Cited by 439Drug Solubulity and Delivery SystemsGranular flow and fluidized bedsCrystallization and Solubility Studies

A review of disintegration mechanisms and measurement techniques

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Markl, Daniel, Zeitler, J. Axel·2017·Pharmaceutical Research

Abstract

Pharmaceutical solid dosage forms (tablets or capsules) are the predominant form to administer active pharmaceutical ingredients (APIs) to the patient. Tablets are typically powder compacts consisting of several different excipients in addition to the API. Excipients are added to a formulation in order to achieve the desired fill weight of a dosage form, to improve the processability or to affect the drug release behaviour in the body. These complex porous systems undergo different mechanisms when they come in contact with physiological fluids. The performance of a drug is primarily influenced by the disintegration and dissolution behaviour of the powder compact. The disintegration process is specifically critical for immediate-release dosage forms. Its mechanisms and the factors impacting disintegration are discussed and methods used to study the disintegration in-situ are presented. This review further summarises mathematical models used to simulate disintegration phenomena and to predict drug release kinetics.

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  • Open porosity is crucial for enabling fluid access and initiating tablet dissolution.

    “The open porosity, i.e., the pore space accessible from the surface, is crucial for enabling fluid access and initiating tablet dissolution, which is an essential process in an effective treatment using an orally delivered drug product.”
  • Disintegration time is known to largely depend on tablet porosity and is in many cases the rate-determining process.

    “DT is known to largely dependent on the tablet porosity and it is in many cases the rate-determining process [6,7].”
  • For IR tablets, drug release and dissolution cannot occur without disintegration.

    “tablet disintegration is a necessary requirement for release and dissolution of the drug from IR tablets”
  • High tablet porosity permits rapid liquid penetration and wicking, which exposes the disintegrant to solvent, increases swelling, and leads to tablet breakdown.

    “Generally, high tablet porosities allow fast liquid penetration/wicking rate, which then quickly exposes the disintegrant to the penetrating solvent and thus culminating in an increased swelling rate and the final breakdown of the tablet 22 .”

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References 205 · Cited by 439

Research works printed but not linked: 2

  1. [24]Maney P Kuever R Enteric coating Journal of the American Pharmaceutical Association 1941 30 10 276 82
  2. [142]Yassin S, Goodwin DJ, Anderson A, Zeitler JA. The Disintegration Process in Microcrystalline Cellulose Based Tablets, Part 2: Role of Binder, Disintegrant, Lubricant and Active Pharmaceutical Ingredient. Journal of Pharmaceutical Sciences. 2017;p. submitted.

Authors
Markl, D., & Zeitler, J. A.
Affiliations
University of Cambridge (GB)
Corresponding author
Zeitler, J. Axel
Venue
Pharmaceutical Research
Published
2017-03-01
Volume
34
Issue
5
Pages
890-917
ISSN
  • 0724-8741 (ISSN-L)
  • 1573-904X
OpenAlex
W2592176131
Cited by
439
References
205
Citations by year
2026: 58 · 2025: 54 · 2024: 64 · 2023: 65 · 2022: 48 · 2021: 57 · 2020: 48 · 2019: 21 · 2018: 18 · 2017: 5
FWCI
2.63
Type
journal article
Language
en
Open access
Locations
  • Pharmaceutical Research (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • Strathprints: The University of Strathclyde institutional repository (University of Strathclyde) (submittedVersion)
  • Apollo (University of Cambridge) (submittedVersion, cc-by)
  • Apollo (cc-by)
Funders
Engineering and Physical Sciences Research Council (EP/L019922/1)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Physical Sciences › Engineering › Computational Mechanics › Granular flow and fluidized beds
  • Physical Sciences › Materials Science › Materials Chemistry › Crystallization and Solubility Studies
Keywords
tablet disintegration, disintegration mechanism, pharmaceutical solid dosage forms, pharmaceutical excipients, immediate-release formulation, dissolution, drug release kinetics
MeSH terms
Capsules, Chemistry, Pharmaceutical, Excipients, Humans, Powders, Solubility, Tablets, Technology, Pharmaceutical

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