• Title/Summary/Keyword: ${\beta}$-Cyclodextrin ( ${\beta}$-CD)

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Effects of Dietary ${\beta}$-Cyclodextrin on Plasma Lipid and Tissue Cholesterol Content in Swine

  • Park, B.S.;Jang, A.
    • Asian-Australasian Journal of Animal Sciences
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    • v.20 no.1
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    • pp.100-105
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    • 2007
  • This study examined the effects of dietary ${\beta}$-cyclodextrin (${\beta}CD$) on the cholesterol of blood and tissues of swine. Thirty six male castrated swine ($Landrace{\times}Yolkshire{\times}Duroc$) weighing 50 kg were randomly assigned to one of four dietary groups until their weight reached 110 kg. The groups were: basal diet without ${\beta}CD$ (control) and basal diets containing 1.5%, 3.0%, or 5.0% ${\beta}CD$. Diets and water were offered ad libitum. No significant difference was found between treatments in terms of feeding performance measured by daily intake, daily weight gain, and feed efficiency. Addition of ${\beta}CD$ to the diets significantly reduced total lipid, triglyceride and total cholesterol levels in swine blood, particularly in the group receiving 5.0% ${\beta}CD$, which showed decreases (p<0.05) of 21.9%, 55.6% and 27.7%, respectively. Cholesterol levels in back fat, loin, belly and ham portions of swine fed ${\beta}CD$ significantly differed (p<0.05) from controls, especially in the 5.0% ${\beta}CD$-fed group, with reductions of 26.0%, 27.5%, 17.9% and 18.3%, respectively. These results suggested that the addition of ${\beta}CD$ to the diet of swine could reduce their body cholesterol by decreasing the migration of cholesterol through the blood.

Complexation of Piroxicam and Tenoxicam with $Hydroxypropyl-{\beta}-cyclodextrin$ (히드록시프로필-베타-시클로덱스트린과 피록시캄 및 테녹시캄 간의 복합체 형성)

  • Kim, Ju-Hyun;Choi, Hoo-Kyun
    • Journal of Pharmaceutical Investigation
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    • v.30 no.1
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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.

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Electrospinning of Asiaticoside/2-Hydroxypropyl-β-cyclodextrin Inclusion Complex-loaded Cellulose Acetate Fiber Mats: Release Characteristics and Potential for Use as Wound Dressing (Asiaticoside/2-Hydroxypropyl-β-cyclodextrin 포접화합물 함유 셀룰로오스 아세테이트 섬유 매트의 전기방사: 창상피복제로서 사용가능성과 방출특성)

  • Panichpakdee, Jate;Pavasant, Prasit;Supaphol, Pitt
    • Polymer(Korea)
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    • v.38 no.3
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    • pp.338-350
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    • 2014
  • Cellulose acetate (CA) fiber mats containing inclusion complexes of asiaticoside (AC) in 2-hydroxypropyl-${\beta}$-cyclodextrin ($HP{\beta}CD$) for potential usage as wound dressings were developed. The AC/$HP{\beta}CD$ complex-loaded CA fibers at various $HP{\beta}CD$ to AC molar ratios of 0.5, 1, and 2 were prepared in 90:10 v/v mixture of 80% (v/v) acetic acid and N,N-dimethylacetamide (DMAc) via electrospinning. The maximum released amounts of AC depended on the $HP{\beta}CD$ content and were much greater than those released from the AC-loaded CA fiber mat. In the in vitro study, indirect cytotoxic evaluation with human dermal fibroblasts (HDFa) showed that these materials released no substances in the levels that were harmful to the cells and the cells appeared to attach and proliferate well on these substrates. However, only the CA fiber mats containing AC/$HP{\beta}CD$ complexes at the $HP{\beta}CD$ to AC molar ratio of 0.5 was effective in upregulating the production of collagen of the cultured cells.

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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Cholesterol Removal of Milk and Dairy Products using ${\beta}-Cyclodextrin$ (${\beta}-Cyclodextrin$을 이용한 우유 및 유제품의 콜레스테롤 제거)

  • Han, Eun-Mi;Kim, Song-Hee;Kwak, Hae-Soo
    • Food Science of Animal Resources
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    • v.26 no.4
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    • pp.540-547
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    • 2006
  • This review highlights areas of interest in the cholesterol removal of milk and dairy products. The demand for cholesterol removal has increased due to consumer demand for cholesterol-reduced products. At present the best method for producing without changing flavor, taste and texture of the products is entrapping cholesterol by ${\beta}-cyclodextrin({\beta}-CD)$. Especially, crosslinking of ${\beta}-CD$ is important due to recycling that could be separated the ${\beta}-CD$ from treated cream or milk. The recycling can be up to 10 times with keeping the rate of cholesterol removal. Various functional milk and dairy products can be produced in this manner. This report reviews general information including methods of cholesterol removal, crosslinking of ${\beta}-CD$, and recycling of the ${\beta}-CD$ in milk and dairy products.

Effect of an Excipient on the Formation of PLGA Particles Using Supercritical Fluid (초임계 유체를 이용한 PLGA 입자 제조에 첨가제가 미치는 영향)

  • Jung, In-Il;Haam, Seung-Joo;Lim, Gio-Bin;Ryu, Jong-Hoon
    • Polymer(Korea)
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    • v.36 no.1
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    • pp.1-8
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    • 2012
  • In this study, we employed hydroxypropyl-${\beta}$-cyclodextrin (HP-${\beta}$-CD) as an excipient to produce poly(lactic-$co$-glycolic acid) (PLGA) fine particles by a supercritical fluid process, called aerosol solvent extraction system (ASES), and investigated the effect of HP-${\beta}$-CD content on the morphology of the particles. The influence of HP-${\beta}$-CD on the drug release characteristics of paclitaxel-loaded PLGA particles was also evaluated. Fine particles were obtained when the HP-${\beta}$-CD content in PLGA/HP-${\beta}$-CD mixtures was greater than 40% and 30%, respectively, for PLGA(75:25) and PLGA(50:50), whereas a film-like precipitate was obtained for lower HP-${\beta}$-CD content. The release rate for paclitaxel loaded PLGA(75:25)/HP-${\beta}$-CD particles was found to increase with HP-${\beta}$-CD content.

