Assessment of taste masking of captopril by ion-exchange resins using electronic gustatory system
- Chikukwa, Mellisa T, Wesoly, Malgorzata, Korzeniowska, Aleksandra B, Ciosek-Skibinska, Patrycja, Walker, Roderick B, Khamanga, Sandile M M
- Authors: Chikukwa, Mellisa T , Wesoly, Malgorzata , Korzeniowska, Aleksandra B , Ciosek-Skibinska, Patrycja , Walker, Roderick B , Khamanga, Sandile M M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184710 , vital:44265 , xlink:href="https://doi.org/10.1080/10837450.2019.1687520"
- Description: The objective of the study was to mask the unpleasant taste of captopril (CPT). Taste masking was achieved by complexation of CPT with a basic ion exchange resin, Dowex® 66, using the batch method. Dowex® 66 was used for the adsorption of CPT, and physical and chemical parameters of the CPT resinates complex were evaluated. A central composite design was used to generate the experiments for the manufacture of resinates using different process and formulation variables. In vitro dissolution studies were performed for 2 h in 0.01N HCl (pH 1.6) using USP Apparatus I. The compatibility of CPT and the resin was evaluated by Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). The resinates were evaluated for micromeritic properties and further characterised using FTIR, DSC, and PXRD. Response surface methodology was used to determine the significance of input variables on the CPT content and release. The CPT resin ratio was found to have a significant impact on content of the resinates and on CPT release. The formulations were also studied for taste masking ability by means of an electronic gustatory system – electronic tongue.
- Full Text:
- Date Issued: 2020
- Authors: Chikukwa, Mellisa T , Wesoly, Malgorzata , Korzeniowska, Aleksandra B , Ciosek-Skibinska, Patrycja , Walker, Roderick B , Khamanga, Sandile M M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184710 , vital:44265 , xlink:href="https://doi.org/10.1080/10837450.2019.1687520"
- Description: The objective of the study was to mask the unpleasant taste of captopril (CPT). Taste masking was achieved by complexation of CPT with a basic ion exchange resin, Dowex® 66, using the batch method. Dowex® 66 was used for the adsorption of CPT, and physical and chemical parameters of the CPT resinates complex were evaluated. A central composite design was used to generate the experiments for the manufacture of resinates using different process and formulation variables. In vitro dissolution studies were performed for 2 h in 0.01N HCl (pH 1.6) using USP Apparatus I. The compatibility of CPT and the resin was evaluated by Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). The resinates were evaluated for micromeritic properties and further characterised using FTIR, DSC, and PXRD. Response surface methodology was used to determine the significance of input variables on the CPT content and release. The CPT resin ratio was found to have a significant impact on content of the resinates and on CPT release. The formulations were also studied for taste masking ability by means of an electronic gustatory system – electronic tongue.
- Full Text:
- Date Issued: 2020
Design, evaluation and optimization of taste masked clarithromycin powder
- Ntemi, Pascal V, Walker, Roderick B, Khamanga, Sandile M
- Authors: Ntemi, Pascal V , Walker, Roderick B , Khamanga, Sandile M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183503 , vital:44001 , xlink:href="https://doi.org/10.1691/ph.2019.8116"
- Description: Clarithromycin (CLA) is an extremely bitter macrolide antibiotic used to treat paediatric and adult infections. The bitter taste affects patient adherence and may compromise therapy. This research developed a taste masked CLA resinate using Indion® 234, a weak acidic cation exchange resin. The factors affecting formation of the CLA-resin complex were assessed. Design of experiments was used to optimize response while evaluating input variables such as temperature, CLA-resin ratio,stirring time and pH. CLA loading efficiency was determined spectrophotometrically and CLA release using USP Apparatus II. Differential Scanning Calorimetry (DSC), Scanning Electron Microscop (SEM), Fourier Transform Infrared (FT-IR) Spectroscopy and X-ray Diffraction (XRD) were used to confirm complex formation. A spectrophotometric method was used to assess taste evaluation. The optimum CLA-resin ratio, temperature, and stirring time were 1:4, 80 °C, 3 hours, respectively, at pH 8. Characterization techniques revealed that CLA was crystalline and the complex amorphous in nature. FT-IR spectra of resinate revealed the absence of resonance due to the tertiary amine functional group that is responsible for the bitter taste of CLA. CLA was stable in simulated salivary fluid and was released within 3 hours in gastric fluid. All CLAresin batches revealed complete taste masking. Taste analysis highlighted the improvement of taste masking properties of the resinate as the CLA to resin ratio, increased.
- Full Text:
- Date Issued: 2019
- Authors: Ntemi, Pascal V , Walker, Roderick B , Khamanga, Sandile M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183503 , vital:44001 , xlink:href="https://doi.org/10.1691/ph.2019.8116"
- Description: Clarithromycin (CLA) is an extremely bitter macrolide antibiotic used to treat paediatric and adult infections. The bitter taste affects patient adherence and may compromise therapy. This research developed a taste masked CLA resinate using Indion® 234, a weak acidic cation exchange resin. The factors affecting formation of the CLA-resin complex were assessed. Design of experiments was used to optimize response while evaluating input variables such as temperature, CLA-resin ratio,stirring time and pH. CLA loading efficiency was determined spectrophotometrically and CLA release using USP Apparatus II. Differential Scanning Calorimetry (DSC), Scanning Electron Microscop (SEM), Fourier Transform Infrared (FT-IR) Spectroscopy and X-ray Diffraction (XRD) were used to confirm complex formation. A spectrophotometric method was used to assess taste evaluation. The optimum CLA-resin ratio, temperature, and stirring time were 1:4, 80 °C, 3 hours, respectively, at pH 8. Characterization techniques revealed that CLA was crystalline and the complex amorphous in nature. FT-IR spectra of resinate revealed the absence of resonance due to the tertiary amine functional group that is responsible for the bitter taste of CLA. CLA was stable in simulated salivary fluid and was released within 3 hours in gastric fluid. All CLAresin batches revealed complete taste masking. Taste analysis highlighted the improvement of taste masking properties of the resinate as the CLA to resin ratio, increased.
