Strongly enhanced dissolution rate of fenofibrate solid dispersion tablets by incorporation of superdisintegrants

Srinarong, Parinda; Faber, J.; Visser, Marinella R; Hinrichs, Wouter L. J.; Frijlink, Henderik W.

doi:10.1016/j.ejpb.2009.05.006

Cited by 77 publications

(38 citation statements)

References 18 publications

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“…If the soluble carrier dissolves rapidly, the poorly soluble drug is hydrated faster, thus; it dissolution faster. In the current study, INPs may be considered a solid dispersion (Srinarong et al, 2009;Visser et al, 2010) for SIL and may improve the rate of SIL release from the hydrophilic multiblock copolymer since INPs acted as a pore-former (Stanković et al, 2013).…”

Section: Discussionmentioning

confidence: 99%

Inulin nanoparticles and silymarin counteract chlorpromazine-induced injury in the liver and kidney of rats

Abdel-Wahhab¹,

Eid²,

Ahmed³

et al. 2017

J App Pharm Sci

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The aim of the current study was to evaluate the protective role of inulin nanoparticles (INPs) prepared by the emulsion method alone or plus silymarin (SIL) against chlorpromazine (CPZ)-induced hepatonephrotoxicity in rats. Eleven groups of female Sprague-Dawley rats were treated orally for 3 weeks as follow: control group, the group treated with CPZ (38.7 mg/kg. b.w in 1 ml saline each 72 h), the groups treated with INPs at low (100 mg/kg b.w) or high (200 mg/ kg b.w) dose, the group treated with SIL (50 mg/kg b.w), the groups treated with SIL plus INPs at the two doses and the groups treated with CPZ plus SIL and INPs at the two tested doses. At the end of the treatment period, blood and tissue samples were collected for different biochemical and histological analyses. The results indicated that CPZ induced significant disturbances in liver and kidney function indices, oxidative stress markers, lipid profile, antioxidant enzyme activity and DNA fragmentation as well as the histological changes in the liver and kidney. SIL alone or plus INPs alone at the low or high dose induce insignificant changes in all the tested parameters or pathological changes in the liver and kidney. SIL and INPs at the two doses could induce a pronounced protection in liver and kidney of CPZ-treated animals due to their antioxidant activity and the role of INPs in the enhancement of SIL solubility. It could be concluded that INPs is a promise drug delivery for SIL and could prevent the liver and kidney injury induced by CPZ.

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Section: Discussionmentioning

confidence: 99%

Inulin nanoparticles and silymarin counteract chlorpromazine-induced injury in the liver and kidney of rats

Abdel-Wahhab¹,

Eid²,

Ahmed³

et al. 2017

J App Pharm Sci

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“…Tablets of solid dispersions containing Polyplasdone XL displayed an average disintegration time of 24.0 min while tablets containing Polyplasdone XL10 showed an average disintegration time of 30.6 min (Srinarong et al, 2009).…”

Section: Effect Of Crospovidones On Tablet Disintegrationmentioning

confidence: 99%

Contrasting the crospovidones functionality as excipients for direct compression

Ramírez

Robles

2015

Braz. J. Pharm. Sci.

