• Title/Summary/Keyword: Inclusion Complex

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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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Enhanced Nasal Absorption of Ketoconazole by Inclusion with Cyclodextrin (시클로덱스트린과의 포접에 의한 케토코나졸의 비점막 흡수증가)

  • Park, Gee-Bae;Seo, Bo-Youn;Ann, Hong-Jik;Rho, Hyun-Goo;Onn, Yun-Sung;Lee, Kwang-Pyo
    • Journal of Pharmaceutical Investigation
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    • v.24 no.2
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    • pp.95-104
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    • 1994
  • Inclusion complexes of ketoconazole(KT) with ${\alpha}^_$, ${\beta}^_$cyclodextrin(CD) and $dimethy1-{\beta}-cyclodextrin$ (CD) and $dimethy1-{\beta}-cyclodextrin(DM{\beta}CD)$ 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$(P_{app}\;:\;cm/sec\;{\time}\;1O^{-5}{\pm}S.E.)$, corrected by surface area of absorption, was $5.10{\pm}0.3(N,\; KT-DM{\beta}CD)$ )> $4.13{\pm}0.4(N,\;KT-{\beta}-CD)$ )> $3.52{\pm}0.2(N,\;KT-{\alpha}-CD)$ )> $2.76{\pm}0.3(J,\; KT-DM{\beta}CD)$ )> $2.61{\pm}0.5(J,\;KT-{\beta}-CD)$ )> $2.42{\pm}0.4(J,\;KT-{\alpha}-CD)$ at pH 4.0. The in crease in permeability of $KT-DM{\beta}CD$ 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 $KT-DM{\beta}CD$ inclusion complex after nasal administration was more rapid than those of ketoconazole alone and $KT-DM{\beta}CD$ 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 $KT-DM{\beta}CD$ inclusion complex in rats. The present results suggest that $KT-DM{\beta}CD$ inclusion complex may serve as a potential nasal absorption enhancer for the nasal delivery of ketoconazole.

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Stress analysis of creep material containing elliptical rigid inclusion by complex pseudo-stress function (복소 유사응력함수에 의한 타원 강체함유물을 내포하는 크립재료의 응력해석)

  • Lee, Kang-Yong;Kim, Jong-Sung
    • Transactions of the Korean Society of Mechanical Engineers A
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    • v.22 no.2
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    • pp.408-415
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    • 1998
  • The analysis model is the power law creep material containing an elliptical rigid inclusion subjected to the arbitrarily directional stress on infinite boudary. The stress analysis is performed using the conformal mapping function and complex pseudo-stress function. The stress distributions near an elliptical rigid inclusion are obtained with various ellipse shapes, strain hardening exponents and directions of applied stress.

Encapsulation of Flavors by Molecular Inclusion Using $\beta$-Cyclodextrin: Comparison with Spray-drying Process Using Carbohydrate-based Wall Materials

  • Cho, Young-Hee;Park, Ji-Yong
    • Food Science and Biotechnology
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    • v.18 no.1
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    • pp.185-189
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    • 2009
  • Microencapsulation of flavor was carried out by molecular inclusion process using $\beta$-cyclodextrin (${\beta}CD$). ${\beta}CD$-flavor complex was prepared at various flavor-to-${\beta}CD$ ratios (1:6-1:12) to determine the effect of ${\beta}CD$ concentration on the inclusion efficiency. Maximum total oil retention and minimal surface oil content were obtained at flavors to ${\beta}CD$ ratio of 1:10. The physical properties and controlled release pattern of flavors from ${\beta}CD$-flavor complex were measured and compared with spray-dried microcapsules prepared using carbohydrate wall system. ${\beta}CD$-flavor complex showed higher total oil retention and surface oil contents, smaller mean particle size, lower moisture uptake, and higher oxidation stability than spray-dried microcapsule. Oxidative stability of flavor was correlated with hygroscopicity of wall materials. The controlled release mechanism was highly affected by temperature and characteristics of wall materials.

복소 유사 응력 함수에 의한 타원 강체 함유물을 내포하는 글잎 재료의 응력 해석

  • 김종성;이강용
    • Proceedings of the Korean Society of Precision Engineering Conference
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    • 1995.10a
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    • pp.740-743
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    • 1995
  • The analysis model is the power law creep material containing an elliptical rigid inclusion subjected to the arbitrarily directional stress on infinite boundary. The stress analysis is performed using the conformal mapping function and complex pseudo-stress function. The stress distributions near an elliptical rigid inclusion are obtained with various ellipse shapes, strain hardening exponents and directions of applied stress.

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Crack Analysis of Creep Material Containing Rigid Inclusion with Line Crack Shape (직선 균열 강체 함유물을 내포하는 크?재료의 균열 해석)

  • 이강용;김종성
    • Journal of the Korean Society for Precision Engineering
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    • v.15 no.7
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    • pp.91-97
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    • 1998
  • The analysis model is the infinite body consisted of power law creep material containing a rigid inclusion with line crack shape subjected to the arbitrarily directional stress on an infinite boundary. The crack analysis is performed using the complex pseudo-stress function. The strain rate intensity factor is determined in the closed form as new fracture mechanics parmeter which represents the magnitudes of stress and strain rate near the tip in power law creep material.

