Aims: This research work was about biorelevant dissolution method development for fluvoxamine extended-release capsule by correlating preprandial and postprandial in vivo performance. Materials and Methods: The mean plasma concentration profile obtained after oral administration of extended-release capsules was deconvoluted using Wagner-Nelson deconvolution technique, to achieve percentage fraction of drug absorbed, and target dissolution profile was derived. Biorelevant dissolution method was developed using USP Apparatus-3, with dissolution media simulating gastrointestinal tract sink condition. A full factorial design of experiment was carried out for optimizing dissolution volume and dips per minutes, to achieve target dissolution profile. Results: The dissolution results observed using office of generic drugs recommend dissolution method were not comparable with target dissolution profile and observed with F2 value of 37 at preprandial and 43 at postprandial condition. The achieved dissolution profile was comparable with target and observed with F2 value of 81 at preprandial condition and 85 at postprandial condition. Conclusion: The developed dissolution method establishes good correlation between in vitro drug release and in vivo drug absorption and observed with R2 value of 0.998 at preprandial condition and 0.997 at postprandial condition. The method gives the advantage of giving biowaiver.
{"title":"A Predictive In vitro Biorelevant Dissolution Method Development for Fluvoxamine Extended-Release Capsules by Simulating Preprandial and Postprandial In vivo Performance","authors":"Devi Thamizhanban","doi":"10.22377/ajp.v14i4.3820","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3820","url":null,"abstract":"Aims: This research work was about biorelevant dissolution method development for fluvoxamine extended-release capsule by correlating preprandial and postprandial in vivo performance. Materials and Methods: The mean plasma concentration profile obtained after oral administration of extended-release capsules was deconvoluted using Wagner-Nelson deconvolution technique, to achieve percentage fraction of drug absorbed, and target dissolution profile was derived. Biorelevant dissolution method was developed using USP Apparatus-3, with dissolution media simulating gastrointestinal tract sink condition. A full factorial design of experiment was carried out for optimizing dissolution volume and dips per minutes, to achieve target dissolution profile. Results: The dissolution results observed using office of generic drugs recommend dissolution method were not comparable with target dissolution profile and observed with F2 value of 37 at preprandial and 43 at postprandial condition. The achieved dissolution profile was comparable with target and observed with F2 value of 81 at preprandial condition and 85 at postprandial condition. Conclusion: The developed dissolution method establishes good correlation between in vitro drug release and in vivo drug absorption and observed with R2 value of 0.998 at preprandial condition and 0.997 at postprandial condition. The method gives the advantage of giving biowaiver.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45923192","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Background: Lumefantrine is a well-known antimalarial drug that has proven to be effective even against the multidrug-resistant Plasmodium sp. Although it is very effective, the shelf life of the drug is very short and is highly hydrophobic, hence, the drug has to be administered along with fat. Lumefantrine is also known for its undesired side effects that are overlooked in case of untreatable (drug resistant) malarial infections. Methodology: In this study, structure-based computational drug development approach was performed on lumefantrine structure to improve the biological properties using OSIRIS property explorer software. A total of 25 ligand molecules were designed that exhibited better Absorption, Distribution, Metabolism, Excretion, Toxicity (ADMET) properties. Results: A total of 20 drug targets were chosen and docked with lumefantrine to identify its potential target. Lumefantrine demonstrated significant affinity toward falcipain-3 protein with a free binding energy of −10.92 Kcal/mol and inhibition constant of 9.94 nM, suggesting that falcipain-3 is the potential drug target of lumefantrine. Among the 25 designed ligands with improved ADMET properties, ligand-107 demonstrated 100-fold higher affinity toward falcipain-3 with a free binding energy of −14.26 Kcal/mol and inhibition constant of 35.11 pM. Based on this improved affinity to inhibit falcipain-3 and based on improved ADMET properties of ligand-107, it was concluded to be the most effective variant of lumefantrine in this study. Conclusion: The result of the study could be greatly useful to pharmaceutical industries to develop an efficient antimalarial drug.
