Advancing the understanding of the tablet disintegration phenomenon – An update on recent studies

Berardi, Alberto; Bisharat, Lorina; Quodbach, Julian; Rahim, Safwan Abdel; Perinelli, Diego Romano; Cespi, Marco

doi:10.1016/j.ijpharm.2021.120390

Cited by 49 publications

(19 citation statements)

References 62 publications

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“…2 B. Tablets composed of MCC/mannitol and MCC/lactose show a slight increase in porosity after storage at 30%RH and a larger increase for tablets stored at 75%RH. At high humidity conditions, hygroscopic excipients such as MCC and the disintegrants can absorb moisture from the air (as shown by the moisture uptake data in Fig 1 ), resulting in particle expansion (often termed ‘disintegrant pre-activation’) ( Berardi et al, 2021 ). After removal from storage, the absorbed moisture will subsequently be lost and enlarged or swollen particles will shrink to their original size, however, the changes to the microstructure caused by this particle expansion will be irreversible.…”

Section: Resultsmentioning

confidence: 99%

Investigating the role of excipients on the physical stability of directly compressed tablets

Maclean

Khadra

Mann

et al. 2022

International Journal of Pharmaceutics: X

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Stability studies are an integral part of the drug development process for any drug product. In addition to monitoring chemical degradation, the physical stability of a drug product must also be evaluated to ensure that the drug release and performance is not affected by storage. In this study, directly compressed tablets of 16 different formulations were exposed to an accelerated stability program to quantify changes in tablet breaking force, porosity, contact angle and disintegration time. Tablets were exposed to five different storage conditions from 37 ∘ C /30% relative humidity (RH) to 70 ∘ C /75%RH with testing after 2 and 4 weeks of storage. Each formulation contained two different fillers (47% w /w each), a disintegrant (5% w /w) and magnesium stearate (1% w/w). The results show that tablets stored at high humidity show increases in porosity and decreases in tensile strength, particularly if they contain a highly hygroscopic filler such as microcrystalline cellulose (MCC). For tablets stored at high temperature, the most commonly affected property was the tablet wettability, measured by sessile drop contact angle measurements. These results are considered in combination with the performance-controlling disintegration mechanism (Maclean et al., 2021) to identify the critical properties which influence the performance after storage.

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Section: Resultsmentioning

confidence: 99%

Investigating the role of excipients on the physical stability of directly compressed tablets

Maclean

Khadra

Mann

et al. 2022

International Journal of Pharmaceutics: X

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“…It was found that NBD-022 having lower HPO content (HPO content = 8.2%) shows the highest swelling pressure and faster water absorption, reaching a plateau within a short period of time, whereas the NBD-020, which has the highest %HPO content (13.8%), shows a slow water absorption and a smaller swelling pressure (Figure 7). This could be attributed to higher hydrophilicity of NBD-020 grade because of the high substitution of the HPO group, due to which absorption of water occurs slowly over a long period time, thus rendering swelling pressure weaker [54,55]. Hence, from the above study, it can be confirmed that particle size and %HPO content of L-HPC grades have significant effects on water absorption and swelling phenomena.…”

Section: Disintegration Behavior Of L-hpc Gradesmentioning

confidence: 70%

“…Disintegration behavior of the tablet is a complex phenomenon involving various mechanisms such as wicking, swelling, strain recovery, interruption of particle-particle bonds, and heat of interaction [54]. Among them, wicking and swelling are the most widely accepted mechanisms [55]. When disintegrant particles come in contact with water, they swell to a larger extent, usually more than 10 times their original size.…”

Section: Disintegration Behavior Of L-hpc Gradesmentioning

confidence: 99%

Effect of Physical Properties and Chemical Substitution of Excipient on Compaction and Disintegration Behavior of Tablet: A Case Study of Low-Substituted Hydroxypropyl Cellulose (L-HPC)

Mishra¹,

Sauer²

2022

Macromol

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As final attributes of dosage form largely depend on the properties of excipients used, understanding the effect of physicochemical properties of excipients is important. In the present study, six grades of L-HPC with varying degrees of particle size and hydroxypropyl content and the influence of the grade on compaction as well as disintegration behavior were studied. All grades of L-HPC were compressed at different compression loads to achieve different tablet porosity. Compressibility and compactibility of L-HPC grades were evaluated using a modified Heckel equation and percolation model. Further effects of particle size and hydroxypropyl content of L-HPC on tablet porosity and disintegration time were evaluated using a 32 full-factorial design. From compaction studies, it was found that compressibility of L-HPC largely depends upon the particle size with lower particle size grade showing lower compressibility. Whereas consolidation/bonding behavior of L-HPC is independent of particle size and % hydroxypropyl content. By factorial design, it was found that particle size and % hydroxypropyl content have a significant effect on the disintegration behavior of L-HPC. It was found that smaller particle sizes and higher hydroxypropyl content of L-HPC show longer disintegration time. Thus, careful consideration of excipients selection should be made to achieve desired quality attribute of the product.

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“…This might be closely related to the low water uptake and volume increase measured for these tablets, indicating hindered water penetration due to the formation of a GPN (Figure 3a,b). Thus, disintegration might have occurred only at the tablet surface, leading to the reduced number and size of particles formed [51]. At lower porosity, the disintegration performance of NaCMCXL seemed to be advantageous compared to PVPP.…”

Section: Investigation Of Tablet Formulationmentioning

confidence: 99%

Tablet Disintegration and Dispersion under In Vivo-like Hydrodynamic Conditions

et al. 2022

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Disintegration and dispersion are functional properties of tablets relevant for the desired API release. The standard disintegration test (SDT) described in different pharmacopoeias provides only limited information on these complex processes. It is considered not to be comparable to the biorelevant conditions due to the frequent occurrence of high hydrodynamic forces, among other reasons. In this study, 3D tomographic laser-induced fluorescence imaging (3D Tomo-LIF) is applied to analyse tablet disintegration and dispersion. Disintegration time (DT) and time-resolved particle size distribution in close proximity to the tablet are determined in a continuously operated flow channel, adjustable to very low fluid velocities. A case study on tablets of different porosity, which are composed of pharmaceutical polymers labelled with a fluorescent dye, a filler, and disintegrants, is presented to demonstrate the functionality and precision of the novel method. DT results from 3D Tomo-LIF are compared with results from the SDT, confirming the analytical limitations of the pharmacopoeial disintegration test. Results from the 3D Tomo-LIF method proved a strong impact of fluid velocity on disintegration and dispersion. Generally, shorter DTs were determined when cross-linked sodium carboxymethly cellulose (NaCMCXL) was used as disintegrant compared to polyvinyl polypyrrolidone (PVPP). Tablets containing Kollidon VA64 were found to disintegrate by surface erosion. The novel method provides an in-depth understanding of the functional behaviour of the tablet material, composition and structural properties under in vivo-like hydrodynamic forces regarding disintegration and the temporal progress of dispersion. We consider the 3D Tomo-LIF in vitro method to be of improved biorelevance in terms of hydrodynamic conditions in the human stomach.

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Advancing the understanding of the tablet disintegration phenomenon – An update on recent studies

Cited by 49 publications

References 62 publications

Investigating the role of excipients on the physical stability of directly compressed tablets

Investigating the role of excipients on the physical stability of directly compressed tablets

Effect of Physical Properties and Chemical Substitution of Excipient on Compaction and Disintegration Behavior of Tablet: A Case Study of Low-Substituted Hydroxypropyl Cellulose (L-HPC)

Tablet Disintegration and Dispersion under In Vivo-like Hydrodynamic Conditions

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