In vitro dissolution kinetics of Captopril from microspheres manufactured by solvent evaporation
- Khamanga, Sandile M, Walker, Roderick B
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2012
- Language: English
- Type: text , Article
- Identifier: vital:6390 , http://hdl.handle.net/10962/d1006311
- Description: The aim of this study was to develop and assess captopril-loaded microspheres in which Methocel and Eudragit RS were used as release-controlling factors and to evaluate captopril (CPT) release using kinetic models. Drug-excipient interactions were evaluated using infrared studies, and the physical appearance was characterized using scanning electron microscopy (SEM). A burst effect was observed during the first stage of dissolution for most batches of microspheres. SEM results reveal that this may be attributed to dissolution of captopril crystals that were present on the surface, embedded in the superficial layer of the matrix materials, trapped near the surface of the microspheres, or that may have diffused rapidly through the porous surface of the capsules. The release data generated during in vitro release studies were fitted to zero-order, first-order, Higuchi, Korsmeyer–Peppas, Kopcha, and Makoid–Banakar models. The release kinetics of captopril from most formulations followed a classical Fickian diffusion mechanism. SEM photographs showed that diffusion took place through pores located in the surface of the microcapsules. The Kopcha model diffusion and erosion terms showed a predominance of diffusion relative to swelling or erosion throughout the entire test period. The drug release mechanism was also confirmed by the Makoid–Banakar and Korsmeyer–Peppas model exponents. This further supports a diffusion–release mechanism for most formulations. The models postulate that the total drug released is a summation of several mechanisms (viz., burst release, relaxation-induced controlled release, and diffusional release). These results also support the potential application of Eudragit/Methocel microspheres as a suitable sustained-release drug delivery system for captopril.
- Full Text:
- Date Issued: 2012
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2012
- Language: English
- Type: text , Article
- Identifier: vital:6390 , http://hdl.handle.net/10962/d1006311
- Description: The aim of this study was to develop and assess captopril-loaded microspheres in which Methocel and Eudragit RS were used as release-controlling factors and to evaluate captopril (CPT) release using kinetic models. Drug-excipient interactions were evaluated using infrared studies, and the physical appearance was characterized using scanning electron microscopy (SEM). A burst effect was observed during the first stage of dissolution for most batches of microspheres. SEM results reveal that this may be attributed to dissolution of captopril crystals that were present on the surface, embedded in the superficial layer of the matrix materials, trapped near the surface of the microspheres, or that may have diffused rapidly through the porous surface of the capsules. The release data generated during in vitro release studies were fitted to zero-order, first-order, Higuchi, Korsmeyer–Peppas, Kopcha, and Makoid–Banakar models. The release kinetics of captopril from most formulations followed a classical Fickian diffusion mechanism. SEM photographs showed that diffusion took place through pores located in the surface of the microcapsules. The Kopcha model diffusion and erosion terms showed a predominance of diffusion relative to swelling or erosion throughout the entire test period. The drug release mechanism was also confirmed by the Makoid–Banakar and Korsmeyer–Peppas model exponents. This further supports a diffusion–release mechanism for most formulations. The models postulate that the total drug released is a summation of several mechanisms (viz., burst release, relaxation-induced controlled release, and diffusional release). These results also support the potential application of Eudragit/Methocel microspheres as a suitable sustained-release drug delivery system for captopril.
