Pub Date : 2023-09-01DOI: 10.22159/ijpps.2023v15i9.47781
E. OFORI-ATTAH, Abigail Aning, Andrew Gordon, R. Appiah-Opong
Objective: Nitric oxide (NO) is a signaling molecule that plays a key role in the pathogenesis of inflammation. Inhibitors of NO may be useful candidates for the treatment of inflammatory diseases. The study aimed to determine the antioxidant and inhibitory effect of commonly used Ghanaian vegetables, namely Corchorus olitorius (CO), Solanum melongena (SM), Solanum torvum (ST), Xanthosoma sagittifolia (XS) and Abelmoschus esculentus (AE) on NO expression in a Lipopolysaccharide (LPS)-induced RAW 264.7 macrophage cell line. Methods: The cytotoxic effects of the vegetables on the cell line were determined using a tetrazolium-based colorimetric assay. The inflammatory activity was determined by measuring the inhibition of NO production in LPS-induced RAW 264.7 macrophage cells. Total antioxidant activity, total phenolic, flavonoid, and reduced glutathione contents were evaluated using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay, Folin-Ciocalteu, aluminium chloride, and O-Phthalaldehyde methods, respectively. Results: Our results showed that CO and ST significantly inhibited NO production in a concentration-dependent manner with good cell viability. Solanum torvum also exhibited strong antioxidant activity (IC50= 0.466±0.23 mg/ml) with total phenolic content of 230.73±1.84 mg/g GAE, while CO showed high flavonoid content (291.45±2.14 mg/g QUE). Abelmoschus esculentus recorded the highest glutathione content (58.6 µg/g GSH. Saponins, alkaloids, tannins, terpenoids, and cardiac glycosides were present in all the samples except SM and AE, which lacked terpenoids. Conclusion: These findings suggest that CO and ST possess anti-inflammatory and antioxidant activities that could be explored as potential therapeutic remedies for inflammatory disorders.
{"title":"ANTIOXIDANT AND INHIBITORY EFFECT OF SELECTED GHANAIAN VEGETABLES ON NITRIC OXIDE EXPRESSION IN LIPOPOLYSACCHARIDE-INDUCED MACROPHAGE CELLS","authors":"E. OFORI-ATTAH, Abigail Aning, Andrew Gordon, R. Appiah-Opong","doi":"10.22159/ijpps.2023v15i9.47781","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i9.47781","url":null,"abstract":"Objective: Nitric oxide (NO) is a signaling molecule that plays a key role in the pathogenesis of inflammation. Inhibitors of NO may be useful candidates for the treatment of inflammatory diseases. The study aimed to determine the antioxidant and inhibitory effect of commonly used Ghanaian vegetables, namely Corchorus olitorius (CO), Solanum melongena (SM), Solanum torvum (ST), Xanthosoma sagittifolia (XS) and Abelmoschus esculentus (AE) on NO expression in a Lipopolysaccharide (LPS)-induced RAW 264.7 macrophage cell line.\u0000Methods: The cytotoxic effects of the vegetables on the cell line were determined using a tetrazolium-based colorimetric assay. The inflammatory activity was determined by measuring the inhibition of NO production in LPS-induced RAW 264.7 macrophage cells. Total antioxidant activity, total phenolic, flavonoid, and reduced glutathione contents were evaluated using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay, Folin-Ciocalteu, aluminium chloride, and O-Phthalaldehyde methods, respectively.\u0000Results: Our results showed that CO and ST significantly inhibited NO production in a concentration-dependent manner with good cell viability. Solanum torvum also exhibited strong antioxidant activity (IC50= 0.466±0.23 mg/ml) with total phenolic content of 230.73±1.84 mg/g GAE, while CO showed high flavonoid content (291.45±2.14 mg/g QUE). Abelmoschus esculentus recorded the highest glutathione content (58.6 µg/g GSH. Saponins, alkaloids, tannins, terpenoids, and cardiac glycosides were present in all the samples except SM and AE, which lacked terpenoids.\u0000Conclusion: These findings suggest that CO and ST possess anti-inflammatory and antioxidant activities that could be explored as potential therapeutic remedies for inflammatory disorders.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"30 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84871100","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 : 2023-08-01DOI: 10.22159/ijpps.2023v15i8.48355
M. Damle, Jay A. Sonule
Objective: Simple, rapid RP-HPLC and HPTLC methods have been developed in order to study the degradation of Roxadustat under various stress conditions. The Kinetics of hydrolytic degradation is studied. Methods: Optimum separation of Roxadustat and its degradation products was achieved using the following conditions in HPLC, Agilent eclipse XDB-C8 (150×4.6 mm) column, the mobile phase was composed of methanol: phosphate buffer (pH 5, 0.05 M) (70:30 v/v) with UV detection at 262 nm. The flow rate was at 1.0 ml/min. The RT was 4.6±0.02 min. HPTLC work for Roxadustat was performed on Aluminium plates precoated with silica gel 60 F254, (10 cm × 10 cm with 250 μm layer thickness). The mobile phase was composed of Toulene: Ethyl Acetate: Glacial acetic acid (5:5:0.5 v/v/v) and then scanned. The system was found to give a compact spot for Roxadustat (Rf value of 0.58±0.02). Results: In HPLC