Application of percolation threshold to disintegration and dissolution of ibuprofen tablets with different microcrystalline cellulose grades. 2020

Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
SSPC Pharmaceutical Research Centre, School of Pharmacy, University College Cork, Cork, Ireland.

The study presented was conducted to determine whether a percolation threshold value, previously determined for ibuprofen/microcrystalline cellulose (MCC) blends using percolation theory and compression data (Queiroz et al., 2019), could translate to tablet disintegration and dissolution data. The influence of MCC grade (air stream dried versus spray dried) on tablet disintegration and dissolution was also investigated. Complementary to conventional disintegration and dissolution testing, Raman imaging determined drug distribution within tablets, and in-line particle video microscopy (PVM) and focused-beam reflectance measurement (FBRM) monitored tablet disintegration. Tablets were prepared containing 0-30% w/w ibuprofen. Raman imaging confirmed the percolation threshold by quantifying the number and equivalent circular diameters of ibuprofen domains on tablet surfaces. Across the percolation threshold, a step change in dissolution behaviour occurred, and tablets containing air stream dried MCC showed slower disintegration rates compared to tablets containing spray dried MCC. Dissolution measurements confirmed experimentally a percolation threshold in agreement with that determined using percolation theory and compression data. An increase in drug domains, due to cluster formation, and less efficient tablet disintegration contributed to slower ibuprofen dissolution above the percolation threshold. Slower dissolution was measured for tablets containing air stream dried compared to spray dried MCC.

UI MeSH Term Description Entries
D007052 Ibuprofen A non-steroidal anti-inflammatory agent with analgesic, antipyretic, and anti-inflammatory properties Advil,Benzeneacetic Acid, alpha-methyl-4-(2-methylpropyl)- trimethylsilyl ester,Brufen,Ibumetin,Ibuprofen, (+-)-Isomer,Ibuprofen, (R)-Isomer,Ibuprofen, (S)-Isomer,Ibuprofen, Aluminum Salt,Ibuprofen, Calcium Salt,Ibuprofen, Copper (2+) Salt,Ibuprofen, Magnesium Salt,Ibuprofen, Potassium Salt,Ibuprofen, Sodium Salt,Ibuprofen, Zinc Salt,Ibuprofen-Zinc,Motrin,Nuprin,Rufen,Salprofen,Trauma-Dolgit Gel,alpha-Methyl-4-(2-methylpropyl)benzeneacetic Acid,Ibuprofen Zinc,Trauma Dolgit Gel
D002482 Cellulose A polysaccharide with glucose units linked as in CELLOBIOSE. It is the chief constituent of plant fibers, cotton being the purest natural form of the substance. As a raw material, it forms the basis for many derivatives used in chromatography, ion exchange materials, explosives manufacturing, and pharmaceutical preparations. Alphacel,Avicel,Heweten,Polyanhydroglucuronic Acid,Rayophane,Sulfite Cellulose,alpha-Cellulose,Acid, Polyanhydroglucuronic,alpha Cellulose
D005079 Excipients Usually inert substances added to a prescription in order to provide suitable consistency to the dosage form. These include binders, matrix, base or diluent in pills, tablets, creams, salves, etc. Excipient,Stabilizing Agent,Stabilizing Agents,Suspending Agent,Suspending Agents,Agent, Stabilizing,Agent, Suspending,Agents, Stabilizing,Agents, Suspending
D012995 Solubility The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Solubilities
D013607 Tablets Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed) Tablet

Related Publications

Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
January 1986, Pharmaceutica acta Helvetiae,
Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
November 2010, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences,
Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
April 2024, International journal of biological macromolecules,
Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
February 1998, Pharmaceutical development and technology,
Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
February 1979, Journal of pharmaceutical sciences,
Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
July 1969, Chemical & pharmaceutical bulletin,
Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
May 1999, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V,
Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
September 2013, International journal of biological macromolecules,
Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
January 2001, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences,
Ana Luiza P Queiroz, and Barbara Wood, and Waleed Faisal, and Fatma Farag, and Hazel Garvie-Cook, and Brian Glennon, and Sonja Vucen, and Abina M Crean
October 2015, Journal of pharmaceutical sciences,
Copied contents to your clipboard!