Introduction: Enhancement of the dissolution rate and solubility of drugs by cocrystals (Cs) may be negatively affected by the manufacturing variables and storage conditions; therefore, the physical and chemical stability of the tablets should be assessed to ensure the maintenance of the Cs’ properties. Objective: The objective of the study was to formulate atorvastatin calcium-cocrystals (ATC-Cs) into tablets and investigate the effect of storage conditions on drug and quality of the developed tablets. Materials and Methods: Five tablet formulations (F1-F5) were developed by direct compression using ATC-Cs prepared by solvent drop grinding and solvent evaporation method using 1:3 drug-coformer molar ratio, using glucosamine and nicotinamide as coformers. The physicochemical properties of the ATC-Cs, their physical mixtures, and the raw ATC, before and after storage were studied by Fourier-transform infrared, differential scanning calorimetry, powder X-ray diffraction, gas chromatography-mass spectrometer, scanning electron microscopy, and dissolution rate. Results: ATC proved to be stable in the Cs and the formulated tablets at 25°C and 40°C ± 2°C/75 RH and the results, never the less after 6-months at 40°C, partial dissociation of the prepared Cs occurred due to the weak intermolecular hydrogen bonding between the drug and the coformers. The tablets exhibited an enhanced dissolution rate, similar to the innovator Lipitor® and showed satisfactory results complying with the pharmacopeial specifications. Conclusion: The developed ATC-Cs were successfully incorporated into tablets. The prepared tablets showed good quality attributes upon storage. Among all the tablet formulations, F4 was the best in terms of the pre-compression and post-compression parameters.
{"title":"Atorvastatin Cocrystals: Tablet Formulation and Stability","authors":"A. Nada","doi":"10.22377/ajp.v14i4.3825","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3825","url":null,"abstract":"Introduction: Enhancement of the dissolution rate and solubility of drugs by cocrystals (Cs) may be negatively affected by the manufacturing variables and storage conditions; therefore, the physical and chemical stability of the tablets should be assessed to ensure the maintenance of the Cs’ properties. Objective: The objective of the study was to formulate atorvastatin calcium-cocrystals (ATC-Cs) into tablets and investigate the effect of storage conditions on drug and quality of the developed tablets. Materials and Methods: Five tablet formulations (F1-F5) were developed by direct compression using ATC-Cs prepared by solvent drop grinding and solvent evaporation method using 1:3 drug-coformer molar ratio, using glucosamine and nicotinamide as coformers. The physicochemical properties of the ATC-Cs, their physical mixtures, and the raw ATC, before and after storage were studied by Fourier-transform infrared, differential scanning calorimetry, powder X-ray diffraction, gas chromatography-mass spectrometer, scanning electron microscopy, and dissolution rate. Results: ATC proved to be stable in the Cs and the formulated tablets at 25°C and 40°C ± 2°C/75 RH and the results, never the less after 6-months at 40°C, partial dissociation of the prepared Cs occurred due to the weak intermolecular hydrogen bonding between the drug and the coformers. The tablets exhibited an enhanced dissolution rate, similar to the innovator Lipitor® and showed satisfactory results complying with the pharmacopeial specifications. Conclusion: The developed ATC-Cs were successfully incorporated into tablets. The prepared tablets showed good quality attributes upon storage. Among all the tablet formulations, F4 was the best in terms of the pre-compression and post-compression parameters.","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":"47568472","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: In Saudi Arabia, over 154,000 people were infected with coronavirus disease (COVID-19). Unfortunately, until now, there are no vaccinations or effective drugs available, so only public health interventions such as physical distancing and hygiene measures in addition to targeted testing followed by isolation and quarantine measures are available. Objective: This study aims to describe the measures that are undertaken by Saudi population to avoid COVID-19 infection in Saudi Arabia. Methodology: This is a cross-sectional using internet-based survey. The survey was adapted from the previous study and from the WHO recommendations for COVID-19 prevention and control. The data included sociodemographic characteristics, level of attention, preventive measures taken by participants, and practice toward curbing the COVID-19 epidemic. Results: The majority of participants’ responded that their attention to the COVID-19 epidemics was very high to high (81.08%) while no one rated their attention at very low. To protect their families or friends, the respondents were mainly persuaded them to stay at home as much as possible (86%) and told them to avoid large gatherings (72.73%). Regarding the participants’ confidence in curbing the COVID-19 epidemic, about 73.47% of the participants were confident (strongly confident or confident). Conclusion: The public followed the hygiene recommendations of health authorities very well but still more education is still needed on some measures to prevent the spreading of the infection specially using the online education to enhance the public awareness about COVID-19.
