Cargando…
Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac
The rapid availability of the drug at the site of action followed by maintaining its effect for a long period of time is of great clinical importance. Thus, the purpose of the present study was to prepare and evaluate multi-layered matrix tablets of diclofenac using Eudragit RL/RS blend to achieve b...
Autores principales: | , , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2017
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5506666/ https://www.ncbi.nlm.nih.gov/pubmed/28725140 http://dx.doi.org/10.1016/j.jsps.2016.10.004 |
_version_ | 1783249609192112128 |
---|---|
author | Elzayat, Ehab Mostafa Abdel-Rahman, Ali Abdelzaher Ahmed, Sayed Mohamed Alanazi, Fars Kaed Habib, Walid Abdulazim Abou-Auda, Hisham Suliman Sakr, Adel |
author_facet | Elzayat, Ehab Mostafa Abdel-Rahman, Ali Abdelzaher Ahmed, Sayed Mohamed Alanazi, Fars Kaed Habib, Walid Abdulazim Abou-Auda, Hisham Suliman Sakr, Adel |
author_sort | Elzayat, Ehab Mostafa |
collection | PubMed |
description | The rapid availability of the drug at the site of action followed by maintaining its effect for a long period of time is of great clinical importance. Thus, the purpose of the present study was to prepare and evaluate multi-layered matrix tablets of diclofenac using Eudragit RL/RS blend to achieve both immediate and sustained therapeutic effects. Diclofenac potassium (25 mg) was incorporated in an outer immediate release layer to provide immediate pain relief whereas diclofenac sodium (75 mg) was incorporated in the inner core to provide extended drug release. Wet granulation was employed to prepare the inner core of the tablets that were further layered with an immediate release drug layer in the perforated pan coater. The in-vitro and in-vivo performance of the developed formulation was compared with the marketed products Voltaren® SR 75 mg and Cataflam® 25 mg. The in-vitro drug release of the prepared formulation showed similarity (f(2) = 66.19) to the marketed product. The pharmacokinetic study showed no significant difference (p > 0.05) in AUC(0-24) and C(max) between the test and reference formulations. The AUC(0-24) values were 105.36 ± 83.3 and 92.87 ± 55.53 μg h/ml whereas the C(max) values were 11.25 ± 6.87 and 12.97 ± 8.45 μg/ml, for the test and reference, respectively. The multi-layered tablets were proved to be bioequivalent with the commercially available tablets and were in agreement with the observed in-vitro drug release results. Stable physical characteristics and drug release profiles were observed in both long term and accelerated conditions stability studies. |
format | Online Article Text |
id | pubmed-5506666 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-55066662017-07-19 Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac Elzayat, Ehab Mostafa Abdel-Rahman, Ali Abdelzaher Ahmed, Sayed Mohamed Alanazi, Fars Kaed Habib, Walid Abdulazim Abou-Auda, Hisham Suliman Sakr, Adel Saudi Pharm J Original Article The rapid availability of the drug at the site of action followed by maintaining its effect for a long period of time is of great clinical importance. Thus, the purpose of the present study was to prepare and evaluate multi-layered matrix tablets of diclofenac using Eudragit RL/RS blend to achieve both immediate and sustained therapeutic effects. Diclofenac potassium (25 mg) was incorporated in an outer immediate release layer to provide immediate pain relief whereas diclofenac sodium (75 mg) was incorporated in the inner core to provide extended drug release. Wet granulation was employed to prepare the inner core of the tablets that were further layered with an immediate release drug layer in the perforated pan coater. The in-vitro and in-vivo performance of the developed formulation was compared with the marketed products Voltaren® SR 75 mg and Cataflam® 25 mg. The in-vitro drug release of the prepared formulation showed similarity (f(2) = 66.19) to the marketed product. The pharmacokinetic study showed no significant difference (p > 0.05) in AUC(0-24) and C(max) between the test and reference formulations. The AUC(0-24) values were 105.36 ± 83.3 and 92.87 ± 55.53 μg h/ml whereas the C(max) values were 11.25 ± 6.87 and 12.97 ± 8.45 μg/ml, for the test and reference, respectively. The multi-layered tablets were proved to be bioequivalent with the commercially available tablets and were in agreement with the observed in-vitro drug release results. Stable physical characteristics and drug release profiles were observed in both long term and accelerated conditions stability studies. Elsevier 2017-07 2016-10-17 /pmc/articles/PMC5506666/ /pubmed/28725140 http://dx.doi.org/10.1016/j.jsps.2016.10.004 Text en © 2016 The Authors http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Original Article Elzayat, Ehab Mostafa Abdel-Rahman, Ali Abdelzaher Ahmed, Sayed Mohamed Alanazi, Fars Kaed Habib, Walid Abdulazim Abou-Auda, Hisham Suliman Sakr, Adel Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac |
title | Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac |
title_full | Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac |
title_fullStr | Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac |
title_full_unstemmed | Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac |
title_short | Formulation and pharmacokinetics of multi-layered matrix tablets: Biphasic delivery of diclofenac |
title_sort | formulation and pharmacokinetics of multi-layered matrix tablets: biphasic delivery of diclofenac |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5506666/ https://www.ncbi.nlm.nih.gov/pubmed/28725140 http://dx.doi.org/10.1016/j.jsps.2016.10.004 |
work_keys_str_mv | AT elzayatehabmostafa formulationandpharmacokineticsofmultilayeredmatrixtabletsbiphasicdeliveryofdiclofenac AT abdelrahmanaliabdelzaher formulationandpharmacokineticsofmultilayeredmatrixtabletsbiphasicdeliveryofdiclofenac AT ahmedsayedmohamed formulationandpharmacokineticsofmultilayeredmatrixtabletsbiphasicdeliveryofdiclofenac AT alanazifarskaed formulationandpharmacokineticsofmultilayeredmatrixtabletsbiphasicdeliveryofdiclofenac AT habibwalidabdulazim formulationandpharmacokineticsofmultilayeredmatrixtabletsbiphasicdeliveryofdiclofenac AT abouaudahishamsuliman formulationandpharmacokineticsofmultilayeredmatrixtabletsbiphasicdeliveryofdiclofenac AT sakradel formulationandpharmacokineticsofmultilayeredmatrixtabletsbiphasicdeliveryofdiclofenac |