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Controlled-release carbamazepine matrix granules and tablets comprising lipophilic and hydrophilic components.

Barakat NS, Elbagory IM, Almurshedi AS - Drug Deliv (2009)

Bottom Line: It was found that increase in the concentration of HPMC results in reduction in the release rate from granules and achievement of zero-order is difficult from the granules.Increasing in drug loading resulted in acceleration of the drug release and in anomalous controlled-release mechanism due to delayed hydration of the tablets.These results suggest that wet granulation followed by compression could be a suitable method to formulate sustained release CBZ tablets.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. nsybarakat@yahoo.com

ABSTRACT
The objective of this study was to investigate the effect of lipophilic (Compritol 888 ATO) and hydrophilic components (combination of HPMC and Avicel) on the release of carbamazepine from granules and corresponding tablet. Wet granulation followed by compression was employed for preparation of granules and tablets. The matrix swelling behavior was investigated. The dissolution profiles of each formulation were compared to those of Tegretol CR tablets and the mean dissolution time (MDT), dissolution efficiency (DE%), and similarity factor (f(2) factor) were calculated. It was found that increase in the concentration of HPMC results in reduction in the release rate from granules and achievement of zero-order is difficult from the granules. The amount of HPMC plays a dominant role for the drug release. The release mechanism of CBZ from matrix tablet formulations follows non-Fickian diffusion shifting to Case II by the increase of HPMC content, indicating significant contribution of erosion. Increasing in drug loading resulted in acceleration of the drug release and in anomalous controlled-release mechanism due to delayed hydration of the tablets. These results suggest that wet granulation followed by compression could be a suitable method to formulate sustained release CBZ tablets.

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Related in: MedlinePlus

DSC thermograms of pure CBZ, Compritol®, HPMC, and Avicel® and of physical and granulated mixture at 7:2:1 Compritol®:HPMC:Avicel® weight ratio.
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fig1: DSC thermograms of pure CBZ, Compritol®, HPMC, and Avicel® and of physical and granulated mixture at 7:2:1 Compritol®:HPMC:Avicel® weight ratio.

Mentions: The differential scanning calorimeter curve of CBZ (Figure 1) displayed a single sharp endothermic peak at 198°C corresponding to its m.p. A single sharp peak at 72°C corresponded to the melting point of Compritol® and large shallow broad endothermic effects, over the temperature range 60–160°C, were observed for the polymers HPMC and Avicel, probably due to evaporation of adsorbed water. The DSC curve of the physical mixture of CBZ, Compritol®, HPMC, and Avicel® shows identical endothermic peaks to pure components but less intense due to the smaller concentration, indicating that the matrix forming components selected neither interfered with CBZ nor made any shift of its melting peak.


Controlled-release carbamazepine matrix granules and tablets comprising lipophilic and hydrophilic components.

Barakat NS, Elbagory IM, Almurshedi AS - Drug Deliv (2009)

DSC thermograms of pure CBZ, Compritol®, HPMC, and Avicel® and of physical and granulated mixture at 7:2:1 Compritol®:HPMC:Avicel® weight ratio.
© Copyright Policy - open-access
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC2637677&req=5

fig1: DSC thermograms of pure CBZ, Compritol®, HPMC, and Avicel® and of physical and granulated mixture at 7:2:1 Compritol®:HPMC:Avicel® weight ratio.
Mentions: The differential scanning calorimeter curve of CBZ (Figure 1) displayed a single sharp endothermic peak at 198°C corresponding to its m.p. A single sharp peak at 72°C corresponded to the melting point of Compritol® and large shallow broad endothermic effects, over the temperature range 60–160°C, were observed for the polymers HPMC and Avicel, probably due to evaporation of adsorbed water. The DSC curve of the physical mixture of CBZ, Compritol®, HPMC, and Avicel® shows identical endothermic peaks to pure components but less intense due to the smaller concentration, indicating that the matrix forming components selected neither interfered with CBZ nor made any shift of its melting peak.

Bottom Line: It was found that increase in the concentration of HPMC results in reduction in the release rate from granules and achievement of zero-order is difficult from the granules.Increasing in drug loading resulted in acceleration of the drug release and in anomalous controlled-release mechanism due to delayed hydration of the tablets.These results suggest that wet granulation followed by compression could be a suitable method to formulate sustained release CBZ tablets.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. nsybarakat@yahoo.com

ABSTRACT
The objective of this study was to investigate the effect of lipophilic (Compritol 888 ATO) and hydrophilic components (combination of HPMC and Avicel) on the release of carbamazepine from granules and corresponding tablet. Wet granulation followed by compression was employed for preparation of granules and tablets. The matrix swelling behavior was investigated. The dissolution profiles of each formulation were compared to those of Tegretol CR tablets and the mean dissolution time (MDT), dissolution efficiency (DE%), and similarity factor (f(2) factor) were calculated. It was found that increase in the concentration of HPMC results in reduction in the release rate from granules and achievement of zero-order is difficult from the granules. The amount of HPMC plays a dominant role for the drug release. The release mechanism of CBZ from matrix tablet formulations follows non-Fickian diffusion shifting to Case II by the increase of HPMC content, indicating significant contribution of erosion. Increasing in drug loading resulted in acceleration of the drug release and in anomalous controlled-release mechanism due to delayed hydration of the tablets. These results suggest that wet granulation followed by compression could be a suitable method to formulate sustained release CBZ tablets.

Show MeSH
Related in: MedlinePlus