{"title":"Measures undertaken to avoid COVID-19 Infection: Internet-based, Cross-Sectional Survey Study","authors":"N. Ahmed","doi":"10.22377/ajp.v14i4.3827","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3827","url":null,"abstract":"Introduction: In Saudi Arabia, over 154,000 people were infected with coronavirus disease (COVID-19). Unfortunately, until now, there are no vaccinations or effective drugs available, so only public health interventions such as physical distancing and hygiene measures in addition to targeted testing followed by isolation and quarantine measures are available. Objective: This study aims to describe the measures that are undertaken by Saudi population to avoid COVID-19 infection in Saudi Arabia. Methodology: This is a cross-sectional using internet-based survey. The survey was adapted from the previous study and from the WHO recommendations for COVID-19 prevention and control. The data included sociodemographic characteristics, level of attention, preventive measures taken by participants, and practice toward curbing the COVID-19 epidemic. Results: The majority of participants’ responded that their attention to the COVID-19 epidemics was very high to high (81.08%) while no one rated their attention at very low. To protect their families or friends, the respondents were mainly persuaded them to stay at home as much as possible (86%) and told them to avoid large gatherings (72.73%). Regarding the participants’ confidence in curbing the COVID-19 epidemic, about 73.47% of the participants were confident (strongly confident or confident). Conclusion: The public followed the hygiene recommendations of health authorities very well but still more education is still needed on some measures to prevent the spreading of the infection specially using the online education to enhance the public awareness about COVID-19.","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":"46152601","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 and Aim: Ischemic preconditioning (IPC) is a phenomenon in which brief episodes of ischemia protect the brain from subsequent, severe ischemic insult. This study evaluated whether the neuroprotective effect of cerebral IPC is mediated by nitric oxide synthase (NOS) inhibition, using non-selective NOS inhibitor, and N-Nitro- L-Arginine-Methylester (L-NAME). Materials and Methods: Fifty adult male Wistar rats divided into five groups ten in each: (1) Sham-operated group (control), (2) ischemia-reperfusion (I/R) group; rats subjected to 30 min of left common carotid artery (CCA) occlusion followed by 24-h of reperfusion, (3) I/R with NOS inhibition group; rats infused with L-NAME intraperitoneally 15 min before the same I/R period, (4) IPC group; rats treated with three 5-min episodes of CCA occlusion (CCAO) with 10 min of reperfusion between stimuli, then 30 min of CCAO followed by 24 h reperfusion, and (5) IPC with NOS inhibition group: Rats were subjected to the same preconditioning stimuli as Group 4 with the infusion of NOS inhibitor (L-NAME) 15 mg/kg, 15 min before CCAO. Neurological assessments were evaluated, enzyme-linked immunosorbent assay used to detect Rho-kinases (ROCK), and nitric oxide metabolites were measured colorimetrically. Results: IPC significantly reduces the neurological deficit and lowering the ROCK level with higher nitrite levels. While administration of L-NAME in IPC rats results in a significant enhancement in neurological scoring compared to IPC without NOS inhibition, with significant inhibition of nitrite and ROCK. Conclusion: Despite previous evidence that NO involves in neuroprotective mechanism of IPC, the current data suggest the potential ofL-NAME as a neuroprotective component of IPC.
