• Title/Summary/Keyword: cyclodextrins

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Studies on Inclusion Compounds of Suprofen with Cyclodextrins (Suprofen과 Cyclodextrin과의 포접화합물(包接化合物)에 관(關)한 연구(硏究))

  • Han, Soon-Young;Yong, Jae-Ick
    • Journal of Pharmaceutical Investigation
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    • v.15 no.3
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    • pp.130-139
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    • 1985
  • Inclusion compounds of suprofen with ${\alpha}-$ and, ${\beta}-cyclodextrins\;({\alpha}-CyD,\;{\beta}-CyD)$ were studied in comparison with suprofen alone and commercial suprofen capsules. Inclusion compound formations of suprofen with ${\alpha}-$, and ${\beta}-CyDs$ in aqueous solution and in solid state were confirmed by UV absorption, circular dichroism spectroscopies, IR spectroscopy, differential scanning calorimetry and X-ray diffraction measurements. Solid inclusion complexes were prepared by freeze-drying method, and their molar ratios were found to be 1 : 1. The dissolution rate of inclusion complexes of suprofen with CyDs was notably higher than that of suprofen alone.

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Immobilization of MTBE using cyclodextrins

  • Baek, Ki-Tae;Yang, Ji-Won
    • Proceedings of the Korean Society of Soil and Groundwater Environment Conference
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    • 2003.04a
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    • pp.120-123
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    • 2003
  • Immobilization behavior of methyl tert-butyl ether (MTBE) by various cyclodextrins(CDs) was studied to investigate the feasibility of MTBE removal using cyclodexrins. Even though MTBE has relatively low hydrophobicity and higher polarity compared to other organics, it was effectively immobilized by CDs. The immobilization isotherms was shown as a type of Freundlich isotherms, and the immobilization capacity of -CDs was the largest among natural COs. The initial apparent association constant for MTBE-CD complex follows the order : gamma = beta > methyl-beta > hydroxypropyl beta > alpha. These differences of the constants are related to the size of MTBE and CDs. The size of beta-CD and gamma-CD is large to encapsulate MTBE molecule into the cavity, which that of alpha-CB is too small to encapsulate MTBE.

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Inclusion Complexation of Chlorpropamide with Cyclodextrins (클로로프로파미드와 싸이클로덱스트린과의 포접 화합물에 관한 연구)

  • 정경혜;김길수;구영순
    • YAKHAK HOEJI
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    • v.30 no.2
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    • pp.87-95
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    • 1986
  • Inclusion complexation of $\alpha$-cyclodextrin($\alpha$-CD), $\beta$-cyclodextrin($\beta$-CD) and tri-O-methyl-$\beta$-cyclodextrin(tri-O-methyl-$\beta$-CD) with chlorpamide(CPA) in aqueous solution and in the solid state were studied by the solubility method, spectroscopy (UV, IR), differential scanning calorimetry (DSC) and powder X-ray diffractometry, and all their molar ratios were found to be 1:1. The solid complexes of CPA with three kinds of cyclodextrins were prepared by a freezedrying method, and their dissolution behaviors were examined. As a result, the release of CPA from the inclusion complexes was significantly improved. The intrinsic dissolution rate of CPA in cyclodextrin inclusion complexes was about 51 times ($\alpha$-CD inclusion complex) and 12 tmies ($\beta$-CD inclusion complex) larger than that of intact CPA.

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Studies on the interaction of thiamines and cyclodextrins

  • Im, In-Seon;Lee, Wang-Kyu;Park, Man-Ki;Kim, Bak-Kwang
    • Archives of Pharmacal Research
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    • v.6 no.1
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    • pp.35-44
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    • 1983
  • Interactions between thiamine.HCl and its disulfide derivatives TTFD. TPD and .alpha., .betha. cyclodextrins were investigated. By measuring the H-NMR, C-NMR chemical shifts, the assumption that cyclodextrin may from a inclusion complex with thiamines was supported qualitatively. To calculated the stability constants of them, anion exchange chromatography was applied. The simple, rapid HPLC method was proved to be pertinent thiamine/cyclodextrin system which was chemically unstable and less soluble.

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Separation of racemic enantiomer carvedilol and its metabolites using capillary electrophoresis (Capillary Electrophoresis에 의한 carvedilol 및 그 대사체의 거울상이성질체 분리)

  • Jo, Cheon-Ho;Koo, So-Hyun;Myung, Seung-Woon
    • Analytical Science and Technology
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    • v.19 no.4
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    • pp.275-279
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    • 2006
  • A capillary electrophoresis method for the separation of carvedilol and its metabolites enantiomers using cyclodextrins as the chiral selectors was developed. The effect of several types of cyclodextrins, concentration and capillary temperature for enantiomer resolution were investigated. Best results were obtained by 15 mM carboxymethyl-${\beta}$-cyclodextrin in the run buffer. Also the effect of capillary temperature on efficiency was assessed. The optimized method was applied for separation of chiral carvedilol and its three metabolites.