{"title":"Designing of Ligand-107 an Effective Variant of Antimalarial Drug Lumefantrine through Structure-Based Computer-Aided Drug Development Approach","authors":"L. Ravi","doi":"10.22377/ajp.v14i4.3819","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3819","url":null,"abstract":"Background: Lumefantrine is a well-known antimalarial drug that has proven to be effective even against the multidrug-resistant Plasmodium sp. Although it is very effective, the shelf life of the drug is very short and is highly hydrophobic, hence, the drug has to be administered along with fat. Lumefantrine is also known for its undesired side effects that are overlooked in case of untreatable (drug resistant) malarial infections. Methodology: In this study, structure-based computational drug development approach was performed on lumefantrine structure to improve the biological properties using OSIRIS property explorer software. A total of 25 ligand molecules were designed that exhibited better Absorption, Distribution, Metabolism, Excretion, Toxicity (ADMET) properties. Results: A total of 20 drug targets were chosen and docked with lumefantrine to identify its potential target. Lumefantrine demonstrated significant affinity toward falcipain-3 protein with a free binding energy of −10.92 Kcal/mol and inhibition constant of 9.94 nM, suggesting that falcipain-3 is the potential drug target of lumefantrine. Among the 25 designed ligands with improved ADMET properties, ligand-107 demonstrated 100-fold higher affinity toward falcipain-3 with a free binding energy of −14.26 Kcal/mol and inhibition constant of 35.11 pM. Based on this improved affinity to inhibit falcipain-3 and based on improved ADMET properties of ligand-107, it was concluded to be the most effective variant of lumefantrine in this study. Conclusion: The result of the study could be greatly useful to pharmaceutical industries to develop an efficient antimalarial drug.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44935254","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Objectives: Ionic gelation-based polyelectrolyte complexes of blend chitosan-sodium alginate polysaccharides based microbeads of methotrexate were prepared by dual cross-linkages with divalent Ca2+ and SO4 -2 ions for colon targeting. Materials and Methods: Those developed dual cross-linked formulations were characterized for particle size, entrapment studies, drug content, swelling degree, etc. Results: The surface morphology results showed that the optimized formulations were semi-spherical and rough-surfaced. The in vitro drug release carried out in various simulated fluids at various pH had shown lesser release profiles in acidic media as compared to alkaline media at the end of 24 h studies. A significant drug release (P > 0.05) was observed in colonic fluids containing 2 and 4% w/v rat cecal as compared with control. In vivo targeting ability for the colon-specific region was established through gamma scintigraphic imaging technique. Differential scanning calorimetry and X-ray diffraction analysis further confirms for semi-crystalline and complete cross-linking state. The release profile and mathematical kinetic modeling revealed for anomalous non-Fickian type formulations were best fitted with Higuchi and Hixson-Crowell model, respectively. Conclusion: It can be concluded that the optimized formulations may be effective for colon targeting and promising to achieve drug targeting for colorectal cancer.
{"title":"“Drug Release Kinetic Modeling and Gamma Scintigraphic Studies of Dual Ca2+ and SO4 2- Cross-linked Microbeads for Colon Specific Targeting”","authors":"S. Lanjhiyana","doi":"10.22377/ajp.v14i4.3835","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3835","url":null,"abstract":"Objectives: Ionic gelation-based polyelectrolyte complexes of blend chitosan-sodium alginate polysaccharides based microbeads of methotrexate were prepared by dual cross-linkages with divalent Ca2+ and SO4 -2 ions for colon targeting. Materials and Methods: Those developed dual cross-linked formulations were characterized for particle size, entrapment studies, drug content, swelling degree, etc. Results: The surface morphology results showed that the optimized formulations were semi-spherical and rough-surfaced. The in vitro drug release carried out in various simulated fluids at various pH had shown lesser release profiles in acidic media as compared to alkaline media at the end of 24 h studies. A significant drug release (P > 0.05) was observed in colonic fluids containing 2 and 4% w/v rat cecal as compared with control. In vivo targeting ability for the colon-specific region was established through gamma scintigraphic imaging technique. Differential scanning calorimetry and X-ray diffraction analysis further confirms for semi-crystalline and complete cross-linking state. The release profile and mathematical kinetic modeling revealed for anomalous non-Fickian type formulations were best fitted with Higuchi and Hixson-Crowell model, respectively. Conclusion: It can be concluded that the optimized formulations may be effective for colon targeting and promising to achieve drug targeting for colorectal cancer.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44442439","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Introduction: Cardiovascular diseases are a very significant sociomedical problem in all countries of the world. Proper therapy of cardiovascular diseases, as well as their timely prevention, is one of the most important conditions for increasing life expectancy and maintaining quality of life. One of the most effective ways to achieve this goal is the timely detection and proper treatment of hypertension. Doctors note that in diseases such as stroke, coronary heart disease, including myocardial infarction, and heart and kidney failure, their level may be reduced as a result of adequate antihypertensive therapy. This is especially important for Ukraine, where the incidence of cardiovascular disease is increasing every year. Recently, along with the expansion of opportunities in the treatment of hypertension, there is enough information about the effectiveness of drugs that lower blood pressure. Materials and Methods: Methods such as questionnaires of patients (content analysis of case histories) were used. Data processing was performed using statistical and mathematical methods and graphical analysis. Results: There were some patterns of lowering blood pressure in patients on the background of monotherapy of hypertension and patients following the doctor’s instructions for treatment. Discussion and Conclusion: As a result of the study, it was found that most patients follow the recommendations of doctors on the appointment of antihypertensive drugs.
