Analysis of the complexation of gemfibrozil with γ- and hydroxypropyl-γ-cyclodextrins

Fernández, L.; Martínez-Ohárriz, María Cristina; Martı́n, Carmen; Vélaz, Itziar; Sánchez, Miguel; Zornoza, Arantza

doi:10.1016/j.jpba.2008.02.029

Cited by 12 publications

(4 citation statements)

References 17 publications

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“…This enhancement can be applied to improve the fluorimetric analysis of this drug in aqueous media. The values obtained for the quantum yields with β-CDs were higher than those of the complexes with γ-CDs [8], most likely because the smaller size of the cavity yields a better host-guest fitting. The fluorescence enhancement of gemfibrozil in the presence of increasing concentrations of β-CDs can be used to determine the stability constants of the complexes.…”

Section: Fluorescence Spectroscopymentioning

confidence: 75%

“…It is a non-hygroscopic lipophilic drug whose poor solubility and low dissolution rate in the gastrointestinal tract limits its bioavailability after oral administration. Several methods have been used to improve its dissolution characteristics, such as micronization [7], solubilization by lipids, and complexation with γ-CD [8] and dimethyl-β-CD [9,10]. The physicochemical characteristics of this drug determine its suitability to achieve a bioavailability enhancement through complexation with β-CD [11].…”

Section: Introductionmentioning

confidence: 99%

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A Comprehensive Study of Gemfibrozil Complexation with β-Cyclodextrins in Aqueous Solution Using Different Analytical Techniques

Zornoza

Vélaz

González‐Gaitano

et al. 2022

IJMS

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Gemfibrozil (GEM) is a hypolipidemic agent, which is effective in reducing serum cholesterol and triglyceride levels. Complexation of GEM with native β-cyclodextrin (β-CD) and with the derivatives hydroxypropyl-β- and randomly methylated β-CD (HPβ-CD and Meβ-CD) was studied in aqueous solution of pH 2.8 and 7.0. The stability constants were determined by spectrofluorimetry, 1H-NMR spectroscopy and solubility assays. Considering the well-known difficulties to obtain similar stability constants by different techniques, the agreement of the values obtained supports the reliability of the results presented. The advantages and drawbacks of each analytical technique for the study of inclusion complexation were discussed as well. In addition, the thermodynamic parameters of complexation, enthalpy (ΔH) and entropy (ΔS), were determined and related to the type of molecular interactions that take place between GEM and the different cyclodextrins. Finally, solid dispersions were prepared by co-evaporation, kneading, vacuum desiccation, and coprecipitation, and complexation was evaluated by X-ray diffraction.

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Section: Fluorescence Spectroscopymentioning

confidence: 75%

Section: Introductionmentioning

confidence: 99%

A Comprehensive Study of Gemfibrozil Complexation with β-Cyclodextrins in Aqueous Solution Using Different Analytical Techniques

Zornoza

Vélaz

González‐Gaitano

et al. 2022

IJMS

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“…Most of the papers available in the literature deal with the properties of complexes of natural CDs. Papers concerning complexes of various compounds with CD derivatives, especially with (2‐hydroxypropyl)‐γ‐cyclodextrin (HP‐γ‐CD), are not numerous .…”

Section: Introductionmentioning

confidence: 99%

“…The study of complexation in solutions requires knowledge of its thermodynamic parameters . A number of techniques are used to determine the thermodynamic parameters , including NMR , UV/Vis , fluorescence spectroscopy , calorimetry , phase‐solubility (PS) method with HPLC , and with UV/Vis spectrophotometry , RP–LC , CE , and others. CE is one of the modern techniques that allow studying the complexes into solutions.…”

Section: Introductionmentioning

confidence: 99%

Thermodynamic parameters for the complexation of water‐insoluble betulin derivatives with (2‐hydroxypropyl)‐γ‐cyclodextrin determined by phase‐solubility technique combined with capillary zone electrophoresis

2019

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The complexation of betulinic and betulonic acids (BIA and BOA) (pentacyclic lupane triterpenoids) with (2‐hydroxypropyl)‐γ‐cyclodextrin (HP‐γ‐CD) was studied at different temperatures using the method combining phase‐solubility technique and CZE. In contrast to mobility shift ACE utilizing the electrophoretic mobility, in this approach, the peak areas are used. The apparent binding (stability, formation) constants are obtained by the Higuchi and Connors method from the linear segment of compound solubility diagrams in CD solutions. It was found that the apparent binding constants of the HP‐γ‐CD complexes of BIA and BOA decrease with increasing temperature. The binding constants of BOA complexes are slightly higher than those of BIA complexes; this can be explained by difference in the hydration degrees of carbonyl and hydroxyl groups. On the basis of the binding constants obtained and their temperature dependences (van't Hoff plot), the enthalpy as well as entropy changes and Gibbs free energies were calculated. It was found that the complexation was characterized by negative changes of enthalpy and entropy, that is, it was controlled by enthalpy changes. The results obtained can be used for the optimization of microcapsulation processes of BOA and BIA with the HP‐γ‐CD application in order to increase solubility and bioavailability of these compounds.

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Inclusion complex of sulfadimethoxine with cyclodextrins: Preparation and characterization

Rajendiran

Siva

2014

Carbohydrate Polymers

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Analysis of the complexation of gemfibrozil with γ- and hydroxypropyl-γ-cyclodextrins

Cited by 12 publications

References 17 publications

A Comprehensive Study of Gemfibrozil Complexation with β-Cyclodextrins in Aqueous Solution Using Different Analytical Techniques

A Comprehensive Study of Gemfibrozil Complexation with β-Cyclodextrins in Aqueous Solution Using Different Analytical Techniques

Thermodynamic parameters for the complexation of water‐insoluble betulin derivatives with (2‐hydroxypropyl)‐γ‐cyclodextrin determined by phase‐solubility technique combined with capillary zone electrophoresis

Inclusion complex of sulfadimethoxine with cyclodextrins: Preparation and characterization

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