• 한국식품위생안전성학회지
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• 제10권1호
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• pp.29-32
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• 1995

Inclusion complex of omeprazol with $\beta$-Cyclodextrin and Hydroxypropyl-$\beta$-Cyclodextrin were prepared by coprecipitation and freeze-drying method respectively. Effects of these inclusion complex on RBCs were monitored with a spectrophotometer by the method of Kahan et al. and the mutagenic activity based on the Ames plate incorporation test in the presence and absence of liver microsomal enzyme(S9 fraction) using Salmonella typhimurium TA98 and TA100. The RBCs hemolysis and mutagenic activity of these complex were not detected.

• Journal of Pharmaceutical Investigation
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• 제17권1호
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• pp.1-14
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• 1987

To increase the bioavailability of norfloxacin, inclusion complex of antimicrobial agent norfloxacin with ${\beta}-Cyclodextrin$ was prepared and studied by the solubility method, spectrophotometric methods(UV, IR, $^1H-NMR$), differential thermal analysis, powder X-ray diffractometry, the physical properties, the antimicrobial activity, DNA binding and in situ recirculation technique. The conclusions are summerized as following; 1) The inclusion complexation was identified by means of solubility, spectrophotometry(UV, IR, NMR), DTA and X-ray diffraction. 2) The molar ratio of $norfloxacin-{\beta}-cyclodextrin$ complex was 1 : 1. 3) The stability constant of $norfloxacin-{\beta}-cyclodextrin$ complex was $21.5\;M^{-1}$, and both true and apparent partition coefficients of the inclusion complex were larger than those of norfloxacin. 4) The time required to dissolve 60% $(T_{60}%)$ of the inclusion complex was 120 min. in distilled water and in the artificial intestinal juice, while norfloxacin did not reach to 60% dissolution within 120 min. 5) The antimicrobial activity of the inclusion complex against Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus showed no significant difference compared to that of norfloxacin alone. 6) Studies on binding properties between the inclusion complex and norfloxacin alone to DNA according to equilibrium dialysis showed no significant differency. 7) In situ absorption rates (Ka) of inclusion complex and norfloxacin alone were 0.229 and $0.102hr^{-1}$, respectively.

• 한국응용과학기술학회지
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• 제6권1호
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• pp.59-66
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• 1989

Inclusion complex formation of octyldimethyl p-aminobenzoate with ${\beta}-cyclodextrin$in aqueous solution and in the solid state was studied by the solubility method, spectroscopic (UV, FT-IR) and X-ray diffractornetry. The solid complex of octyldimethyl p-aminobenzoate with ${\beta}-cyclodextrin$ was obtained in molar ratio of 1:2 (guest/host). A spatial relationship between host and guest molecule was clearly reflected in the magnitude of the apparent stability constant (K') and in the stoichiometry of the inclusion complex. Furthermore, a typical type Bs phase-solubility diagram was obtained for octyldimethyl p-aminobenzoate and ${\beta}-cyclodextrin$ in water at $25^{\circ}C$. The results indicated that the solubility of the guest molecule was higher by the formation of ${\beta}-cyclodextrin$ inclusion complex.

• Bulletin of the Korean Chemical Society
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• 제13권2호
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• pp.179-183
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• 1992

A stable solid new inclusion complex with benzaldehyde and $permethyl-\beta-cyclodextrin$ was obtained by recrystallization method. The structure of the $benzaldehyde-permethyl-\beta-cyclodextrin$ inclusion complex in the solid and solution state have been studied by UV, IR, $^1H-NMR$, $^{13}C-NMR$ and FAB-mass spectroscopy.

• 약학회지
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• 제37권4호
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• pp.331-340
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• 1993

Inclusion complex of omeprazole(OMZ) with hydroxypropyl-$\beta$-cyclodextrin(HP-$\beta$-CD) was prepared by freeze-drying method. The complexation was confirmed by means of UV, CD, IR, DSC, XRD and $^{1}$H-NMR spectra. The benzimidazole moiety of OMZ might be found to be included into the cavity of HP-$\beta$-CD and the inclusion complex appeared to be $A_{L}$ type. The stoichiometric ratio of OMZ : HP-$\beta$-CD was found to be 1:1, and the stability constants of the inclusion complex by solubility and UV method were about 34 and 45 M$^{-1}$, respectively. The dissolution of OMZ was significantly enhanced from powder and. yablet of OMZ-HP-$\beta$-CD complex when compared to those of OMZ alone, and oil-to-water partition coefficient of OMZ-HP-$\beta$-CD complex was significantly higher than that of OMZ alone. Therefore, it was expected that the bioavailability of OMZ could be improved markedly by inclusion complexation of OMZ with HP-$\beta$-CD.

• 대한화장품학회지
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• 제15권1호
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• pp.51-62
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• 1989

Inclusion complex formation of octyldimethl p-aminobenzoate with $\beta$-cyclodextrin in aqueous solution and in the solid state was studied by the solubility method, spectroscopic(UV, FT-lR) and X -ray diffractometry. The solid complex of octyldimethy p-aminobenzoate with $\beta$-cyclodextrin was obtained in molar ratio of 1 : 2(guest/host). A spatial relationship between host and guest molecule was clearly reflected in the magnitude of the apparent stability constant (K') and in the stoichiometry of the inclusion complex. Furthermore, a typical type Bs phase-solubility diagram was obtained for octyldimethyl p-aminobenzoate and p -cyclodextrin in water at $25^{\circ}C$. The results indicated that the solubility of the guest molecule was higher by the formation of $\beta$-cyclodextrin inclusion complex.

• Journal of Pharmaceutical Investigation
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• 제14권3호
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• pp.136-143
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• 1984

Inclusion complex formation of fenbufen with ${\beta}-cyclodextrin$ in water and in solid state was comfirmed by solubility method, ultra violet absorption, circular dichroism and infra-red spectroscopies, differential thermal analysis, and X-ray diffractometry. A solid complex of fenbufen with ${\beta}-cyclodextrin$ in 1 : 1 molar ratio was prepared by the freeze-drying method, its dissolution characteristics in water and its analgesic and antiinflammatory effect in mouse or rat were examined. The apparent release of fenbufen from the inclusion complex was significantly improved, hut no significant difference in its analgesic and antiinflammatory effect was found.

• 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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• 제27권4호
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• pp.265-269
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• 1997

An inclusion complex of muscone with ${\beta}-cyclodextrin$ (CD), as a solid form of muscone, was prepared to increase the solubility of muscone. The molar ratio of muscone to ${\beta}-CD$ in complex was in the range of $1:1{\sim}1:5$ when prepared by freeze-drying method. The interaction of muscone with ${\beta}-CD$ in solid state was investigated by Infrared (IR) spectroscopy and differential scanning calorimetry (DSC). IR and DSC studies between $muscone-{\beta}-CD$ inclusion complex and physical mixture showed that $muscone-{\beta}-CD$ inclusion complex was prepared stably. From the amount of muscone incorporated in the inclusion complex, it was found that the molar ratio of muscone : ${\beta}-CD$ was 1:1. Relative spatial position of muscone and ${\beta}-CD$ was observed by Hyperchem molecular modelling program.

• 약학회지
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• 제30권2호
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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.