Carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use

This study aimed to develop a carbamazepine (CBZ) sustained release formulation suitable for pediatric use with a lower risk of precipitation. The CBZ was first prepared as sustained release microparticles, and then the microparticles were embedded in alginate beads, and finally, the beads were susp...

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Main Authors: Mawazi, Saeid Mezail, Abdullah Al-Mahmood, Sinan Mohammed, Chatterjee, Bappaditya, Ab. Hadi, Hazrina, Doolaanea, Abd Almonem
Format: Article
Language:English
English
Published: MDPI AG 2019
Subjects:
Online Access:http://irep.iium.edu.my/76103/
http://irep.iium.edu.my/76103/
http://irep.iium.edu.my/76103/1/pharmaceutics-11-00488-v2.pdf
http://irep.iium.edu.my/76103/7/Scopus%20-%20carbamazepine.pdf
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spelling iium-761032019-11-13T03:57:37Z http://irep.iium.edu.my/76103/ Carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use Mawazi, Saeid Mezail Abdullah Al-Mahmood, Sinan Mohammed Chatterjee, Bappaditya Ab. Hadi, Hazrina Doolaanea, Abd Almonem RS Pharmacy and materia medica RS192 Materia Medica-Pharmaceutical Technology This study aimed to develop a carbamazepine (CBZ) sustained release formulation suitable for pediatric use with a lower risk of precipitation. The CBZ was first prepared as sustained release microparticles, and then the microparticles were embedded in alginate beads, and finally, the beads were suspended in a gel vehicle. The microparticles were prepared by a solvent evaporation method utilizing ethyl cellulose as a sustained release polymer and were evaluated for particle size, encapsulation efficiency, and release profile. The beads were fabricated by the dropwise addition of sodium alginate in calcium chloride solution and characterized for size, shape, and release properties. The gel was prepared using iota carrageenan as the gelling agent and evaluated for appearance, syneresis, drug content uniformity, rheology, release profile, and stability. The microparticles exhibited a particle size of 135.01 ± 0.61 µm with a monodisperse distribution and an encapsulation efficiency of 83.89 ± 3.98%. The beads were monodispersed with an average size of 1.4 ± 0.05 mm and a sphericity factor of less than 0.05. The gel was prepared using a 1:1 ratio (gel vehicle to beads) and exhibited no syneresis, good homogeneity, and good shearthinning properties. The release profile from the beads and from the gel was not significantly affected, maintaining similarity to the tablet form. The gel properties were maintained for one month real time stability, but the accelerated stability showed reduced viscosity and pH with time. In conclusion, CBZ in a gel sustained release dosage form combines the advantages of the suspension form in terms of dosing flexibility, and the advantages of the tablet form in regards to the sustained release profile. This dosage form should be further investigated in vivo in animal models before being considered in clinical trials. MDPI AG 2019-11 Article PeerReviewed application/pdf en cc_by http://irep.iium.edu.my/76103/1/pharmaceutics-11-00488-v2.pdf application/pdf en http://irep.iium.edu.my/76103/7/Scopus%20-%20carbamazepine.pdf Mawazi, Saeid Mezail and Abdullah Al-Mahmood, Sinan Mohammed and Chatterjee, Bappaditya and Ab. Hadi, Hazrina and Doolaanea, Abd Almonem (2019) Carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use. Pharmaceutics, 11 (10). pp. 1-13. ISSN 1999-4923 10.3390/pharmaceutics11100488
repository_type Digital Repository
institution_category Local University
institution International Islamic University Malaysia
building IIUM Repository
collection Online Access
language English
English
topic RS Pharmacy and materia medica
RS192 Materia Medica-Pharmaceutical Technology
spellingShingle RS Pharmacy and materia medica
RS192 Materia Medica-Pharmaceutical Technology
Mawazi, Saeid Mezail
Abdullah Al-Mahmood, Sinan Mohammed
Chatterjee, Bappaditya
Ab. Hadi, Hazrina
Doolaanea, Abd Almonem
Carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use
description This study aimed to develop a carbamazepine (CBZ) sustained release formulation suitable for pediatric use with a lower risk of precipitation. The CBZ was first prepared as sustained release microparticles, and then the microparticles were embedded in alginate beads, and finally, the beads were suspended in a gel vehicle. The microparticles were prepared by a solvent evaporation method utilizing ethyl cellulose as a sustained release polymer and were evaluated for particle size, encapsulation efficiency, and release profile. The beads were fabricated by the dropwise addition of sodium alginate in calcium chloride solution and characterized for size, shape, and release properties. The gel was prepared using iota carrageenan as the gelling agent and evaluated for appearance, syneresis, drug content uniformity, rheology, release profile, and stability. The microparticles exhibited a particle size of 135.01 ± 0.61 µm with a monodisperse distribution and an encapsulation efficiency of 83.89 ± 3.98%. The beads were monodispersed with an average size of 1.4 ± 0.05 mm and a sphericity factor of less than 0.05. The gel was prepared using a 1:1 ratio (gel vehicle to beads) and exhibited no syneresis, good homogeneity, and good shearthinning properties. The release profile from the beads and from the gel was not significantly affected, maintaining similarity to the tablet form. The gel properties were maintained for one month real time stability, but the accelerated stability showed reduced viscosity and pH with time. In conclusion, CBZ in a gel sustained release dosage form combines the advantages of the suspension form in terms of dosing flexibility, and the advantages of the tablet form in regards to the sustained release profile. This dosage form should be further investigated in vivo in animal models before being considered in clinical trials.
format Article
author Mawazi, Saeid Mezail
Abdullah Al-Mahmood, Sinan Mohammed
Chatterjee, Bappaditya
Ab. Hadi, Hazrina
Doolaanea, Abd Almonem
author_facet Mawazi, Saeid Mezail
Abdullah Al-Mahmood, Sinan Mohammed
Chatterjee, Bappaditya
Ab. Hadi, Hazrina
Doolaanea, Abd Almonem
author_sort Mawazi, Saeid Mezail
title Carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use
title_short Carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use
title_full Carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use
title_fullStr Carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use
title_full_unstemmed Carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use
title_sort carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use
publisher MDPI AG
publishDate 2019
url http://irep.iium.edu.my/76103/
http://irep.iium.edu.my/76103/
http://irep.iium.edu.my/76103/1/pharmaceutics-11-00488-v2.pdf
http://irep.iium.edu.my/76103/7/Scopus%20-%20carbamazepine.pdf
first_indexed 2023-09-18T21:47:35Z
last_indexed 2023-09-18T21:47:35Z
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