Effects of Excipients on Swelling and Drug Release from Compressed Matrices

Efentakis, M.; Vlachou, Marilena; Choulis, N.H.

doi:10.3109/03639049709148487

Cited by 32 publications

(14 citation statements)

References 10 publications

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“…Increasing ratio of Na-CMC in the formulations resulted in increasing S.I. and more gel formation which is in similarity to the previous finding in which Na-CMC was used in combination with HPMC (Efentakis et al 1997). Figure 7 shows that Na-CMC increased Swelling Index of the tablets in every pH environment studied when PVAc was replaced by Na-CMC in formulations.…”

Section: Mdt = [N / (N + 1)] X K -1/nsupporting

confidence: 79%

Formulation and characterization of modified release tablets containing ionizid using swellable polymers

Akhtar¹,

Rabbani²,

Sharif³

et al. 2011

Afr. J. Trad. Compl. Alt. Med.

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The aim of this work was to develop swellable modified release (MR) isoniazid tablets using different combinations of polyvinyl acetate (PVAc) and sodium-carboxymethylcellulose (Na-CMC). Granules were prepared by moist granulation technique and then compressed into tablets. In vitro release studies for 12 hr were carried out in dissolution media of varying pH i.e. pH 1.2, 4.5, 7.0 and 7.5. Tablets of all formulations were found to be of good physical quality with respect to appearance (width and thickness), content uniformity, hardness, weight variation and friability. In vitro release data showed that increasing total polymer content resulted in more retarding effect. Formulation with 35% polymer content exhibited zero order release profile and it released 35% of the drug in first hr, later on, controlled drug release was observed upto the 12 th hour. Formulations with PVAc to Na-CMC ratio 20:80 exhibited zero order release pattern at levels of studied concentrations, which suggested that this combination can be used to formulate zero order release tablets of water soluble drugs like isoniazid. Korsmeyer-Peppas modeling of drug release showed that non-Fickian transport is the primary mechanism of isoniazid release from PVAc and Na-CMC based tablets. The value of mean dissolution time decreased with the increase in the release rate of drug clearly showing the retarding behavior of the swellable polymers. The application of a mixture of PVAc to Na-CMC in a specific ratio may be feasible to formulate zero order release tablets of water soluble drugs like isoniazid.

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Section: Mdt = [N / (N + 1)] X K -1/nsupporting

confidence: 79%

Formulation and characterization of modified release tablets containing ionizid using swellable polymers

Akhtar¹,

Rabbani²,

Sharif³

et al. 2011

Afr. J. Trad. Compl. Alt. Med.

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“…At 0.25, 0.5 h and then at hourly intervals up to 7 h, the previously weighed baskets containing the compacts were removed, gently wiped with a tissue in order to remove surface water, reweighed, and then placed back into the vessel as quickly as possible. The mean weights were determined for three compacts of each formulation, and the percentage of swelling (S%) was calculated according to the following relationship: (19).…”

Section: Water Uptake (Swelling) Of Compacted Matrix Componentsmentioning

confidence: 99%

Controlled-Release Carbamazepine Granules and Tablets Comprising Lipophilic and Hydrophilic Matrix Components

2008

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Abstract. The objective of this study was to investigate the effect of lipophilic (Compritol ® 888 ATO) and hydrophilic components (combination of HPMC and Avicel) on the release of carbamazepine from granules and corresponding tablet. Wet granulation followed by compression was employed for preparation of granules and tablets. The matrix swelling behavior was investigated. The dissolution profiles of each formulation were compared to those of Tegretol ® CR tablets and the mean dissolution time (MDT), dissolution efficiency (DE %) and similarity factor (f 2 factor) were calculated. It was found that increase in the concentration of HPMC results in reduction in the release rate from granules and achievement of zero-order is difficult from the granules. The amount of HPMC plays a dominant role for the drug release. The release mechanism of CBZ from matrix tablet formulations follows non-Fickian diffusion shifting to case II by the increase of HPMC content, indicating significant contribution of erosion. Increasing in drug loading resulted in acceleration of the drug release and in anomalous controlled-release mechanism due to delayed hydration of the tablets. These results suggest that wet granulation followed by compression could be a suitable method to formulate sustained release CBZ tablets.

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“…Em tempos previamente determinados (0,25; 0,5; 1; 2; 3 e 4 horas), os comprimidos foram retirados do meio e avaliado o grau de intumescimento (GI) da matriz polimérica, utilizando o método gravimétrico, pela diferença de peso do comprimido seco (Ps) e intumescido (Pi), através da seguinte relação: GI(%) = (Pi -Ps)/ Ps x 100. O ensaio foi realizado em triplicata [17] .…”

Section: Grau De Intumescimento (Gi)unclassified

Avaliação da Goma Guar no desenvolvimento de comprimidos matriciais de liberação controlada de teofilina

et al. 2015

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ResumoO objetivo desse estudo foi formular e avaliar comprimidos de liberação controlada. Comprimidos de liberação controlada de teofilina foram preparadas pelo método de compressão direta usando dois polímeros como, o HPMC K 100M (polímero hidrofílico) e a Goma Guar (Polímero natural), isolado ou em mistura (GG:HPMC 3:1) e GG:HPMC 1:3). Os comprimidos foram caracterizados através do peso médio, diâmetro, altura, dureza, friabilidade. Todos os resultados estiveram em conformidade com os limites aceitáveis. O ensaio de intumescimento foi realizado em água destilada durante 4 horas, sendo determinado pela diferença de peso do comprimido seco e intumescido. O ensaio de dissolução foi realizado em água destilada (900 mL, 37 ± 0,5ºC, 50 rpm, aparato II) durante 8 horas. Os resultados demonstraram que a Goma guar isolada não possui capacidade de retardar a liberação da teofilina por 8 horas. Comprimidos matriciais contendo GG:HPMC (3:1) apresentaram um melhor controle de liberação da teofilina. Palavras-chave: Goma Guar, teofilina, comprimidos, liberação controlada. AbstractGuar gum (GG) has been widely used in drug delivery systems due to its low cost and nontoxicity. Theophylline controlled release tablets were prepared by directly compressed method using two polymers such as HPMC K 100M (hydrophilic polymer) and Guar Gum (natural polymer), isolated or in mixture (GG:HPMC 3:1 and GG:HPMC 1:3). The formulated tablets were evaluated for: weight variation, diameter, height, hardness and friability. All the parameters were within the acceptable limits. The swelling test was performed in distilled water for 4 hours, it was determined by the difference in weight of the dry and swollen tablet. The dissolution test was performed in distilled water (900 mL, 37 ± 0.5ºC, 50 rpm, apparatus II) for 8 hours. The results showed that guar gum alone could not control the theophylline release effectively for 8 hours. Matrix tablet prepared from GG: HPMC (3:1) is a better formulation for the sustained released matrix tablets of theophylline.

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Effects of Excipients on Swelling and Drug Release from Compressed Matrices

Cited by 32 publications

References 10 publications

Formulation and characterization of modified release tablets containing ionizid using swellable polymers

Formulation and characterization of modified release tablets containing ionizid using swellable polymers

Controlled-Release Carbamazepine Granules and Tablets Comprising Lipophilic and Hydrophilic Matrix Components

Avaliação da Goma Guar no desenvolvimento de comprimidos matriciais de liberação controlada de teofilina

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