The influence of pellet shape and surface properties on the drug release from uncoated and coated pellets

Pellets of different shape, varying from spherical to cylindrical, without and with film coating were tested for their drug release properties. For non-disintegrating uncoated pellets, drug release was found to be inversely related to the pellet porosity. A change of 5% in porosity doubled the value...

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Veröffentlicht in:International journal of pharmaceutics 2002-06, Vol.239 (1), p.171-178
Hauptverfasser: Chopra, Ranjana, Alderborn, Göran, Podczeck, Fridrun, Newton, J.Michael
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container_end_page 178
container_issue 1
container_start_page 171
container_title International journal of pharmaceutics
container_volume 239
creator Chopra, Ranjana
Alderborn, Göran
Podczeck, Fridrun
Newton, J.Michael
description Pellets of different shape, varying from spherical to cylindrical, without and with film coating were tested for their drug release properties. For non-disintegrating uncoated pellets, drug release was found to be inversely related to the pellet porosity. A change of 5% in porosity doubled the value of the mean dissolution time (MDT). As coat thickness increased, the MDT value of coated pellets increased. For those pellets, which are nearly spherical, once a thickness of about 20 μm had been achieved, there was little further reduction in retardation. Pellets produced by extrusion/spheronisation appeared to prolong drug release to a larger extent than those where the extrusion step had been omitted. There was a strong inverse relationship between the surface area by volume of the coated pellets and the value of the MDT. The values of the relative dispersion coefficient (RD), which is an indicator of the drug release mechanism, were related to the amount of fluid used to manufacture the pellets and the pellet shape, in a similar fashion for both uncoated and coated pellets. This suggested that the presence of the film coating changed the rate but not the mechanism of drug release.
doi_str_mv 10.1016/S0378-5173(02)00104-7
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For non-disintegrating uncoated pellets, drug release was found to be inversely related to the pellet porosity. A change of 5% in porosity doubled the value of the mean dissolution time (MDT). As coat thickness increased, the MDT value of coated pellets increased. For those pellets, which are nearly spherical, once a thickness of about 20 μm had been achieved, there was little further reduction in retardation. Pellets produced by extrusion/spheronisation appeared to prolong drug release to a larger extent than those where the extrusion step had been omitted. There was a strong inverse relationship between the surface area by volume of the coated pellets and the value of the MDT. The values of the relative dispersion coefficient (RD), which is an indicator of the drug release mechanism, were related to the amount of fluid used to manufacture the pellets and the pellet shape, in a similar fashion for both uncoated and coated pellets. 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source Elsevier ScienceDirect Journals Complete - AutoHoldings; MEDLINE
subjects Algorithms
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Biological and medical sciences
Drug release
Film coating
General pharmacology
Hydrogen-Ion Concentration
Kinetics
Mean dissolution time
Medical sciences
Models, Chemical
Pellet porosity
Pellet shape
Pellet surface area
Pharmaceutical Preparations - chemistry
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Piroxicam - chemistry
Relative dispersion coefficient
Solubility
Solvents
Sulfonamides - chemistry
title The influence of pellet shape and surface properties on the drug release from uncoated and coated pellets
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