{"title":"Comparison and Subjective Evaluation of Safety and Efficacy of Antihypertensive Drugs from the Group Angiotensin-Converting Enzyme and Diuretics","authors":"Sakhanda Ivanna","doi":"10.22377/ajp.v14i4.3829","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3829","url":null,"abstract":"Introduction: Cardiovascular diseases are a very significant sociomedical problem in all countries of the world. Proper therapy of cardiovascular diseases, as well as their timely prevention, is one of the most important conditions for increasing life expectancy and maintaining quality of life. One of the most effective ways to achieve this goal is the timely detection and proper treatment of hypertension. Doctors note that in diseases such as stroke, coronary heart disease, including myocardial infarction, and heart and kidney failure, their level may be reduced as a result of adequate antihypertensive therapy. This is especially important for Ukraine, where the incidence of cardiovascular disease is increasing every year. Recently, along with the expansion of opportunities in the treatment of hypertension, there is enough information about the effectiveness of drugs that lower blood pressure. Materials and Methods: Methods such as questionnaires of patients (content analysis of case histories) were used. Data processing was performed using statistical and mathematical methods and graphical analysis. Results: There were some patterns of lowering blood pressure in patients on the background of monotherapy of hypertension and patients following the doctor’s instructions for treatment. Discussion and Conclusion: As a result of the study, it was found that most patients follow the recommendations of doctors on the appointment of antihypertensive drugs.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43983086","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Objective: This current study objective is to develop cefuroxime axetil (CA) nasal mucoadhesive microspheres for an alternative utilization of dosage form for respiratory tract infections Materials and Methods: CA microspheres were prepared by modified emulsion-lyophilization method in which chitosan and beta-cyclodextrin were used as a release retardant polymer. The model is optimization by 24 factorial designs and validated using ANOVA. CA microspheres evaluated for entrapment efficiency, ex vivo mucoadhesion and % drug release. The optimized formulations were performed for its Fourier transform infrared (FT-IR) analysis, particle size and polydispersity index (PDI) and zeta potential, thermal analysis DSC and XRD, and surface morphology by scanning electron microscopy followed by in vitro and ex vivo release kinetic studies. Key Findings: Results of these evaluations showed that entrapment efficiency was found to be 69.21–80.45%, particle size in the range of 12.55–17.22 μm, mucoadhesion in the range of 72.51–79.68%, and drug release in the range of 72.21–83.65%. FT-IR studies ensured that no drug-polymer interaction in the formulated microspheres. PDI and zeta potential were measured and the mean particle size and distribution of microspheres were in the range and the surface topography revealed a spherical surface for all the formulations and a round cavity enclosed by an outer shell composed of the drug and polymer. DSC and XRD were found to be in fairly acceptable and in vitro and ex vivo release profile of microspheres formulation was found to be 80.25 and 76.28% at the end of 6 h. Stability studies for 6 months revealed that the optimized formulation was stable, no changes in physical appearance. Conclusion: Finally, it was concluded that the nasal microspheres of CA may have potential enough for effective drug delivery
{"title":"Formulation Development, Characterization, and Evaluation of Controlled Nasal Drug Delivery Systems for Cefuroxime Axetil","authors":"S. Rajarajan","doi":"10.22377/AJP.V14I4.3830","DOIUrl":"https://doi.org/10.22377/AJP.V14I4.3830","url":null,"abstract":"Objective: This current study objective is to develop cefuroxime axetil (CA) nasal mucoadhesive microspheres for an alternative utilization of dosage form for respiratory tract infections Materials and Methods: CA microspheres were prepared by modified emulsion-lyophilization method in which chitosan and beta-cyclodextrin were used as a release retardant polymer. The model is optimization by 24 factorial designs and validated using ANOVA. CA microspheres evaluated for entrapment efficiency, ex vivo mucoadhesion and % drug release. The optimized formulations were performed for its Fourier transform infrared (FT-IR) analysis, particle size and polydispersity index (PDI) and zeta potential, thermal analysis DSC and XRD, and surface morphology by scanning electron microscopy followed by in vitro and ex vivo release kinetic studies. Key Findings: Results of these evaluations showed that entrapment efficiency was found to be 69.21–80.45%, particle size in the range of 12.55–17.22 μm, mucoadhesion in the range of 72.51–79.68%, and drug release in the range of 72.21–83.65%. FT-IR studies ensured that no drug-polymer interaction in the formulated microspheres. PDI and zeta potential were measured