A Simple and Inexpensive Image Analysis Technique to Study the Effect of Disintegrants Concentration and Diluents Type on Disintegration

Berardi, Alberto; Bisharat, Lorina; Blaibleh, Anaheed; Pavoni, Lucia; Cespi, Marco

doi:10.1016/j.xphs.2018.06.008

Cited by 34 publications

(27 citation statements)

References 28 publications

(57 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…On the contrary, zein, which has poor tabletability [13], is not likely to undergo significant plastic deformation, and thus, swells in all directions. A similar correlation between compaction properties and mechanism of tablets expansion has also been found in immediate-release tablets containing swelling disintegrants [23,25].…”

Section: Resultssupporting

confidence: 63%

“…The “hour-glass” shape can be ascribed to the release of the stored energy of compression upon hydration of the plastic MCC. This shape of expansion has been previously documented for immediate release tablets containing highly plastic, so-called shape-recovery disintegrants (e.g., crospovidone) [23,40]. Since the density of a flat-shaped tablet is greater at the edges [41,42], the release of energy of the compressed MCC particles upon hydration is greater at the edges than in other areas of the tablet, ultimately resulting in the formation of this “hour-glass” shape.…”

Section: Resultsmentioning

confidence: 61%

“…The volumetric swelling of tablets was measured by taking pictures of the tablets using a USB-microscope and analyzing the collected images with an image analysis software. A technique previously developed to study the disintegration of immediate-release tablets was adapted here to study tablet swelling [23,24,25].…”

Section: Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients

et al. 2019

View full text Add to dashboard Cite

Zein is an insoluble, yet swellable, biopolymer that has been extensively studied for its applications in drug delivery. Here, we screened the effect of co-excipients on the swelling and drug release of zein tablets. All throughout the study the behavior of zein was benchmarked against that of hydroxypropyl methylcellulose (HPMC) and ethylcellulose (EC). Tablets containing either zein, HPMC, or EC alone or in combination with co-excipients, namely lactose, dicalcium phosphate (DCP), microcrystalline cellulose (MCC), polyvinylpyrrolidone (PVP), or sodium lauryl sulfate (SLS) were prepared by direct compression. Matrix swelling was studied by taking continuous pictures of the tablets over 20 h, using a USB microscope connected to a PC. The overall size change and the axial and radial expansion of the tablets were automatically extrapolated from the pictures by image analysis. Moreover, drug release from tablets containing ternary mixtures of zein, co-excipients and 10% propranolol HCl was also studied. Results showed that zein matrices swelled rapidly at first, but then a plateau was reached, resulting in an initial rapid drug burst followed by slow drug release. HPMC tablets swelled to a greater extent and more gradually, providing a more constant drug release rate. EC did not practically swell, giving a nearly constant drug release pattern. Among the additives studied, only MCC increased the swelling of zein up to nearly three-fold, and thus suppressed drug burst from zein matrices and provided a nearly constant drug release over the test duration. Overall, the incorporation of co-excipients influenced the swelling behavior of zein to a greater extent compared to that of HPMC and EC, indicating that the molecular interactions of zein and additives are clearly more complex and distinct.

show abstract

Section: Resultssupporting

confidence: 63%

Section: Resultsmentioning

confidence: 61%

See 1 more Smart Citation

Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients

et al. 2019

View full text Add to dashboard Cite

show abstract

“…Under storage, tablets might undergo changes that hamper disintegration. This is because disintegrants are amorphous polymers that can hydrate on exposure -not only to water 20,21 -but also to moisture, 22 leading to changes on storage. It is intuitive that the "pre-activation" of the disintegrant swelling due to absorbed moisture can be deleterious to the disintegrant performance.…”

Section: Introductionmentioning

confidence: 99%

“…On exposure to fluids, the hydrated particles tend to regain their pre-compression shape, thus expanding axially, in the opposite direction of compression, a phenomenon called shape-recovery. 20,21,26 The hydration of the particles exposed to moisture appears to be sufficient to initiate, prematurely, the strain recovery, ultimately dissipating the disintegrant efficacy. 24,25 SSG and CCS, which act mainly by swelling rather than shape-recovery, 20,21,26 are less prone to humidity effects.…”

Section: Introductionmentioning

confidence: 99%

Disintegrant Selection in Hydrophobic Tablet Formulations

Bauhuber¹,

Warnke²,

Berardi

2021

Journal of Pharmaceutical Sciences

Self Cite

View full text Add to dashboard Cite

The hydrophobicity of poorly soluble drugs can delay tablets disintegration. We probed here the influence of different disintegrants on the disintegration of challenging hydrophobic formulations. Tablets containing diluents, hydrogenated vegetable oil and either sodium starch glycolate (SSG), croscarmellose sodium (CCS) or crospovidone (XPVP) were prepared. The disintegration time of tablets was tested immediately and after storage at 40 C and 75% RH in sealed bags. Results show that storage and compression force had a negative effect on disintegration, particularly with 1% disintegrant. The performance of the three disintegrants was in the following order: CCS (best) > SSG > XPVP. For example, tablets containing 1% CCS, SSG and XPVP, compressed at 20 kN, disintegrated in z3, z12 and z69 min, respectively, after two months storage. Settling volume, liquid uptake and effect of storage on physical properties of the pure disintegrants were also studied and revealed that the reduced performance of XPVP is related to: 1) its rapid, yet short-range expansion upon liquid exposure and 2) its change of behaviour on storage. In conclusion, CCS ensured rapid disintegration at low concentration across various compression forces and storage times. Thus, the use of CCS in hydrophobic tablet formulations is recommended.

show abstract

Seeing Is Believing: Time-Lapse Macro-Imaging of Morphological Changes of Solid Dosages as a Teaching and Research Tool

Deng

2022

Pharm Res

View full text Add to dashboard Cite

A Simple and Inexpensive Image Analysis Technique to Study the Effect of Disintegrants Concentration and Diluents Type on Disintegration

Cited by 34 publications

References 28 publications

Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients

Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients

Disintegrant Selection in Hydrophobic Tablet Formulations

Seeing Is Believing: Time-Lapse Macro-Imaging of Morphological Changes of Solid Dosages as a Teaching and Research Tool

Contact Info

Product

Resources

About