- Full Text:
- Date Issued: 2019
Formulation and Characterisation of a Combination Captopril and Hydrochlorothiazide Microparticulate Dosage Form
- Chikukwa, Mellisa T R, Walker, Roderick B, Khamanga, Sandile M
- Authors: Chikukwa, Mellisa T R , Walker, Roderick B , Khamanga, Sandile M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183200 , vital:43926 , xlink:href="https://doi.org/10.3390/pharmaceutics12080712"
- Description: Cardiovascular diseases such as hypertension and cardiac failure in South African children and adolescents are effectively managed long term, using a combination treatment of captopril and hydrochlorothiazide. The majority of commercially available pharmaceutical products are designed for adult patients and require extemporaneous manipulation, prior to administration to paediatric patients. There is a need to develop an age appropriate microparticulate dosing technology that is easy to swallow, dose and alter doses whilst overcoming the pharmacokinetic challenges of short half-life and biphasic pharmacokinetic disposition exhibited by hydrochlorothiazide and captopril. An emulsion solvent evaporation approach using different combinations of polymers was used to manufacture captopril and hydrochlorothiazide microparticles. Design of experiments was used to develop and analyse experimental data, and identifyoptimum formulation and process conditions for the preparation of the microparticles. Characterisation studies to establish encapsulation efficiency, in vitro release, shape, size and morphology of the microparticles were undertaken. The microparticles produced were in the micrometre size range, with an encapsulation efficiency >75% for both hydrochlorothiazide and captopril. The microparticulate technology is able to offer potential resolution to the half-life mediated dosing frequency of captopril as sustained release of the molecule was observed over a 12-h period. The release of hydrochlorothiazide of >80% suggests an improvement in solubility limited dissolution.
- Full Text:
- Date Issued: 2020
- Authors: Chikukwa, Mellisa T R , Walker, Roderick B , Khamanga, Sandile M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183200 , vital:43926 , xlink:href="https://doi.org/10.3390/pharmaceutics12080712"
- Description: Cardiovascular diseases such as hypertension and cardiac failure in South African children and adolescents are effectively managed long term, using a combination treatment of captopril and hydrochlorothiazide. The majority of commercially available pharmaceutical products are designed for adult patients and require extemporaneous manipulation, prior to administration to paediatric patients. There is a need to develop an age appropriate microparticulate dosing technology that is easy to swallow, dose and alter doses whilst overcoming the pharmacokinetic challenges of short half-life and biphasic pharmacokinetic disposition exhibited by hydrochlorothiazide and captopril. An emulsion solvent evaporation approach using different combinations of polymers was used to manufacture captopril and hydrochlorothiazide microparticles. Design of experiments was used to develop and analyse experimental data, and identifyoptimum formulation and process conditions for the preparation of the microparticles. Characterisation studies to establish encapsulation efficiency, in vitro release, shape, size and morphology of the microparticles were undertaken. The microparticles produced were in the micrometre size range, with an encapsulation efficiency >75% for both hydrochlorothiazide and captopril. The microparticulate technology is able to offer potential resolution to the half-life mediated dosing frequency of captopril as sustained release of the molecule was observed over a 12-h period. The release of hydrochlorothiazide of >80% suggests an improvement in solubility limited dissolution.
- Full Text:
- Date Issued: 2020
Evaluation of rate of swelling and erosion of verapamil (VRP) sustained-release matrix tablets
- Khamanga, Sandile M, Walker, Roderick B
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2006
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184232 , vital:44192 , xlink:href="https://doi.org/10.1080/03639040600599822"
- Description: Tablets manufactured in-house were compared to a marketed sustained-release product of verapamil to investigate the rate of hydration, erosion, and drug-release mechanism by measuring the wet and subsequent dry weights of the products. Swelling and erosion rates depended on the polymer and granulating fluid used, which ultimately pointed to their permeability characteristics. Erosion rate of the marketed product was highest, which suggests that the gel layer that formed around these tablets was weak as opposed to the robust and resistant layers of test products. Anomalous and near zero-order transport mechanisms were dominant in tests and commercial product, respectively.
- Full Text:
- Date Issued: 2006
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2006
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184232 , vital:44192 , xlink:href="https://doi.org/10.1080/03639040600599822"
- Description: Tablets manufactured in-house were compared to a marketed sustained-release product of verapamil to investigate the rate of hydration, erosion, and drug-release mechanism by measuring the wet and subsequent dry weights of the products. Swelling and erosion rates depended on the polymer and granulating fluid used, which ultimately pointed to their permeability characteristics. Erosion rate of the marketed product was highest, which suggests that the gel layer that formed around these tablets was weak as opposed to the robust and resistant layers of test products. Anomalous and near zero-order transport mechanisms were dominant in tests and commercial product, respectively.
- Full Text:
- Date Issued: 2006
Swelling, erosion and drug release characteristics of salbutamol sulfate from hydroxypropyl methylcellulose-based matrix tablets
- Chaibva, Faith A, Khamanga, Sandile M, Walker, Roderick B
- Authors: Chaibva, Faith A , Khamanga, Sandile M , Walker, Roderick B
- Date: 2010
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184139 , vital:44177 , xlink:href="https://doi.org/10.3109/03639045.2010.488648"
- Description: Background: Hydrophilic matrix formulations are important and simple technologies that are used to manufacture sustained release dosage forms. Method: Hydroxypropyl methylcellulose-based matrix tablets, with and without additives, were manufactured to investigate the rate of hydration, rate of erosion, and rate and mechanism of drug release. Scanning electron microscopy was used to assess changes in the microstructure of the tablets during drug release testing and whether these changes could be related to the rate of drug release from the formulations. Results: The results revealed that the rate of hydration and erosion was dependent on the polymer combination(s) used, which in turn affected the rate and mechanism of drug release from these formulations. It was also apparent that changes in the microstructure of matrix tablets could be related to the different rates of drug release that were observed from the test formulations. Conclusion: The use of scanning electron microscopy provides useful information to further understand drug release mechanisms from matrix tablets.