and the mean particle size and distribution of microspheres were in the range and the surface topography revealed a spherical surface for all the formulations and a round cavity enclosed by an outer shell composed of the drug and polymer. DSC and XRD were found to be in fairly acceptable and in vitro and ex vivo release profile of microspheres formulation was found to be 80.25 and 76.28% at the end of 6 h. Stability studies for 6 months revealed that the optimized formulation was stable, no changes in physical appearance. Conclusion: Finally, it was concluded that the nasal microspheres of CA may have potential enough for effective drug delivery","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":"26 6","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41268800","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Objective: The objective of the study was to study the surgical management of inguinal hernia (groin hernia) among geriatric (elderly) patients. Materials and Methods: A retrospective study was conducted from December 2016 to August 2018 in the surgical ward of a university hospital in Malaysia. Geriatric patients operated for surgery during the study period were recruited in the study. A total of 116 cases operated for groin hernia with or without comorbidities and their influence on the overall results of surgical interventions were studied. Results: The mean age of the patients was 71.02 ± 3.1 years, of whom 94 (81%) were male and 22 (19%) were female. In 66 (56.9%) patients, the hernias were simple, while 21 (18.1%) had an obstructive inguinal hernia. In 17 (14.7%) patients, the hernia was incarcerated while 12 cases presented had strangulations. Comorbidities were present in 97 (83.6%) patients. No mortality was found either in elective or in emergency surgery. Conclusion: Comorbidities, type of surgery (elective or emergency), type of hernia (simple or complicated), and age of the patients can make surgery more challenging in the geriatric population.
{"title":"Geriatric Inguinal Hernia and its Surgical Management – Findings From a Retrospective Study","authors":"M. S. Iqbal","doi":"10.22377/AJP.V14I4.3821","DOIUrl":"https://doi.org/10.22377/AJP.V14I4.3821","url":null,"abstract":"Objective: The objective of the study was to study the surgical management of inguinal hernia (groin hernia) among geriatric (elderly) patients. Materials and Methods: A retrospective study was conducted from December 2016 to August 2018 in the surgical ward of a university hospital in Malaysia. Geriatric patients operated for surgery during the study period were recruited in the study. A total of 116 cases operated for groin hernia with or without comorbidities and their influence on the overall results of surgical interventions were studied. Results: The mean age of the patients was 71.02 ± 3.1 years, of whom 94 (81%) were male and 22 (19%) were female. In 66 (56.9%) patients, the hernias were simple, while 21 (18.1%) had an obstructive inguinal hernia. In 17 (14.7%) patients, the hernia was incarcerated while 12 cases presented had strangulations. Comorbidities were present in 97 (83.6%) patients. No mortality was found either in elective or in emergency surgery. Conclusion: Comorbidities, type of surgery (elective or emergency), type of hernia (simple or complicated), and age of the patients can make surgery more challenging in the geriatric population.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46264710","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Objective: Darunavir ethanolate is the last United States Food and Drug Administration approved protease inhibitor (PI). The drug is used along with other PIs (ritonavir/cobicistat) for the effective management of human immunodeficiency virus (HIV) HIV-1 infection. Darunavir ethanolate exerts its action by binding noncompetitively to HIV protease enzyme. The main objective of the present research work was to develop a new profound and novel reverse-phase high-performance liquid chromatography (RP-HPLC) for the estimation of darunavir ethanolate. Methods: As per the guidelines of the Food and Drug Administration and International Council for harmonization, the method was validated. The HPLC analysis was performed on the waters 2695 equipped with symmetry C18 column 3.5 μm, 150 mm × 4.6 mm, with a mixture of acetonitrile:0.1% phosphate buffer (50:50 V/V) as the mobile phase, at the flow rate of 1 ml/min. The total run time was 5 min and the detection was performed at the wavelength (λ) of 262 nm. Results: The retention time for darunavir ethanolate was found to be 2.269 min. The standard curves were obtained with R2 0.9997 and linear at the concentration range of 8–120 μg/ml. The limit of quantitation and limit of detection for darunavir ethanolate were found to be 0.08 μg/ml and 0.8 μg/ml, respectively. The method’s accuracy was tested by percentage recovery tests and found to be 100.3%. The results obtained were within the accepted standards for linearity, accuracy, precision, specificity, and robustness. Conclusion: The proposed RP-HPLC method can be applied for the routine analytical estimation of darunavir ethanolate in bulk and tablet formulations.
