Sustained delivery of captopril from floating matrix tablets

Jiménez-Martínez, Inéz; Quirino-Barreda, Carlos Tomás; Villafuerte-Robles, Leopoldo

doi:10.1016/j.ijpharm.2008.05.040

Cited by 69 publications

(48 citation statements)

References 15 publications

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“…Moreover, Captopril lies in the Class III of BCS classification showing high aqueous solubility as well as less intestinal permeability leading to variable absorption of drug via the intestine [18]. Owing to free water solubility, the drug can undergo dose dumping and burst phenomenon which can affect its sustained release formulation [19].…”

Section: Introductionmentioning

confidence: 99%

Formulation Optimization and <i>In-vitro</i> Evaluation of Oral Floating Captopril Matrix Tablets using Factorial Design

Ahsan¹,

Abbas²,

Hussain³

et al. 2015

Trop. J. Pharm Res

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Section: Introductionmentioning

confidence: 99%

Formulation Optimization and <i>In-vitro</i> Evaluation of Oral Floating Captopril Matrix Tablets using Factorial Design

Ahsan¹,

Abbas²,

Hussain³

et al. 2015

Trop. J. Pharm Res

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“…Therefore, development of a controlled delivery system for CAP would bring many advantages for hypertension patients, who compose almost 25% of the world's population. 4,5 Development of oral controlled-release formulations for CAP is very difficult due to both in vivo and in vitro instability. The drug also undergoes dose dumping and burst phenomena (being freely water soluble) when formulated as controlled-or sustainedrelease formulations.…”

Section: Introductionmentioning

confidence: 99%

New formulation of an old drug in hypertension treatment: the sustained release of captopril from cyclodextrin nanoparticles

Azevedo¹,

Tasic²,

Fattori³

et al. 2011

IJN

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Captopril (CAP) was the first angiotensin I-converting enzyme (ACE) inhibitor to be developed and is widely used in hypertension treatment. On the other hand, cyclodextrins (CDs) are cyclic oligosaccharides whose cone-shaped cavity allows formation of noncovalent inclusion complexes with appropriately sized guest molecules, thus modifying guest physical, chemical, and biological properties. Herein, the physicochemical characterization and in vivo ACE inhibition evaluation of seven CAP/CD complexes are reported. The inclusion complexes were prepared by spray-drying, freeze-drying, kneading, or lyophilization methods and characterized by nuclear magnetic resonance, Fourier-transformed infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy techniques. In vivo assays compared CAP and CAP/CD complex administration (0.5 mg kg −1 or 0.09 mg kg −1 , n = 4–7) to evaluate the ACE inhibition by continuous infusion of angiotensin I (30 ng 50 μL −1 min −1 ) in conscious Wistar rats. The physicochemical analysis demonstrated complete amorphization and complexation between CAP and CDs, indicating the substitution of water molecules inside the CD cavity with CAP. During the infusion of angiotensin I, the administration of all CAP/CD complexes induced a reduction in mean arterial pressure similar to that observed upon CAP administration. The nanoparticles obtained by the kneading method (CAP/α-CD:KM) showed a potent and long-lasting inhibitory activity (∼22 hours) on the angiotensin I pressor effect. The results suggest that the inclusion complex of CAP and α-CD can function as a novel antihypertensive formulation that may improve therapeutic use of CAP by reducing its oral dose administration to once per day, thus providing better quality of life for almost 25% of the world’s population who suffer from hypertension.

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“…Among other, one of the systems that can be used to maintain floating a dosage form in the stomach is that based on a reduction of the matrices density; facilitated by the carbon dioxide resulting from the reaction of sodium bicarbonate with an acidic medium like that of the stomach (Xu, Groves, 2001;Jiménez-Martínez et al, 2008;Sriamornsak et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

Effect of stearic acid on the properties of metronidazole/methocel K4M floating matrices

Lara-Hernández

Hernández-León

Villafuerte-Robles

2009

Braz. J. Pharm. Sci.

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The properties of metronidazole/Methocel K4M sustained release floating tablets have been studied varying the proportion of the lubricant, stearic acid, on formulations with and without sodium bicarbonate. The variables studied include technological properties of the tablets such as tablet hardness and ejection pressure, the drug release profile, the hydration kinetics and the floating behaviour. The presence of stearic acid and sodium bicarbonate improves the floating behaviour for more than 8 hours. The hydration volume, the tablet hardness and the ejection pressure decrease as the stearic acid content increases and the polymer content decreases. Drug dissolution increases with increasing proportions of stearic acid and decreasing proportions of the polymer in the tablets. The presence of sodium bicarbonate extends the differences in dissolution produced by stearic acid. These results are attributed to decreasing matrices coherence with an increasing quantity of stearic acid and a reducing polymer proportion. The carbon dioxide bubbles produced by sodium bicarbonate expand the matrices facilitating the dissolution, although their presence obstructs also the diffusion path through the hydrated gel layer. Uniterms:Metronidazole. Methocel K4M. Stearic acid. Matrices hydration. Gastric retention. Sodium bicarbonate. Sustained release. Drugs/release mechanism.Estudaram-se as propriedades de comprimidos flutuantes de metronidazol/Methocel K4M de liberação controlada, variando-se a proporção do lubrificante, ácido esteárico, nas formulações com e sem bicarbonato de sódio. As variáveis estudadas incluem propriedades tecnológicas dos comprimidos, tais como dureza, pressão de ejeção, perfil de liberação do fármaco, cinética de hidratação e comportamento de flutuação. A presença de ácido esteárico e do bicarbonato de sódio melhora o comportamento de flutuação para mais de 8 horas. O volume de hidratação, a dureza e a pressão de ejeção do comprimido decrescem à medida que o conteúdo de ácido esteárico e de polímero diminui. A dissolução do fármaco aumenta com o aumento das proporções de ácido esteárico e a diminuição das proporções de polímero nos comprimidos. A presença de bicarbonato de sódio amplia as diferenças na dissolução produzidas pelo ácido esteárico. Estes resultados são atribuídos à coesão decrescente das matrizes, com o aumento da quantidade de ácido esteárico e a redução da proporção de polímero. Bolhas de dióxido de carbono produzidas pelo bicarbonato de sódio expandem as matrizes, facilitando a dissolução, embora a presença delas obstrua, também, a difusão através da camada de gel hidratado. Unitermos:Metronidazol. Methocel K4M. Ácido esteárico. Hidratação das matrizes. Retenção gástrica. Bicarbonato de sódio. Fármacos/mecanismo de liberação.

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Sustained delivery of captopril from floating matrix tablets

Cited by 69 publications

References 15 publications

Formulation Optimization and <i>In-vitro</i> Evaluation of Oral Floating Captopril Matrix Tablets using Factorial Design

Formulation Optimization and <i>In-vitro</i> Evaluation of Oral Floating Captopril Matrix Tablets using Factorial Design

New formulation of an old drug in hypertension treatment: the sustained release of captopril from cyclodextrin nanoparticles

Effect of stearic acid on the properties of metronidazole/methocel K4M floating matrices

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