- Full Text:
- Date Issued: 2010
- Authors: Chaibva, Faith A , Khamanga, Sandile M , Walker, Roderick B
- Date: 2010
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184139 , vital:44177 , xlink:href="https://doi.org/10.3109/03639045.2010.488648"
- Description: Background: Hydrophilic matrix formulations are important and simple technologies that are used to manufacture sustained release dosage forms. Method: Hydroxypropyl methylcellulose-based matrix tablets, with and without additives, were manufactured to investigate the rate of hydration, rate of erosion, and rate and mechanism of drug release. Scanning electron microscopy was used to assess changes in the microstructure of the tablets during drug release testing and whether these changes could be related to the rate of drug release from the formulations. Results: The results revealed that the rate of hydration and erosion was dependent on the polymer combination(s) used, which in turn affected the rate and mechanism of drug release from these formulations. It was also apparent that changes in the microstructure of matrix tablets could be related to the different rates of drug release that were observed from the test formulations. Conclusion: The use of scanning electron microscopy provides useful information to further understand drug release mechanisms from matrix tablets.
- Full Text:
- Date Issued: 2010
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
Drug transport mechanisms from carbopol/eudragit verapamil sustained-release tablets
- Khamanga, Sandile M, Walker, Roderick B
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2011
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184801 , vital:44273 , xlink:href="https://doi.org/10.14227/dt180311p30"
- Description: The objectives of this study were to compare dissolution profiles of a verapamil (VRP) formulation manufactured inhouse and Isoptin SR using USP Apparatus 2 and 3 and to elucidate drug release kinetics of these dosage forms. Eudragit NE 30D (ethyl acrylate–methyl methacrylate copolymer in a 2:1 ratio) aqueous dispersion was used as a granulating binder for the manufacture of VRP mini-matrix sustained-release tablets. The wet granulation process was performed to prepare free-flowing granules that were blended with Carbopol. The tablets were manufactured using a single-punch press by compression of the granules with magnesium stearate as a lubricant. Drug release was determined in phosphate buffer solution using USP Apparatus 2 and 3. Dissolution data were fitted to zero- and first-order models; in addition, the kinetic data were determined by evaluation of Higuchi release kinetics. The mechanism of drug release was established using the Korsmeyer–Peppas model. In general, all tablets showed high mechanical resistance with less than 1% friability. There was no significant difference between the dissolution profiles of the formulation manufactured in-house and the commercially available product. The release mechanism of the formulated and marketed products was controlled by anomalous non-Fickian diffusion. VRP release was prolonged for 12 h indicating the usefulness of the formulation as a twice-daily dosage form. The mechanism of drug release for the dosage forms was unaffected by the choice of apparatus.
- Full Text:
- Date Issued: 2011
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2011
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184801 , vital:44273 , xlink:href="https://doi.org/10.14227/dt180311p30"
- Description: The objectives of this study were to compare dissolution profiles of a verapamil (VRP) formulation manufactured inhouse and Isoptin SR using USP Apparatus 2 and 3 and to elucidate drug release kinetics of these dosage forms. Eudragit NE 30D (ethyl acrylate–methyl methacrylate copolymer in a 2:1 ratio) aqueous dispersion was used as a granulating binder for the manufacture of VRP mini-matrix sustained-release tablets. The wet granulation process was performed to prepare free-flowing granules that were blended with Carbopol. The tablets were manufactured using a single-punch press by compression of the granules with magnesium stearate as a lubricant. Drug release was determined in phosphate buffer solution using USP Apparatus 2 and 3. Dissolution data were fitted to zero- and first-order models; in addition, the kinetic data were determined by evaluation of Higuchi release kinetics. The mechanism of drug release was established using the Korsmeyer–Peppas model. In general, all tablets showed high mechanical resistance with less than 1% friability. There was no significant difference between the dissolution profiles of the formulation manufactured in-house and the commercially available product. The release mechanism of the formulated and marketed products was controlled by anomalous non-Fickian diffusion. VRP release was prolonged for 12 h indicating the usefulness of the formulation as a twice-daily dosage form. The mechanism of drug release for the dosage forms was unaffected by the choice of apparatus.
- Full Text:
- Date Issued: 2011
Development and assessment of a USP Apparatus 3 dissolution test method for sustained-release Nevirapine matrix tablets
- Mwila, Chiluba, Khamanga, Sandile M M, Walker, Roderick B
- Authors: Mwila, Chiluba , Khamanga, Sandile M M , Walker, Roderick B
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184779 , vital:44271 , xlink:href="https://doi.org/10.14227/dt230316p22"
- Description: Dissolution testing is a quality control tool used to assess batch-to-batch performance of dosage forms, thereby providing continued assurance of product quality. Analytical methods for the assessment of pharmaceutical product quality must be validated according to regulatory guidelines to ensure that tests are reliable and valid. Agitation rate, mesh pore size, surfactant concentration, and dissolution medium molarity are experimental parameters that may affect nevirapine (NVP) release and were investigated and optimized to ensure that consistent, reliable, and valid results using Apparatus 3 were produced. Agitation rate was investigated to establish an equivalent response to that observed for NVP release using Apparatus 2 at 50 rpm. A reciprocation rate of 5–10 dpm produced dissolution profiles that were similar to those observed using Apparatus 2. An increase in the molarity of the dissolution medium slightly increased the release rate of NVP, and a 50 mM buffer maintained at pH values mimicking gastrointestinal tract (GIT) conditions was selected for all experiments. With the addition of 2% sodium lauryl sulfate (SLS) to the dissolution medium, >80% NVP was released from the tablets over the test period. The NVP release rate increased with an increase in the mesh pore size; however, the extent of release was not affected by this parameter. Dissolution test samples were analyzed using HPLC, and dissolution methods were validated for NVP stability in the dissolution medium, specificity, linearity and range, repeatability, intermediate precision, and accuracy as defined by ICH. The dissolution method used for testing NVP tablets can be regarded as an appropriate tool for the evaluation of sustained-release (SR) NVP formulations and the impact of formulation composition and product quality attributes on drug release.
