• 분석과학
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• 제17권3호
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• pp.282-288
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• 2004

Inclusion selectivities of the cyanocadmate host complexes with ammonium oniums, $[Cd_x(CN)_{2x}][onium{\cdot}zG]$ (onium = $NMe_3Et^+$, $NMeEt{_3}^+$ and $NEt{_4}^+$, G = guest), have been investigated for $C_6H_6$ (B), PhMe (T), PhEt (E), ortho (O), meta (M), and para (P) isomers of $C_6H_4Me_2$ as the aromatic guest molecules. From the binary, ternary, quaternary and quinary mixed guests of B, T, E, O, M and P, the order of preference in the $NMe_3Et+$-host is $B{\gg}$T>P${\fallingdotseq}O{\fallingdotseq}M$ and E>O${\gg}P{\fallingdotseq}M$; in the $NMeEt{_3}^+$-host is T>B>P${\gg}O{\fallingdotseq}M$ and E>P${\gg}$M>O; in the $NEt{_4}^+$-host is $B{\gg}T{\fallingdotseq}O{\fallingdotseq}M{\fallingdotseq}P$. However, the $NEt{_4}^+$-host complexes of E, O, M and P mixed-guests were not obtained. These inclusion selectivities were compared to our previous results of the $NMe{_4}^+$-host; T>B>P${\gg}$M>O and E>P${\gg}$M>O.

• Journal of Pharmaceutical Investigation
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• 제25권3호
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• pp.205-211
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• 1995

To increase the solubility of iodine and iodine releasing agents, which are used widely as a topical broad spectrum antiseptics and disinfectant sanitizers, its inclusion complexes were prepared and studied. Inclusion complexes of iodine with ${\beta}-cyclodextrin$ were prepared by coprecipitation method and complex formation was acertained by differential scanning calorimetry and microscopic observation. Iodine content of inclusion complex was determined by means of iodometry. Tablets containing inclusion complex were manufactured with sugar, citric acid, magnesium stearate, dextrose. Stability of inclusion complexes and tablets was evaluated by accelerated stability test, and comparing with PVP-iodine. During preparation, use of 50% ethanol solution is preferable to water as the medium because the former resulted in more stable complex for a month under accelerated storage conditions. Solubility of iodine in KI aqueous solution was 0.048 g/ml and lower than in 50% ethanol solution. Inclusion complex and its tablets were very stable at severe condition for one month, and comparable to PVP-iodine in the aspect of stability. Inclusion complex tabletswere not affected with citric acid, sugar, dextrose, and direct tableting method was recommendable because wet granulation using ethanol gave some release of included iodine during process.

• Journal of Pharmaceutical Investigation
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• 제15권3호
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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.

• Journal of Pharmaceutical Investigation
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• 제28권4호
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• pp.257-266
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• 1998

To improve the solubility and dissolution rate of acyclovir (ACV), which is low oral bioavailability due to its properties of slight solubility in water and incomplete gastrointestinal absorption, the solid inclusion complexes of ACV with ${\alpha}CD$, ${\beta}CD$, $DM{\beta}CD$ in molar ratio of 1:1 were prepared by the freeze-drying method. The inclusion complexes were investigated by solubility study, UV, IR and DSC. The dissolution rate of ACV was significantly increased by ACV-CDs inclusion complex formation in artificial intestinal fluid at pH 6.8. The enhanced dissolution rate of ACV could be due to an increase of solubility and the formation of an amorphous structures through inclusion complexation with CDs. Especially, $ACV-DM{\beta}CD$ inclusion complex enhanced the maximum plasma concentration levels and AUC following oral administration compared to those of ACV alone. The present results suggest that $ACV-DM{\beta}CD$ inclusion complex serves as a potential carrier for improving the solubility, the dissolution rate and the bioavailability of ACV.

• 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.

• Bulletin of the Korean Chemical Society
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• 제26권12호
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• pp.2061-2064
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• 2005

• Journal of Pharmaceutical Investigation
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• 제25권4호
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• pp.283-289
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• 1995

The aim of this study is to increase the solubility and dissolution rate of clonixin by inclusion complex formation. Inclusion complexes of clonixin, a non-steroidal antiinflammatory drug, with ${\beta]-cyclodextrin$ were $2-hydrolrypropyl-{\beta]-cyclodextrin$ were prepared by freeze drying method. Inclusion complex formation of clonixin with cyclodextrins was determined by UV, IR and DSC. The apparent stability constants were calculated from the phase solubility diagrams. Dissolution rate and solubility of clonixin in water markedly increased by the complex formation.

