Increased dissolution rates of carbamazepine--gluconolactone binary blends processed by hot melt extrusion.
Pharm Dev Technol
; 21(4): 445-52, 2016.
Article
em En
| MEDLINE
| ID: mdl-25757644
ABSTRACT
Carbamazepine (CBZ) shows a poor dissolution, therefore, it is important to enhance its dissolution in GI tract to improve its bioavailability. In the present study, a new hydrophilic carrier, d-gluconolactone (GNL), was extruded with CBZ at various molar ratios to produce granules by using hot melt extrusion (HME) processing. The granular extrudates were characterised by X-ray powder diffraction, differential scanning calorimetry and hot stage microscopy to determine the solid state of CBZ. It was found that bulk CBZ (Form-III) transformed to the polymorphic Form-I during the HME processing. GNL was proved to be an efficient carrier for CBZ to enhance the dissolution rate. The increase in the dissolution rate was observed for both physical mixtures and the extrudates of CBZ-GNL. However, the extrudates showed faster dissolution rates compared to physical mixtures in an ascending order of 21 < 11 < 1.51 (CBZGNL). The increase in the dissolution rates was attributed to the transformation of CBZ III to Form-I and also to the increased drug wettability/solubilisation in the presence of the carrier.
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Texto completo:
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Carbamazepina
/
Portadores de Fármacos
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Gluconatos
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Lactonas
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Anticonvulsivantes
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article