- Full Text:
- Date Issued: 2016
- Authors: Mwila, Chiluba , Khamanga, Sandile M M , Walker, Roderick B
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184779 , vital:44271 , xlink:href="https://doi.org/10.14227/dt230316p22"
- Description: Dissolution testing is a quality control tool used to assess batch-to-batch performance of dosage forms, thereby providing continued assurance of product quality. Analytical methods for the assessment of pharmaceutical product quality must be validated according to regulatory guidelines to ensure that tests are reliable and valid. Agitation rate, mesh pore size, surfactant concentration, and dissolution medium molarity are experimental parameters that may affect nevirapine (NVP) release and were investigated and optimized to ensure that consistent, reliable, and valid results using Apparatus 3 were produced. Agitation rate was investigated to establish an equivalent response to that observed for NVP release using Apparatus 2 at 50 rpm. A reciprocation rate of 5–10 dpm produced dissolution profiles that were similar to those observed using Apparatus 2. An increase in the molarity of the dissolution medium slightly increased the release rate of NVP, and a 50 mM buffer maintained at pH values mimicking gastrointestinal tract (GIT) conditions was selected for all experiments. With the addition of 2% sodium lauryl sulfate (SLS) to the dissolution medium, >80% NVP was released from the tablets over the test period. The NVP release rate increased with an increase in the mesh pore size; however, the extent of release was not affected by this parameter. Dissolution test samples were analyzed using HPLC, and dissolution methods were validated for NVP stability in the dissolution medium, specificity, linearity and range, repeatability, intermediate precision, and accuracy as defined by ICH. The dissolution method used for testing NVP tablets can be regarded as an appropriate tool for the evaluation of sustained-release (SR) NVP formulations and the impact of formulation composition and product quality attributes on drug release.
- Full Text:
- Date Issued: 2016
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 in the evaluation of captopril microparticles manufactured using an oil in oil solvent evaporation technique
- Khamanga, Sandile M, Walker, Roderick B
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184221 , vital:44191 , xlink:href="https://doi.org/10.3109/02652048.2011.629744"
- Description: Captopril (CPT) microparticles were manufactured by solvent evaporation using acetone (dispersion phase) and liquid paraffin (manufacturing phase) with Eudragit® and Methocel® as coat materials. Design of experiments and response surface methodology (RSM) approaches were used to optimize the process. The microparticles were characterized based on the percent of drug released and yield, microcapsule size, entrapment efficiency and Hausner ratio. Differential scanning calorimetry (DSC), Infrared (IR) spectroscopy, scanning electron microscopy (SEM) and in vitro dissolution studies were conducted. The microcapsules were spherical, free-flowing and IR and DSC thermograms revealed that CPT was stable. The percent drug released was investigated with respect to Eudragit® RS and Methocel® K100M, Methocel® K15M concentrations and homogenizing speed. The optimal conditions for microencapsulation were 1.12 g Eudragit® RS, 0.67 g Methocel® K100M and 0.39 g Methocel® K15M at a homogenizing speed of 1643 rpm and 89% CPT was released. The value of RSM-mediated microencapsulation of CPT was elucidated.
- Full Text:
- Date Issued: 2012
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184221 , vital:44191 , xlink:href="https://doi.org/10.3109/02652048.2011.629744"
- Description: Captopril (CPT) microparticles were manufactured by solvent evaporation using acetone (dispersion phase) and liquid paraffin (manufacturing phase) with Eudragit® and Methocel® as coat materials. Design of experiments and response surface methodology (RSM) approaches were used to optimize the process. The microparticles were characterized based on the percent of drug released and yield, microcapsule size, entrapment efficiency and Hausner ratio. Differential scanning calorimetry (DSC), Infrared (IR) spectroscopy, scanning electron microscopy (SEM) and in vitro dissolution studies were conducted. The microcapsules were spherical, free-flowing and IR and DSC thermograms revealed that CPT was stable. The percent drug released was investigated with respect to Eudragit® RS and Methocel® K100M, Methocel® K15M concentrations and homogenizing speed. The optimal conditions for microencapsulation were 1.12 g Eudragit® RS, 0.67 g Methocel® K100M and 0.39 g Methocel® K15M at a homogenizing speed of 1643 rpm and 89% CPT was released. The value of RSM-mediated microencapsulation of CPT was elucidated.
- Full Text:
- Date Issued: 2012
The impact of manufacturing variables on in vitro release of clobetasol 17-propionate from pilot scale cream formulations
- Fauzee, Ayesha F B, Khamanga, Sandile M, Walker, Roderick B
- Authors: Fauzee, Ayesha F B , Khamanga, Sandile M , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183872 , vital:44077 , xlink:href="https://doi.org/10.3109/03639045.2013.842579"
- Description: The purpose of the study was to evaluate the effect of different homogenization speeds and times, anchor speeds and cooling times on the viscosity and cumulative % clobetasol 17-propionate released per unit area at 72 h from pilot scale cream formulations. A 24 full factorial central composite design for four independent variables were investigated. Thirty pilot scale batches of cream formulations were manufactured using a Wintech® cream/ointment plant. The viscosity and in vitro release of CP were monitored and compared to an innovator product that is commercially available on the South African market, namely, Dermovate® cream. Contour and three-dimensional response surface plots were produced and the viscosity and cumulative % CP released per unit area at 72 h were found to be primarily dependent on the homogenization and anchor speeds. An increase in the homogenization and anchor speeds appeared to exhibit a synergistic effect on the resultant viscosity of the cream whereas an antagonistic effect was observed for the in vitro release of CP from the experimental cream formulations. The in vitro release profiles were best fitted to a Higuchi model and diffusion proved to be the dominant mechanism of drug release that was confirmed by use of the Korsmeyer–Peppas model. The research was further validated and confirmed by the high prognostic ability of response surface methodology (RSM) with a resultant mean percentage error of (±SD) 0.17 ± 0.093 suggesting that RSM may be an efficient tool for the development and optimization of topical formulations.
