Dissolution behavior of β-cyclodextrin molecular inclusion complexes of aceclofenac

Dua, Kamal; Pabreja, Kavita; Ramana, M. M. V.; Lather, Vinny

doi:10.4103/0975-7406.84457

Cited by 50 publications

(27 citation statements)

References 23 publications

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“…In the spectra of all physical mixture and SD formulations, major characteristic peaks of both drug individually and polymer were retained. We expect that there was no chemical interactions amongst the components of the formulation and compatibility of the drug with the carrier (Arora et al, 2010;Dua et al, 2011). The study indicates that CA Probability has strong physical interaction with poloxamer 188 in solid state.…”

Section: Ftir Analysismentioning

confidence: 92%

Preparation and characterization of cefuroxime axetil solid dispersions using poloxamer 188

Sankari

Al-Hariri

2018

Braz. J. Pharm. Sci.

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The main objective of the present work was to enhance the solubility and dissolution rate of poorly water-soluble drug cefuroxime axetil (CA) by formulating it into solid dispersions (SDs) with water soluble carrier poloxamer 188. Different methods were employed to prepare the dispersion, such as: Solvent method (SM), Kneading method (KM), Melt evaporation method (MEM) and Physical mixture (PM) in different drug: carrier ratios 1:1, 1:2 and 1:3 (cefuroxime axetil: poloxamer 188). The physical mixture(s) and solid dispersion(s) were characterized for drug carrier interaction, drug content, solubility, dissolution rate, differential scanning calorimetry (DSC) and FT-IR study. The dissolution rate of the prepared solid dispersion systems was determined in phosphate buffer (pH 6.8) for 1 h. The solubility of drug from different systems was also determined in water. All SD formulations were found to have a higher dissolution rate comparatively to pure CA. The dissolution rate was enhanced in the following order SM > MEM > KM. The enhancement of dissolution rate may be caused by increase wettability, dispersibillity reduction in particle size or the formation of CA β crystalline. The FT-IR study probability revealed that there was no chemical interaction between drug and poloxamer 188.

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Section: Ftir Analysismentioning

confidence: 92%

Preparation and characterization of cefuroxime axetil solid dispersions using poloxamer 188

Sankari

Al-Hariri

2018

Braz. J. Pharm. Sci.

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“…ICs with βCD increased the dissolution rate, due to the formation of watersoluble inclusion complexes. It clearly indicates the interactions between the hydrophobic part of the drug and the apolar cavity causes dehydration of the hydrophobic drug molecule and its transfer into the cavity, thereby increasing the affinity towards water and hence increasing the dissolution 26 . These findings confirm that the addition of small amounts of PEG 4000 improves solubilizing and complexing ability of cyclodextrin which further related to increased release of drug in dissolution medium.…”

Section: In Vitro Disintegration Time (Dt)mentioning

confidence: 99%

Dissolution Rate Enhancement of Entacapone and Formulation of its Oro- Dispersible Tablets: Applying Statistical Design

Kumar¹,

Murthy²,

Sameeraja³

et al. 2016

IJPER

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The major aim of the study was to enhance the solubility and dissolution rate of entacapone by complexation with cyclodextrins (β-CD/HP β-CD). Further the selected cyclodextrin complexes are deigned to formulate oro-dispersible tablets (ODTs) using selected concentration of PEG 4000 as hydrophilic polymer and crospovidone as superdisintegrant. The phase solubility behavior of entacapone in presence of various concentrations of β-CD, HP β-CD, PEG 4000, PVP and Poloxamer 188 (0.25-5% w/v) was studied at 37 ± 2 o C. Gibbs free energy (∆G°t r ) values in negative, indicates the spontaneous nature of entacapone solubilization. From dissolution rate studies it was observed β-CD complexes were better over HP β-CD and are formulated to ODTs by direct compression method. Response surface modeling approach (2 3 full factorial design) was used for design, development and data interpretation. The responses of the design were analyzed using Design Expert 8.0.7.1 (Stat-Ease Inc., USA). The optimized formulation was selected on the basis of software analysis with an overall desirability factor. The optimized formulation showed disintegration time of 40-42s, friability of 0.55% and a release of more than 85% within 45 m. The physicochemical characterizations of inclusion complexes and the optimized tablet formulation were done by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD).

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“…Solid dispersions are among the techniques successfully employed to enhance the dissolution of poorly watersoluble drugs. [1][2][3][4][5][6][7][8][9] Traditionally, solid dispersions are prepared by the melting, melting-solvent or solvent methods. Newer methods for the manufacture of solid dispersions include hot spin mixing, 10 supercritical fluid technology and hot-melt extrusion (HME).…”

Section: Introductionmentioning

confidence: 99%

Preparation, characterization and in vitro evaluation of tablets containing microwave-assisted solid dispersions of apremilast

et al. 2019

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Background. Solid dispersions are among the techniques successfully employed to enhance the dissolution of poorly water-soluble drugs. Microwave (MW)-assisted evaporative crystallization has been used to prepare solid dispersions of drugs and polymers.Objectives. The aim of the study was to investigate the solubility of apremilast (APM) in water by exploring the effect of MW-assisted solid dispersion technology. Material and methods.In the present study, solid dispersions of APM, a poorly water-soluble drug, were prepared. The solid dispersions were prepared using the conventional method (CM) and the MW-based solvent evaporation technique. Microwave energy was used to enhance the solubility and dissolution rate of APM. The physical mixture and solid dispersions were characterized using Fourier-transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Apremilast tablets containing MW-assisted solid dispersions were prepared by the direct compression technique and compared with the marketed formulation (Aprezo tablets). Results.The results obtained confirmed the conversion of crystalline APM to an amorphous form. The XRPD pattern of the MW-assisted formulation at a 2:1 ratio suggests the amorphous structure of APM within the formulation. Based on solubility studies results, Syloid ® 244FP was selected as the best carrier. The dissolution study results suggested that the APM tablet prepared using MW-assisted solid dispersions at a 2:1 carrier/drug ratio improved the APM dissolution rate compared to the marketed formulation.Conclusions. Based on the results, it can be concluded that the MW-assisted solid dispersion technique may be an effective approach to enhancing the dissolution profile of other poorly water-soluble drugs. Cite asMadan JR, Pawar AR, Patil RB, Awasthi R, Dua K. Preparation, characterization and in vitro evaluation of tablets containing microwave-assisted solid dispersions of apremilast.

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Dissolution behavior of β-cyclodextrin molecular inclusion complexes of aceclofenac

Cited by 50 publications

References 23 publications

Preparation and characterization of cefuroxime axetil solid dispersions using poloxamer 188

Preparation and characterization of cefuroxime axetil solid dispersions using poloxamer 188

Dissolution Rate Enhancement of Entacapone and Formulation of its Oro- Dispersible Tablets: Applying Statistical Design

Preparation, characterization and in vitro evaluation of tablets containing microwave-assisted solid dispersions of apremilast

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