Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modelling
Dexketoprofen trometamol (DT) is an active S (+) enantiomer of ketoprofen, and a non-steroidal anti-inflammatory agent. DT has a short biological half-life and the dosing interval is quite short when there is a need to maintain the desirable effect for longer time periods. Consequently, a controlled release DT tablet was designed for oral administration aiming to minimize the number of doses and the possible side effects. Calculations of the parameters for controlled release DT tablets were shown clearly. Controlled release matrix-type tablet formulations were prepared using hydroxypropyl methylcellulose (HPMC) (low and high viscosity), Eudragit RS and Carbopol, and the effects of different polymers on DT release from the tablet formulations were investigated. The dissolution rate profiles were compared and analyzed kinetically. An Artificial Neural Network (ANN) model was developed to predict drug release and a successful model was obtained. Subsequently, an optimum formulation was selected and evaluated in terms of its analgesic and anti-inflammatory activity. Although the developed controlled release tablets did not have an initial dose, they were found to be as effective as commercially available tablets on the market. Dissolution and in vivo studies have shown that the prepared tablets were able to release DT for longer time periods, making the tablets more effective, convenient and more tolerable.
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Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
2020
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oai:scielo:S1984-825020200001006532021-06-16Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modellingSaraçoğlu,Özlem KışlalUludağ,Mecit OrhanÖzdemir,Elif DeryaDeğim,İsmail Tuncer Dexketoprofen Controlled release Oral tablet HPMC Eudragit Carbopol Dexketoprofen trometamol (DT) is an active S (+) enantiomer of ketoprofen, and a non-steroidal anti-inflammatory agent. DT has a short biological half-life and the dosing interval is quite short when there is a need to maintain the desirable effect for longer time periods. Consequently, a controlled release DT tablet was designed for oral administration aiming to minimize the number of doses and the possible side effects. Calculations of the parameters for controlled release DT tablets were shown clearly. Controlled release matrix-type tablet formulations were prepared using hydroxypropyl methylcellulose (HPMC) (low and high viscosity), Eudragit RS and Carbopol, and the effects of different polymers on DT release from the tablet formulations were investigated. The dissolution rate profiles were compared and analyzed kinetically. An Artificial Neural Network (ANN) model was developed to predict drug release and a successful model was obtained. Subsequently, an optimum formulation was selected and evaluated in terms of its analgesic and anti-inflammatory activity. Although the developed controlled release tablets did not have an initial dose, they were found to be as effective as commercially available tablets on the market. Dissolution and in vivo studies have shown that the prepared tablets were able to release DT for longer time periods, making the tablets more effective, convenient and more tolerable.info:eu-repo/semantics/openAccessUniversidade de São Paulo, Faculdade de Ciências FarmacêuticasBrazilian Journal of Pharmaceutical Sciences v.56 20202020-01-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100653en10.1590/s2175-97902019000418540 |
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Saraçoğlu,Özlem Kışlal Uludağ,Mecit Orhan Özdemir,Elif Derya Değim,İsmail Tuncer |
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Saraçoğlu,Özlem Kışlal Uludağ,Mecit Orhan Özdemir,Elif Derya Değim,İsmail Tuncer Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modelling |
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Saraçoğlu,Özlem Kışlal Uludağ,Mecit Orhan Özdemir,Elif Derya Değim,İsmail Tuncer |
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Saraçoğlu,Özlem Kışlal |
title |
Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modelling |
title_short |
Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modelling |
title_full |
Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modelling |
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Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modelling |
title_full_unstemmed |
Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modelling |
title_sort |
development of controlled release dexketoprofen tablets and prediction of drug release using artificial neural network (ann) modelling |
description |
Dexketoprofen trometamol (DT) is an active S (+) enantiomer of ketoprofen, and a non-steroidal anti-inflammatory agent. DT has a short biological half-life and the dosing interval is quite short when there is a need to maintain the desirable effect for longer time periods. Consequently, a controlled release DT tablet was designed for oral administration aiming to minimize the number of doses and the possible side effects. Calculations of the parameters for controlled release DT tablets were shown clearly. Controlled release matrix-type tablet formulations were prepared using hydroxypropyl methylcellulose (HPMC) (low and high viscosity), Eudragit RS and Carbopol, and the effects of different polymers on DT release from the tablet formulations were investigated. The dissolution rate profiles were compared and analyzed kinetically. An Artificial Neural Network (ANN) model was developed to predict drug release and a successful model was obtained. Subsequently, an optimum formulation was selected and evaluated in terms of its analgesic and anti-inflammatory activity. Although the developed controlled release tablets did not have an initial dose, they were found to be as effective as commercially available tablets on the market. Dissolution and in vivo studies have shown that the prepared tablets were able to release DT for longer time periods, making the tablets more effective, convenient and more tolerable. |
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Universidade de São Paulo, Faculdade de Ciências Farmacêuticas |
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2020 |
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http://old.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100653 |
work_keys_str_mv |
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