- Full Text:
- Date Issued: 2014
- Authors: Fauzee, Ayesha F B , Khamanga, Sandile M , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183872 , vital:44077 , xlink:href="https://doi.org/10.3109/03639045.2013.842579"
- Description: The purpose of the study was to evaluate the effect of different homogenization speeds and times, anchor speeds and cooling times on the viscosity and cumulative % clobetasol 17-propionate released per unit area at 72 h from pilot scale cream formulations. A 24 full factorial central composite design for four independent variables were investigated. Thirty pilot scale batches of cream formulations were manufactured using a Wintech® cream/ointment plant. The viscosity and in vitro release of CP were monitored and compared to an innovator product that is commercially available on the South African market, namely, Dermovate® cream. Contour and three-dimensional response surface plots were produced and the viscosity and cumulative % CP released per unit area at 72 h were found to be primarily dependent on the homogenization and anchor speeds. An increase in the homogenization and anchor speeds appeared to exhibit a synergistic effect on the resultant viscosity of the cream whereas an antagonistic effect was observed for the in vitro release of CP from the experimental cream formulations. The in vitro release profiles were best fitted to a Higuchi model and diffusion proved to be the dominant mechanism of drug release that was confirmed by use of the Korsmeyer–Peppas model. The research was further validated and confirmed by the high prognostic ability of response surface methodology (RSM) with a resultant mean percentage error of (±SD) 0.17 ± 0.093 suggesting that RSM may be an efficient tool for the development and optimization of topical formulations.
- Full Text:
- Date Issued: 2014
Development, manufacture and characterization of niosomes for the delivery for nevirapine
- Witika, Bwalya A, Walker, Roderick B
- Authors: Witika, Bwalya A , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183514 , vital:44002 , xlink:href="https://doi.org/10.1691/ph.2019.8168"
- Description: Nevirapine (NVP), used for the treatment of HIV/AIDS, exhibits unpredictable oral bioavailability, has a poor side effect profile and requires frequent dosing. Niosomes are novel drug delivery systems that have the potential to overcome these challenges. A thin layer hydration approach was used to produce niosomes and optimisation was undertaken using design of experiments (DoE) and response surface methodology (RSM) establish and identify parameters that may affect the manufacture of niosomes. The impact of cholesterol and surfactant content, hydration time and temperature on manufacture was investigated. Critical quality attributes (CQA) in respect of particle size (PS), entrapment efficiency (EE), polydispersity index (PDI) and the amount of NVP released at 48 hours was also assessed. The optimised niosome composition was identified and manufactured and the CQA characterised prior to placing the batch on stability for 12 weeks at 4±2 °C and 22±2 °C. The PS, PDI, EE and % NVP released at 48 h was 523.36±23.16 nm, 0.386±0.054, 96.8 % and 25.3 % for niosomes manufactured with Span® 20. Similarly, the parameters were 502.87±21.77 nm and 0.394±0.027, 98.0 % and 25.0 % for mean PS, PDI, EE and %NVP released at 48 h for Span® 80 niosomes. All characterisation was undertaken on the day of manufacture. In conclusion, a simple, cheap, rapid and precise method of manufacture of NVP niosomes was developed, validated and optimised using DoE and RSM and the product exhibited the target CQA.
- Full Text:
- Date Issued: 2019
- Authors: Witika, Bwalya A , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183514 , vital:44002 , xlink:href="https://doi.org/10.1691/ph.2019.8168"
- Description: Nevirapine (NVP), used for the treatment of HIV/AIDS, exhibits unpredictable oral bioavailability, has a poor side effect profile and requires frequent dosing. Niosomes are novel drug delivery systems that have the potential to overcome these challenges. A thin layer hydration approach was used to produce niosomes and optimisation was undertaken using design of experiments (DoE) and response surface methodology (RSM) establish and identify parameters that may affect the manufacture of niosomes. The impact of cholesterol and surfactant content, hydration time and temperature on manufacture was investigated. Critical quality attributes (CQA) in respect of particle size (PS), entrapment efficiency (EE), polydispersity index (PDI) and the amount of NVP released at 48 hours was also assessed. The optimised niosome composition was identified and manufactured and the CQA characterised prior to placing the batch on stability for 12 weeks at 4±2 °C and 22±2 °C. The PS, PDI, EE and % NVP released at 48 h was 523.36±23.16 nm, 0.386±0.054, 96.8 % and 25.3 % for niosomes manufactured with Span® 20. Similarly, the parameters were 502.87±21.77 nm and 0.394±0.027, 98.0 % and 25.0 % for mean PS, PDI, EE and %NVP released at 48 h for Span® 80 niosomes. All characterisation was undertaken on the day of manufacture. In conclusion, a simple, cheap, rapid and precise method of manufacture of NVP niosomes was developed, validated and optimised using DoE and RSM and the product exhibited the target CQA.
- Full Text:
- Date Issued: 2019
Syntheses, protonation constants and antimicrobial activity of 2-substituted N-alkylimidazole derivatives
- Kleyi, Phumelele, Walmsley, Ryan S, Gundhla, Isaac Z, Walmsley, Tara A, Jauka, Tembisa I, Dames, Joanna F, Walker, Roderick B, Torto, Nelson, Tshentu, Zenixole R
- Authors: Kleyi, Phumelele , Walmsley, Ryan S , Gundhla, Isaac Z , Walmsley, Tara A , Jauka, Tembisa I , Dames, Joanna F , Walker, Roderick B , Torto, Nelson , Tshentu, Zenixole R
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184066 , vital:44165 , xlink:href="https://www.ajol.info/index.php/sajc/article/view/123858"
- Description: A series of N-alkylimidazole-2-carboxylic acid, N-alkylimidazole-2-carboxaldehyde and N-alkylimidazole-2-methanol derivatives [alkyl = benzyl, methyl, ethyl, propyl, butyl, heptyl, octyl and decyl] have been synthesized and the protonation constants determined. The antimicrobial properties of the compounds were tested against Gram-negative (Escherichi coli), Gram-positive (Staphylococcus aureus and Bacillus subtilis subsp. spizizenii) bacterial strains and yeast (C. albicans). Both the disk diffusion and broth microdilution methods for testing the antimicrobial activity showed that N-alkylation of imidazole with longer alkyl chains and the substitution with low pKa group at 2-position resulted in enhanced antimicrobial activity. Particularly, the N-alkylimidazole-2-carboxylic acids exhibited the best antimicrobial activity due to the low pKa of the carboxylic acid moiety. Generally, all the N-alkylimidazole derivatives were most active against the Gram-positive bacteria [S. aureus (MIC = 5–160 µg mL–1) and B. subtilis subsp. spizizenii (5–20 µg mL–1)], with the latter more susceptible. All the compounds showed poor antimicrobial activity against both Gram-negative (E. coli, MIC = 0.15 to >2500 µg mL–1) bacteria and all the compounds were inactive against the yeast (Candida albicans).
