Preparation, Physical Characterization, Mechanisms of Drug/Polymer Interactions, and Stability Studies of Controlled-Release Solid Dispersion Granules Containing Weak Base as Active Substance

Goračinova, Katerina; Klisarova, L.; Simov, A.; Fredro-Kumbaradzi, Emilija; Petrusevska-tozi, L.

doi:10.3109/03639049609058569

Cited by 16 publications

(10 citation statements)

References 9 publications

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“…The release of drug from all formulations was observed to follow the first order release kinetics, since the correlation coefficient (R 2 ) for first order was higher in comparison to zero order release. The results were in agreement with the previous investigations performed by Goracinova et al, [40] Shivkumar et al, [41] and El-Maradny et al [42] The data was further subjected to Higuchi equation and Hixson-Crowell cube root law. A higher correlation, as indicated by R 2 was observed for the Higuchi matrix release kinetics in all the selected formulations suggesting the diffusion as a probable prominent mechanism of drug release.…”

Section: In Vitro Release Studiessupporting

confidence: 87%

“…A higher correlation, as indicated by R 2 was observed for the Higuchi matrix release kinetics in all the selected formulations suggesting the diffusion as a probable prominent mechanism of drug release. [40,41] In diffusion, the rate of dissolution of drug particles within the matrix must be much faster than that of the diffusion rate of drug leaving the matrix. The selection criteria (R 2 ) and the equations best describing the kinetics of in vitro drug release is given in Table 4.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

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Preparation, Characterization, and In Vitro Evaluation of Aceclofenac PVP-Solid Dispersions

Dua

Pabreja

Ramana

et al. 2011

Journal of Dispersion Science and Technology

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The objective of the present investigation was to study the effect of polyvinylpyrrolidone (PVP) on in vitro dissolution of aceclofenac from solid dispersions. Aceclofenac binary solid dispersions (SD) with different drug loadings were prepared using the melting or fusion method. In vitro dissolution of pure drug, physical mixtures, and solid dispersions were carried out. Solid dispersion of aceclofenac with PVP showed considerable increase in the dissolution rate in comparison with physical mixture and pure drug in 0.1 N HCl, pH 1.2 and phosphate buffer, pH 7.4. Solid dispersions in 1:2 ratio showed maximum dissolution rate in comparison to other ratios. The amorphous nature of the drug in solid dispersion was confirmed by scanning electron microscopy and a decrease in enthalpy of drug melting in solid dispersion compared to the pure drug. FTIR spectroscopy and differential scanning calorimetry studies indicated no interaction between aceclofenac and PVP in solid dispersions in solid state. Dissolution enhancement was attributed to decreased crystallinity of the drug and to the wetting, eutectic formation, and solubilizing effect of the carrier from the solid dispersions of aceclofenac. In conclusion, dissolution of aceclofenac can be enhanced by the use of hydrophilic carriers like PVP.

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Section: In Vitro Release Studiessupporting

confidence: 87%

Section: In Vitro Release Studiesmentioning

confidence: 99%

Preparation, Characterization, and In Vitro Evaluation of Aceclofenac PVP-Solid Dispersions

Dua

Pabreja

Ramana

et al. 2011

Journal of Dispersion Science and Technology

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show abstract

“…The results were in agreement with the previous investigations performed by Shivkumar et al [33] A higher correlation, as indicated by R 2 was observed for the Higuchi matrix release kinetics in all the selected formulations suggesting the diffusion as a probable prominent mechanism of drug release. [33,34] In diffusion, the rate of dissolution of drug particles within the matrix must be much faster than that of the diffusion rate of drug leaving the matrix (Tables 4 and 5).…”

Section: Kinetic Analysis Of Drug Releasementioning

confidence: 98%

Enhancement of Dissolution Behavior of Aceclofenac by Complexation with β-Cyclodextrin-Choline Dichloride Coprecipitate

Dua

Pabreja

Ramana

2011

Journal of Dispersion Science and Technology

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The objective of the present investigation was to study the effect of presence of choline dichloride (CDC) in b-cyclodextrin (b-CD) on in vitro dissolution of aceclofenac (AF) from molecular inclusion complexes. The molecular inclusion complexes of AF with b-CD coprecipitated with CDC in 1:1 and 1:2 M ratio were prepared using kneading method. In vitro dissolution of pure drug, physical mixtures, and cyclodextrin inclusion complexes (AF-b-CD-CDC) were carried out. Molecular inclusion complexes of aceclofenac with coprecipitated b-CD showed considerable increase in the dissolution rate in comparison with physical mixture and pure drug in 0.1 N HCl, pH 1.2 and phosphate buffer, pH, 7.4. Inclusion complexes with 1:2 M ratio showed maximum dissolution rate in comparison to other ratios. FTIR spectroscopy and differential scanning calorimetry studies indicated no interaction between AF and b-CD-CDC in complexes in solid state. Dissolution enhancement was attributed to the formation of water soluble inclusion complexes with the precipitated form of b-CD. The in vitro release from all the formulations was best described by first order kinetics (R 2 ¼ 0.9354 and 0.9268 in 0.1 N HCl and phosphate buffer, respectively) followed by Higuchi release model (R 2 ¼ 0.9029 and 0.9578 in 0.1 N HCl and phosphate buffer, respectively). In conclusion, dissolution of aceclofenac can be enhanced by using the b-CD-CDC coprecipitate as a host molecule.

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“…Atualmente, os ensaios de dissolução constituem importante ferramenta no desenvolvimento de novas formulações (Dredán et al, 1996;Goracinova et al, 1996;O'Hara et al, 1997;Pinho, Storpirtis, 1999;Williams et al, 1991) e na garantia de qualidade dos medicamentos (Steinijans et al, 1988). Estes testes adquirem maior relevância quando podem ser correlacionados com dados obtidos em testes in vivo, o que permite prever o comportamento de uma formulação específica no organismo humano a partir de dados obtidos in vitro.…”

Section: Introductionunclassified

Avaliação biofarmacêutica in vitro de cápsulas de fluconazol

Porta¹,

Yamamichi²,

Storpirtis³

2002

Rev. Bras. Cienc. Farm.

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Preparation, Physical Characterization, Mechanisms of Drug/Polymer Interactions, and Stability Studies of Controlled-Release Solid Dispersion Granules Containing Weak Base as Active Substance

Cited by 16 publications

References 9 publications

Preparation, Characterization, and In Vitro Evaluation of Aceclofenac PVP-Solid Dispersions

Preparation, Characterization, and In Vitro Evaluation of Aceclofenac PVP-Solid Dispersions

Enhancement of Dissolution Behavior of Aceclofenac by Complexation with β-Cyclodextrin-Choline Dichloride Coprecipitate

Avaliação biofarmacêutica in vitro de cápsulas de fluconazol

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