the calibration curves plotted were found to be linear over the concentration range of 2.5-25μg/ml, with a correlation coefficient of R2=0.9994. In HPTLC the calibration curves plotted were found to be linear over the concentration range of 500-2500 ng/band, with a regression coefficient of R2=0.9957. The analytical performance of the proposed methods was validated as per ICH Q2 (R1) guidelines. The degradant peaks were well resolved from the Roxadustat peak. Significant degradation was observed in acid hydrolysis, alkali hydrolysis, and oxidative degradation. The drug is relatively stable towards photolysis, neutral hydrolysis, and thermal conditions. Conclusion: In the current work, simple RP-HPLC and HPTLC analytical methods for the determination of Roxadustat in the presence of its degradation products have been developed. The information presented herein could be very useful while developing formulation procedures to prevent hydrolytic degradation. It can be used as a routine quality control test.
{"title":"HYDROLYTIC DEGRADATION STUDY OF ROXADUSTAT BY RP-HPLC AND HPTLC","authors":"M. Damle, Jay A. Sonule","doi":"10.22159/ijpps.2023v15i8.48355","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i8.48355","url":null,"abstract":"Objective: Simple, rapid RP-HPLC and HPTLC methods have been developed in order to study the degradation of Roxadustat under various stress conditions. The Kinetics of hydrolytic degradation is studied.\u0000Methods: Optimum separation of Roxadustat and its degradation products was achieved using the following conditions in HPLC, Agilent eclipse XDB-C8 (150×4.6 mm) column, the mobile phase was composed of methanol: phosphate buffer (pH 5, 0.05 M) (70:30 v/v) with UV detection at 262 nm. The flow rate was at 1.0 ml/min. The RT was 4.6±0.02 min. HPTLC work for Roxadustat was performed on Aluminium plates precoated with silica gel 60 F254, (10 cm × 10 cm with 250 μm layer thickness). The mobile phase was composed of Toulene: Ethyl Acetate: Glacial acetic acid (5:5:0.5 v/v/v) and then scanned. The system was found to give a compact spot for Roxadustat (Rf value of 0.58±0.02).\u0000Results: In HPLC the calibration curves plotted were found to be linear over the concentration range of 2.5-25μg/ml, with a correlation coefficient of R2=0.9994. In HPTLC the calibration curves plotted were found to be linear over the concentration range of 500-2500 ng/band, with a regression coefficient of R2=0.9957. The analytical performance of the proposed methods was validated as per ICH Q2 (R1) guidelines. The degradant peaks were well resolved from the Roxadustat peak. Significant degradation was observed in acid hydrolysis, alkali hydrolysis, and oxidative degradation. The drug is relatively stable towards photolysis, neutral hydrolysis, and thermal conditions.\u0000Conclusion: In the current work, simple RP-HPLC and HPTLC analytical methods for the determination of Roxadustat in the presence of its degradation products have been developed. The information presented herein could be very useful while developing formulation procedures to prevent hydrolytic degradation. It can be used as a routine quality control test.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"42 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91469006","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 : 2023-08-01DOI: 10.22159/ijpps.2023v15i8.48573
Abdul Mannan, Mohammed Fahad, Faizah Ayesha Amjad, Juveria Fatima
Intrathecal drug delivery systems (IDDS) have emerged as a valuable treatment option for patients with chronic pain who have failed to achieve adequate relief with conventional therapies. These systems provide targeted delivery of medications directly to the cerebrospinal fluid, resulting in improved pain control and reduced systemic side effects. However, the use of IDDS is not without potential complications and considerations that must be addressed to ensure optimal patient outcomes. This comprehensive review examines the various complications associated with IDDS and the considerations that healthcare providers and patients need to be aware of. Surgical complications, such as infection, bleeding, spinal fluid leaks, and nerve damage, are discussed, along with strategies to minimize these risks. Device malfunctions, including pump failure, catheter issues, and electronic problems, are explored, highlighting the importance of regular monitoring and maintenance. Medication-related side effects, such as nausea, sedation, and respiratory depression, are addressed, emphasizing the need for close monitoring and appropriate dosage adjustments. Long-term considerations, including tolerance to medication, physical dependence, and withdrawal symptoms, are also examined, emphasizing the significance of gradual tapering and proper discontinuation protocols. The review underscores the importance of regular follow-up appointments to assess the system's functionality, medication dosages, and patient response to treatment. By proactively managing and addressing complications, healthcare providers can optimize pain relief and minimize adverse effects, ensuring the long-term effectiveness and safety of IDDS.
