Pub Date : 2023-07-20DOI: 10.32947/ajps.v23i3.1051
N. Z. Yousif, Z. Salman
The technology of drug delivery has become massively competitive and quickly growing. Enhancing efficacy is the primary objective of delivery system development, and hence cost-effectiveness of the treatment. Nevertheless, controlling the rate of delivery of active pharmaceutical moieties to a target site within the body has been one of the major obstacles confronted by the drug industry. Microsponge represents a delivery system considered a promising innovation that overcomes the different challenges, since, this dosage form provides the delivery of active pharmaceutical moieties in a timely manner, in addition to responding to different stimuli (pressure, temperature, pH). Microsponge drug delivery technology proposed capturing of active moieties into tiny spongy spheres thus, donating towards reducing side effects, improving stability, increasing elegance, and enhancing formulation flexibility. The goal behind this contribution is to cover microsponge as a successful innovation, summarizing the characteristics, advantages, and limitations with certain insight into the mechanism and factors triggering the release. Furthermore, shed light on the methodology of preparation.
{"title":"Microsponge as a Strategy for Effective Drug Delivery System","authors":"N. Z. Yousif, Z. Salman","doi":"10.32947/ajps.v23i3.1051","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1051","url":null,"abstract":"The technology of drug delivery has become massively competitive and quickly growing. Enhancing efficacy is the primary objective of delivery system development, and hence cost-effectiveness of the treatment. \u0000Nevertheless, controlling the rate of delivery of active pharmaceutical moieties to a target site within the body has been one of the major obstacles confronted by the drug industry. Microsponge represents a delivery system considered a promising innovation that overcomes the different challenges, since, this dosage form provides the delivery of active pharmaceutical moieties in a timely manner, in addition to responding to different stimuli (pressure, temperature, pH). Microsponge drug delivery technology proposed capturing of active moieties into tiny spongy spheres thus, donating towards reducing side effects, improving stability, increasing elegance, and enhancing formulation flexibility. The goal behind this contribution is to cover microsponge as a successful innovation, summarizing the characteristics, advantages, and limitations with certain insight into the mechanism and factors triggering the release. Furthermore, shed light on the methodology of preparation. \u0000 ","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"65 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74064844","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 : 2023-07-20DOI: 10.32947/ajps.v23i3.1040
Ghassan Mudher Hashim, Ghaidaa S. Hameed, D. Hanna
In early March of 2020, the world was hit by a pandemic caused by the new SARS-COV-2 coronavirus dubbed by the WHO (World health organization) as COVID-19. More than two years later and a series of lockdowns worldwide as a measure to combat the viral spread, had the world facing detrimental effects on health, economic and social fronts. The principal weapon in the worldwide fight against viruses such as corona virus illness in 2019 (COVID-19) is antiviral medicines (AvDs). Because of their low oral bioavailability and limited effectiveness owing to their low solubility/permeability, most AvDs need numerous doses, and their usage commonly results in drug resistance. Solving the issues with AvDs and improving their effectiveness might be aided by a better understanding of their in vivo metabolic and pharmacokinetic properties. In this review the AvDs, were systematically investigated regarding their cellular pharmacology, pharmacokinetics and pharmacodynamics. Additionally, delivery systems used for AvDs to achieve better pharmacology were reviewed. This review assumed that using sophisticated nanotechnology and the right administration routes, together with proper solid dispersion technology and nanosystems, may assist to obtain superior pharmacological activity and pharmacokinetic behavior of AvDs. Antiviral drugs (AvDs) that have been shown to bind to the SARS-CoV-2 receptor are promising candidates for treating COVID-19. These include ribavirin, remdesivir, favipiravir (FAV), chloroquine, lopinavir, and ritonavir.
