Disintegrating efficiency of croscarmellose sodium in a direct compression formulation

Ferrero, C; Muñoz, Nydia; Velasco, María V.; Muñoz‐Ruiz, Angel; Jiménez-Castellanos, R.

doi:10.1016/s0378-5173(96)04784-9

Cited by 42 publications

(33 citation statements)

References 14 publications

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“…It can be concluded that the optimum concentration of superdisintegrant is 5%, which gave rapid disintegration of CL tablets. These results are in agreement with those found by Ferrero et al, who studied the disintegration efficiency of croscarmellose sodium and reported that at high concentrations (> 8%), the disintegration time was found to be longer (Ferrero et al, 1997). Moreover, Jagdale et al (2010) mentioned that CCS gave a short disintegration time at low concentrations with a sudden rise when the concentration was increased from 4% to 6%.…”

Section: Tablet Disintegrationsupporting

confidence: 91%

Formulation and evaluation of orally disintegrating clopidogrel tablets

Mahrous

Kassem

Ibrahim

et al. 2016

Braz. J. Pharm. Sci.

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Recent advances in drug delivery systems have aimed to achieve better patient compliance. One of these advances is the formulation of orally disintegrating tablets (ODTs) that dissolve instantaneously, releasing drugs within a few seconds without the need of water. The main objective of this paper was to prepare and develop ODTs of clopidogrel. The ODTs were prepared by direct compression. The effect of three superdisintegrants, namely crospovidone, croscarmellose sodium, and sodium starch glycolate, using three different disintegration times on the dissolution rate was investigated. The prepared tablets were evaluated for hardness, friability, disintegration time and in vitro drug release. Furthermore, the interaction of clopidogrel with the formulation excipients was studied using differential scanning calorimetry (DSC). DSC studies revealed that there were no interactions between the drug and the excipients used. All tablets had hardness values in the range 4.0-5.2 kp and friability lower than 1%. The weight and drug content uniformity of all formulations was within official limits according to BP. In vitro drug release studies of the ODTs showed that more than 90% of the drug was released within ten minutes. A palatability test in human volunteers showed acceptable taste and mouth feel. Thus, the obtained results conclusively demonstrated successful rapid disintegration of the formulated tablets and acceptable palatability.Uniterms: Clopidogrel/orally disintegrating tablets. Superdisintegrants. Orally disintegrating tablets/ formulation. Orally disintegrating tablets/evaluation.Recentes avanços em sistemas de liberação de fármacos novos visam à obtenção de melhor adesão do paciente. Um destes avanços é a formulação de comprimidos de desintegração oral (ODTs), que se dissolvem instantaneamente, liberando o fármaco, em alguns segundos, sem a necessidade de água. O principal objetivo deste trabalho foi preparar e desenvolver ODTs de clopidogrel. Os ODTs foram preparados pelo método de compressão direta. Estudou-se o efeito de várias concentrações de diferentes agentes de desintegração, tais como super-crospovidona, croscarmelose de sódio, glicolato de amido de sódio no tempo de desintegração e velocidade de dissolução. Os comprimidos preparados foram avaliados quanto à dureza, à friabilidade, ao tempo de desintegração e à liberação do fármaco in vitro. Além disso, estudou-se a interação de clopidogrel com os excipientes de formulação, utilizando calorimetria de varredura diferencial (DSC). Estudos de DSC revelaram não haver interação entre o fármaco e os excipientes utilizados. Todos os comprimidos possuíam dureza na faixa de 4,0-5,2 kp e a friabilidade inferior a 1%. A variação de peso e o teor de fármaco de todas as formulações mostraram-se dentro do limite oficial, de acordo com a BP. O estudo de liberação do fármaco in vitro de comprimidos ODTs mostrou que mais de 90% do fármaco foram liberados em10 minutos. O teste de palatabilidade em voluntários humanos mostrou sabor e sensação na boca aceitáveis. Assim,...

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Section: Tablet Disintegrationsupporting

confidence: 91%

Formulation and evaluation of orally disintegrating clopidogrel tablets

Mahrous

Kassem

Ibrahim

et al. 2016

Braz. J. Pharm. Sci.

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“…Croscarmellose sodium has a high swelling capacity even at low concentrations, disintegrating tablets rapidly (37,39), which in theory should have a positive effect on disintegration time (i.e., decrease with increased concentration); however, in our particular case, it increased disintegration time. A possible explanation might be that sodium croscarmellose reached its peak efficiency at low concentrations and higher ratios of the disintegrant with fibrous structure led to a slight increase in disintegration time due to cohesive forces.…”

Section: Evaluation Of Variables Affecting Tablet Propertiesmentioning

confidence: 74%

Study of the effect of formulation variables on the characteristics of combination tablets containing enalapril maleate and indapamide as active substances using experimental design

Szabó

Székely-Szentmiklósi²,

Deák

et al. 2016

Acta Pharmaceutica

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Study of the effect of formulation variables on the characteristics of combination tablets containing enalapril maleate and indapamide as active substances using experimental designTo evaluate the influence of different variables on tablet formulations containing enalapril maleate and indapamide as active substances, two separate experimental designs were employed: one for evaluating powder properties and the other for tablet characteristics. Because of the low active pharmaceutical ingredient content, it was hypothesized that both powder and tablet properties could be determined only by the characteristics of excipients. In order to test this assumption, both experimental designs were done with placebo mixtures. The optimized formulation was then evaluated both with and without APIs. Results indicated that filler and lubricant percentage, along with compression force, were the most important variables during the formulation study. The optimized formulation showed similar characteristics in both cases for all responses, except for angle of repose and friability where only minor differences were observed. The combination of the applied approaches (using placebo composition and fractional experimental design) proved to be efficient, cost effective and time saving.Keywords: design of experiments, optimization, factorial design, placebo formulation Proper management of hypertension, one of the leading causes of cardiovascular disease, is of the utmost importance. It has been established that lowering of blood pressure can effectively reduce the risk of cardiovascular events and stroke, but finding the most appropriate therapy is often difficult (1). Combinational therapies employing an angiotensin-converting enzyme inhibitor (ACEi) and indapamide (IND) offer the advantage of using two highly effective agents, increasing both clinical efficiency and patient compliance (2-4). Low dose combinations of ACEis and diuretics have shown greater reduction in blood pressure and higher success rates in managing hypertension than either of the treatments alone (4-6). The most popular ACEis present in these combinations include perin- Szabo et al.: Study of the effect of formulation variables on the characteristics of combination tablets containing enalapril maleate and indapamide as active substances using experimental design, Acta Pharm. 66 (2016) 191-206.

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“…This pattern is usually found for most disintegrants, which exhibits a limited concentration range for creating an efficient disintegration [3]. Outside of this limited range, not only can the disintegration time not be decreased, but it can also increase [16]. Due to the poor compactibility of the resin, the increased concentration of resin resulted in the softer and less-compact (i.e.…”

Section: Discussionmentioning

confidence: 99%