{"title":"Role of N-Nitro-L-Arginine-Methylester in Neuroprotection of Cerebral Ischemic Preconditioning in Rats","authors":"Hiba A Awooda","doi":"10.22377/ajp.v14i4.3833","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3833","url":null,"abstract":"Background and Aim: Ischemic preconditioning (IPC) is a phenomenon in which brief episodes of ischemia protect the brain from subsequent, severe ischemic insult. This study evaluated whether the neuroprotective effect of cerebral IPC is mediated by nitric oxide synthase (NOS) inhibition, using non-selective NOS inhibitor, and N-Nitro- L-Arginine-Methylester (L-NAME). Materials and Methods: Fifty adult male Wistar rats divided into five groups ten in each: (1) Sham-operated group (control), (2) ischemia-reperfusion (I/R) group; rats subjected to 30 min of left common carotid artery (CCA) occlusion followed by 24-h of reperfusion, (3) I/R with NOS inhibition group; rats infused with L-NAME intraperitoneally 15 min before the same I/R period, (4) IPC group; rats treated with three 5-min episodes of CCA occlusion (CCAO) with 10 min of reperfusion between stimuli, then 30 min of CCAO followed by 24 h reperfusion, and (5) IPC with NOS inhibition group: Rats were subjected to the same preconditioning stimuli as Group 4 with the infusion of NOS inhibitor (L-NAME) 15 mg/kg, 15 min before CCAO. Neurological assessments were evaluated, enzyme-linked immunosorbent assay used to detect Rho-kinases (ROCK), and nitric oxide metabolites were measured colorimetrically. Results: IPC significantly reduces the neurological deficit and lowering the ROCK level with higher nitrite levels. While administration of L-NAME in IPC rats results in a significant enhancement in neurological scoring compared to IPC without NOS inhibition, with significant inhibition of nitrite and ROCK. Conclusion: Despite previous evidence that NO involves in neuroprotective mechanism of IPC, the current data suggest the potential ofL-NAME as a neuroprotective component of IPC.","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":"44233082","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}
Aim: The aim of the study was to develop gastroretentive floating pellets containing H2 –receptor antagonist, nizatidine which is primarily absorbed from stomach and has low oral bioavailability. Materials and Methods: The gastroretentive floating pellets of nizatidine were formulated using hydroxypropyl methylcellulose (HPMC) K100M and ethyl cellulose (EC) as sustained-release polymer, and NaHCO3 as a gas-forming agent. Pellets were prepared by extrusion–spheronization technique using microcrystalline cellulose as spheronizing agent. A 32 full factorial design was applied to investigate the effect of the two independent variables, that is, concentration of HPMC K100M (X1) and concentration of EC (X2) on the dependent variables, in vitro drug release at 1 h (Y1), in vitro drug release at 4 h (Y2), in vitro drug release at 8 h (Y3), and floating lag time (Y4). Results: The optimized formulation (F0) exhibits a floating lag time of around 70 ± 2 s and in vitro drug release of 99.89% at 12 h. The in vitro release of F1-F9 batches were found in between 99.87% and 84.43% at 12 h. Floating lag time of F1-F9 batches was found to be 36 ± 1 s–84 ± 3 s. Conclusion: HPMC K100 M and EC had a significant effect on floating lag time and in vitro drug release. Scanning electron microscope photomicrograph of pellets revealed that the surface was rough and the pellets were spherical shaped in nature. The in-vitro release kinetics revealed Korsmeyer-Peppas model is followed and drug release is by anomalous diffusion.