{"title":"The possible techniques that used to improve the bioavailablity, pharmacological activity, solubility and permeability of anti-viral drugs: Insight for COVID-19 antiviral drugs","authors":"Ghassan Mudher Hashim, Ghaidaa S. Hameed, D. Hanna","doi":"10.32947/ajps.v23i3.1040","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1040","url":null,"abstract":"In early March of 2020, the world was hit by a pandemic caused by the new SARS-COV-2 coronavirus dubbed by the WHO (World health organization) as COVID-19. More than two years later and a series of lockdowns \u0000worldwide as a measure to combat the viral spread, had the world facing detrimental effects on health, economic and social fronts. The principal weapon in the worldwide fight against viruses such as corona virus illness in 2019 (COVID-19) is antiviral medicines (AvDs). Because of their low oral bioavailability and limited effectiveness owing to their low solubility/permeability, most AvDs need numerous doses, and their usage commonly results in drug resistance. Solving the issues with AvDs and improving their effectiveness might be aided by a better understanding of their in vivo metabolic and pharmacokinetic properties. In this review the AvDs, were systematically investigated regarding their cellular pharmacology, pharmacokinetics and pharmacodynamics. Additionally, delivery systems used for AvDs to achieve better pharmacology were reviewed. This review assumed that using sophisticated nanotechnology and the right administration routes, together with proper solid dispersion technology and nanosystems, may assist to obtain superior pharmacological activity and pharmacokinetic behavior of AvDs. Antiviral drugs (AvDs) that have been shown to bind to the SARS-CoV-2 receptor are promising candidates for treating COVID-19. These include ribavirin, remdesivir, favipiravir (FAV), chloroquine, lopinavir, and ritonavir.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"73 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72842963","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 : 2023-07-20DOI: 10.32947/ajps.v23i3.1045
Z. Abdul, Hameed Ibrahim ⃰ ،Manal, Khaled, Abdulrida, Basil Razoqi, Article Info
PCOS is a complicated endocrine disorder that mostly affects between 5% and 10% of women who are of reproductive age. Obesity, hyperandrogenism, and oligo- or anovulation are frequent clinical PCOS signs. Objective: the study was designed to evaluate the effect of combining Metformin and Myoinositol; the main insulin-sensitizing drugs on improving symptoms and HRQOLQ in PCOS women. Materials and Methods: A study was a prospective, interventional, comparative clinical study conducted on 54 patients (aged 18-40 y) who are divided into three groups: group1 patients allocated to receive Myo-inositol(4g), group2 patients allocated to receive Metformin(1g) and group3 patients allocated to receive Myo-inositol(4g) + Metformin(1g) all for 3 months. Baseline and after 3 months, patients’ information and health related quality of life were documented. Result: Metformin and Myoinositol resulted in symptoms improvement within each study groups as (68.8%, 87.5% and 94.1%) for group 1,2 and 3 respectively, only 4 patients from all groups became pregnant. Also, significant change in HRQOLQ in all study groups after three months of treatment were reported. Conclusion: combining Myoinositol with metformin results in improved PCOS symptoms and pregnancy outcome in addition to improved patient’s quality of life.
{"title":"Assessment of Symptoms, Pregnancy Outcome, and Health-Related Quality of Life among PCOS women Treated with Myo inositol and Metformin","authors":"Z. Abdul, Hameed Ibrahim ⃰ ،Manal, Khaled, Abdulrida, Basil Razoqi, Article Info","doi":"10.32947/ajps.v23i3.1045","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1045","url":null,"abstract":"PCOS is a complicated endocrine disorder that mostly affects between 5% and 10% of women who are of reproductive age. Obesity, hyperandrogenism, and oligo- or anovulation are frequent clinical PCOS signs. \u0000Objective: the study was designed to evaluate the effect of combining Metformin and Myoinositol; the main insulin-sensitizing drugs on improving symptoms and HRQOLQ in PCOS women. \u0000Materials and Methods: A study was a prospective, interventional, comparative clinical study conducted on 54 patients (aged 18-40 y) who are divided into three groups: group1 patients allocated to receive Myo-inositol(4g), group2 patients allocated to receive Metformin(1g) and group3 patients allocated to receive Myo-inositol(4g) + Metformin(1g) all for 3 months. Baseline and after 3 months, patients’ information and health related quality of life were documented. \u0000Result: Metformin and Myoinositol resulted in symptoms improvement within each study groups as (68.8%, 87.5% and 94.1%) for group 1,2 and 3 respectively, only 4 patients from all groups became pregnant. Also, significant change in HRQOLQ in all study groups after three months of treatment were reported. \u0000Conclusion: combining Myoinositol with metformin results in improved PCOS symptoms and pregnancy outcome in addition to improved patient’s quality of life.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86892897","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 : 2023-07-20DOI: 10.32947/ajps.v23i3.1048
