^{13}C NMR$. and FAB-MS spectroscopy in solution and solid state, A stable solid inclusion complex was prepared by the recrystallization method, From the spectral changes of the host and guest molecules, orientational preference for binding in the cyclodextrin cavity was determined.

• Journal of Pharmaceutical Investigation
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• 제1권1호
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• pp.22-29
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• 1971

Barbituric acid 및 thiobarbituric acid 유도체와 beta-cyclodextrin과의 상호반응(相互反應)을 수용액(水溶液)과 유기용매중(有機溶媒中)에서 각(各) 약물(藥物)을 용해도(溶解度), 분자용(分子容), 열역학적(熱力學的)인 면(面)에서 분석(分析) 검계(檢計)하였다. 본실험(本實驗)에 사용한 약물(藥物)이 모두 용액(溶液)에서는 beta-cyclodextrin과 반응(反應)하여 용해도(溶解度)가 증가(增加)하였으며 고형(固型)의 침전을 형성(形成)하지는 않았으나 비교적(比較的) 안정(安定)한 회합(會合)이 이루어졌다. 본반응(本反應)의 기전(機轉)은 주(主)로 beta-cyclodextrin의 주요(主要)한 성질(性質)의 하나인 inclusion능(能)에 의(依)하여 이루어 졌음을 보고(報告)한다.

• Journal of Pharmaceutical Investigation
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• 제30권1호
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• pp.33-37
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• 2000

One of the methods to increase the solubility of a drug is to use complexation with a cyclodextrin. Due to the hydrophobic nature of the interior cavity of the cyclodextrin, it has been known that undissociated lipophilic drugs can be included within the cyclodextrin by hydrophobic interaction. Recently, inclusion of hydrophilic or dissociated form of a drug has been investigated. In this study, the synergism of pH and complexation with $hydroxypropy-{\beta}-cyclodextrin\;(HP\;{\beta}\;CD)$ to increase the solubility of two oxicam derivatives was investigated. In addition, the effect of partition coefficient of dissociated and undissociated form of the drug on the extent of complexation with HP ${\beta}$ CD was studied. The solubility was measured by equilibrium solubility method. The solubility of tenoxicam and piroxicam increased exponentially with an increase in solution pH above the pKa of the drug in the presence and absence of HP ${\beta}$ CD. The solubility of the drugs increased linearly as a function of HP ${\beta}CD$ concentration at fixed pH. Although the stability constant of ionized species is less than that of the unionized species, the concentration of the ionized drug complex is greater than that of the unionized drug complex due to higher concentration of ionized species at pH 7.3.

• Food Science and Biotechnology
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• 제17권4호
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• pp.700-704
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• 2008

Anti-obesity effects of $\beta$-cyclodextrin in obese C57BL/6J mice induced by a high fat diet (HD) were observed. The administration of $\beta$-cyclodextrin reduced the gain of body weight, abdominal fat, liver weight, the lipid deposits of hepatocytes and the size of adipocytes in the HD group. In serum analysis, the total and low-density lipoprotein-cholesterols were significantly decreased in the $\beta$-cyclodextrin-supplemented HD group than in the HD group. However, high-density lipoprotein-cholesterol was not changed in these groups. In hypothalamic homogenates, the decrease of neuropeptide Y and increase of $\alpha$-melanocyte stimulating hormone were detected in the $\beta$-cyclodextrin-supplemented HD group compared to that in the HD group. These effects of $\beta$-cyclodextrin were similar to those of Garcinia cambogia, which is widely used as a natural anti-obesity product. These results suggest that $\beta$-cyclodextrin has anti-obesity effects through the lowering of the abdominal fat pad and inhibits the central effects of hunger.

• 공업화학
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• 제18권4호
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• pp.326-329
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• 2007

수용액 상에서 ${\beta}$-cyclodextrin에 2,4'-dibromoacetophenone (8)을 반응시켜 착물을 형성한 후 arylidenethiosemicarbazone 7a-f를 가하여 2-arylidenehydrazinyl-4-arylthiazole 유도체들 9a-f를 70~88% 수율로 합성하였다. 합성한 새로운 화합물들 9a-f의 구조를 IR과 $^1H-NMR$ 스펙트럼 자료로 확인하였다. 이와 같은 실험결과 ${\beta}$-cyclodextrin의 역할은 반응물 7 및 8의 활성화로 반응을 촉진시켜 반응시간이 단축되는 것으로 나타났다.