{"title":"CURRENT ADVANCEMENTS AND COMPLICATIONS IN INTRATHECAL DRUG DELIVERY SYSTEM","authors":"Abdul Mannan, Mohammed Fahad, Faizah Ayesha Amjad, Juveria Fatima","doi":"10.22159/ijpps.2023v15i8.48573","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i8.48573","url":null,"abstract":"Intrathecal drug delivery systems (IDDS) have emerged as a valuable treatment option for patients with chronic pain who have failed to achieve adequate relief with conventional therapies. These systems provide targeted delivery of medications directly to the cerebrospinal fluid, resulting in improved pain control and reduced systemic side effects. However, the use of IDDS is not without potential complications and considerations that must be addressed to ensure optimal patient outcomes. This comprehensive review examines the various complications associated with IDDS and the considerations that healthcare providers and patients need to be aware of. Surgical complications, such as infection, bleeding, spinal fluid leaks, and nerve damage, are discussed, along with strategies to minimize these risks. Device malfunctions, including pump failure, catheter issues, and electronic problems, are explored, highlighting the importance of regular monitoring and maintenance. Medication-related side effects, such as nausea, sedation, and respiratory depression, are addressed, emphasizing the need for close monitoring and appropriate dosage adjustments. Long-term considerations, including tolerance to medication, physical dependence, and withdrawal symptoms, are also examined, emphasizing the significance of gradual tapering and proper discontinuation protocols. The review underscores the importance of regular follow-up appointments to assess the system's functionality, medication dosages, and patient response to treatment. By proactively managing and addressing complications, healthcare providers can optimize pain relief and minimize adverse effects, ensuring the long-term effectiveness and safety of IDDS.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81036474","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 : 2023-08-01DOI: 10.22159/ijpps.2023v15i8.48035
Ayefounin Ogoubi, Kodjo Selom Evenamede, K. Kpegba, Oudjaniyobi Simalou, A. Agbonon
Objective: Faced with the devastating effect of diabetes, the search for new natural antidiabetic molecules is an exploratory avenue. Methods: In this study, the leaves of Flacourtia indica were collected from the Togolese flora, and their antioxidant activity was evaluated using DPPH and FRAP assays, following a phytochemical screening conducted through colorimetric and precipitation reactions. The content of total phenols was determined using Folin-Ciocalteu's reagent and flavonoids by aluminum trichloride. The antibacterial activity of the extracts was evaluated using the method of dilution in agar wells with Muller-Hinton® agar. Additionally, the extracts' antidiabetic effect was evaluated in rats made diabetic by alloxan at a dose of 120 mg/kg. b.w. Results: The results of our work showed the presence of flavonoids, tannins, anthocyanins, and saponins in the extracts. The best polyphenol and flavonoid contents were measured in the hydroethanolic extract and were 186.46±0.308 mg EqAG/g and 464.14±17.043 mgEqQ/g. ES respectively. The hydroethanolic extract has a higher antioxidant power with an IC50 = 110.22 µg/ml. The reducing powers of the ferric ions were 3706±12.124 and 3777±9.238 µmol/ml, respectively for the hydroethanolic and aqueous extracts. The extracts were active against Staphylococcus aureus and are bacteriostatic. The hydroethanolic extract of the leaves of Flacourtia indica significantly reduced (p = 0.0014) blood glucose levels in diabetic rats. Conclusion: This plant can therefore be a potential medicine in the treatment of diabetes.