Jian Lateif
Most common inflammatory markers like C-reactive protein, which is a protein produced by the liver in response to inflammation and infection in the body, is used to quantify circulating molecules that are released as a cause of an inflammatory response in clinical studies. The aim of this study is to estimate the levels of serum seromucoid and protein bound-hexose (PBH) as inflammatory markers in sera of COVID-19 patients in comparison with normal subjects. For this purpose, Thirty COVID-19 patients were selected as control (male and female) in addition to 30 healthy subjects as the control group. The findings indicated that seromucoid and PBH levels were highly significant increase in COVID-19 patients (P< 0.0001) comparing with normal subjects This study provides evidence that, despite some potential physiological differences, the levels of seromucoid and PBH showed no significant differences for both male and female patients. The results from both parameters showed that COVID-19 severity is associated with inflammatory markers.
{"title":"Seromucoid and Protein-Bound Hexose as Inflammatory Markers in Sera of COVID-19 Patients","authors":"Jian Lateif","doi":"10.32947/ajps.v23i3.1048","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1048","url":null,"abstract":"Most common inflammatory markers like C-reactive protein, which is a protein produced by the liver in response to inflammation and infection in the body, is used to quantify circulating molecules that are released as a cause of an inflammatory response in clinical studies. \u0000The aim of this study is to estimate the levels of serum seromucoid and protein bound-hexose (PBH) as inflammatory markers in sera of COVID-19 patients in comparison with normal subjects. For this purpose, Thirty COVID-19 patients were selected as control (male and female) in addition to 30 healthy subjects as the control group. The findings indicated that seromucoid and PBH levels were highly significant increase in COVID-19 patients (P< 0.0001) comparing with normal subjects This study provides evidence that, despite some potential physiological differences, the levels of seromucoid and PBH showed no significant differences for both male and female patients. The results from both parameters showed that COVID-19 severity is associated with inflammatory markers.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"127 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91357428","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 : 2023-07-20DOI: 10.32947/ajps.v23i3.1042
Bushra K. Jameel, Ayad M. R. Raauf, Wassan Abdul, Kareem Abbas
New pyridine derivatives of nabumetone containing 2-amino 3-cyano moieties were synthesized and aimed to introduce new EGFR kinase inhibitors through two methods either by synthesis of chalcone derivatives initially (1a-d) followed by reacting it with malononitrile and ammonium acetate to form (2a-d) or from a one-pot synthesis of all reactants together to synthesis compounds (2a-e). Melting point, and FT-IR spectra were used to characterize all the synthesized compounds and were confirmed by 1H-NMR, and 13C-NMR spectroscopy. The final compounds (2a-e) were investigated in vitro against A549 (lung cancer cell line) and WRL68 (human normal cell line). compounds (2a, 2b, and 2e) produced marked cytotoxic activity with IC50 (24.62, 23.43, and 24.06 μg/ml) respectively, higher than what obtained from erlotinib with IC50 (25 μg/ml) as a reference drug. Measuring the selectivity index (SI) reveals that all the compounds have high selectivity especially compound (2a) being the most selective towards cancerous cells rather than normal cells with SI two folds higher than erlotinib. The molecular docking study reveals good binding to the EGFR kinase that has a good correlation to the MTT Assay results. In silico ADME study exposes that this synthesized series not only have interesting activity but also shows promised pharmacokinetic properties.