• 약학회지
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• 제38권1호
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• pp.78-85
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• 1994

From phase solubility studies bile acids and bile salts were found to form stable inclusion complexes with ${\beta}-cyclodextrin$ in aqueous solution. Stability constant of bile acids were larger than that of bile salts. Phase solubility diagrams of most bile acids showed Higuchi's $A_I$ type but lithocholic acid showed $B_S$ type. Not only the solubility of bile acids but also that of ${\beta}-cyclodextrin$ increased, especially in cases of cholic acid and ursodeoxycholic acid. Solubility increase of bile acids from their ${\beta}-cyclodextrin$ inclusion complex followed the order : cholic acid>ursodeoxycholic acid>chenodeoxycholic acid>deoxycholic acid>lithocholic acid. It seems that solubility of inclusion complexes was directly related with the hydrophilicity of bile acids.

• Journal of Pharmaceutical Investigation
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• 제17권2호
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• pp.75-78
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• 1987

The release rate of heparin from monolithic devices composed of raffinose, ${\beta}-cyclodextrin$, polyethylene oxide (Mw 20,000, PEO), and hydrophobic polyether urethane (biomer) was investigated. Water soluble raffinose, ${\beta}-cyclodextrin$, and PEO blended into the biomer provided a controlled release of heparin. The release rate of heparin could be controlled by the content of raffinose, ${\beta}-cyclodextrin$, and PEO in the devices. The mechanism of release rate increased by the raffinose, ${\beta}-cyclodextrin$, and PEO may result from the formation of channels and pores in the biomer matrices following the swelling and the change in the physical structure of polymer net work. Hydrophobic polyurethane containing raffinose, ${\beta}-cyclodextrin$, and PEO can provide a hydrophilic antithrombogenic material for prolonged release of heparin.

• Macromolecular Research
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• 제14권4호
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• pp.443-448
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• 2006

A novel ${\beta}$-cyclodextrin derivative (CCD-C) was synthesized with chitosan and carboxymethyl-${\beta}$-cyclodextrin. Its structure was characterized by elemental analysis, infrared spectra analysis, and X-ray diffraction analysis. The adsorption properties for guanosine 5'-monophosphate, cytidine 5'-monophosphate and uridine 5'-monophosphate were studied. Experimental results demonstrated that CCD-C had higher adsorption capability for guanosine 5'-monophosphate, and that the adsorption capacity for guanosine 5'-monophosphate was 74.20mg/g. The adsorption capacity was greatly influenced by pH, time and temperature. The introduction of chitosan enhanced the adsorption ability and adsorption selectivity of ${\beta}$-cyclodextrin for guanosine 5'-monophosphate. This novel derivative of chitosan is expected to have wide applications in the separation, concentration and analysis of nucleotides in biological samples.

• Archives of Pharmacal Research
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• 제10권2호
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• pp.69-74
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• 1987

The characteristics of zipeprol-$\beta$-cyclodextrin system were studied by circular dichroism, competitive UV method and dialysis method. In this experiment, binding constants by competitive UV method, circular dichroism and dialysis method were 155 M$^{-1}$ 187 M$\^{-1}$/($\pm$ 5%) and 315 $^{-1}$, repectively. It shows that zipeprol forms 1:1 compelx with $\beta$-cyclodextrin by circular dichroism and 1:2 by dialysis method. pH profile shows that binding force seems to be a hydrophobic interaction. It is suggested that benzene ring be accomodated in the cavity of $\beta$-cyclodextrin.

• 한국미생물·생명공학회지
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• 제19권4호
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• pp.362-367
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• 1991

Pullulanase 생산균으로서 토양으로부터 분리한 Aeromonas caviae No.S-76을 진탕배양하여 얻은 조효소액을 ammonium sulfate 침전, DAEA Sephadex A-50 column chromatoraphy, Sephadex G-150 column chromatography에 의하여 정제하였다. 이때 수율은 21이었고 50배의 정제도를 가진 효소단백질을 얻었다. 정제효소는 SDS-polyacrylamide slab gel 정기영동에 의하여 분자량 118,000의 단일단백질이었고, 등전점은 4.3, 작용 최적온도는 $50^{\circ}C$, 작용 최적 pH는 8.0이었다. 또한 이효소는 $45^{\circ}C$ 이하, pH 6.0-90. 범위에서 안정성을 나타내었다. 이 효소를 $\beta$-cyclodextrin과 maltose의 고농도 혼합액에서 작용시켜 maltosyl-$\beta$-cyclodextrin을 합성하였다.