{"title":"PHYTOCHEMICAL STUDY AND ANTIOXIDANT, ANTIBACTERIAL AND ANTIDIABETIC ACTIVITIES OF FLACOURTIA INDICA LEAVES EXTRACTS FROM THE TOGOLESE FLORA","authors":"Ayefounin Ogoubi, Kodjo Selom Evenamede, K. Kpegba, Oudjaniyobi Simalou, A. Agbonon","doi":"10.22159/ijpps.2023v15i8.48035","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i8.48035","url":null,"abstract":"Objective: Faced with the devastating effect of diabetes, the search for new natural antidiabetic molecules is an exploratory avenue.\u0000Methods: In this study, the leaves of Flacourtia indica were collected from the Togolese flora, and their antioxidant activity was evaluated using DPPH and FRAP assays, following a phytochemical screening conducted through colorimetric and precipitation reactions. The content of total phenols was determined using Folin-Ciocalteu's reagent and flavonoids by aluminum trichloride. The antibacterial activity of the extracts was evaluated using the method of dilution in agar wells with Muller-Hinton® agar. Additionally, the extracts' antidiabetic effect was evaluated in rats made diabetic by alloxan at a dose of 120 mg/kg. b.w.\u0000Results: The results of our work showed the presence of flavonoids, tannins, anthocyanins, and saponins in the extracts. The best polyphenol and flavonoid contents were measured in the hydroethanolic extract and were 186.46±0.308 mg EqAG/g and 464.14±17.043 mgEqQ/g. ES respectively. The hydroethanolic extract has a higher antioxidant power with an IC50 = 110.22 µg/ml. The reducing powers of the ferric ions were 3706±12.124 and 3777±9.238 µmol/ml, respectively for the hydroethanolic and aqueous extracts. The extracts were active against Staphylococcus aureus and are bacteriostatic. The hydroethanolic extract of the leaves of Flacourtia indica significantly reduced (p = 0.0014) blood glucose levels in diabetic rats.\u0000Conclusion: This plant can therefore be a potential medicine in the treatment of diabetes.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"81 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86219168","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 : 2023-08-01DOI: 10.22159/ijpps.2023v15i8.48403
Deepika Badkur, Suchita Singh
Objective: To assess immunization coverage in up to 23 mo old children with respect to economic status and Knowledge, Attitude and Practice of mothers regarding immunization. Methods: A cross-sectional study was conducted, including 125 mothers who had children aged grouped between 0-23 mo from 7 fully functional anganwadis. The data was collected using a semi-structured questionnaire and analyzed using Microsoft Excel. The chi-square test/Fisher exact test was applied, and results were presented in the form of tables. Findings were compared against standards and/or findings from similar studies and discussed. Results: Immunization coverage was found to be 79%. Almost 85% of mothers believe that the vaccine prevents communicable diseases, and 82.4% agree that immunization at birth is important. The majority of mothers (92%) agreed that their children should be vaccinated as soon as possible. Related to the attitude of mothers towards immunization, a maximum (93.6%) percent of mothers believed that even a healthy child should be fully immunized for protection from diseases, and 86% had no fear related to vaccinating their child. More than half (72.8%) of mothers informed that they would contact anganwadi workers for the next dose of vaccine. Almost 62% of mothers agreed to breastfeed their children after an oral vaccine, and 87.2% of mothers said that they would take their children for regular vaccination. No association (P>0.05) was found between the child’s immunization status and the socioeconomic status of the family. Conclusion: The study concludes immunization coverage is 79% and there is a positive attitude towards immunization, but less knowledge is related to the age appropriate vaccine. So services focusing on immunization education and provision need to be improved.
{"title":"A CROSS-SECTIONAL STUDY TO ASSESS IMMUNIZATION COVERAGE AND KNOWLEDGE, ATTITUDE and PRACTICE OF MOTHERS REGARDING IMMUNIZATION IN SEEPAT BILASPUR","authors":"Deepika Badkur, Suchita Singh","doi":"10.22159/ijpps.2023v15i8.48403","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i8.48403","url":null,"abstract":"Objective: To assess immunization coverage in up to 23 mo old children with respect to economic status and Knowledge, Attitude and Practice of mothers regarding immunization.\u0000Methods: A cross-sectional study was conducted, including 125 mothers who had children aged grouped between 0-23 mo from 7 fully functional anganwadis. The data was collected using a semi-structured questionnaire and analyzed using Microsoft Excel. The chi-square test/Fisher exact test was applied, and results were presented in the form of tables. Findings were compared against standards and/or findings from similar studies and discussed.