{"title":"Synthesis, characterization, molecular docking, in silico ADME study, and in vitro cytotoxicity evaluation of new pyridine derivatives of nabumetone.","authors":"Bushra K. Jameel, Ayad M. R. Raauf, Wassan Abdul, Kareem Abbas","doi":"10.32947/ajps.v23i3.1042","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1042","url":null,"abstract":"New pyridine derivatives of nabumetone containing 2-amino 3-cyano moieties were synthesized and aimed to introduce new EGFR kinase inhibitors through two methods either by synthesis of chalcone derivatives initially (1a-d) \u0000followed by reacting it with malononitrile and ammonium acetate to form (2a-d) or from a one-pot synthesis of all reactants together to synthesis compounds (2a-e). Melting point, and FT-IR spectra were used to characterize all the synthesized compounds and were confirmed by 1H-NMR, and 13C-NMR spectroscopy. The final compounds (2a-e) were investigated in vitro against A549 (lung cancer cell line) and WRL68 (human normal cell line). compounds (2a, 2b, and 2e) produced marked cytotoxic activity with IC50 (24.62, 23.43, and 24.06 μg/ml) respectively, higher than what obtained from erlotinib with IC50 (25 μg/ml) as a reference drug. Measuring the selectivity index (SI) reveals that all the compounds have high selectivity especially compound (2a) being the most selective towards cancerous cells rather than normal cells with SI two folds higher than erlotinib. The molecular docking study reveals good binding to the EGFR kinase that has a good correlation to the MTT Assay results. In silico ADME study exposes that this synthesized series not only have interesting activity but also shows promised pharmacokinetic properties.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"40 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80910507","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 : 2023-07-20DOI: 10.32947/ajps.v23i3.1043
Mina J. Jabbar, W. Ali
In recent years, gels have been preferentially used for cosmetics and topical pharmaceutical preparations due to their favorable characteristics, such as being greaseless, readily spreadable and easily removable. However, one obstacle that faced it was the inability to enclose hydrophobic compounds. Therefore, a novel approach was developed to circumvent this limitation by mixing the gel with an emulsion, which led to creation of a new topical drug delivery system known as emulgel. Emulgel preserves all favorable features of gel and provides also dual release for drug, thus can be utilized effectively in controlling release and absorption of medication after topical application. Emulgel preparation requires coherent steps, this includes preparation of emulsion and gel and determining their mixing ratio. Finally, the prepared emulgels should be evaluated to ensure their suitability and efficacy for the topical application.
{"title":"An overview of emulgels for topical application","authors":"Mina J. Jabbar, W. Ali","doi":"10.32947/ajps.v23i3.1043","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1043","url":null,"abstract":"In recent years, gels have been preferentially used for cosmetics and topical pharmaceutical preparations due to their favorable characteristics, such as being greaseless, readily spreadable and easily removable. However, one \u0000obstacle that faced it was the inability to enclose hydrophobic compounds. Therefore, a novel approach was developed to circumvent this limitation by mixing the gel with an emulsion, which led to creation of a new topical drug delivery system known as emulgel. Emulgel preserves all favorable features of gel and provides also dual release for drug, thus can be utilized effectively in controlling release and absorption of medication after topical application. Emulgel preparation requires coherent steps, this includes preparation of emulsion and gel and determining their mixing ratio. Finally, the prepared emulgels should be evaluated to ensure their suitability and efficacy for the topical application.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"72 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88116685","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 : 2023-07-20DOI: 10.32947/ajps.v23i3.1049
Talar Ibrahim, Hasan, A. Ahmed
Antimicrobial resistance is regarded as one of the top three terrible events threatening the worldwide existence of humans Here of, Acinetobacter baumannii evolved as the most challenging pathogen threatening to initiate the post-antibiotic era. Their ability to withstand antibiotics is attributed to a set of virulence determinants in particular biofilms which are known to enhance pathogenesis and drug resistance potency. Studies regarding green silver nanoparticles (AgNP)s as an alternative treatment modality to antibiotics increased over recent years. Considering these facts, we aimed to explore the antibiofilm effect of AgNPs in the multi-drug-resistant Acinetobacter baumannii. AgNPs were bio-fabricated by Pseudomonas aeruginosa and characterized via FTIR, UV-Vis, XRD, EDS, and SEM. Well-diffusion was used to screen the antimicrobial effects of AgNPs. Minimal-inhibitory concentrations of AgNPs were determined to study their antibiofilm effect at sub-inhibitory concentrations (SIC). Results showed that all isolates were biofilm producers and portrayed high resistance to the tested antibiotics. Characterization results supported the successful fabrication of crystalline nanoparticles. Exposure of the isolates to the bacteriogenic AgNPs resulted in pronounced inhibition zones and reduced biofilms at SICs values. These results indicate that Pseudomonas aeruginosa can be employed to produce AgNPs with an aptitude to disrupt biofilm development and growth in the multi-drug resistant Acinetobacter baumannii.
