Studies and evaluation of compressed microspheres

This work was aimed at the use of dissolution testing and similarity factor to assess the level of damage taken by active drug microspheres during compression in tablet dosage form. To achieve that, combinations of suitable excipients were used to protect drug microspheres during compression. The ex...

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Main Authors: Idris M. El-Mahdi, Atef M. Madi
Format: Article
Language:English
Published: Thieme Medical and Scientific Publishers Pvt. Ltd. 2016-01-01
Series:Libyan International Medical University Journal
Subjects:
Online Access:http://www.thieme-connect.de/DOI/DOI?10.21502/limuj.002.01.2016
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author Idris M. El-Mahdi
Atef M. Madi
author_facet Idris M. El-Mahdi
Atef M. Madi
author_sort Idris M. El-Mahdi
collection DOAJ
description This work was aimed at the use of dissolution testing and similarity factor to assess the level of damage taken by active drug microspheres during compression in tablet dosage form. To achieve that, combinations of suitable excipients were used to protect drug microspheres during compression. The excipients were used in the form of powders, granules or placebo pellets prepared by extrusion-spheronization technology. The excipients were evaluated alone, in combinations and post-compression into compacts. Preliminary experiments included assessing density, hardness, friability and disintegration of all the selected excipients. Based on such experiments it was found that the flowability of combination of powders was more acceptable than individual excipients. Two combinations of microcrystalline -starch and microcrystalline cellulose -calcium carbonate granules were selected to be compressed with pellets of the active pharmaceutical ingredient ketoprofen. In all the combinations used there was a significant amount of damage to drug pellets. The kinetics of drug release appears to follow the zero-order rate, which remained unchanged even when a significant degree of damage to pellets occurs. It was found that a high level of excipients is required in order to prepare microspheres as a rapid disintegrating tablet.
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spelling doaj-art-65ba263a132c4db597ebfb8ac2e375dc2025-08-20T03:18:09ZengThieme Medical and Scientific Publishers Pvt. Ltd.Libyan International Medical University Journal2519-139X2016-01-01010161610.21502/limuj.002.01.20162Studies and evaluation of compressed microspheresIdris M. El-Mahdi0Atef M. Madi1Department of Pharmaceutics, Faculty of Pharmacy, University of Benghazi, Benghazi, LibyaDepartment of Pharmaceutics, School of Pharmacy, Queens University Belfast (QUB), Belfast, Northern Ireland, UKThis work was aimed at the use of dissolution testing and similarity factor to assess the level of damage taken by active drug microspheres during compression in tablet dosage form. To achieve that, combinations of suitable excipients were used to protect drug microspheres during compression. The excipients were used in the form of powders, granules or placebo pellets prepared by extrusion-spheronization technology. The excipients were evaluated alone, in combinations and post-compression into compacts. Preliminary experiments included assessing density, hardness, friability and disintegration of all the selected excipients. Based on such experiments it was found that the flowability of combination of powders was more acceptable than individual excipients. Two combinations of microcrystalline -starch and microcrystalline cellulose -calcium carbonate granules were selected to be compressed with pellets of the active pharmaceutical ingredient ketoprofen. In all the combinations used there was a significant amount of damage to drug pellets. The kinetics of drug release appears to follow the zero-order rate, which remained unchanged even when a significant degree of damage to pellets occurs. It was found that a high level of excipients is required in order to prepare microspheres as a rapid disintegrating tablet.http://www.thieme-connect.de/DOI/DOI?10.21502/limuj.002.01.2016degree of damage to microspheres under compressiondirect compressionketoprofendissolution testing and similarity function
spellingShingle Idris M. El-Mahdi
Atef M. Madi
Studies and evaluation of compressed microspheres
Libyan International Medical University Journal
degree of damage to microspheres under compression
direct compression
ketoprofen
dissolution testing and similarity function
title Studies and evaluation of compressed microspheres
title_full Studies and evaluation of compressed microspheres
title_fullStr Studies and evaluation of compressed microspheres
title_full_unstemmed Studies and evaluation of compressed microspheres
title_short Studies and evaluation of compressed microspheres
title_sort studies and evaluation of compressed microspheres
topic degree of damage to microspheres under compression
direct compression
ketoprofen
dissolution testing and similarity function
url http://www.thieme-connect.de/DOI/DOI?10.21502/limuj.002.01.2016
work_keys_str_mv AT idrismelmahdi studiesandevaluationofcompressedmicrospheres
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