\u0000Results: Immunization coverage was found to be 79%. Almost 85% of mothers believe that the vaccine prevents communicable diseases, and 82.4% agree that immunization at birth is important. The majority of mothers (92%) agreed that their children should be vaccinated as soon as possible. Related to the attitude of mothers towards immunization, a maximum (93.6%) percent of mothers believed that even a healthy child should be fully immunized for protection from diseases, and 86% had no fear related to vaccinating their child. More than half (72.8%) of mothers informed that they would contact anganwadi workers for the next dose of vaccine. Almost 62% of mothers agreed to breastfeed their children after an oral vaccine, and 87.2% of mothers said that they would take their children for regular vaccination. No association (P>0.05) was found between the child’s immunization status and the socioeconomic status of the family.\u0000Conclusion: The study concludes immunization coverage is 79% and there is a positive attitude towards immunization, but less knowledge is related to the age appropriate vaccine. So services focusing on immunization education and provision need to be improved.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"25 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83309353","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 : 2023-08-01DOI: 10.22159/ijpps.2023v15i8.48526
Madhurita Chakrabarti
Objective: This study focuses on designing potential antimicrobial agents, evaluating their binding affinity against target proteins, and assessing their Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) properties using computational methods. Methods: This study employed six target proteins from the Research Collaboratory for Structural Bioinformatics Protein Data Bank (RCSB PDB) and utilized Biovia Discovery Studio 2021 for their preparation. Marvin Sketch is used to draw the ten potential candidates and subjected to molecular docking using Python Prescription (PyRx) software. The Biovia Discovery Studio 2021 was used to visualize the docking outcomes, and ADMET properties were determined using Swiss ADME software. Results: Docking experiments conducted on ten derivatives against six protein targets, specifically Sortase-A, Clumping factor A, Undecaprenyl diphosphate synthase, Dehydrosqualene synthase, Tyrosyl tRNA synthetase, and Dihydrofolate reductase. Out of the ten derivatives, compounds 1, 2, 3, 5, and 7 demonstrated a significant binding affinity for one or two target proteins. Notably, compound 8 exhibited exceptional docking scores against five of the six protein targets, establishing itself as the most potent ligand among the compounds tested. These results highlight the paramount significance of compound 8 for subsequent investigation. Furthermore, comprehensive documentation of the physicochemical properties of the potent derivatives was carried out. Conclusion: The findings indicate that the examined compounds have the potential to effectively inhibit various microbial protein targets. In silico ADMET studies suggest that these compounds possess desirable drug-like properties. Therefore, these compounds hold promise as lead molecules for further research, potentially leading to the development of novel antimicrobial drugs.
目的:设计潜在的抗菌药物，评估其与靶蛋白的结合亲和力，并利用计算方法评估其吸收、分布、代谢、排泄和毒性(ADMET)特性。方法:本研究采用结构生物信息学蛋白质数据库(RCSB PDB)研究合作实验室的6种靶蛋白，利用Biovia Discovery Studio 2021进行制备。使用Marvin Sketch绘制10个潜在候选分子，并使用Python Prescription (PyRx)软件进行分子对接。Biovia Discovery Studio 2021用于可视化对接结果，并使用瑞士ADME软件确定ADMET特性。结果:针对Sortase-A、结块因子A、十一烯丙烯二磷酸合成酶、脱氢角鲨烯合成酶、酪氨酸tRNA合成酶、二氢叶酸还原酶等6个蛋白靶点进行了10个衍生物的对接实验。在10个衍生物中，化合物1、2、3、5和7对一个或两个靶蛋白具有显著的结合亲和力。值得注意的是，化合物8对6个蛋白靶点中的5个表现出特殊的对接得分，在测试的化合物中确立了自己最有效的配体。这些结果突出了化合物8对后续研究的重要意义。此外，对有效衍生物的物理化学性质进行了全面的记录。结论:所获化合物具有有效抑制多种微生物蛋白靶点的潜力。计算机ADMET研究表明，这些化合物具有理想的药物样特性。因此，这些化合物有望成为进一步研究的先导分子，可能导致新型抗菌药物的开发。
{"title":"REVOLUTIONIZING ANTIMICROBIAL DRUG DISCOVERY: COMPUTATIONAL DESIGN AND ADMET STUDIES OF EMERGING POTENT ANTI-MICROBIAL AGENTS","authors":"Madhurita Chakrabarti","doi":"10.22159/ijpps.2023v15i8.48526","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i8.48526","url":null,"abstract":"Objective: This study focuses on designing potential antimicrobial agents, evaluating their binding affinity against target proteins, and assessing their Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) properties using computational methods.\u0000Methods: This study employed six target proteins from the Research Collaboratory for Structural Bioinformatics Protein Data Bank (RCSB PDB) and utilized Biovia Discovery Studio 2021 for their preparation. Marvin Sketch is used to draw the ten potential candidates and subjected to molecular docking using Python Prescription (PyRx) software. The Biovia Discovery Studio 2021 was used to visualize the docking outcomes, and ADMET properties were determined using Swiss ADME software.