{"title":"Characterization, antibacterial and antibiofilm evaluation of biosynthesized silver nanoparticles from Pseudomonas aeruginosa against drug resistant Acinetobacter baumannii","authors":"Talar Ibrahim, Hasan, A. Ahmed","doi":"10.32947/ajps.v23i3.1049","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1049","url":null,"abstract":"Antimicrobial resistance is regarded as one of the top three terrible events threatening the worldwide existence of humans Here of, Acinetobacter baumannii evolved as the most challenging pathogen threatening to initiate the post-antibiotic era. \u0000Their ability to withstand antibiotics is attributed to a set of virulence determinants in particular biofilms which are known to enhance pathogenesis and drug resistance potency. Studies regarding green silver nanoparticles (AgNP)s as an alternative treatment modality to antibiotics increased over recent years. Considering these facts, we aimed to explore the antibiofilm effect of AgNPs in the multi-drug-resistant Acinetobacter baumannii. AgNPs were bio-fabricated by Pseudomonas aeruginosa and characterized via FTIR, UV-Vis, XRD, EDS, and SEM. Well-diffusion was used to screen the antimicrobial effects of AgNPs. Minimal-inhibitory concentrations of AgNPs were determined to study their antibiofilm effect at sub-inhibitory concentrations (SIC). Results showed that all isolates were biofilm producers and portrayed high resistance to the tested antibiotics. Characterization results supported the successful fabrication of crystalline nanoparticles. Exposure of the isolates to the bacteriogenic AgNPs resulted in pronounced inhibition zones and reduced biofilms at SICs values. These results indicate that Pseudomonas aeruginosa can be employed to produce AgNPs with an aptitude to disrupt biofilm development and growth in the multi-drug resistant Acinetobacter baumannii.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"5 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87503551","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 : 2023-07-20DOI: 10.32947/ajps.v23i3.1052
Mustafa Taha Abdull, M. Mahdi, A. K. Khan
In this work the pharmacological study and synthesis of new thiadiazine bearing on triazole which obtained from hippuric acid , indomethacin and mefenamic acid that have carboxylic acid moiety, Drugs with carboxylic groups and thiocarbohydrazide interacted to produce the 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol (1a-c). and the starting products 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol) were treated with chloroacetyl chloride to produce final products (2a-c). To confirm the structure of the generated compounds, FT-IR, 1H-NMR, and mass spectroscopy were used to characterize all derivatives (intermediate and final products). The in vivo anti-inflammatory efficacy of some derivatives and thier toxicity to animals (in vivo) were evaluated. And then derivatives were subjected to molecular docking to create safe and efficient molecules. To test each derivative's ability to bind to the enzyme's active site, it was docked into the active sites. To determine the synthetic compound's topological polar surface area, bioavailability, and drug-likeness, An investigation of absorption, distribution, metabolism and elimination was performed. According to the findings, the tested derivatives adhered to the Lipinski rule and were ingested
{"title":"Molecular docking, Synthesis and Characterization of New Indomethacin and Mefenamic Acid Analogues as Potential Anti-inflammatory Agents","authors":"Mustafa Taha Abdull, M. Mahdi, A. K. Khan","doi":"10.32947/ajps.v23i3.1052","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1052","url":null,"abstract":"In this work the pharmacological study and synthesis of new thiadiazine bearing on triazole which obtained from hippuric acid , indomethacin and mefenamic acid that have carboxylic acid moiety, Drugs with carboxylic groups and thiocarbohydrazide interacted to produce the 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol (1a-c). \u0000and the starting products 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol) were treated with chloroacetyl chloride to produce final products (2a-c). To confirm the structure of the generated compounds, FT-IR, 1H-NMR, and mass spectroscopy were used to characterize all derivatives (intermediate and final products). The in vivo anti-inflammatory efficacy of some derivatives and thier toxicity to animals (in vivo) were evaluated. And then derivatives were subjected to molecular docking to create safe and efficient molecules. To test each derivative's ability to bind to the enzyme's active site, it was docked into the active sites. To determine the synthetic compound's topological polar surface area, bioavailability, and drug-likeness, An investigation of absorption, distribution, metabolism and elimination was performed. According to the findings, the tested derivatives adhered to the Lipinski rule and were ingested","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"7 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85428738","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 : 2023-07-20DOI: 10.32947/ajps.v23i3.1053
