Formulation, Release Characteristics and Bioavailability Study of Oral Monolithic Matrix Tablets Containing Carbamazepine

Barakat, Nahla S.; El-Bagory, Ibrahim M.; Almurshedi, Alanood S.

doi:10.1208/s12249-008-9108-y

Cited by 28 publications

(11 citation statements)

References 20 publications

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“…CBZ is currently administered by peroral route, with an irregular and slow absorption when immediate-release tablets are administered (13). The bioavailability and absorption of this drug are limited due to their low solubility in water (14), and thus alternative routes for the CBZ delivery have recently been proposed.…”

Section: Permeability Of Carbamazepine Through Fresh and Frozen Buccamentioning

confidence: 99%

Effect of Freezing and Type of Mucosa on Ex Vivo Drug Permeability Parameters

Caon

Simões

2011

AAPS PharmSciTech

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Abstract. The porcine esophageal mucosa has been proposed as a substitute for the buccal mucosa barrier on ex vivo permeability studies mainly due to its large surface area as well as its easier preparation. Therefore, this study compared the ex vivo permeability parameters of two drugs (carmabazepine (CBZ) and triamcinolone acetonide (TAC)) with different permeabilities and physicochemical properties through buccal and esophageal mucosae using a Franz diffusion cell system and HPLC as detection method. The freezing effects on drug permeability parameters were also evaluated by comparing them when fresh and frozen tissues were used. The barrier properties were not affected by the freezing process since the obtained parameters for both drugs were similar in frozen and fresh tissues (buccal and esophageal mucosae). However, an increase of CBZ retention was shown in frozen tissues. Fresh and frozen esophageal mucosae provided higher permeation of TAC than on buccal mucosae while the obtained permeability parameters for CBZ were similar on both mucosae. According to our results, porcine esophageal mucosa could be used as a substitute for buccal mucosa on ex vivo studies involving CBZ but not TAC. Frozen tissues could be used as substitute for fresh tissues in both cases. However, any substitution should be done with care and only if previous tests were performed, because the results could differ depending on the tested drug.

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Section: Permeability Of Carbamazepine Through Fresh and Frozen Buccamentioning

confidence: 99%

Effect of Freezing and Type of Mucosa on Ex Vivo Drug Permeability Parameters

Caon

Simões

2011

AAPS PharmSciTech

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“…Since the hydration ability and the mechanical strength of the gel developed in combination with the mechanical stress applied in the stomach and intestine can influence the integrity and subsequently the in vivo drug release mechanism, the formulation containing 75% w/w CBZ in a matrix composed of Compritol ® /HPMC/Avicel at 1:8:1 weight ratio was selected for further in vivo study in dogs (36 ).…”

Section: Combination Of Compritolmentioning

confidence: 99%

Controlled-Release Carbamazepine Granules and Tablets Comprising Lipophilic and Hydrophilic Matrix Components

2008

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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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“…Although olanzapine may not be an ideal drug for formulation in controlled-release tablet form, its side effect-dependent poor tolerability makes it a good candidate for formulating in such a form. Extended-release (ER) tablet of carbamazepine, instead of its long mean half-life of 37.5 h (19), has got official status in United States Pharmacopeia, USPXXXI, and a group of investigators prepared ER tablet of carbamazepine to improve its tolerability and adherence profile (20).…”

Section: Introductionmentioning

confidence: 99%

Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In Vitro Release and Bioavailability

2010

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Abstract. Controlled-release (CR) tablet formulation of olanzapine was developed using a binary mixture of Methocel® K100 LV-CR and Ethocel® standard 7FP premium by the dry granulation slugging method. Drug release kinetics of CR tablet formulations F1, F2, and F3, each one suitably compressed for 9-, 12-, and 15-kg hardness, were determined in a dissolution media of 0.1 N HCl (pH 1.5) and phosphate buffer (pH 6.8) using type II dissolution apparatus with paddles run at 50 rpm. Ethocel® was found to be distinctly controlling drug release, whereas the hardness of tablets and pH of the dissolution media did not significantly affect release kinetics. The CR test tablets containing 30% Methocel® and 60% Ethocel® (F3) with 12-kg hardness exhibited pH-independent zero-order release kinetics for 24 h. In vivo performance of the CR test tablet and conventional reference tablet were determined in rabbit serum using high-performance liquid chromatography coupled with electrochemical detector. Bioavailability parameters including C max , T max , and AUC 0-48 h of both tablets were compared. The CR test tablets produced optimized C max and extended T max (P<0.05). A good correlation of drug absorption in vivo and drug release in vitro (R 2 =0.9082) was observed. Relative bioavailability of the test tablet was calculated as 94%. The manufacturing process employed was reproducible and the CR test tablets were stable for 6 months at 40±2°C/75±5% relative humidity. It was concluded that the CR test tablet formulation successfully developed may improve tolerability and patient adherence by reducing adverse effects.

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Formulation, Release Characteristics and Bioavailability Study of Oral Monolithic Matrix Tablets Containing Carbamazepine

Cited by 28 publications

References 20 publications

Effect of Freezing and Type of Mucosa on Ex Vivo Drug Permeability Parameters

Effect of Freezing and Type of Mucosa on Ex Vivo Drug Permeability Parameters

Controlled-Release Carbamazepine Granules and Tablets Comprising Lipophilic and Hydrophilic Matrix Components

Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In Vitro Release and Bioavailability

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