- Full Text:
- Date Issued: 2012
- Authors: Kleyi, Phumelele , Walmsley, Ryan S , Gundhla, Isaac Z , Walmsley, Tara A , Jauka, Tembisa I , Dames, Joanna F , Walker, Roderick B , Torto, Nelson , Tshentu, Zenixole R
- Date: 2012
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184066 , vital:44165 , xlink:href="https://www.ajol.info/index.php/sajc/article/view/123858"
- Description: A series of N-alkylimidazole-2-carboxylic acid, N-alkylimidazole-2-carboxaldehyde and N-alkylimidazole-2-methanol derivatives [alkyl = benzyl, methyl, ethyl, propyl, butyl, heptyl, octyl and decyl] have been synthesized and the protonation constants determined. The antimicrobial properties of the compounds were tested against Gram-negative (Escherichi coli), Gram-positive (Staphylococcus aureus and Bacillus subtilis subsp. spizizenii) bacterial strains and yeast (C. albicans). Both the disk diffusion and broth microdilution methods for testing the antimicrobial activity showed that N-alkylation of imidazole with longer alkyl chains and the substitution with low pKa group at 2-position resulted in enhanced antimicrobial activity. Particularly, the N-alkylimidazole-2-carboxylic acids exhibited the best antimicrobial activity due to the low pKa of the carboxylic acid moiety. Generally, all the N-alkylimidazole derivatives were most active against the Gram-positive bacteria [S. aureus (MIC = 5–160 µg mL–1) and B. subtilis subsp. spizizenii (5–20 µg mL–1)], with the latter more susceptible. All the compounds showed poor antimicrobial activity against both Gram-negative (E. coli, MIC = 0.15 to >2500 µg mL–1) bacteria and all the compounds were inactive against the yeast (Candida albicans).
- Full Text:
- Date Issued: 2012
Academy of Pharmaceutical Sciences
- Authors: Walker, Roderick B
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184768 , vital:44270 , xlink:href="https://hdl.handle.net/10520/EJC-98c37d47c"
- Description: It is an honour and a pleasure to report on the activities of the Academy of Pharmaceutical Sciences since the PSSA AGM in 2016. The Academy of Pharmaceutical Sciences of the Pharmaceutical Society of South Africa (APSSA) held their 37th Annual Conference and 38th Annual General Meeting at the All African Congress on Pharmacology and Pharmacy. The conference was jointly organised by the Academy of Pharmaceutical Sciences of South Africa (APSSA), the South African Society for Basic and Clinical Pharmacology (SASBCP) on behalf of Pharmacology for Africa (Pharfa) and the Toxicology Society of South Africa (ToxSA). The annual APSSA conference was hosted by the Department of Pharmaceutical Sciences, Tshwane University of Technology under the leadership of Dr Ilze Vermaak and was held from 5-8 October 2016 at Misty Hills Conference Centre, situated close to the Cradle of Humankind.
- Full Text:
- Date Issued: 2017
- Authors: Walker, Roderick B
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184768 , vital:44270 , xlink:href="https://hdl.handle.net/10520/EJC-98c37d47c"
- Description: It is an honour and a pleasure to report on the activities of the Academy of Pharmaceutical Sciences since the PSSA AGM in 2016. The Academy of Pharmaceutical Sciences of the Pharmaceutical Society of South Africa (APSSA) held their 37th Annual Conference and 38th Annual General Meeting at the All African Congress on Pharmacology and Pharmacy. The conference was jointly organised by the Academy of Pharmaceutical Sciences of South Africa (APSSA), the South African Society for Basic and Clinical Pharmacology (SASBCP) on behalf of Pharmacology for Africa (Pharfa) and the Toxicology Society of South Africa (ToxSA). The annual APSSA conference was hosted by the Department of Pharmaceutical Sciences, Tshwane University of Technology under the leadership of Dr Ilze Vermaak and was held from 5-8 October 2016 at Misty Hills Conference Centre, situated close to the Cradle of Humankind.
- Full Text:
- Date Issued: 2017
Development and Validation of a Stability-indicating RP-HPLC Method Using Quality by Design for Estimating Captopril
- Veerubhotla, Krishna, Walker, Roderick B
- Authors: Veerubhotla, Krishna , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183525 , vital:44003 , xlink:href="10.4172/pharmaceutical-sciences.1000478"
- Description: The applicability of a quality by design framework for the development of a sensitive, simple and selective, stability-indicating reversed-phase high-performance liquid chromatography analytical method for the analysis of captopril was investigated. Design of experiments using a central composite design approach was used for method development. Twenty experimental runs were performed with acetonitrile content ranging between 28 and 36 % v/v, pH from 2.8 to 3.6 and temperature between 22° and 32°. The experimental data obtained was used to derive a quadratic model for the retention time of captopril. The optimized method produced sharp peaks with good resolution (>2) for captopril and the internal standard with retention times of 3.1 and 6.2 min, respectively. The experimental data revealed that acetonitrile content in the mobile phase and pH are significant factors that affect the retention time and resolution of captopril. Normal probability plots revealed that the residual and predicted data fall approximately on a straight line, indicating that the experimental error for these studies was evenly distributed suggesting that the model could be used to navigate the design space. This approach is useful to expedite method development and optimization activities in analytical laboratories.
- Full Text:
- Date Issued: 2019
- Authors: Veerubhotla, Krishna , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183525 , vital:44003 , xlink:href="10.4172/pharmaceutical-sciences.1000478"
- Description: The applicability of a quality by design framework for the development of a sensitive, simple and selective, stability-indicating reversed-phase high-performance liquid chromatography analytical method for the analysis of captopril was investigated. Design of experiments using a central composite design approach was used for method development. Twenty experimental runs were performed with acetonitrile content ranging between 28 and 36 % v/v, pH from 2.8 to 3.6 and temperature between 22° and 32°. The experimental data obtained was used to derive a quadratic model for the retention time of captopril. The optimized method produced sharp peaks with good resolution (>2) for captopril and the internal standard with retention times of 3.1 and 6.2 min, respectively. The experimental data revealed that acetonitrile content in the mobile phase and pH are significant factors that affect the retention time and resolution of captopril. Normal probability plots revealed that the residual and predicted data fall approximately on a straight line, indicating that the experimental error for these studies was evenly distributed suggesting that the model could be used to navigate the design space. This approach is useful to expedite method development and optimization activities in analytical laboratories.
