Physicochemical characterization of solid dispersions of the antiviral agent UC-781 with polyethylene glycol 6000 and Gelucire 44/14

Damian, F.; Blaton, N. M.; Naesens, Lieve; Balzarini, Jan; Kinget, Renaat; Augustijns, Patrick; Mooter, Guy Van den

doi:10.1016/s0928-0987(00)00084-1

Cited by 203 publications

(103 citation statements)

References 19 publications

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“…The dissolution profile of the pure gliclazide and marketed tablet showed 38.3 ± 5.5% and 43.7 ± 4.6 % in 30 min respectively [15]. Drug release of SD with different ratios prepared with PEG 4000 (1:2) showed 81.6 ± 4.6 %, PEG 6000 (1:2) showed 87.4 ± 3.7 % whereas PVP K 30 (1:1) showed 95 ± 3.8 % release in 30 min indicating better release when compared to pure drug and other formulations prepared with PEG 4000 and 6000 [16].…”

Section: Dissolution Studiesmentioning

confidence: 98%

Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques.

Shavi

Kumar

Usha

et al. 2010

Int. J. Drug Delivery

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Abstract:Gliclazide is practically insoluble in water and its bioavailability is limited by dissolution rate. To enhance the dissolution rate and bioavailability the present study was aimed to formulate solid dispersions using different water soluble polymers such as polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000) using fusion method and polyvinyl pyrrolidone K-30 (PVP K 30) by solvent evaporation method. The interaction of gliclazide with the hydrophilic polymers was studied by Differential Scanning Calorimetry (DSC), Fourier Transformation-Infrared Spectroscopy (FTIR) and X-Ray diffraction analysis. Solid dispersions were characterized for physicochemical properties like drug content, surface morphology and dissolution studies. Various factors like type of polymer and ratio of the drug to polymer on the solubility and dissolution rate of the drug were also evaluated. Pharmacokinetic studies of optimized formulation were compared with pure drug and marketed formulation in wistar rats. The dissolution of the pure drug and solid dispersion prepared with PVP K 30 (1:1) showed 38.3 + 4.5 % and 95 + 5.2 % release respectively within 30 min. Peak plasma concentration of pure drug, solid dispersion (PVP K 30) and marketed formulation was found to be 8.76 + 2.5, 16.04 + 5.5 and 9.24 + 3.6 μg/ml respectively, from these results it was observed that there is two fold increase in peak plasma concentration compared to pure drug. Solid dispersion is an effective technique in increasing solubility, dissolution rate and bioavailability of the poorly soluble drugs.

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Section: Dissolution Studiesmentioning

confidence: 98%

Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques.

Shavi

Kumar

Usha

et al. 2010

Int. J. Drug Delivery

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“…[12] Many researchers reported SD using Gelucire (polyglycolized glyceride) by fusion and solvent evaporation techniques. [13][14] Gelucire is a varying mixture of mono, di and triglycerides with polyethylene glycol esters of fatty acids. …”

Section: Introductionmentioning

confidence: 99%

Improvement in Micromeritic Properties and Dissolution Rate of Glimepiride

Sahoo¹

2017

WJPR

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“…The use of solid dispersions in improving the solubility of poorly water-soluble drugs dates back to 1961 (Sekiguchi, Obi, 1961;Patil et al, 2013;Damian et al, 2000). Solid dispersions could be prepared by different methods, including melting, solvent and melting-solvent techniques (Patil et al, 2013;Chiou, Riegelman, 1971).…”

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

Adeli

2016

Braz. J. Pharm. Sci.

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Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical mixtures of azithromycin were made using PEG 4000, 6000, 8000, 12000 and 20000 in various ratios, based on the solvent evaporation method. From the studied drug release profile, it was discovered that the dissolution rate of the physical mixture, as the well as the solid dispersions, were higher than those of the drug alone. There was no chemical incompatibility between the drug and polymer from the observed Infrared (IR) spectra. Drug-polymer interactions were also investigated using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Election Microscopy (SEM). In conclusion, the dissolution rate and solubility of azithromycin were found to improve significantly, using hydrophilic carriers, especially PEG 6000.

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Physicochemical characterization of solid dispersions of the antiviral agent UC-781 with polyethylene glycol 6000 and Gelucire 44/14

Cited by 203 publications

References 19 publications

Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques.

Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques.

Improvement in Micromeritic Properties and Dissolution Rate of Glimepiride

Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

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