{"title":"A New Validated RP-HPLC Method for the Estimation of Darunavir Ethanolate in Bulk and Tablets","authors":"A. Kavitha","doi":"10.22377/ajp.v14i4.3834","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3834","url":null,"abstract":"Objective: Darunavir ethanolate is the last United States Food and Drug Administration approved protease inhibitor (PI). The drug is used along with other PIs (ritonavir/cobicistat) for the effective management of human immunodeficiency virus (HIV) HIV-1 infection. Darunavir ethanolate exerts its action by binding noncompetitively to HIV protease enzyme. The main objective of the present research work was to develop a new profound and novel reverse-phase high-performance liquid chromatography (RP-HPLC) for the estimation of darunavir ethanolate. Methods: As per the guidelines of the Food and Drug Administration and International Council for harmonization, the method was validated. The HPLC analysis was performed on the waters 2695 equipped with symmetry C18 column 3.5 μm, 150 mm × 4.6 mm, with a mixture of acetonitrile:0.1% phosphate buffer (50:50 V/V) as the mobile phase, at the flow rate of 1 ml/min. The total run time was 5 min and the detection was performed at the wavelength (λ) of 262 nm. Results: The retention time for darunavir ethanolate was found to be 2.269 min. The standard curves were obtained with R2 0.9997 and linear at the concentration range of 8–120 μg/ml. The limit of quantitation and limit of detection for darunavir ethanolate were found to be 0.08 μg/ml and 0.8 μg/ml, respectively. The method’s accuracy was tested by percentage recovery tests and found to be 100.3%. The results obtained were within the accepted standards for linearity, accuracy, precision, specificity, and robustness. Conclusion: The proposed RP-HPLC method can be applied for the routine analytical estimation of darunavir ethanolate in bulk and tablet formulations.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49166145","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Introduction: The present research work was intended to develop and optimize transdermal matrix patch of clozapine using Box–Behnken experimental design (Box–Behnken design [BBD]) for improved bioavailability as compared to oral formulation. The 3-factor, 3-level BBD was employed to investigate the combined influence of formulation variables on flux, tensile strength (TS), and in vitro drug release. The generated polynomial equation was validated and desirability function was utilized for optimization. Materials and Methods: Optimized formulation evaluated for physicochemical characterization, Fourier transform infrared, differential scanning calorimetry, in vitro drug release, permeability enhancement potential by ex vivo, skin irritation, and in vivo pharmacokinetics and stability studies. Results: The results of the optimized formulation (F15) showed TS of 6.84 ± 0.64 MPa, flux of 104.80 ± 1.39 (μg/h/cm2), and % drug release after 20 h (Q20) of 82.19 ± 1.12% which was stable up to 6 months in accelerated condition. Observed and the predicted values of the responses were found to be in good agreement. Optimized transdermal patch of clozapine found free from skin irritation as per Draize score method. The pharmacokinetic result had shown the bioavailability of clozapine improved about 2.18-fold after transdermal drug delivery when compared with oral marketed formulation. Discussion and Conclusion: The results of the study revealed that the developed transdermal patch of clozapine can be a promising alternative which provides effective management of schizophrenia in terms of improved patient compliance.
