Investigation of the Dissolution Difference between Acidic and Neutral Media of Acetaminophen Tablets Containing a Super Disintegrant and a Soluble Excipient.

Chen, Chun-Ren; Lin, Yaw-Hung; Cho, Shu-Ling; Yen, Shu-Yang; Wu, Hsueh-Ling S.

doi:10.1248/cpb.45.509

Cited by 18 publications

(10 citation statements)

References 1 publication

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“…The different pH media specified by the dissolution test also can contribute to lack of correlation since medium pH is reported to influence the efficiency of several tablet disintegrants. [9][10][11] In addition, this lack of correlation can also in part be attributed to the specific design of the USP disintegration apparatus. According to the USP specification, "complete disintegration is defined as that state in which any residue of the unit, except fragments of insoluble coating or capsule shell, remaining on the screen of the test apparatus is a soft mass having no palpably firm core."…”

Section: Introductionmentioning

confidence: 99%

Functionality comparison of 3 classes of superdisintegrants in promoting aspirin tablet disintegration and dissolution

2005

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The aims of this study are (1) to compare the disintegration efficiency, and (2) to develop a discriminating test model for the 3 classes of superdisintegrants represented by AcDi-Sol, Primojel, and Polyplasdone XL10. Using a digital video camera to examine the disintegration process of tablets containing the same wt/wt percentage concentration of the disintegrants, Ac-Di-Sol was found to disintegrate tablets rapidly into apparently primary particles; Primojel also apparently disintegrated tablets into primary particles but more slowly; Polyplasdone XL10 disintegrated tablets rapidly but into larger masses of aggregated particles. The differences in the size distribution generated in the disintegrated tablets likely contribute to the drug dissolution rate differences found for aspirin tablets with similar disintegration rates. The aspirin tablet matrix is proposed as a model formulation for disintegrant efficiency comparison and performance consistency testing for quality control purposes.

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Section: Introductionmentioning

confidence: 99%

Functionality comparison of 3 classes of superdisintegrants in promoting aspirin tablet disintegration and dissolution

2005

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“…However, water uptake properties and swelling do not necessarily correlate well with disintegration performance and the effect may be complicated by the pH of the medium in which the study is conducted. [1,2] In the mid 1980s, Caramella et al proposed that the development of a disintegration force inside a compact is fundamental to tablet disintegration. [3][4][5] However, its acceptance is largely limited by the inaccessible measurement of in loci force generated inside a compact during disintegration and the inevitable simultaneous dissolution of soluble components from the compact.…”

Section: Introductionmentioning

confidence: 99%

The Influence of Product Brand-to-Brand Variability on Superdisintegrant PerformanceA Case Study with Croscarmellose Sodium

Zhao¹,

Augsburger²

2006

Pharmaceutical Development and Technology

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The purpose of this study is to investigate factors influencing croscarmellose sodium functionality with special emphasis on developing a discriminating model tablet formulation to evaluate product brand-to-brand variability. The particle size distribution, water uptake, and swelling properties of five brands of croscarmellose sodium in either neutral water or 0.1 N HCl were studied. Differences were observed in all properties between brands. Media with acidic pH had a negative impact, but to different extents, on both the water uptake and swelling of all croscarmellose sodium brands due to the presence of carboxymethyl sodium substituents. A tablet matrix composed of lactose (75% w/w) and dicalcium phosphate (25% wt/wt) was used to compare the functional equivalency of the five brands of croscarmellose sodium. The tablet disintegration times were inversely proportional to the swelling ability of superdisintegrant in the testing medium regardless of medium temperature and disintegrant concentration. In conclusion; the particle size, total degree of substitution, and the ratio of basic to acidic substituents are important factors that should be considered during product optimization. The tablet matrix composed of lactose and dicalcium phosphate at a weight ratio of 3:1 can be used as a model formulation for product lot-to-lot consistency and product brand-to-brand comparison purposes.

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“…Furthermore, the swelling of some disintegrant particles is also dependent on the pH of the medium. 5,10 Shangraw et al observed that the sedimentation volumes of anionic cross-linked starches and celluloses were significantly reduced in acidic medium, whereas Polyplasdone XL and Starch 1500 remained unchanged.…”

Section: Introductionmentioning

confidence: 99%

The influence of swelling capacity of superdisintegrants in different pH media on the dissolution of hydrochlorothiazide from directly compressed tablets

2005

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The purpose of this study was to investigate the efficiency of superdisintegrants in promoting tablet disintegration and drug dissolution under varied media pH. Significant reductions in the rate and extent of water uptake and swelling were observed for both sodium starch glycolate (Primojel) and croscarmellose sodium (Ac-Di-Sol) in an acidic medium (0.1 N HCl) but not for crospovidone NF (Polyplasdone XL10), a nonionic polymer. When Primojel and Ac-Di-Sol were incorporated in model formulations, a significant increase in tablet disintegration time was observed for slowly disintegrating tablets (lactose-based tablets) but not for the rapidly disintegrating tablets (dicalcium phosphate-based tablets). The dissolution rate of the model drug, hydrochlorothiazide, was found highly dependent on both tablet disintegration efficiency and the solubility of base material(s) in the testing medium. A laser diffraction particle size analyzer proved to be an effective tool for determining the intrinsic swelling of disintegrant particles in different media. Water uptake and swelling were confirmed as 2 important functions of superdisintegrants. The reduced water uptake and swelling capacity of disintegrants containing ionizable substituents in an acidic medium can potentially jeopardize their efficiency in promoting tablet disintegration and the drug dissolution rate.

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Investigation of the Dissolution Difference between Acidic and Neutral Media of Acetaminophen Tablets Containing a Super Disintegrant and a Soluble Excipient.

Cited by 18 publications

References 1 publication

Functionality comparison of 3 classes of superdisintegrants in promoting aspirin tablet disintegration and dissolution

Functionality comparison of 3 classes of superdisintegrants in promoting aspirin tablet disintegration and dissolution

The Influence of Product Brand-to-Brand Variability on Superdisintegrant PerformanceA Case Study with Croscarmellose Sodium

The influence of swelling capacity of superdisintegrants in different pH media on the dissolution of hydrochlorothiazide from directly compressed tablets

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