{"title":"Formulation and Evaluation of Gastroretentive Floating Pellets of Nizatidine","authors":"Keyur S. Patel","doi":"10.22377/ajp.v14i4.3818","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3818","url":null,"abstract":"Aim: The aim of the study was to develop gastroretentive floating pellets containing H2 –receptor antagonist, nizatidine which is primarily absorbed from stomach and has low oral bioavailability. Materials and Methods: The gastroretentive floating pellets of nizatidine were formulated using hydroxypropyl methylcellulose (HPMC) K100M and ethyl cellulose (EC) as sustained-release polymer, and NaHCO3 as a gas-forming agent. Pellets were prepared by extrusion–spheronization technique using microcrystalline cellulose as spheronizing agent. A 32 full factorial design was applied to investigate the effect of the two independent variables, that is, concentration of HPMC K100M (X1) and concentration of EC (X2) on the dependent variables, in vitro drug release at 1 h (Y1), in vitro drug release at 4 h (Y2), in vitro drug release at 8 h (Y3), and floating lag time (Y4). Results: The optimized formulation (F0) exhibits a floating lag time of around 70 ± 2 s and in vitro drug release of 99.89% at 12 h. The in vitro release of F1-F9 batches were found in between 99.87% and 84.43% at 12 h. Floating lag time of F1-F9 batches was found to be 36 ± 1 s–84 ± 3 s. Conclusion: HPMC K100 M and EC had a significant effect on floating lag time and in vitro drug release. Scanning electron microscope photomicrograph of pellets revealed that the surface was rough and the pellets were spherical shaped in nature. The in-vitro release kinetics revealed Korsmeyer-Peppas model is followed and drug release is by anomalous diffusion.","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":"42278308","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}
Aims: The present study focuses on a comparison between three voltammetric methods for enalapril assay in a pharmaceutical formulation, in addition to optimization of voltammetric analysis parameters such as working electrode and supporting electrolyte. Materials and Methods: Glassy carbon (GC) working electrode and KNO3 (1 M) supporting electrolyte exhibited the best performance compared to other working electrodes and supporting electrolytes used in this study. Results and Discussion: Voltammograms of enalapril exhibited two oxidization peaks at 1.4 V and 1.75 V. Square wave voltammetry (SWV) showed the lowest limit of detection (LOD) and limit of quantitation (LOQ) with values of 90.1 and 247 μg/mL LOD and LOQ, respectively. Furthermore, SWV exhibited the lowest relative standard deviation values of 2.33 and 3.87% for inter and intraday analysis, respectively. SWV showed high-performance in recovery study of commercially available enalapril tablets ANGIOTEC 20 mg® reach 99.06%. Conclusion: Accuracy, precession, and detection limit of SWV are the best for enalapril analysis compared to other methods in this study.
{"title":"Electrochemical Method Development for Enalapril Determination in a Pharmaceutical Formulation","authors":"A. Amro","doi":"10.22377/ajp.v14i4.3822","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3822","url":null,"abstract":"Aims: The present study focuses on a comparison between three voltammetric methods for enalapril assay in a pharmaceutical formulation, in addition to optimization of voltammetric analysis parameters such as working electrode and supporting electrolyte. Materials and Methods: Glassy carbon (GC) working electrode and KNO3 (1 M) supporting electrolyte exhibited the best performance compared to other working electrodes and supporting electrolytes used in this study. Results and Discussion: Voltammograms of enalapril exhibited two oxidization peaks at 1.4 V and 1.75 V. Square wave voltammetry (SWV) showed the lowest limit of detection (LOD) and limit of quantitation (LOQ) with values of 90.1 and 247 μg/mL LOD and LOQ, respectively. Furthermore, SWV exhibited the lowest relative standard deviation values of 2.33 and 3.87% for inter and intraday analysis, respectively. SWV showed high-performance in recovery study of commercially available enalapril tablets ANGIOTEC 20 mg® reach 99.06%. Conclusion: Accuracy, precession, and detection limit of SWV are the best for enalapril analysis compared to other methods in this study.","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":"46635062","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: In literature, fewer studies are evident that quality of life (QoL) among healthcare providers (HCPs) is a paramount concern, especially to have optimum and best patient care. If the QoL of the HCPs is not up to the satisfactory level, it will have a direct effect on QoL of their patients. Objective: This study aimed to determine socioeconomic determinants of QoL among HCPs in Malaysia. Materials and Methods: A cross-sectional study was conducted using among HCPs using World Health Organization QoL-BREF using a convenience sampling method. The socioeconomic determinants of QoL among HCPs were determined using descriptive and inferential statistics. Data were entered and analyzed using Statistical Package for the Social Sciences ver. 24.0. Results: Out of total (n = 310) studied HCPs, more females (n = 188, 60.6%), than males (n = 122, 39.4%) participated in this study. According to the study findings, in the psychological domain, marital status, in social domain marital status and job nature, and in environmental domain experience were observed as pure socioeconomic determinants that showed statistically significant values (P < 0.05). Conclusion: In Malaysia, overall, the HCPs had better QoL and had good access to excellent healthcare services, self-confidence, and social life.