\u0000Results: Docking experiments conducted on ten derivatives against six protein targets, specifically Sortase-A, Clumping factor A, Undecaprenyl diphosphate synthase, Dehydrosqualene synthase, Tyrosyl tRNA synthetase, and Dihydrofolate reductase. Out of the ten derivatives, compounds 1, 2, 3, 5, and 7 demonstrated a significant binding affinity for one or two target proteins. Notably, compound 8 exhibited exceptional docking scores against five of the six protein targets, establishing itself as the most potent ligand among the compounds tested. These results highlight the paramount significance of compound 8 for subsequent investigation. Furthermore, comprehensive documentation of the physicochemical properties of the potent derivatives was carried out.\u0000Conclusion: The findings indicate that the examined compounds have the potential to effectively inhibit various microbial protein targets. In silico ADMET studies suggest that these compounds possess desirable drug-like properties. Therefore, these compounds hold promise as lead molecules for further research, potentially leading to the development of novel antimicrobial drugs.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89307381","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 : 2023-08-01DOI: 10.22159/ijpps.2023v15i8.47750
H. Nair, Gaayathri Gadhiraju, Gundeti Sunny
Objective: The objective of the present work was to develop an orodispersible tablet of loratadine, an orally active, non-sedating anti-histaminic, belonging to BCS Class II. The drug was prepared as a solid dispersion using Soluplus® as carrier and formulated into an optimal tablet using Design of Experiments. Methods: Solid dispersions of loratadine with varying ratios of Soluplus® were prepared by solvent evaporation and subjected to solubility study in simulated salivary fluid. Selected composition was characterized by differential scanning calorimetry and X-ray diffraction and formulated into an orodispersible tablet by direct compression after addition of suitable excipients. DOE based on a full factorial design was used to optimize the product using a trial version of JMP software, so as to obtain a tablet with low friability, rapid disintegration and maximal drug dissolution within 5 min. The optimized tablet was prepared and evaluated for several attributes, including in vivo disintegration and palatability. Results: A solid dispersion prepared with a 1: 4 ratio of loratadine: Soluplus® was found to show a 130-fold increase in drug solubility in the simulated salivary fluid. X-ray diffraction revealed loratadine in amorphous form. The exercise using DOE for optimization of the orodispersible tablet formula served to balance the proportion of crospovidone as super disintegrant and PVP as dry binder and yielded a formulation with good mechanical strength, rapid in vitro disintegration (39 sec) and dissolution of 93.78% of the drug within 5 min. When evaluated in vivo, the tablets were found to disintegrate in about 60 secs and were reported to be palatable. Conclusion: A patient-friendly dosage form containing a highly soluble form of loratadine was prepared and could be of potential benefit in offering quick relief from allergic conditions.
{"title":"DEVELOPMENT OF ORODISPERSIBLE TABLETS OF LORATADINE CONTAINING AN AMORPHOUS SOLID DISPERSION OF THE DRUG IN SOLUPLUS® USING DESIGN OF EXPERIMENTS","authors":"H. Nair, Gaayathri Gadhiraju, Gundeti Sunny","doi":"10.22159/ijpps.2023v15i8.47750","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i8.47750","url":null,"abstract":"Objective: The objective of the present work was to develop an orodispersible tablet of loratadine, an orally active, non-sedating anti-histaminic, belonging to BCS Class II. The drug was prepared as a solid dispersion using Soluplus® as carrier and formulated into an optimal tablet using Design of Experiments.\u0000Methods: Solid dispersions of loratadine with varying ratios of Soluplus® were prepared by solvent evaporation and subjected to solubility study in simulated salivary fluid. Selected composition was characterized by differential scanning calorimetry and X-ray diffraction and formulated into an orodispersible tablet by direct compression after addition of suitable excipients. DOE based on a full factorial design was used to optimize the product using a trial version of JMP software, so as to obtain a tablet with low friability, rapid disintegration and maximal drug dissolution within 5 min. The optimized tablet was prepared and evaluated for several attributes, including in vivo disintegration and palatability.\u0000Results: A solid dispersion prepared with a 1: 4 ratio of loratadine: Soluplus® was found to show a 130-fold increase in drug solubility in the simulated salivary fluid. X-ray diffraction revealed loratadine in amorphous form. The exercise using DOE for optimization of the orodispersible tablet formula served to balance the proportion of crospovidone as super disintegrant and PVP as dry binder and yielded a formulation with good mechanical strength, rapid in vitro disintegration (39 sec) and dissolution of 93.78% of the drug within 5 min. When evaluated in vivo, the tablets were found to disintegrate in about 60 secs and were reported to be palatable.\u0000Conclusion: A patient-friendly dosage form containing a highly soluble form of loratadine was prepared and could be of potential benefit in offering quick relief from allergic conditions.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"54 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88401960","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 : 2023-08-01DOI: 10.22159/ijpps.2023v15i8.48216
