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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

Infrared spectra 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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fig2: Infrared spectra of pure CBZ, Compritol®, HPMC, and Avicel® and of physical and granulated mixture at 7:2:1 Compritol®:HPMC:Avicel® weight ratio.

Mentions: IR spectra of CBZ, Compritol, HPMC, Avicel, and their physical and granulated mixtures are shown in Figure 2. Bands of CBZ are observed at 3474 cm−1 (-NH valence vibration), 1686 cm−1 (-CO-R) vibration, 1603 and 1593 cm−1 (range of –C=C= and –C=O vibration and –NH deformation), and 1395 cm−1, which are the same as described for CBZ polymorph II. The presence of –NH valence vibration at an intermediate wave number (3474 cm−1) was the major indicative sign that CBZ could be neither polymorph III (3464 cm−1) or polymorph I (3484 cm−1). The spectrum of wet granulations shows that the peak at 3474 cm−1 was partially reduced; as was expected, since CBZ content was only 40% w/w, but the main CBZ characteristic peaks were not affected.


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

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

Infrared spectra 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

fig2: Infrared spectra of pure CBZ, Compritol®, HPMC, and Avicel® and of physical and granulated mixture at 7:2:1 Compritol®:HPMC:Avicel® weight ratio.
Mentions: IR spectra of CBZ, Compritol, HPMC, Avicel, and their physical and granulated mixtures are shown in Figure 2. Bands of CBZ are observed at 3474 cm−1 (-NH valence vibration), 1686 cm−1 (-CO-R) vibration, 1603 and 1593 cm−1 (range of –C=C= and –C=O vibration and –NH deformation), and 1395 cm−1, which are the same as described for CBZ polymorph II. The presence of –NH valence vibration at an intermediate wave number (3474 cm−1) was the major indicative sign that CBZ could be neither polymorph III (3464 cm−1) or polymorph I (3484 cm−1). The spectrum of wet granulations shows that the peak at 3474 cm−1 was partially reduced; as was expected, since CBZ content was only 40% w/w, but the main CBZ characteristic peaks were not affected.

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