{"title":"Formulation, Optimization, and In vivo Evaluation of Clozapine Loaded Transdermal Drug Delivery System for the Treatment of Schizophrenia","authors":"Mayur M. Patel","doi":"10.22377/ajp.v14i4.3823","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3823","url":null,"abstract":"Introduction: The present research work was intended to develop and optimize transdermal matrix patch of clozapine using Box–Behnken experimental design (Box–Behnken design [BBD]) for improved bioavailability as compared to oral formulation. The 3-factor, 3-level BBD was employed to investigate the combined influence of formulation variables on flux, tensile strength (TS), and in vitro drug release. The generated polynomial equation was validated and desirability function was utilized for optimization. Materials and Methods: Optimized formulation evaluated for physicochemical characterization, Fourier transform infrared, differential scanning calorimetry, in vitro drug release, permeability enhancement potential by ex vivo, skin irritation, and in vivo pharmacokinetics and stability studies. Results: The results of the optimized formulation (F15) showed TS of 6.84 ± 0.64 MPa, flux of 104.80 ± 1.39 (μg/h/cm2), and % drug release after 20 h (Q20) of 82.19 ± 1.12% which was stable up to 6 months in accelerated condition. Observed and the predicted values of the responses were found to be in good agreement. Optimized transdermal patch of clozapine found free from skin irritation as per Draize score method. The pharmacokinetic result had shown the bioavailability of clozapine improved about 2.18-fold after transdermal drug delivery when compared with oral marketed formulation. Discussion and Conclusion: The results of the study revealed that the developed transdermal patch of clozapine can be a promising alternative which provides effective management of schizophrenia in terms of improved patient compliance.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46942961","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Objective: This study aimed to measure the impact of diabetes mellitus (DM) on patients’ quality of life (QoL). Materials and Methods: This cross-sectional study involved DM patients that underwent follow-up at a hospital in central Malaysia. Data were collected using self-developed and self-administered questionnaire. Statistical analysis was performed using Statistical Package for the Social Sciences version 24. Results: Around 75 (56.8%) of the patients were satisfied with their daily routine life activities. A total of 88 (66.7%) were also satisfied with their family and friends’ relationships. On the contrary, 109 (82.6%) were not satisfied with their sexual life. There was a statistically significant correlation observed between age and QoL. Conclusion: This study showed that the majority of DM patients had moderate QoL. Diet, living conditions, and concerns about the future had also a greater influence on their overall QoL.
{"title":"The Impact of Diabetes Mellitus on Patients’ Quality of Life","authors":"M. Iqbal","doi":"10.22377/ajp.v14i4.3831","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3831","url":null,"abstract":"Objective: This study aimed to measure the impact of diabetes mellitus (DM) on patients’ quality of life (QoL). Materials and Methods: This cross-sectional study involved DM patients that underwent follow-up at a hospital in central Malaysia. Data were collected using self-developed and self-administered questionnaire. Statistical analysis was performed using Statistical Package for the Social Sciences version 24. Results: Around 75 (56.8%) of the patients were satisfied with their daily routine life activities. A total of 88 (66.7%) were also satisfied with their family and friends’ relationships. On the contrary, 109 (82.6%) were not satisfied with their sexual life. There was a statistically significant correlation observed between age and QoL. Conclusion: This study showed that the majority of DM patients had moderate QoL. Diet, living conditions, and concerns about the future had also a greater influence on their overall QoL.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43385151","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-09-18DOI: 10.22377/AJP.V14I03.3757
M. Iqbal
Objective: The current study aimed to evaluate practicing pharmacists’ awareness and perceptions about biosimilars in Saudi Arabia. Materials and Methods: A cross-sectional study was performed using a prevalidated and self-administered research tool by convenience sampling method. Registered pharmacists were approached to participate in the study. Descriptive and inferential statistics were performed using the Statistical Package for the Social Sciences version 24.0. P 60%) had good awareness and positive perception toward biosimilars. Conclusion: This study concluded an appropriate awareness and positive perception toward biosimilars among pharmacists in Saudi Arabia. Statistically non-significant association regarding biosimilars’ perception and awareness was observed between male and female pharmacists.
{"title":"Pharmacists’ Awareness and Perceptions of Biosimilars in Saudi Arabia","authors":"M. Iqbal","doi":"10.22377/AJP.V14I03.3757","DOIUrl":"https://doi.org/10.22377/AJP.V14I03.3757","url":null,"abstract":"Objective: The current study aimed to evaluate practicing pharmacists’ awareness and perceptions about biosimilars in Saudi Arabia. Materials and Methods: A cross-sectional study was performed using a prevalidated and self-administered research tool by convenience sampling method. Registered pharmacists were approached to participate in the study. Descriptive and inferential statistics were performed using the Statistical Package for the Social Sciences version 24.0. P 60%) had good awareness and positive perception toward biosimilars. Conclusion: This study concluded an appropriate awareness and positive perception toward biosimilars among pharmacists in Saudi Arabia. Statistically non-significant association regarding biosimilars’ perception and awareness was observed between male and female pharmacists.","PeriodicalId":8489,"journal":{"name":"Asian Journal of Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2020-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45188269","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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