Essa Bahauldeen Fadhil, M. Mohammed, UlaMohammedReda AlKawaz, Article Info
Background: The definition of World Health Organization (WHO) to the infertile couple is the failure of female get pregnancy in spite of having regular sexual activity for at least 1 year without using any contraceptive methods, worldwide it is estimated that 15 % of reproductive-age couples are struggling with infertility. In many cases, infertility cannot be treated, new treatment options with promising value were involved in the recent clinical trials. Aim: This study was designed to evaluate the effects of letrozole plus coenzyme Q10 combination on spermiogram and sex hormones in men with idiopathic oligoasthenoteratozoospermia (iOAT) syndrome. Patient and methods: fifty-five patients are enrolled in this study, but only 40 patients complete the study, they are treated with a combination of Letrozole 2.5 mg tablet orally twice a week plus Co-enzyme Q10 400mg per day for three months. Seminal fluid sample, follicle-stimulating hormone, estradiol, and testosterone were analyzed before starting the treatment and at the end of month 1, 2 and 3.Results: sperm concentration, sperm morphology, total sperm count and motility, serum testosterone and follicle stimulation hormone levels, in addition to testosterone/estradiol ratio were significantly improved, while estradiol levels significantly decreased after 3 months of treatment. However, seminal fluid volume showed no significant change. Finally, as a notable outcome, one spontaneous conception occurred after treatment as well as three azoospermia cases responded well after completing the course of treatment. Conclusions: a combination of Letrozole and CO Q10 can effectively improve sperm parameters in Iraqi men with iOAT.
{"title":"Influence of Letrozole and Co Q10 on Sex Hormones and Spermiogram in Infertile Men; sample of Iraqi patients","authors":"Essa Bahauldeen Fadhil, M. Mohammed, UlaMohammedReda AlKawaz, Article Info","doi":"10.32947/ajps.v23i3.1053","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1053","url":null,"abstract":"Background: The definition of World Health Organization (WHO) to the infertile couple is the failure of female get pregnancy in spite of having regular sexual activity for at least 1 year without using any contraceptive methods, worldwide it is estimated that 15 % of reproductive-age couples are struggling with infertility. \u0000In many cases, infertility cannot be treated, new treatment options with promising value were involved in the recent clinical trials. \u0000Aim: This study was designed to evaluate the effects of letrozole plus coenzyme Q10 combination on spermiogram and sex hormones in men with idiopathic oligoasthenoteratozoospermia (iOAT) syndrome. \u0000Patient and methods: fifty-five patients are enrolled in this study, but only 40 patients complete the study, they are treated with a combination of Letrozole 2.5 mg tablet orally twice a week plus Co-enzyme Q10 400mg per day for three months. Seminal fluid sample, follicle-stimulating hormone, estradiol, and testosterone were analyzed before starting the treatment and at the end of month 1, 2 and 3.Results: sperm concentration, sperm morphology, total sperm count and motility, serum testosterone and follicle stimulation hormone levels, in addition to testosterone/estradiol ratio were significantly improved, while estradiol levels significantly decreased after 3 months of treatment. However, seminal fluid volume showed no significant change. Finally, as a notable outcome, one spontaneous conception occurred after treatment as well as three azoospermia cases responded well after completing the course of treatment. \u0000Conclusions: a combination of Letrozole and CO Q10 can effectively improve sperm parameters in Iraqi men with iOAT.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81344776","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}
