Metoprolol tartrate-ethylcellulose tabletted microparticles: formulation and in vitro evaluation

This study introduced a novel phase separation technique for the microencapsulation of metoprolol tartrate as a model. Non-solvent addition coacervation technique was employed for the loading of drug into ethylcellulose, a hydrophobic plastic polymer. Dichloromethane (DCM) and paraffin oil were emp...

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Autores principales: Rasool, Fatima, Ahmad, Mahmood, Murtaza, Ghulam, Khan, Haji M. S., Khan, Shujaat A.
Formato: Articulo
Lenguaje:Inglés
Publicado: 2010
Materias:
Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/8014
http://www.latamjpharm.org/resumenes/29/6/LAJOP_29_6_1_19.pdf
Aporte de:
id I19-R120-10915-8014
record_format dspace
institution Universidad Nacional de La Plata
institution_str I-19
repository_str R-120
collection SEDICI (UNLP)
language Inglés
topic Farmacia
dissolution; ethylcellulose; kinetic models; metoprolol tartrate; non-solvent addition coacervation
Farmacología
Disolución
Polímeros
Química orgánica
spellingShingle Farmacia
dissolution; ethylcellulose; kinetic models; metoprolol tartrate; non-solvent addition coacervation
Farmacología
Disolución
Polímeros
Química orgánica
Rasool, Fatima
Ahmad, Mahmood
Murtaza, Ghulam
Khan, Haji M. S.
Khan, Shujaat A.
Metoprolol tartrate-ethylcellulose tabletted microparticles: formulation and in vitro evaluation
topic_facet Farmacia
dissolution; ethylcellulose; kinetic models; metoprolol tartrate; non-solvent addition coacervation
Farmacología
Disolución
Polímeros
Química orgánica
description This study introduced a novel phase separation technique for the microencapsulation of metoprolol tartrate as a model. Non-solvent addition coacervation technique was employed for the loading of drug into ethylcellulose, a hydrophobic plastic polymer. Dichloromethane (DCM) and paraffin oil were employed as solvent and non-solvent, respectively. Microparticle batches abbreviated as M1, M2 and M3 were formulated by embedding 1 g of drug into 1 g, 2 g and 3 g of polymer, respectively followed by direct compression into tabletted microparticulate batches named a T1, T2 and T3, respectively. The drug and polymer remained intact in encapsulated form as confirmed by FTIR, XRD and DSC. However, a slight change in drug nature from crystalline to amorphous behavior and an endothermic peak for metoprolol tartrate at 130 ºC was observed in drug and microparticle thermograms. Slightly aggregated spherical free flowing microparticles in a size range of 64 μm-103 μm were obtained. The entrapment efficiency ranged from 77% to 89%. The straight line obtained from a plot between square root of time (Hrs) versus drug release (%) and regression co-efficient (R<sup>2</sup>) confirmed that best fit model to all dissolution profiles was Higuchi's model. The modes of drug release from microparticles and tabletted microparticles were Quasi-Fickian diffusion and anomalous diffusion, respectively. T3 was selected as an optimum formulation as its dissolution profile resembled (f<sub>2</sub> = 76.25) Mepressor® (Novartis Pharma-Pakistan). The accelerated stability study, regarding dissolution behavior and drug contents, at 40ºC/75% RH proved T3 stable in 40 ºC/75% RH for six months. Non-solvent addition coacervation technique involving comparatively safe solvents such as dichloromethane and paraffin oil as solvent and non-solvent, respectively is a good techniques for the encapsulation of Biopharmaceutics Classification System class I drugs such as metoprolol tartrate.
format Articulo
Articulo
author Rasool, Fatima
Ahmad, Mahmood
Murtaza, Ghulam
Khan, Haji M. S.
Khan, Shujaat A.
author_facet Rasool, Fatima
Ahmad, Mahmood
Murtaza, Ghulam
Khan, Haji M. S.
Khan, Shujaat A.
author_sort Rasool, Fatima
title Metoprolol tartrate-ethylcellulose tabletted microparticles: formulation and in vitro evaluation
title_short Metoprolol tartrate-ethylcellulose tabletted microparticles: formulation and in vitro evaluation
title_full Metoprolol tartrate-ethylcellulose tabletted microparticles: formulation and in vitro evaluation
title_fullStr Metoprolol tartrate-ethylcellulose tabletted microparticles: formulation and in vitro evaluation
title_full_unstemmed Metoprolol tartrate-ethylcellulose tabletted microparticles: formulation and in vitro evaluation
title_sort metoprolol tartrate-ethylcellulose tabletted microparticles: formulation and in vitro evaluation
publishDate 2010
url http://sedici.unlp.edu.ar/handle/10915/8014
http://www.latamjpharm.org/resumenes/29/6/LAJOP_29_6_1_19.pdf
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AT ahmadmahmood metoprololtartrateethylcellulosetablettedmicroparticlesformulationandinvitroevaluation
AT murtazaghulam metoprololtartrateethylcellulosetablettedmicroparticlesformulationandinvitroevaluation
AT khanhajims metoprololtartrateethylcellulosetablettedmicroparticlesformulationandinvitroevaluation
AT khanshujaata metoprololtartrateethylcellulosetablettedmicroparticlesformulationandinvitroevaluation
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