Combined UV/Vis and micro-tomography investigation of acetaminophen dissolution from granules

The x-ray micro-tomography (micro-CT) technique has been used to visualize the microstructure of granules produced by high shear wet granulation and the dynamic evolution of porosity during granule dissolution. Using acetaminophen (paracetamol) as the active pharmaceutical ingredient (API) and micro...

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Bibliographic Details
Published in:International journal of pharmaceutics 2013-10
Main Authors: Kašpar, Ondřej, Tokárová, Viola, Oka, Sarang, Sowrirajan, Koushik, Ramachandran, Rohit, Stěpánek, František
Format: Article
Language:English
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Summary:The x-ray micro-tomography (micro-CT) technique has been used to visualize the microstructure of granules produced by high shear wet granulation and the dynamic evolution of porosity during granule dissolution. Using acetaminophen (paracetamol) as the active pharmaceutical ingredient (API) and microcrystalline cellulose (Avicel PH-200) as an excipient, the porosity of the granules was systematically influenced by the granulation process parameters (binder/solids ratio, impeller speed and wet massing time). An increase of granule porosity from 7% to 10% and 18% lead to a decrease of the dissolution time t from 435min to 98min and 37min, respectively. The combination of time-resolved micro-CT imaging with UV/VIS detection of the quantity dissolved made it possible to evaluate the effective diffusion coefficient of the API through the granule structure, and thus establish a quantitative structure-property relationship for dissolution. A power-law dependence of the effective diffusivity on porosity (Archie's law) was found to hold.
ISSN:1873-3476