E. Ayogu, C. Anosike, Stephen Ikechukwu Azumara, Desmond NNIA ANI
Objective: The objective of the study was to determine the prevalence of asymptomatic malaria and anaemia among primary school children in Enugu State, Nigeria. Methods: This research was a quantitative cross-sectional survey conducted among children in 8 primary schools in Nsukka, Enugu State, Nigeria. Asymptomatic children aged 5 to 13 were randomly selected and screened for malaria parasitemia and anaemia. The presence of malaria parasites in the blood sample was detected using the rapid diagnostic test (RDT) kit. At the same time, haemoglobin concentration was measured using a portable Mission® Plus Hemoglobin (Hb) Testing kit. The clinical status of the children was obtained from a self-administered questionnaire completed by their parents or guardians. Descriptive statistics and the Chi-square test were used for data analysis. Results: The prevalence of asymptomatic malaria and anaemia was 24.1% and 45.8%, respectively. The school-age children with both asymptomatic malaria and anaemia were 13.7%. The prevalence of asymptomatic malaria was significantly associated with asymptomatic anaemia (p = 0.013). Sleeping under insecticide-treated nets was significantly associated with a lower prevalence of asymptomatic malaria (p = 0.024) and anaemia (p = 0.015). Conclusion: The study revealed a high burden of asymptomatic malaria and anaemia among primary school children in Nsukka. This study, thus, underscores the need for robust implementation of malaria and anaemia screening, prevention, and treatment programmes in this population.
{"title":"PREVALENCE OF ASYMPTOMATIC MALARIA AND ANEMIA AMONG PRIMARY SCHOOL CHILDREN IN ENUGU STATE, NIGERIA","authors":"E. Ayogu, C. Anosike, Stephen Ikechukwu Azumara, Desmond NNIA ANI","doi":"10.22159/ijpps.2023v15i8.48216","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i8.48216","url":null,"abstract":"Objective: The objective of the study was to determine the prevalence of asymptomatic malaria and anaemia among primary school children in Enugu State, Nigeria.\u0000Methods: This research was a quantitative cross-sectional survey conducted among children in 8 primary schools in Nsukka, Enugu State, Nigeria. Asymptomatic children aged 5 to 13 were randomly selected and screened for malaria parasitemia and anaemia. The presence of malaria parasites in the blood sample was detected using the rapid diagnostic test (RDT) kit. At the same time, haemoglobin concentration was measured using a portable Mission® Plus Hemoglobin (Hb) Testing kit. The clinical status of the children was obtained from a self-administered questionnaire completed by their parents or guardians. Descriptive statistics and the Chi-square test were used for data analysis. \u0000Results: The prevalence of asymptomatic malaria and anaemia was 24.1% and 45.8%, respectively. The school-age children with both asymptomatic malaria and anaemia were 13.7%. The prevalence of asymptomatic malaria was significantly associated with asymptomatic anaemia (p = 0.013). Sleeping under insecticide-treated nets was significantly associated with a lower prevalence of asymptomatic malaria (p = 0.024) and anaemia (p = 0.015). \u0000Conclusion: The study revealed a high burden of asymptomatic malaria and anaemia among primary school children in Nsukka. This study, thus, underscores the need for robust implementation of malaria and anaemia screening, prevention, and treatment programmes in this population.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74980872","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 : 2023-08-01DOI: 10.22159/ijpps.2023v15i8.48552
Case Study, Guna Gouru, B. Sneha, T. Prasad
Hematohidrosis is a rare clinical condition in which an individual sweats blood. Even though there are several causes, such as systemic diseases, vicarious menstruation, extreme physical activity, psychogenic reasons, and idiopathic causes, acute fear and intensive mental pondering are the most frequent. Bloody perspiration, bloody tears (Hemoclaria), bleeding from the nose, bleeding from the ears (Otorrhoea), and leaking blood from various skin surfaces are all indications and symptoms of this condition. Here, we present a case of hematohidrosis in a 9y old female child with bleeding for two months from her forehead, nose, ear, and vagina, who responded to propranolol.
