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 use of response surface methodology to evaluate the impact of level 2 SUPAC–IR changes on the in vitro release of metronidazole and ranitidine from a fixed-dose combination tablet
- King’ori, Loti D, Walker, Roderick B
- Authors: King’ori, Loti D , Walker, Roderick B
- Date: 2012
- Language: English
- Type: text , Article
- Identifier: vital:6391 , http://hdl.handle.net/10962/d1006313
- Description: The purpose of this study was to evaluate the effect of different levels of disintegrant (croscarmellose sodium, CCS), binder (polyvinylprrolidone K30, PVP–K30), and lubricant (magnesium stearate) on the in vitro release of metronidazole (MTZ) and rantidine (RTD) from a solid oral fixed-dose combination tablet. The excipient levels investigated were Level 2 changes in component and composition described in the Scale-Up and Post Approval Changes for Immediate Release (SUPAC–IR) guidance (1). Batches of tablets (1000 units) were manufactured by wet granulation using a Saral high-shear mixer granulator and a Manesty B3B rotary tablet press. Weight uniformity, friability, and disintegration of all tablets were assessed, and all batches complied with compendial specifications. The amount of drug released (Q) at ten minutes was dependent on the levels of CCS in the formulation, and the effect of PVP–K30 and magnesium stearate was dependent on the levels of CCS. Synergistic interactions between independent variables were observed for the Q10 value for RTD, whereas PVP–K30 and magnesium stearate exhibited an antagonistic effect on the Q10 values for MTZ and RTD. The use of response surface methodology facilitated an investigation into the effect of Level 2 component and composition changes, as described in SUPAC–IR, on the in vitro release of MTZ and RTD from a fixed-dose combination (FDC) solid oral dosage form (SODF).
- Full Text:
- Date Issued: 2012
- Authors: King’ori, Loti D , Walker, Roderick B
- Date: 2012
- Language: English
- Type: text , Article
- Identifier: vital:6391 , http://hdl.handle.net/10962/d1006313
- Description: The purpose of this study was to evaluate the effect of different levels of disintegrant (croscarmellose sodium, CCS), binder (polyvinylprrolidone K30, PVP–K30), and lubricant (magnesium stearate) on the in vitro release of metronidazole (MTZ) and rantidine (RTD) from a solid oral fixed-dose combination tablet. The excipient levels investigated were Level 2 changes in component and composition described in the Scale-Up and Post Approval Changes for Immediate Release (SUPAC–IR) guidance (1). Batches of tablets (1000 units) were manufactured by wet granulation using a Saral high-shear mixer granulator and a Manesty B3B rotary tablet press. Weight uniformity, friability, and disintegration of all tablets were assessed, and all batches complied with compendial specifications. The amount of drug released (Q) at ten minutes was dependent on the levels of CCS in the formulation, and the effect of PVP–K30 and magnesium stearate was dependent on the levels of CCS. Synergistic interactions between independent variables were observed for the Q10 value for RTD, whereas PVP–K30 and magnesium stearate exhibited an antagonistic effect on the Q10 values for MTZ and RTD. The use of response surface methodology facilitated an investigation into the effect of Level 2 component and composition changes, as described in SUPAC–IR, on the in vitro release of MTZ and RTD from a fixed-dose combination (FDC) solid oral dosage form (SODF).
- Full Text:
- Date Issued: 2012
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