Superporouse hydrogel (SPH) is widely used and investigated as a gastro retentive drug delivery system to extend drug residence time in the stomach However, their mechanical strength represents a problem because they need to withstand the peristaltic movement of the stomach. Properties of SPH are widely affected by the materials used for their synthesis. The aim of the research is to study the effect of changing the foaming agent and foam stabilizer amount on physical properties, in particular mechanical strength, and drug release from SPH. Trifluoperazine HCl will be used as model drug in the study. SPH formulations was prepared using fixed amount of acrylamide (AM) and polyvinyl alcohol (PVA) as monomers, polyethylene glycol diacrylate (PEGDA) as cross-linker, TRFP as model drug and variable amount of sodium bicarbonate (NaHCO3) as foaming agent, and tween 20 as foam stabilizer. Ammonium persulphate (APS) / tetramethyl ethylenediamine (TEMED) system was used as polymerization initiator. The effect of changing foaming agent and foam stabilizer on mechanical strength, buoyancy, porosity, density, drug release, drug content, swelling ratio, and swelling time was investigated. Modifying both factors affected all the physical properties and drug release profile. When tween 20 was increased the mechanical strength, density and floating lag time was increased with a reduction in porosity and drug release. While increasing NaHCO3 reduced mechanical strength, density and floating lag time with increased porosity and faster drug release was observed. Optimum physical properties were observed in formula 2 which had 230 µl of Tween 20 (v/v) and 50 mg of NaHCO3 in which the mechanical strength was 579±0.4, floating lag time 14 min and 80% of the drug was released within 12 hr. As a conclusion SPH with improved mechanical strength, physical properties and drug release pattern can be achieved by changing foam stabilizer and foaming agent amount in the formulations.
{"title":"Effect of modification of formulation variables on physical characterization of superporouse hydrogel","authors":"Safa Mohammed Nser, Athmar Dhahir, Habeeb Al-Shohani, رصن دمحم افص, . امثا","doi":"10.32947/ajps.v23i3.1046","DOIUrl":"https://doi.org/10.32947/ajps.v23i3.1046","url":null,"abstract":"Superporouse hydrogel (SPH) is widely used and investigated as a gastro retentive drug delivery system to extend drug residence time in the stomach \u0000 \u0000However, their mechanical strength represents a problem because they need to withstand the peristaltic movement of the stomach. Properties of SPH are widely affected by the materials used for their synthesis. The aim of the research is to study the effect of changing the foaming agent and foam stabilizer amount on physical properties, in particular mechanical strength, and drug release from SPH. Trifluoperazine HCl will be used as model drug in the study. \u0000SPH formulations was prepared using fixed amount of acrylamide (AM) and polyvinyl alcohol (PVA) as monomers, polyethylene glycol diacrylate (PEGDA) as cross-linker, TRFP as model drug and variable amount of sodium bicarbonate (NaHCO3) as foaming agent, and tween 20 as foam stabilizer. Ammonium persulphate (APS) / tetramethyl ethylenediamine (TEMED) system was used as polymerization initiator. The effect of changing foaming agent and foam stabilizer on mechanical strength, buoyancy, porosity, density, drug release, drug content, swelling ratio, and swelling time was investigated. \u0000Modifying both factors affected all the physical properties and drug release profile. When tween 20 was increased the mechanical strength, density and floating lag time was increased with a reduction in porosity and drug release. While increasing NaHCO3 reduced mechanical strength, density and floating lag time with increased porosity and faster drug release was observed. Optimum physical properties were observed in formula 2 which had 230 µl of Tween 20 (v/v) and 50 mg of NaHCO3 in which the mechanical strength was 579±0.4, floating lag time 14 min and 80% of the drug was released within 12 hr. \u0000 As a conclusion SPH with improved mechanical strength, physical properties and drug release pattern can be achieved by changing foam stabilizer and foaming agent amount in the formulations. ","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":"9 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90849116","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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