Effect of Superdisintegrants on Dissolution of Cationic Drugs

Balasubramaniam, J.; K, Bindu; Rao, Vinay Umesh; Ray, Debajyoti; Haldar, Rohit; Brzeczko, Albert W.

doi:10.14227/dt150208p18

Cited by 47 publications

(23 citation statements)

References 12 publications

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“…These results are in accordance with an earlier study by Balasubramaniam et al (2008), where the disintegration time of clopidogrel tablets containing Polyplasdone XL showed the fastest release in compendial medium (pH 2.0), compared with SSG and croscarmellose sodium. The authors explained their results on the basis that of the commonly used superdisintegrants, crospovidone is nonionic, while SSG and croscarmellose sodium are anionic.…”

Section: Tablet Disintegrationsupporting

confidence: 93%

“…The authors explained their results on the basis that of the commonly used superdisintegrants, crospovidone is nonionic, while SSG and croscarmellose sodium are anionic. It has been proposed that any weakly basic (cationic) drug, when present in an environment where the pH is >2 and near or below the pKa of the cationic drug, should be expected to interact with ionised polymers like croscarmellose sodium and SSG (Balasubramaniam et al, 2008).…”

Section: Tablet Disintegrationmentioning

confidence: 99%

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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: 93%

Section: Tablet Disintegrationmentioning

confidence: 99%

Formulation and evaluation of orally disintegrating clopidogrel tablets

Mahrous

Kassem

Ibrahim

et al. 2016

Braz. J. Pharm. Sci.

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“…The T 30% was determined by fitting the dissolution data to a four parametric logistic model using the Marquardt-Levenberg algorithm (Sigmaplot 9.0 SPSS Inc., Chicago, IL, U.S.A.). 17) In this equation, y, represents the cumulative % drug released; x, the time in min; min, the baseline of % drug released at time 0 min; max, the plateau of % drug released at time 60 min and hill slope, the slope of the curve at transition center EC 50 .…”

Section: In-vitro Dissolution Studiesmentioning

confidence: 99%

Enhanced Dissolution and Bioavailability of Raloxifene Hydrochloride by Co-grinding with Different Superdisintegrants

Jagadish¹,

Yelchuri²,

K³

et al. 2010

Chem. Pharm. Bull.

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The present study investigated the effect of co-grinding raloxifene HCL (RHCL) with different superdisintegrants, namely crospovidone (CP), croscarmellose sodium (CCS) and sodium starch glycolate (SSG), using a ball mill, in order to determine the potential effect on dissolution rate and bioavailability of raloxifene hydrochloride (RHCL). The dissolution studies of the co-ground compositions and the corresponding physical mixtures were carried out in U.S. Pharmacopeia (USP) Type II apparatus. The solid state interactions of the co-ground and the physical mixtures were evaluated by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The pharmacokinetics of co-ground mixture (1 : 5 RHCL : CP) and milled RHCL was evaluated following oral administration (25 mg/kg) in healthy female Sprague-Dawley rats. DSC studies showed that the crystalline nature of RHCL was reduced after co-grinding with superdisintegrants, while co-grinding with CP resulted in significant particle-size reduction of the mixture. Significant enhancement in dissolution rate was observed with coground mixture of RHCL with CP (1 : 5). The extent of the mean plasma exposures of RHCL was 7-fold higher in animals treated with co-ground mixture of RHCL, CP (1 : 5) compared to animals treated with milled RHCL. Co-grinding of RHCL with CP, reduced drug crystallinity, increased the rate and extent of dissolution, and improved bioavailability.

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“…This may be due to crospovidone swell by 95% to 120% upon contact with water; in addition, during tablet compaction the highly compressible crosspovidone particles become extremely deformed. As the deformed crosspovidone particles come in contact with water that is wicked into the tablet, the particles recover their normal structure and then swell, resulting in rapid volume expansion and high hydrostatic pressures that cause tablet disintegration (Balasubramaniam et al 2008). Moreover, Zade, Kawtikwar et al investigated the effect of type and concentration of the disintegrants (Croscarmellose Sodium, Sodium starch glycolate and crospovidone) on tizanidine ODTs properties.…”

Section: Analysis Of Fitted Datamentioning

confidence: 99%

Formulation and Optimization of Vardenafil Hydrochloride Oral Disintegrating Tablets: Effect of Superdisintegrants

Mourad

Kadry

2016

Al-Azhar Journal of Pharmaceutical Sciences

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One of the fruitful results of oral technological advancement in dosage forms is the orally disintegrating tablets (ODTs) as they disintegrate rapidly in the mouth and do not require water for administration. This work employed mixture design approach for developing and optimizing oral disintegrating tablets of a slightly water soluble drug, vardenafil hydrochloride. Three component mixture design was used to optimize the type and concentration of superdisntegrants, crosscarmellose sodium (X 1 ), crosspovidone (X 2 ) and sodium starch glycolate (X 3 ) using water soluble dextrates (Emdex of the ODTs. The lowest disintegration time, wetting time and t 90 were showed by ODTs formula composed of 1.72 % of crosscarmellose in combination with 4.28 % of crosspovidone. So, this formula was chosen as the optimized formula. Stability studies also showed that the optimized formula was stable under accelerated conditions. And, by comparing the selected formula with Prosolv ® ODT G2 as a ready ODT system, it showed faster disintegration time and higher dissolution rate. Hence, the best superdisintegrants to be used with the water soluble dextrates are crosspovidone in combination with crosscarmellose sodium.

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Effect of Superdisintegrants on Dissolution of Cationic Drugs

Cited by 47 publications

References 12 publications

Formulation and evaluation of orally disintegrating clopidogrel tablets

Formulation and evaluation of orally disintegrating clopidogrel tablets

Enhanced Dissolution and Bioavailability of Raloxifene Hydrochloride by Co-grinding with Different Superdisintegrants

Formulation and Optimization of Vardenafil Hydrochloride Oral Disintegrating Tablets: Effect of Superdisintegrants

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