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Specific values of technological properties of excipients allow the establishment of numerical parameters to define and compare their functionality. This study investigates the functionality of Polyplasdones XL and XL10. Parameters studied included tablet disintegration profiles, compactibility profiles and powder flow. The results allowed the establishment of quantitative surrogate functionalities of technological performance, such as absolute number, and as a value relative to the known microcrystalline cellulose type 102. Moreover, the establishment of an explicit functionality to improve the technological performance of two diluents and a model drug was investigated, as was setting up of these functionalities, as quantitative values, to determine the input variables of each material and its probable functionality in a drug product. Disintegration times of pure Polyplasdone XL and its admixtures were around half that of Polyplasdone XL10. The improvement in tablet compactibility was 25-50% greater for Polyplasdone XL10 than Polyplasdone XL. Crospovidones proportions of up to 10% have little effect on the flow properties of other powders, although pure Polyplasdone XL10 and its admixtures display compressibility indexes about 20% greater than Polyplasdone XL. The observed results are in line with a smaller particle size of Polyplasdone XL10 compared to Polyplasdone XL.Uniterms: Excipients/functionality. Polyplasdones XL/functionality. Polyplasdones XL10/functionality. Tablets/compactibility. Tablets/disintegration time. Tablets/powder flow. Amoxicillin. Magnesium stearate. Superdisintegrants.Os valores específicos de propriedades tecnológicas de excipientes permitem o estabelecimento de parâmetros numéricos para definir e comparar a sua funcionalidade. Este estudo investiga a funcionalidade dos excipientes. Os parâmetros estudados foram perfis de desintegração dos comprimidos, perfis de compactação e fluxo de pó. Os resultados permitiram expressar o desempenho tecnológico através de valores absolutos e valores relativos à conhecida celulose microcristalina tipo 102. Do mesmo modo, permitiram estabelecer uma funcionalidade explícita para melhorar o desempenho tecnológico de dois diluentes e um fármaco modelo. A criação destas funcionalidades, como valores quantitativos, permite conhecer as variáveis de entrada de cada material e sua provável funcionalidade em um medicamento. Os tempos de desintegração do Poliplasdone XL e das suas misturas são cerca da metade do observado para as misturas com o Poliplasdone XL10. Melhoria da compressão de comprimidos que contêm Polyplasdone XL10 é 25-50% maior do que o Polyplasdone XL. Crospovidonas em proporções de até 10% têm pouco efeito sobre as propriedades de fluxo dos outros pós embora o Poliplasdone XL10 e suas misturas exibam índices de compressibilidade cerca de 20% maior do que o Poliplasdone XL. Os resultados observados estão em sintonia com o menor tamanho de partícula do Poliplasdone XL10, em comparação com o Poliplasdone XL.

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“…The SDs are twocomponent systems consisting of a hydrophilic carrier in which the drug is incorporated. The SD technology gives the possibility to reduce the drug particle size almost to a molecular level and increased wettability [4]. In addition to this, the crystalline drug is transformed to amorphous form, which can be beneficial, since the…”

Section: Introductionmentioning

confidence: 99%

Development of Fast-Dissolving Tablets of Amlodipine Besylate by Solid Dispersion Technology Using Poloxamer 407 and Poloxamer 188

Manimaran

Damodharan

2017

Asian J Pharm Clin Res

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Objective: Amlodipine besylate is a calcium channel blocker used in the treatment of hypertension which is practically insoluble in water. The present study aims to design oral fast-release tablets of amlodipine besylate and to optimize the dissolution of the drug by altering the carrier concentration. Materials and Methods:Poloxamer 407 (P407) and poloxamer 188 (P188) were selected as carriers for the preparation of solid dispersion (SD) by the solvent evaporation method with different drug-polymer ratios. The prepared SDs were evaluated for the physical state, drug:carrier interactions by X-ray diffraction (XRD), infrared spectroscopy, differential scanning calorimetry, and scanning electron microscopy. Results:From the dissolution studies, it is confirmed that all SDs showed increased dissolution rate when compared to pure amlodipine besylate. Among the two polymers used, P407 was found to be better than P188 in enhancing dissolution efficiency. The tablets were prepared using SD of amlodipine besylate containing P407 as a carrier. The results showed that P407 SD-based tablets gave a significantly higher release of amlodipine besylate when compared with control tablets. The infrared spectral studies showed that there was no significant interaction between amlodipine besylate and its formulation with different polymers used in the preparation of SDs. XRD studies revealed that the degree of crystallinity of amlodipine besylate reduced when the concentration of carriers increased, which reveals that the drug is in amorphous nature. Conclusion:The combination of SD technology and using superdisintegrants in the formulation is a promising approach for preparing efficient, fastdissolving tablet of poorly water-soluble drugs, viz., amlodipine besylate.

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Strongly enhanced dissolution rate of fenofibrate solid dispersion tablets by incorporation of superdisintegrants

Cited by 77 publications

References 18 publications

Inulin nanoparticles and silymarin counteract chlorpromazine-induced injury in the liver and kidney of rats

Inulin nanoparticles and silymarin counteract chlorpromazine-induced injury in the liver and kidney of rats

Contrasting the crospovidones functionality as excipients for direct compression

Development of Fast-Dissolving Tablets of Amlodipine Besylate by Solid Dispersion Technology Using Poloxamer 407 and Poloxamer 188

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