Solubilization and Dissolution Enhancement of Benzimidazole Antnelmintic Drugs by Cyclodextrin Complexation (시클로덱스트린류와의 복합체 형성에 의한 벤즈이미다졸계 구충 약물의 용해성 및 용출 증가)

  • 전인구;박인숙
    • YAKHAK HOEJI
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    • v.37 no.3
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    • pp.216-227
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    • 1993
  • Complex formations of practically insoluble antelmintic drugs such as mebendazole (MBZ), albendazole (ABZ) and flubendazole (FBZ) with dimethyl-$\beta$-cyclodextrin (DM-$\beta$-CyD) and 2-hydroxypropyl-$\beta$-cyclodextrin (HP-$\beta$-CyD) together with $\alpha$-, $\beta$- and $\gamma$-cyclodextrins(CyDs) in duffered solutions were investigated by solubility method. $A_{L}$ type phase solubility diagrams were obtained in all cases except for the complexation (B$_{s}$, type) of FBZ with $\gamma$-CyD. The highest stability constants were obtained with DM-$\beta$-CyD, followed by $\alpha$-CyD > $\beta$-CyD > HP-$\beta$-CyD > $\gamma$-CyD for ABZ, and HP-$\beta$-CyD > $\gamma$-CyD > $\beta$-CyD > $\alpha$-CyD for FBZ at pH 1.2. On the other hand, solid dispersion systems of ABZ and FBZ with $\beta$- and DM-$\beta$-CyDs were prepared by solvent evaporation method and evaluated by dissolution, differential thermal analysis and powder x-ray diffractometry. The dissolution rates of ABZ- and FBZ-DM-$\beta$-CyD solid dispersions were much faster than those of drugs alone, corresponding physical mixtures and tablets on market both at pH 1.2 and 6.8. Although dissolution rates of all samples at pH 6.8 were by far lower than those obtained at pH 1.2, as explained by pH-solubility profiles for ABZ and FBZ, the dissolution rates at pH 6.8 of ABZ from $\beta$- and DM-$\beta$-CyD solid dispersions exceeded the respective equilibrium solubility (23.9 $\mu\textrm{g}$/ml). Fast dissolution of ABZ from solid dispersions with CyDs was attributed to the reduction of drug crystallinity and particle size which was supported by DTA and powder x-ray diffractometry. Consequently these results suggest that solid dispersion systems with CyDs may provide useful means to markedly enhance the solubility and dissolution of benzimidazole antelmintic drugs.

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Cyclodextrins' effect on the enatioseparation of some PPIs and capillary electrophoresis method development for determining rabeprazole enantiomers

  • Choi, Yusung;Pham, Thuy-Vy;Mai, Xuan-Lan;Truong, Quoc-Ky;Le, Thi-Anh-Tuyet;Nguyen, Thi-Ngoc-Van;Lee, Gunhee;Kang, Jong-Seong;Mar, Woongchon;Kim, Kyeong Ho
    • Analytical Science and Technology
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    • v.32 no.5
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    • pp.185-195
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    • 2019
  • Over the past decades, chiral switch of the proton pump inhibitors (PPIs) has been received widespread attention in therapeutic advantages as well as pharmaceutical analysis. In present study, the influence of cyclodextrins (CDs) on the chiral separation of four common PPIs (lansoprazole, omeprazole, pantoprazole, and rabeprazole) was investigated. The results demonstrated that capillary electrophoresis (CE) with dual CDs as a chiral selector system is a possible and promising method for the enantioseparation of these PPIs. Rabeprazole, which is the most challenging and acid-labile candidate among four PPIs, was selected for further development of the technique. To optimize CE condition, the effects of capillary parameters and background electrolytes on the enantioseparation were investigated. Finally, the best chiral separation was acheived by using sulfobutyl ether-${\beta}$-CD, and ${\gamma}$-CD as dual chiral selectors. The developed CE method not only provided the effective chiral separation but also showed the good stability of rabeprazole. The proposed method was successfully validated according to the International Conference on Harmonization guideline and effectively applied to determine rabeprazole enantiomers in commercial rabeprazole tablets, with recoveries ranging from 97.17 % to 103.29 % of the label content.