{"title":"Evaluation of Socioeconomic Determinants of Quality of Life among Healthcare Providers","authors":"M. Iqbal","doi":"10.22377/ajp.v14i4.3836","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3836","url":null,"abstract":"Background: In literature, fewer studies are evident that quality of life (QoL) among healthcare providers (HCPs) is a paramount concern, especially to have optimum and best patient care. If the QoL of the HCPs is not up to the satisfactory level, it will have a direct effect on QoL of their patients. Objective: This study aimed to determine socioeconomic determinants of QoL among HCPs in Malaysia. Materials and Methods: A cross-sectional study was conducted using among HCPs using World Health Organization QoL-BREF using a convenience sampling method. The socioeconomic determinants of QoL among HCPs were determined using descriptive and inferential statistics. Data were entered and analyzed using Statistical Package for the Social Sciences ver. 24.0. Results: Out of total (n = 310) studied HCPs, more females (n = 188, 60.6%), than males (n = 122, 39.4%) participated in this study. According to the study findings, in the psychological domain, marital status, in social domain marital status and job nature, and in environmental domain experience were observed as pure socioeconomic determinants that showed statistically significant values (P < 0.05). Conclusion: In Malaysia, overall, the HCPs had better QoL and had good access to excellent healthcare services, self-confidence, and social life.","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":"46875217","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}
Aim: The objective of this study was to develop a novel self-nanoemulsifying drug delivery system which produced very small and uniform emulsion droplets, resulting in enhanced solubility, dissolution, and oral bioavailability of poorly water-soluble rosuvastatin calcium. Material and Methods: The effects of oil, surfactant, and cosurfactant on the drug solubility were assessed, and pseudoternary phase diagrams were plotted. Among the liquid SNEDDS formulations tested, the liquid SNEDDS composed of cinnamon oil (oil), Cremophor RH 40 (surfactant), and Transcutol P (cosurfactant) at a ratio of 1:5 (o/Smix), produced the smallest emulsion droplet size. The rosuvastatin-loaded liquid SNEDDS formulation was assessed for the emulsion droplet size, solubility, and dissolution of the emulsified SNEDDS and compared to the pure drug. Different SNEDDS formulations of rosuvastatin calcium were prepared by aqueous phase titration method. Prepared SNEDDS was filled in capsule shells as drugs with high solubility or low dose can be filled in capsule shell. Prepared SNEDDS was subjected to different thermodynamic stability tests. Thermodynamically stable SNEDDS was selected for self-nanoemulsification efficiency test. Selected formulations were characterized in terms of droplet size distribution, viscosity. Finally, selected SNEDDS (F1–F8) was subjected to in vitro dissolution/drug release studies. Results and Discussion: Droplet size and viscosity of formulation F6 were found to be lowest as compared to other formulations. The results of zeta potential indicated the formation of stable SNEDDS. In vitro drug release studies showed 97.7% release of drug from optimized formulation F6, where initial drug release profile of rosuvastatin calcium from optimized formulation F6 was found to be much faster than marketed rosuvastatin calcium capsule. Conclusion: Thus, this novel SNEDDS developed represents a potentially powerful oral delivery system for rosuvastatin calcium to enhance solubility and thereby bioavailability.