• KSBB Journal
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• 제19권4호
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• pp.321-326
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• 2004

본 연구에서는 초임계 이산화탄소를 이용한 SAS 공정을 난용성 약물인 이트라코나졸과 친수성 물질인 HP-$\beta$-CD의 포접복합체 미세입자의 제조에 적용하기 위한 기초 연구를 수행하였다. 이트라코나졸과 HP-$\beta$-CD를 1:2의 몰비로 혼합한 용액을 사용하여 35∼$65^{\circ}C$의 온도범위와 83∼140 bar의 압력범위에서 SAS 공정으로 이트라코나졸/HP-$\beta$-CD 포접복합체 미세입자를 제조하였으며, 이트라코나졸 및 HP-$\beta$-CD 원재료의 열적 특성과 비교함으로써 초임계 유체 공정에 의해 포접복합체를 제조할 수 있음을 확인하였다. 또한, SAS 공정에 의해 제조된 이트라코나졸/HP-$\beta$-CD 포접복합체의 인공위액에 대한 이트라코나졸의 용출시험을 수행한 결과 이트라코나졸 원재료와 이트라코나졸을 함유한 대표적 시판 제제인 스포라녹스 캡슐제와 비교해 투입된 이트라코나졸의 50∼80%에 해당하는 양이 용출개시 5분 만에 방출되는 매우 빠른 초기 용출특성을 보임을 확인할 수 있었다. 이트라코나졸 /HP-$\beta$-CD 포접복합체의 제조시 SAS 공정 조건이 35$^{\circ}C$에서 $65^{\circ}C$로 높아짐에 따라 이트라코나졸의 용출률이 감소하였을 뿐만 아니라 열분석 결과 이트라코나졸의 용융 피크의 세기도 점차로 증가하게 된다는 결과로부터 포접복합체의 형성이 이루어지는 주변 매질의 온도가 높아짐에 따라 초임계 이산화탄소 분자의 활동도가 증가하게 되어 이트라코나졸과 HP-$\beta$-CD의 포접복합체 형성에 필요한 결합력이 점차로 약해져서 포접 효율이 저하하게 됨을 확인할 수 있었다.

• Journal of Pharmaceutical Investigation
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• 제16권2호
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• pp.55-67
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• 1986

Inclusion complexation of tiaprofenic acid (TPA) with cyclodextrins $({\alpha}-,\;{\beta}-,\;{\gamma}-CyDs)$ in aqueous solution and in solid phase was investigated by solubility method, measurement of partition coefficient, ultra-violet, circular dichroism, infrared spectroscopies, powder X-ray diffractometry and differential scanning calorimetry. Investigations were made to prepare inclusion complexes of TPA with ${\beta}-CyD$ in solid powdered form by coprecipitation, freeze-drying, spray-drying and co-pulverization methods. The coprecipitation, freeze-drying and spray-drying methods were successful in obtaining inclusion complexes. The results showed that the latter two methods might be originally superior to the former in obtaining powdered inclusion completes. Especially, it was shown by powder X-ray diffractometry that spray-dried ${\beta}-CyD$ alone, TPA-spray-dried ${\beta}-CyD$ physical mixture, and spray-dried $TPA-{\beta}-CyD$ complex were amorphous. The dissolution behaviours of $TPA-{\beta}-CyD$ systems prepared by above four methods were compared with those of TPA alone and $TPA-{\beta}-CyD$ physical mixture, and the rates of dissolution of TPA in pH 1.2 buffer were greatly enhanced by inclusion complexation and copulverization.

• 한국식품과학회지
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• 제35권2호
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• pp.266-271
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• 2003

CD의 inclusion complex 형성능을 이용하여 대표적인 polyphenol계 천연 항산화 물질인 quercertin 및 catechin을 안정화시키는 분자 캡슐화 기술을 연구하였다. 먼저 ${\alpha}-,\;{\beta}-$, 그리고 ${\gamma}-CD$의 quercetin 및 catechin의 포접능을 비교하였다. Quercetin/catechin-CD inclusion complex 형성을 DSC thermogram을 이용하여 확인하였다. 또한 ${\beta}-CD$와의 포접에 따른 저용해성 quercetin과 catechin의 물에 대한 용해도의 변화를 관찰한 결과 inclusion complex 형성 시 용해도가 증가하는 것을 관찰할 수 있었다. Inclusion complex의 온도 및 pH에 대한 안정성을 검토한 결과 inclusion complex가 원래의 물질보다 높은 항산화능을 유지하였으며 특히 catechin의 안정성이 크게 향상되었다. Catechin-CD inclusion complex의 식품보존제로서의 적합성을 지방산인 linoleic acid를 시료로 검토하기 위하여 저장 중 과산화물가의 변화를 측정한 결과 포접된 catechin이 보다 높은 항산화능을 보였다. 이와 같은 용해도 및 항산화능의 증가로 볼 때 quercetin/catechin-CD inclusion complex는 신선식품의 보존제로 효과적으로 활용될 수 있는 것으로 판단된다.