Effects of process variables on micromeritic properties and drug release of non-degradable microparticles

Introduction: The purpose of this investigation was to evaluate microencapsulated controlled release preparation of theophylline using Eudragit RS 100 as the retardant material with high entrapment efficiency. Methods: Microspheres were prepared by the emulsion-solvent evaporation method. A mixed so...

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Main Authors: Mitra Jelvehgari, Jaleh Barar, Ali Nokhodchi, Sanam Shadrou, Hadi Valizadeh
Format: Article
Language:English
Published: Tabriz University of Medical Sciences 2011-06-01
Series:Advanced Pharmaceutical Bulletin
Subjects:
Online Access:http://apb.tbzmed.ac.ir/Portals/0/Archive/Vol1No1/3-Jelvehgari.pdf
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author Mitra Jelvehgari
Jaleh Barar
Ali Nokhodchi
Sanam Shadrou
Hadi Valizadeh
author_facet Mitra Jelvehgari
Jaleh Barar
Ali Nokhodchi
Sanam Shadrou
Hadi Valizadeh
author_sort Mitra Jelvehgari
collection DOAJ
description Introduction: The purpose of this investigation was to evaluate microencapsulated controlled release preparation of theophylline using Eudragit RS 100 as the retardant material with high entrapment efficiency. Methods: Microspheres were prepared by the emulsion-solvent evaporation method. A mixed solvent system consisting of methanol and acetone and light liquid paraffin as oily phase were chosen. Sucrose stearate was used as the surfactant to stabilize the emulsification process. The prepared microspheres were characterized by drug loading, Fourier-transform infrared spectroscopy (FTIR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in vitro release studies were performed at pH 1.2 and 7.4 aqueous medium. Results: Increasing the concentration of emulsifier, sucrose fatty acid ester F-70, decreased the particle size which contributed to increased drug release rate. The drug loading microparticle Eudragit RS100 (1:6) showed 60-75% of entrapment and mean particle size 205.93-352.76 µm. The results showed that, an increase in the ratio of polymer: drug (F5, 6: 1) resulted in a reduction in the release rate of the drug which may be attributed to the hydrophobic nature of the polymer. Conclusion: The release of theophylline is influenced by the drug to polymer ratio and particle size. Drug release is controlled by diffusion and the best-fit release kinetic is Higuchi model.
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spelling doaj.art-62b71f4e513c4bc2b81769a2155391292022-12-22T03:20:19ZengTabriz University of Medical SciencesAdvanced Pharmaceutical Bulletin2228-58812251-73082011-06-01111826Effects of process variables on micromeritic properties and drug release of non-degradable microparticlesMitra JelvehgariJaleh BararAli NokhodchiSanam ShadrouHadi ValizadehIntroduction: The purpose of this investigation was to evaluate microencapsulated controlled release preparation of theophylline using Eudragit RS 100 as the retardant material with high entrapment efficiency. Methods: Microspheres were prepared by the emulsion-solvent evaporation method. A mixed solvent system consisting of methanol and acetone and light liquid paraffin as oily phase were chosen. Sucrose stearate was used as the surfactant to stabilize the emulsification process. The prepared microspheres were characterized by drug loading, Fourier-transform infrared spectroscopy (FTIR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in vitro release studies were performed at pH 1.2 and 7.4 aqueous medium. Results: Increasing the concentration of emulsifier, sucrose fatty acid ester F-70, decreased the particle size which contributed to increased drug release rate. The drug loading microparticle Eudragit RS100 (1:6) showed 60-75% of entrapment and mean particle size 205.93-352.76 µm. The results showed that, an increase in the ratio of polymer: drug (F5, 6: 1) resulted in a reduction in the release rate of the drug which may be attributed to the hydrophobic nature of the polymer. Conclusion: The release of theophylline is influenced by the drug to polymer ratio and particle size. Drug release is controlled by diffusion and the best-fit release kinetic is Higuchi model.http://apb.tbzmed.ac.ir/Portals/0/Archive/Vol1No1/3-Jelvehgari.pdfMicrospheresEudragit RS 100Theophylline anhydrousEster sucrose
spellingShingle Mitra Jelvehgari
Jaleh Barar
Ali Nokhodchi
Sanam Shadrou
Hadi Valizadeh
Effects of process variables on micromeritic properties and drug release of non-degradable microparticles
Advanced Pharmaceutical Bulletin
Microspheres
Eudragit RS 100
Theophylline anhydrous
Ester sucrose
title Effects of process variables on micromeritic properties and drug release of non-degradable microparticles
title_full Effects of process variables on micromeritic properties and drug release of non-degradable microparticles
title_fullStr Effects of process variables on micromeritic properties and drug release of non-degradable microparticles
title_full_unstemmed Effects of process variables on micromeritic properties and drug release of non-degradable microparticles
title_short Effects of process variables on micromeritic properties and drug release of non-degradable microparticles
title_sort effects of process variables on micromeritic properties and drug release of non degradable microparticles
topic Microspheres
Eudragit RS 100
Theophylline anhydrous
Ester sucrose
url http://apb.tbzmed.ac.ir/Portals/0/Archive/Vol1No1/3-Jelvehgari.pdf
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AT sanamshadrou effectsofprocessvariablesonmicromeriticpropertiesanddrugreleaseofnondegradablemicroparticles
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