{"title":"SNEDDS in Shell: A Novel Approach to Enhance the Solubility of Rosuvastatin Calcium","authors":"Madhuri Desavathu","doi":"10.22377/ajp.v14i4.3816","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3816","url":null,"abstract":"Aim: The objective of this study was to develop a novel self-nanoemulsifying drug delivery system which produced very small and uniform emulsion droplets, resulting in enhanced solubility, dissolution, and oral bioavailability of poorly water-soluble rosuvastatin calcium. Material and Methods: The effects of oil, surfactant, and cosurfactant on the drug solubility were assessed, and pseudoternary phase diagrams were plotted. Among the liquid SNEDDS formulations tested, the liquid SNEDDS composed of cinnamon oil (oil), Cremophor RH 40 (surfactant), and Transcutol P (cosurfactant) at a ratio of 1:5 (o/Smix), produced the smallest emulsion droplet size. The rosuvastatin-loaded liquid SNEDDS formulation was assessed for the emulsion droplet size, solubility, and dissolution of the emulsified SNEDDS and compared to the pure drug. Different SNEDDS formulations of rosuvastatin calcium were prepared by aqueous phase titration method. Prepared SNEDDS was filled in capsule shells as drugs with high solubility or low dose can be filled in capsule shell. Prepared SNEDDS was subjected to different thermodynamic stability tests. Thermodynamically stable SNEDDS was selected for self-nanoemulsification efficiency test. Selected formulations were characterized in terms of droplet size distribution, viscosity. Finally, selected SNEDDS (F1–F8) was subjected to in vitro dissolution/drug release studies. Results and Discussion: Droplet size and viscosity of formulation F6 were found to be lowest as compared to other formulations. The results of zeta potential indicated the formation of stable SNEDDS. In vitro drug release studies showed 97.7% release of drug from optimized formulation F6, where initial drug release profile of rosuvastatin calcium from optimized formulation F6 was found to be much faster than marketed rosuvastatin calcium capsule. Conclusion: Thus, this novel SNEDDS developed represents a potentially powerful oral delivery system for rosuvastatin calcium to enhance solubility and thereby bioavailability.","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":"44312672","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 evaluate drug utilization pattern among stroke patients. Materials and Methods: A cross-sectional study was conducted among 96 stroke patients aged from 30 to 92 years in a hospital in Malaysia. A total of 88 patients were available for descriptive analysis and logistic regression analysis. Descriptive and logistic regression analyses were performed. Results: On average, patients were aged 67.62 years (standard deviation of 13.14) and had a higher incidence in Malay ethnicity (42.7%). Ischemic stroke accounts for 91.67% of the study, with a slightly higher proportion of female patients (51.04%). Majority of stroke patient complaint generalized body weakness as their major symptom (19.81%). Calcium channel blocker was found to be the most used antihypertensive agent among stroke patients (40.9%) followed by angiotensin-converting enzyme inhibitors (ACEIs) (31.8%). Conclusion: Using logistic regression modeling, it was determined that the factors of a subject would affect the choice of prescribing of ACEIs and anticoagulant drugs.