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Molecular Recognition : ${\alpha}$-Cyclodextrin and Aspirin Inclusion Complexation

  • Hee Sook Choi
    • Bulletin of the Korean Chemical Society
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    • v.13 no.5
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    • pp.474-479
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    • 1992
  • Molecular interaction between ${\alpha}$-cyclodextrin and aspirin was studied by UV, $^2H$-NMR and $^2H$-NMR spectroscopy analyses for solution complex and by FT-IR analyses for solid complex. The inclusion structure provides a basic understanding of the aspirin and ${\alpha}$-cyclodextrin interaction.

Determination of thermal Stress Intensity Factors for General Cusp-Crack Shaped Rigid Inclusion (일반 형상의 커프스형 강체균열에 대한 열응력세기계수 결정)

  • 이강용;장용훈
    • Transactions of the Korean Society of Mechanical Engineers
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    • v.16 no.6
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    • pp.1216-1220
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    • 1992
  • In case that a general cusp-crack shaped inclusion expressed in a polynominal form of conformal mapping function exists in a two dimensional elastic body under uniform heat flow, the complex potential and thermal stress intensity factors are derived. Two thermal boundary conditions are considered, one an insulated rigid inclusion and the other a rigid inclusion with fixed boundary temperature. The previous solutions of the thermal stress intensity factors for symmetrical airfoil and lip type rigid inclusions are obtained from the general solution of the thermal stress intensity factors.

Nuclear Magnetic Resonance Spectroscopic Study on Inclusion Complexation of Paracyclophane with Naphthalene Derivatives in Aqueous Solution (프로톤 핵자기공명스펙트럼 측정법에 의한 수용액중 파라시클로판과 나프탈렌 유도체들간의 포접 복합체 형성에 관한 연구)

  • Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.23 no.3
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    • pp.155-163
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    • 1993
  • Inclusion complexation of 1,7,21,27-tetraaza[7.1.7.1]paracyclophane (CPM 55) with 2,7-dihydroxynaphthalene (2,7-DHN) or 1,3-dihydroxynaphthalene (1,3-DHN) in pD 1.17 $DCl-D_2O$ solution was investigated by $^1H$ nuclear magnetic resonance spectroscopy (NMR) using 4,4'-dimethylaminodiphenylmethane (ACM 11) as an acyclic analog of CPM 55. In CPM 55-naphthalene derivative complex, alkyl protons located in the cavity of CPM 55 were shown to be subjected to anisotropic shielding and protons of naphthalene moiety shifted remarkably to upfield. However, in ACM 11-naphthalene derivative systems, chemical shifts for protons of both DHN compounds were not significant. The remarkable chemical shift changes suggested that the naphthalene moiety of 2,7-DHN or 1,3-DHN was included in the hydrophobic cavity of CPM 55 in aqueous solution. From the continuous variation plots of induced chemical shifts of 2,7-DHN, it was found that 2,7-DHN was included in the cavity of CPM 55 at 1:1 molar stoichiometry. Both computer simulation of a inclusion complex and strong upfield chemical shift changes of 2,7-DHN protons supported the conformation of pseudoaxial inclusion as the presumed geometry of the host-guest complex.

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Improvement of Solubility and Dissolution of Ketoconazole by Inclusion with Cyclodextrin (시클로덱스트린과의 포접에 의한 케토코나졸의 용해성 및 용출 증가)

  • Park, Gee-Bae;Ann, Hong-Jik;Chang, Young-Soo;Seo, Bo-Youn;Lee, Kwang-Pyo
    • Journal of Pharmaceutical Investigation
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    • v.24 no.2
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    • pp.85-94
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    • 1994
  • Inclusion complexes of ketoconazole (KT) with ${\alpha}-$, ${\beta}-cyclodextrin$ (CD) and dimethyl-${\beta}-cyclodextrin$ $(DM{\beta}CD)$ in a molar ratio of 1:2 were prepared by freeze-drying and solvent evaporation methods. The interactions of KT with ${\alpha}-CD$, ${\beta}-CD$ and $DM{\beta}CD$ in aqueous solution and in solid state were investigated by solubility study, infrared (lR) spectroscopy and differential scanning calorimetry (DSC). The stability constant of $KT-DM{\beta}CD$ inclusion complex (lC) 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 $KT-DM{\beta}CD$ IC (3.20) < $KT-{\beta}-CD$ IC (4.36) < $KT-{\alpha}-CD$ IC (6.99) < $KT-{\alpha}-CD$ PM (17.46)< $KT-{\beta}-CD$ PM (19.36) < $KT-{\beta}-CD$ 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.

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