- Full Text:
- Date Issued: 2012
The evaluation of Eudragit microcapsules manufactured by solvent evaporation using USP Apparatus 1
- Khamanga, Sandile M, Parfitt, Natalie R, Nyamuzhiwa, Tsitsi, Haidula, Hendrina, Walker, Roderick B
- Authors: Khamanga, Sandile M , Parfitt, Natalie R , Nyamuzhiwa, Tsitsi , Haidula, Hendrina , Walker, Roderick B
- Date: 2009
- Language: English
- Type: text , Article
- Identifier: vital:6389 , http://hdl.handle.net/10962/d1006310
- Description: The objectives of this study were to prepare microcapsules containing verapamil and propranolol and to evaluate the kinetics and mechanism of drug release from the microcapsules using USP Apparatus 1. The effects of polymer concentration and polymer type on the cumulative amount of drug released were evaluated. The microcapsules were manufactured using Eudragit RS and RL polymers by solvent evaporation with the ultimate aim of prolonging drug release. Twenty-four formulations were prepared using different drug/polymer ratios. The effects of polymer type and polymer/drug ratios on the size, flow properties, surface morphology, and the release characteristics of the microcapsules were examined. The effects of drug inclusion methods on drug loading, encapsulation efficiency, and release properties of the complex microcapsules were also investigated. The formulations containing drug/polymer ratio 1:4 (w/w) were the most appropriate with respect to encapsulation efficiency (70%), flow properties (HR = 1.2), drug loading (15–20%), and drug release characteristics, in all cases. The release kinetics from the different formulations followed mainly a diffusion-controlled mechanism.
- Full Text:
- Date Issued: 2009
- Authors: Khamanga, Sandile M , Parfitt, Natalie R , Nyamuzhiwa, Tsitsi , Haidula, Hendrina , Walker, Roderick B
- Date: 2009
- Language: English
- Type: text , Article
- Identifier: vital:6389 , http://hdl.handle.net/10962/d1006310
- Description: The objectives of this study were to prepare microcapsules containing verapamil and propranolol and to evaluate the kinetics and mechanism of drug release from the microcapsules using USP Apparatus 1. The effects of polymer concentration and polymer type on the cumulative amount of drug released were evaluated. The microcapsules were manufactured using Eudragit RS and RL polymers by solvent evaporation with the ultimate aim of prolonging drug release. Twenty-four formulations were prepared using different drug/polymer ratios. The effects of polymer type and polymer/drug ratios on the size, flow properties, surface morphology, and the release characteristics of the microcapsules were examined. The effects of drug inclusion methods on drug loading, encapsulation efficiency, and release properties of the complex microcapsules were also investigated. The formulations containing drug/polymer ratio 1:4 (w/w) were the most appropriate with respect to encapsulation efficiency (70%), flow properties (HR = 1.2), drug loading (15–20%), and drug release characteristics, in all cases. The release kinetics from the different formulations followed mainly a diffusion-controlled mechanism.
- Full Text:
- Date Issued: 2009
The effects of buffer molarity, agitation rate and mesh size on verapamil release from modified release mini-tablets using USP Apparatus 3
- Khamanga, Sandile M, Walker, Roderick B
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2007
- Language: English
- Type: text , Article
- Identifier: vital:6386 , http://hdl.handle.net/10962/d1006307
- Description: The effects of agitation rate, buffer molarity,and mesh size on the dissolution rate of verapamil hydrochloride from sustained release matrix tablets were studied using USP Apparatus 3. Eudragit® and Carbopol® were used as rate-retarding polymers in tablets prepared by wet granulation.The study was conducted to determine whether the drugs exhibit similar release characteristics when tested under the same dissolution conditions. It was found that the dissolution rate of verapamil hydrochloride was affected by the variables assessed in these studies.
- Full Text:
- Date Issued: 2007
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2007
- Language: English
- Type: text , Article
- Identifier: vital:6386 , http://hdl.handle.net/10962/d1006307
- Description: The effects of agitation rate, buffer molarity,and mesh size on the dissolution rate of verapamil hydrochloride from sustained release matrix tablets were studied using USP Apparatus 3. Eudragit® and Carbopol® were used as rate-retarding polymers in tablets prepared by wet granulation.The study was conducted to determine whether the drugs exhibit similar release characteristics when tested under the same dissolution conditions. It was found that the dissolution rate of verapamil hydrochloride was affected by the variables assessed in these studies.
- Full Text:
- Date Issued: 2007
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