Crystal modification of phenytoin with polyethylene glycol for improving mechanical strength, dissolution rate and bioavailability by a spherical crystallization technique.

Kawashima, Yasunaru; Handa, Tetsurou; Takeuchi, Hirofumi; Okumura, Motonari; Katou, Hideo; Nagata, Osamu

doi:10.1248/cpb.34.3376

Cited by 30 publications

(21 citation statements)

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“…The mechanism behind the solubility and dissolution rate enhancing effect of celecoxib in crystal form may resemble the solid dispersion mechanism despite the large particle size of the crystals. This effect may be due to improved wettability of the surface of crystals by the adsorption of PVP onto the surfaces of crystals (17). These results clearly reveal that the dissolution rate of celecoxib was increased in the form of spherical agglomerates when compared to its pure form.…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 72%

Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties

Gupta¹,

Mutalik

Patel³

et al. 2007

Acta Pharmaceutica

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Direct tabletting of pharmaceutical materials is desirable to reduce the cost of production (1). However, compressing a high-dosed drug directly requires good micromeritic properties, such as flowability, and good and reproducible compression behavior. Spherical crystallization technique transforms directly the fine particles produced in crystallization or in the reaction process into a spherical shape. Agglomerates exhibit improved secondary characteristics, like flowability and compressibility, so that direct tabletting or coating is possible without further processing (mixing, agglomeration, sieving, etc.) (2, 3). Celecoxib, a non-steroidal anti-inflammatory drug (NSAID), is the first selective cyclooxygenase-2 inhibitor used in the treatment of osteoarthritis and rheumatoid arthritis in adult patients (4). Celecoxib exhibits poor flow and compression charac- Celecoxib spherical agglomerates were prepared with polyvinylpyrrolidone (PVP) using acetone, water and chloroform as solvent, non-solvent and bridging liquid, respectively. The agglomerates were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The IR spectroscopy and DSC results indicated the absence of any interactions between drug and additives. XRD studies showed a decrease in crystallinity in agglomerates. The crystals exhibited significantly improved micromeritic properties compared to pure drug. The loading efficiency (% or mg drug per 100 mg crystals) was in the range of 93.9 ± 2.3 and 97.3 ± 1.3% (n = 3) with all formulations. The aqueous solubility and dissolution rate of the drug from crystals was significantly (p < 0.05) increased (nearly two times). The solubility and in vitro drug release rates increased with an increase in PVP concentration (from 2.5 to 10%). The SEM studies showed that the crystal posseses a good spherical shape with smooth and regular surface.

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Section: In Vitro Dissolution Studiesmentioning

confidence: 72%

Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties

Gupta¹,

Mutalik

Patel³

et al. 2007

Acta Pharmaceutica

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“…Here, increased viscosity reduced the destructive forces acting on the agglomerates. PEG, because of its tendency to reduce interfacial tension, is reported to generate smaller agglomerates [24,25].…”

Section: Resultsmentioning

confidence: 99%

Improvement of Micromeritic, Compressibility and Solubility Characteristics of Linezolid by Crystallo-Co-Agglomeration Technique

Kadam

Patil

2017

Int J App Pharm

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Objective: The purpose of current study was to improve physicochemical properties such as micrometric, compressibility and solubility of linezolid (LNZ) by preparing crystallo-co-agglomerates (CCA) in the presence of polymer for the enhancement of overall physicochemical performance. Methods:The process of agglomeration involves the use of dichloromethane (DCM) as a good solvent and chloroform as bridging liquid were used to prepare agglomerates. Agglomerates were characterised in the solid state using several techniques such as Scanning electronic microscopy(SEM), Fourier transformation infrared spectroscopy (FTIR), X-ray powder diffraction analysis (XRPD) The agglomerates obtained were evaluated for micrometric, mechanical, deformation, compressibility and drug release properties.Results: It was found that micrometric properties and dissolution characteristics of agglomerates were significantly improved than that of pure linezolid. Solubility was found to be increased than pure linezolid. The solubility of crystallo co-agglomerates was found an increase in 5 fold 3 fold and 3.7 fold for PVPK30 (0.5%), PVPK30 (0.25%) and PVPK30 (0.75%) respectively. The angle of repose for all batches was found between 22 ° to 30 °Carrs index was between 12.27±0.6 to 18.73±0.4 and Hausners ratio Near to 1, indicated good flow ability of agglomerates. The time required for drug release over a period of 60 min, is as LA1>LA2>LA3. LA3 shows fast drug release than LA1 and LA2, due to solubilization of drug due to more concentration of PVPK30 and less concentration of talc.Conclusion: Based on the above results, it was revealed that CCA of linezolid prepared with DCM and HPMC (Hydroxypropyl methyl cellulose)/PEG (Polyethylene glycol)/PVP (Polyvinylpyrrolidone) K30 exhibited improved micrometric properties, compressibility and in addition to improving solubility and dissolution rate.

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“…In case of agglomerates with PEG, β-CD, EU, GG and XG average diameter was higher than for the original crystals but lower than for plain agglomerates. These findings suggest that these additives were poorly adsorbed at the surface which would reduce interfacial tension between bridging liquid and crystals, with a consequent decrease in the adhesive force acting to agglomerate the crystals [18].…”

Section: Micrometric Propertiesmentioning

confidence: 99%

Effect of Additives on the Physicochemical and Drug Release Properties of Pioglitazone Hydrochloride Spherical Agglomerates

Patil¹,

Pawar²,

Kumar³

2012

Trop. J. Pharm Res

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Crystal modification of phenytoin with polyethylene glycol for improving mechanical strength, dissolution rate and bioavailability by a spherical crystallization technique.

Cited by 30 publications

References 1 publication

Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties

Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties

Improvement of Micromeritic, Compressibility and Solubility Characteristics of Linezolid by Crystallo-Co-Agglomeration Technique

Effect of Additives on the Physicochemical and Drug Release Properties of Pioglitazone Hydrochloride Spherical Agglomerates

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