- Full Text:
- Date Issued: 2019
Electropolymerized Fluorinated Aniline-Based Fiber for Headspace Solid-Phase Microextraction and Gas Chromatographic Determination of Benzaldehyde in Injectable Pharmaceutical Formulations
- Mohammadi, Ali, Mohammadi, Somayeh, Moghaddam, Bayandori A, Masoumi, Vahideh, Walker, Roderick B
- Authors: Mohammadi, Ali , Mohammadi, Somayeh , Moghaddam, Bayandori A , Masoumi, Vahideh , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184120 , vital:44175 , xlink:href="https://doi.org/10.1093/chromsci/bmt152"
- Description: In this study, a simple method was developed and validated to detect trace levels of benzaldehyde in injectable pharmaceutical formulations by solid-phase microextraction coupled with gas chromatography–flame ionization detector. Polyaniline was electrodeposited on a platinum wire in trifluoroacetic acid solvent by cyclic voltammetry technique. This fiber shows high thermal and mechanical stability and high performance in extraction of benzaldehyde. Extraction and desorption time and temperature, salt effect and gas chromatography parameters were optimized as key parameters. At the optimum conditions, the fiber shows good linearity between peak area ratio of benzaldehyde/3-chlorobenzaldehyde and benzaldehyde concentration in the range of 50–800 ng/mL with percent relative standard deviation values ranging from 0.75 to 8.64% (n 5 3). The limits of quantitation and detection were 50 and 16 ng/mL, respectively. The method has the requisite selectivity, sensitivity, accuracy and precision to assay benzaldehyde in injectable pharmaceutical dosage forms.
- Full Text:
- Date Issued: 2014
- Authors: Mohammadi, Ali , Mohammadi, Somayeh , Moghaddam, Bayandori A , Masoumi, Vahideh , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184120 , vital:44175 , xlink:href="https://doi.org/10.1093/chromsci/bmt152"
- Description: In this study, a simple method was developed and validated to detect trace levels of benzaldehyde in injectable pharmaceutical formulations by solid-phase microextraction coupled with gas chromatography–flame ionization detector. Polyaniline was electrodeposited on a platinum wire in trifluoroacetic acid solvent by cyclic voltammetry technique. This fiber shows high thermal and mechanical stability and high performance in extraction of benzaldehyde. Extraction and desorption time and temperature, salt effect and gas chromatography parameters were optimized as key parameters. At the optimum conditions, the fiber shows good linearity between peak area ratio of benzaldehyde/3-chlorobenzaldehyde and benzaldehyde concentration in the range of 50–800 ng/mL with percent relative standard deviation values ranging from 0.75 to 8.64% (n 5 3). The limits of quantitation and detection were 50 and 16 ng/mL, respectively. The method has the requisite selectivity, sensitivity, accuracy and precision to assay benzaldehyde in injectable pharmaceutical dosage forms.
- Full Text:
- Date Issued: 2014
Forced degradation studies of clobetasol 17‐propionate in methanol, propylene glycol, as bulk drug and cream formulations by RP‐HPLC
- Fauzee, Ayesha F, Walker, Roderick B
- Authors: Fauzee, Ayesha F , Walker, Roderick B
- Date: 2013
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184005 , vital:44154 , xlink:href="https://doi.org/10.1002/jssc.201200969"
- Description: A rapid, simple, stability-indicating forced degradation study of clobetasol 17-propionate was conducted using RP-HPLC. The method was used to analyze clobetasol 17-propionate in methanol, propylene glycol, and a cream formulation. Isocratic elution of clobetasol and its degradation products was achieved using a Nova-Pak® 4 μm C18 150 mm × 3.9 mm id cartridge column and a mobile phase of methanol: water (68:32 v/v) at a flow rate of 0.9 mL min−1. Quantitation was achieved with UV detection at 239 nm. Nondegraded clobetasol was eluted at a retention time of 6.0 min. Clobetasol 17-propionate was subjected to different stress conditions viz., acidic, basic, heat, oxidation, light, and neutral hydrolysis. The greatest degradation occurred under strong base and oxidative conditions. Strong base-degraded clobetasol produced additional peaks at retention times of 1.8, 4.0, 5.0, and 8.0 min and clobetasol oxidation degradation peaks eluted at 2.2 and 24 min. Complete validation was performed for linearity, accuracy, and precision over the concentration range 0.15–15 μg mL−1. All data were analyzed statistically and this RP-HPLC method proved to be accurate, precise, linear, and stability indicating for the quantitation of clobetasol 17-propionate in methanol, propylene glycol, and cream formulations.
- Full Text:
- Date Issued: 2013
- Authors: Fauzee, Ayesha F , Walker, Roderick B
- Date: 2013
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184005 , vital:44154 , xlink:href="https://doi.org/10.1002/jssc.201200969"
- Description: A rapid, simple, stability-indicating forced degradation study of clobetasol 17-propionate was conducted using RP-HPLC. The method was used to analyze clobetasol 17-propionate in methanol, propylene glycol, and a cream formulation. Isocratic elution of clobetasol and its degradation products was achieved using a Nova-Pak® 4 μm C18 150 mm × 3.9 mm id cartridge column and a mobile phase of methanol: water (68:32 v/v) at a flow rate of 0.9 mL min−1. Quantitation was achieved with UV detection at 239 nm. Nondegraded clobetasol was eluted at a retention time of 6.0 min. Clobetasol 17-propionate was subjected to different stress conditions viz., acidic, basic, heat, oxidation, light, and neutral hydrolysis. The greatest degradation occurred under strong base and oxidative conditions. Strong base-degraded clobetasol produced additional peaks at retention times of 1.8, 4.0, 5.0, and 8.0 min and clobetasol oxidation degradation peaks eluted at 2.2 and 24 min. Complete validation was performed for linearity, accuracy, and precision over the concentration range 0.15–15 μg mL−1. All data were analyzed statistically and this RP-HPLC method proved to be accurate, precise, linear, and stability indicating for the quantitation of clobetasol 17-propionate in methanol, propylene glycol, and cream formulations.