{"title":"HEMATOHIDROSIS-A RARE BLEEDING PHENOMENON","authors":"Case Study, Guna Gouru, B. Sneha, T. Prasad","doi":"10.22159/ijpps.2023v15i8.48552","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i8.48552","url":null,"abstract":"Hematohidrosis is a rare clinical condition in which an individual sweats blood. Even though there are several causes, such as systemic diseases, vicarious menstruation, extreme physical activity, psychogenic reasons, and idiopathic causes, acute fear and intensive mental pondering are the most frequent. Bloody perspiration, bloody tears (Hemoclaria), bleeding from the nose, bleeding from the ears (Otorrhoea), and leaking blood from various skin surfaces are all indications and symptoms of this condition. Here, we present a case of hematohidrosis in a 9y old female child with bleeding for two months from her forehead, nose, ear, and vagina, who responded to propranolol.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"18 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81892671","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 : 2023-07-01DOI: 10.22159/ijpps.2023v15i7.48092
Mehedi Hasan Shahed, Samia Tasneem, H. Sultana, Imam Ibne Wahed, Netish Kumar Kundo, MD Ashraf Ali
Objective: The COVID-19 pandemic has triggered several stress factors throughout the entire world. Some stress factors, such as mental, economical, educational etc., have created consequences like hair fall, as seen in individuals in many countries, including Bangladesh. The present study was designed to investigate the covid-19-induced stress factors and their relation with hair loss in the people of Bangladesh. Methods: An online-based survey study was carried out using a self-made questionnaire, and quantitative data were analyzed by a cross-sectional analysis over the period of two months from November 25, 2020, to January 24, 2021. Participants who were willing to participate into this survey were considered as study individuals. This survey was conducted among participants with age’s ≥18 y. The participants were selected by snowball sampling technique, and the final collected sample size was 808. Results: Among 808 participants, males and females were 50.3% (406) and 49.7% (402), respectively. We found that 5% (37) participants were infected with Covid-19, 89% (715) were not infected, and 7% (56) were unknown. It is found that COVID-19-induced stress conditions including educational 28%, mental 25%, and economical 20% were found in 81% (655) participants and rendered 68% (550) people facing the hair fall problem due to COVID-19-related stress. Female individuals who were more stressed were 74.6% (300) and had hair fall, whereas males were 38.7% (157). In addition, the increased rate of hair fall in COVID-19 is associated with other factors, such as eating disorders and scalp infections, as reported by some respondents. Conclusion: In pandemic situations, most of the people (81%) passed through the stressful condition, and the females experienced more hair fall problems than male one. High blood pressure, eating disorder and irregular sleep pattern are considered stress-induced factors that were responsible for increased hair loss.
{"title":"THE IMPACT OF COVID-19 PANDEMIC ON VARIOUS STRESS FACTORS AND ITS CORRELATION WITH HAIR FALL: AN ONLINE-BASED SURVEY AMONG BANGLADESHI RESIDENTS","authors":"Mehedi Hasan Shahed, Samia Tasneem, H. Sultana, Imam Ibne Wahed, Netish Kumar Kundo, MD Ashraf Ali","doi":"10.22159/ijpps.2023v15i7.48092","DOIUrl":"https://doi.org/10.22159/ijpps.2023v15i7.48092","url":null,"abstract":"Objective: The COVID-19 pandemic has triggered several stress factors throughout the entire world. Some stress factors, such as mental, economical, educational etc., have created consequences like hair fall, as seen in individuals in many countries, including Bangladesh. The present study was designed to investigate the covid-19-induced stress factors and their relation with hair loss in the people of Bangladesh.\u0000Methods: An online-based survey study was carried out using a self-made questionnaire, and quantitative data were analyzed by a cross-sectional analysis over the period of two months from November 25, 2020, to January 24, 2021. Participants who were willing to participate into this survey were considered as study individuals. This survey was conducted among participants with age’s ≥18 y. The participants were selected by snowball sampling technique, and the final collected sample size was 808.\u0000Results: Among 808 participants, males and females were 50.3% (406) and 49.7% (402), respectively. We found that 5% (37) participants were infected with Covid-19, 89% (715) were not infected, and 7% (56) were unknown. It is found that COVID-19-induced stress conditions including educational 28%, mental 25%, and economical 20% were found in 81% (655) participants and rendered 68% (550) people facing the hair fall problem due to COVID-19-related stress. Female individuals who were more stressed were 74.6% (300) and had hair fall, whereas males were 38.7% (157). In addition, the increased rate of hair fall in COVID-19 is associated with other factors, such as eating disorders and scalp infections, as reported by some respondents.\u0000Conclusion: In pandemic situations, most of the people (81%) passed through the stressful condition, and the females experienced more hair fall problems than male one. High blood pressure, eating disorder and irregular sleep pattern are considered stress-induced factors that were responsible for increased hair loss.","PeriodicalId":14188,"journal":{"name":"International Journal of Pharmacy and Pharmaceutical Sciences","volume":"33 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86201881","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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