{"title":"Drug Utilization Pattern among Stroke Patients – A Cross-sectional Insight","authors":"M. Iqbal","doi":"10.22377/ajp.v14i4.3826","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3826","url":null,"abstract":"Objective: This study aimed to evaluate drug utilization pattern among stroke patients. Materials and Methods: A cross-sectional study was conducted among 96 stroke patients aged from 30 to 92 years in a hospital in Malaysia. A total of 88 patients were available for descriptive analysis and logistic regression analysis. Descriptive and logistic regression analyses were performed. Results: On average, patients were aged 67.62 years (standard deviation of 13.14) and had a higher incidence in Malay ethnicity (42.7%). Ischemic stroke accounts for 91.67% of the study, with a slightly higher proportion of female patients (51.04%). Majority of stroke patient complaint generalized body weakness as their major symptom (19.81%). Calcium channel blocker was found to be the most used antihypertensive agent among stroke patients (40.9%) followed by angiotensin-converting enzyme inhibitors (ACEIs) (31.8%). Conclusion: Using logistic regression modeling, it was determined that the factors of a subject would affect the choice of prescribing of ACEIs and anticoagulant 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":"43870641","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: Poor solubility and dissolution of drugs are major hindering factors in the development of their oral dosage forms with acceptable bioavailability. Of the various approaches, employing amorphous form of drugs is frequently utilized to develop drug products. Inclusion complexation is widely employed to prepare stable and fast dissolving forms of drug compounds. Objective: The objective of this work was to characterize the inclusion complexes of a poorly soluble drug loratadine prepared by employing sulfobutyl ether beta-cyclodextrin (SBE7-β-CD) in the presence or absence of water-soluble polymers. The investigation aims to find out the effect of water-soluble polymers on complexation efficiency and enhanced dissolution of the ternary complexes (TC). Materials and Methods: Binary and ternary inclusion complexes of loratadine in SBE7-β-CD were prepared by freeze drying method. TC were prepared using gelucire (50/13) and soluplus as the auxiliary hydrophilic polymers and formulated as tablets. The prepared complexes are evaluated by X-ray diffraction, differential scanning calorimetry, Fourier-transform infrared, and dissolution study. Results: X-ray diffraction and DSC studies confirmed that inclusion complexation converted crystalline loratadine into an amorphous form enhancing its dissolution. Gelucire and soluplus were effective in promoting dissolution and forming complexes of higher efficiency at a low concentration of 0.3% w/v and 0.6%w/v, respectively. The formulated tablets of inclusion complexes exhibited satisfactory pharmaceutical properties. Conclusion: Employing ternary inclusion complexes prepared by utilizing gelucire (50/13) and soluplus is a promising approach to develop fast dissolving formulations of poorly soluble drugs such as loratadine.
{"title":"Characterization of Sulfobutyl Ether Beta-cyclodextrin Binary and Ternary Inclusion Complexes of Loratadine","authors":"K. Ramesh","doi":"10.22377/ajp.v14i4.3832","DOIUrl":"https://doi.org/10.22377/ajp.v14i4.3832","url":null,"abstract":"Background: Poor solubility and dissolution of drugs are major hindering factors in the development of their oral dosage forms with acceptable bioavailability. Of the various approaches, employing amorphous form of drugs is frequently utilized to develop drug products. Inclusion complexation is widely employed to prepare stable and fast dissolving forms of drug compounds. Objective: The objective of this work was to characterize the inclusion complexes of a poorly soluble drug loratadine prepared by employing sulfobutyl ether beta-cyclodextrin (SBE7-β-CD) in the presence or absence of water-soluble polymers. The investigation aims to find out the effect of water-soluble polymers on complexation efficiency and enhanced dissolution of the ternary complexes (TC). Materials and Methods: Binary and ternary inclusion complexes of loratadine in SBE7-β-CD were prepared by freeze drying method. TC were prepared using gelucire (50/13) and soluplus as the auxiliary hydrophilic polymers and formulated as tablets. The prepared complexes are evaluated by X-ray diffraction, differential scanning calorimetry, Fourier-transform infrared, and dissolution study. Results: X-ray diffraction and DSC studies confirmed that inclusion complexation converted crystalline loratadine into an amorphous form enhancing its dissolution. Gelucire and soluplus were effective in promoting dissolution and forming complexes of higher efficiency at a low concentration of 0.3% w/v and 0.6%w/v, respectively. The formulated tablets of inclusion complexes exhibited satisfactory pharmaceutical properties. Conclusion: Employing ternary inclusion complexes prepared by utilizing gelucire (50/13) and soluplus is a promising approach to develop fast dissolving formulations of poorly soluble drugs such as loratadine.","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":"48599037","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}
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