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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Entrapment of Milk Nutrients during Cholesterol Removal from Milk by Crosslinked β-Cyclodextrin

  • Ha, H.J.;Jeon, S.S.;Chang, Y.H.;Kwak, H.S.
    • Food Science of Animal Resources
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    • v.29 no.5
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    • pp.566-572
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    • 2009
  • This study was designed to elucidate the quantities of milk nutrients entrapped during cholesterol removal from milk by crosslinked $\beta$-cyclodextrin ($\beta$-CD, 0.4~1.2%, w/v) and to evaluate the amounts of the residual $\beta$-CD in cholesterol-reduced milk treated by crosslinked $\beta$-CD. The content of lactose in the control milk (without treatment by crosslinked $\beta$-CD) was 4.86%, and the amounts of lactose entrapped by crosslinked $\beta$-CD ranged from 0.00 to 0.03%. The total amounts of the entrapped short-chain free fatty acid (FFA) and free amino acid (FAA) ranged from 0.03 to 0.09 ppm and from 0.28 to $0.71{\mu}mol/mL$, respectively. The amounts of the entrapped water-soluble vitamins (L-ascorbic acid, niacin, thiamine and riboflavin) ranged from 0.02 to 0.05 ppm, 0.01 to 0.06 ppm, 0.00 to 0.06 ppm and 0.01 to 0.06 ppm, respectively. The entrapped amounts of lactose, short-chain FFAs, FAAs and water-soluble vitamins were not remarkably affected by the concentrations of crosslinked $\beta$-CD (0.4~1.2%, w/v). Only very small amounts of residual $\beta$-CD in the cholesterol-removed milk were measured (1.22~3.00 ppm). Based on the data obtained from the present study, it was concluded that the amounts of entrapped nutrients were negligible during cholesterol removal from milk by crosslinked $\beta$-CD, and only trace amounts of residual $\beta$-CD were present in cholesterol-removed milk.

Preparation and Evaluation of Inclusion Complex of Muscone with ${\beta}-Cyclodextrin$ (무스콘의 ${\beta}$-시클로덱스트린 포접 복합체의 제조 및 평가)

  • Kwack, Eun-Sun;Cho, In-Sook;Lee, Gye-Won;Jee, Ung-Kil;Park, Dae-Kyu
    • Journal of Pharmaceutical Investigation
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    • v.27 no.4
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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.

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Hydrophobic Cyclodextrin Derivatives as a Sustained Release Carrier of Azidothymidine (아지도싸이미딘의 지속성방출형담체로서의 소수성시클로덱스트린유도체)

  • Seo, Bo-Youn;Park, Gee-Bae;Lee, Kwang-Pyo
    • Journal of Pharmaceutical Investigation
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    • v.26 no.2
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    • pp.71-82
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    • 1996
  • This study has been undertaken to evaluate hydrophobic cyclodextrin(CD) derivatives as a sustained release carrier of azidothymidine(AZT), AZT, which has potent activity against AIDS and AIDS-related complex as thymidine analogue, has been reported that it has significant toxicity and short half life. Therefore, it is necessary to design sustained release oral dosage form to avoid undesirable side effects attributable to an excessive plasma concentration and to reduce the frequency of administration of AZT. Inclusion complexes of AZT with $acetyl-{\beta}-cyclodextrin\;(AC{\beta}CD)$ and $triacetyl-{\beta}-cyclodextrin(TA{\beta}CD)$ were prepared by solvent evaporation method. Interactions of AZT with CD were investigated by Differential Scanning Calorimetry(DSC) and Infrared Spectrophotometry(IR). The decreasing order of water solubilities of AZT and AZT-CD inclusion complexes were as follows; $AZT\;(27.873{\pm}0.015,mg/ml)\;>\;AZT-AC{\beta}CD\;(3.377{\pm}0.003)\;>\;AZT-TA{\beta}CD\;(2.528{\pm}0.001)$. Partition coefficients of $AZT-AC{\beta}CD\;and;\AZT-TA{\beta}CD$ inclusion complexes were increased by 1.27-fold, 1.54-fold in pH 1.2 and 1.32-fold, 1.47-fold in pH 6.8 in comparison with that of AZT. The mean dissolution time (MDT, min) which represents the rapidity of dissolution rate of AZT, $AZT-AC{\beta}CD,\;AZT-TA{\beta}CD$ were 5.12, 14.02 and 19.38 min in pH 1.2 and 2.52, 15.19 and 18.19 min in pH 6.8. AZT was very rapidly and completely dissolved in pH 1.2 and pH 6.8 within 5 minutes. But AZT-CD inclusion complexes showed the sustained release pattern in comparison with AZT alone. The simultaneous in situ nasal and jejunal recirculation study to compare the intrinsic absorptivity and the property of absorption sites revealed that the absorption of $AZT-TA{\beta}CD\;(N:35.35{\pm}1.08%,\;J:27.47{\pm}1.18%)$ was more than that of $AZT\;(N:16.89{\pm}2.25%,\;J:15.86{\pm}2.33%)$. The above results suggest that $TA{\beta}CD$ which is a hydrophobic cyclodextrin may serve as sustained release carrier with absorption enhancing effect.

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