Effect of disintegrants with different hygroscopicity on dissolution of Norfloxacin/Pharmatose DCL 11 tablets

López-Solı́s, J; Villafuerte-Robles, Leopoldo

doi:10.1016/s0378-5173(01)00584-1

Cited by 18 publications

(6 citation statements)

References 7 publications

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“…As a result, the use of insoluble fillers leaves more water available for the disintegrants. These results supported previous studies which have shown that increased hygroscopicity of the tablet components could also result in decreased disintegration efficiency (Gordon and Chowhan, 1987;López-Solís and Villafuerte-Robles, 2001;Johnson et al, 1991).…”

Section: Introductionsupporting

confidence: 92%

Exploring the performance-controlling tablet disintegration mechanisms for direct compression formulations

Maclean

Walsh

Soundaranathan

et al. 2021

International Journal of Pharmaceutics

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Section: Introductionsupporting

confidence: 92%

Exploring the performance-controlling tablet disintegration mechanisms for direct compression formulations

Maclean

Walsh

Soundaranathan

et al. 2021

International Journal of Pharmaceutics

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“…The addition of Pharmatose DCL, 11 to tablets of the low hygroscopic PVP XL 10 and norfloxacin, showed no inhibition but potentiated the dissolution of norfloxacin substantially. These effects were attributed to competition for the available water inside the tablet and to different water consume, for dissolution or hydration, by the diluent and the disintegrants [25]. Fig.…”

Section: Fig 3: Release Profiles Of Metronidazole Tablets Containingmentioning

confidence: 99%

Influence of Free-Flow Excipients on Functional Performance of Noveonaa1 in Controlled-Release Tablets

Islas

Robles

2016

Int J Pharm Pharm Sci

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Objective: The aim of this work is the assessment of an eventual improvement in flowability of free flowing excipients on formulations containing Noveon AA1 and their influence on compactibility and release profile. Methods:Mixtures containing 20% Noveon AA1 and variable proportions of metronidazole and the free flowing excipients Prosolv EasyTab and GalenIQ 720 and 721were tested in their powder flow rate and the tablets compactibility and released profiles. Results:The powder flowability obtained with GalenIQ is about 20% better than that obtained with EasyTab. However, it is lesser than that considered as acceptable for a high-speed tableting machine. EasyTab reduces the drug release up to a half along with a continuing flattening of the release profile. This is attributed to an increasing tortuosity of the drug release path as the proportion EasyTab increases. GalenIQ restricts drug release in about a third with a lesser change in the release mechanism. This is attributed to competition for the available water inside the tablet, between the hydrating Noveon AA1 and the dissolving GalenIQ. The compactibility of the metronidazole/Noveon AA1 mixtures increases after addition of EasyTab in about 3.5 N per unit percentage of the added excipient while GalenIQ does it in about 2.6 N. Conclusion:The powder flowability of mixtures of metronidazole with Noveon AA1 was not suited for direct compression after addition of 40% of the free-flow excipient. The free-flow excipients reduce the metronidazole release rate and increase its compactibility. It was not observed a different clear functioning between both types of GalenIQ.

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“…In fact, it has been observed that Starch 1500, working as an active disintegrant, and Pharmatose DCL11, as a passive dissolving disintegrant, displayed mutual inhibition to promote norfloxacin tablet dissolution. On the other hand, the addition of mixtures of Starch 1500 and the insoluble diluent calcium phosphate potentiated the disintegrant effect to promote norfloxacin dissolution (López-Solis, Villafuerte-Robles, 2001). …”

Section: Effect Of Crospovidones On Tablet Disintegrationmentioning

confidence: 99%

“…In this sense, it can be useful to test their functionality with tablets of drugs that do not disintegrate easily, such as amoxicillin, and with excipients representing water soluble (lactose) and water insoluble (calcium phosphate) materials. These materials are known to display an important degree of difference in the effectiveness of superdisintegrants (López-Solis, Villafuerte-Robles, 2001). …”

Section: Introductionmentioning

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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Effect of disintegrants with different hygroscopicity on dissolution of Norfloxacin/Pharmatose DCL 11 tablets

Cited by 18 publications

References 7 publications

Exploring the performance-controlling tablet disintegration mechanisms for direct compression formulations

Exploring the performance-controlling tablet disintegration mechanisms for direct compression formulations

Influence of Free-Flow Excipients on Functional Performance of Noveonaa1 in Controlled-Release Tablets

Contrasting the crospovidones functionality as excipients for direct compression

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