- Full Text:
- Date Issued: 2013
HPLC method for simultaneous analysis of ranitidine and metronidazole in dosage forms
- King'ori, Loti D, Walker, Roderick B
- Authors: King'ori, Loti D , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184790 , vital:44272 , xlink:href="https://doi.org/10.14233/ajchem.2014.15432"
- Description: A simple, rapid, precise and accurate stability indicating HPLC method for the simultaneous analysis of metronidazole and ranitidine in dosage forms has been developed and validated. Calibration curves for metronidazole and ranitidine exhibited linearity (R2 = 0.9995 for both compounds) over the concentration ranges investigated. The method was sensitive, selective and accurate for both compounds. Both drugs were found to be stable following acid hydrolysis studies. However, following alkali hydrolysis degradation of both compounds was observed. Furthermore metronidazole appeared to be stable following oxidative studies however ranitidine underwent complete degradation under these conditions. Both drugs were well resolved from the degradation products. The stability indicating chromatographic method has the necessary precision and accuracy for the simultaneous analysis of metronidazole and ranitidine in dosage forms.
- Full Text:
- Date Issued: 2014
- Authors: King'ori, Loti D , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184790 , vital:44272 , xlink:href="https://doi.org/10.14233/ajchem.2014.15432"
- Description: A simple, rapid, precise and accurate stability indicating HPLC method for the simultaneous analysis of metronidazole and ranitidine in dosage forms has been developed and validated. Calibration curves for metronidazole and ranitidine exhibited linearity (R2 = 0.9995 for both compounds) over the concentration ranges investigated. The method was sensitive, selective and accurate for both compounds. Both drugs were found to be stable following acid hydrolysis studies. However, following alkali hydrolysis degradation of both compounds was observed. Furthermore metronidazole appeared to be stable following oxidative studies however ranitidine underwent complete degradation under these conditions. Both drugs were well resolved from the degradation products. The stability indicating chromatographic method has the necessary precision and accuracy for the simultaneous analysis of metronidazole and ranitidine in dosage forms.
- Full Text:
- Date Issued: 2014
Enhancement of Biological and Pharmacological Properties of an Encapsulated Polyphenol: Curcumin
- Witika, Bwalya A, Makoni, Pedzisai A, Matafwali, Scott K, Mweetwa, Larry L, Shandele, Ginnethon C, Walker, Roderick B
- Authors: Witika, Bwalya A , Makoni, Pedzisai A , Matafwali, Scott K , Mweetwa, Larry L , Shandele, Ginnethon C , Walker, Roderick B
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183161 , vital:43917 , xlink:href="https://doi.org/10.3390/molecules26144244"
- Description: There is a dearth of natural remedies available for the treatment of an increasing number of diseases facing mankind. Natural products may provide an opportunity to produce formulations and therapeutic solutions to address this shortage. Curcumin (CUR), diferuloylmethane; I,7-bis-(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione is the major pigment in turmeric powder which has been reported to exhibit a number of health benefits including, antibacterial, antiviral, anti-cancer, anti-inflammatory and anti-oxidant properties. In this review, the authors attempt to highlight the biological and pharmacological properties of CUR in addition to emphasizing aspects relating to the biosynthesis, encapsulation and therapeutic effects of the compound. The information contained in this review was generated by considering published information in which evidence of enhanced biological and pharmacological properties of nano-encapsulated CUR was reported. CUR has contributed to a significant improvement in melanoma, breast, lung, gastro-intestinal, and genito-urinary cancer therapy. We highlight the impact of nano-encapsulated CUR for efficient inhibition of cell proliferation, even at low concentrations compared to the free CUR when considering anti-proliferation. Furthermore nano-encapsulated CUR exhibited bioactive properties, exerted cytotoxic and anti-oxidant effects by acting on endogenous and cholinergic anti-oxidant systems. CUR was reported to block Hepatitis C virus (HCV) entry into hepatic cells, inhibit MRSA proliferation, enhance wound healing and reduce bacterial load. Nano-encapsulated CUR has also shown bioactive properties when acting on antioxidant systems (endogenous and cholinergic). Future research is necessary and must focus on investigation of encapsulated CUR nano-particles in different models of human pathology.
- Full Text:
- Date Issued: 2021
- Authors: Witika, Bwalya A , Makoni, Pedzisai A , Matafwali, Scott K , Mweetwa, Larry L , Shandele, Ginnethon C , Walker, Roderick B
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183161 , vital:43917 , xlink:href="https://doi.org/10.3390/molecules26144244"
- Description: There is a dearth of natural remedies available for the treatment of an increasing number of diseases facing mankind. Natural products may provide an opportunity to produce formulations and therapeutic solutions to address this shortage. Curcumin (CUR), diferuloylmethane; I,7-bis-(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione is the major pigment in turmeric powder which has been reported to exhibit a number of health benefits including, antibacterial, antiviral, anti-cancer, anti-inflammatory and anti-oxidant properties. In this review, the authors attempt to highlight the biological and pharmacological properties of CUR in addition to emphasizing aspects relating to the biosynthesis, encapsulation and therapeutic effects of the compound. The information contained in this review was generated by considering published information in which evidence of enhanced biological and pharmacological properties of nano-encapsulated CUR was reported. CUR has contributed to a significant improvement in melanoma, breast, lung, gastro-intestinal, and genito-urinary cancer therapy. We highlight the impact of nano-encapsulated CUR for efficient inhibition of cell proliferation, even at low concentrations compared to the free CUR when considering anti-proliferation. Furthermore nano-encapsulated CUR exhibited bioactive properties, exerted cytotoxic and anti-oxidant effects by acting on endogenous and cholinergic anti-oxidant systems. CUR was reported to block Hepatitis C virus (HCV) entry into hepatic cells, inhibit MRSA proliferation, enhance wound healing and reduce bacterial load. Nano-encapsulated CUR has also shown bioactive properties when acting on antioxidant systems (endogenous and cholinergic). Future research is necessary and must focus on investigation of encapsulated CUR nano-particles in different models of human pathology.
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- Date Issued: 2021