Pub Date : 2023-05-23DOI: 10.32947/ajps.v23i2.1024
Mohammed Abdulzahra Hussein, Mohanad Naji Sahib
This study was aimed to evaluate biphasic dissolution system and its applicability to discriminate between different formulas. Two different tablet formulas of furosemide were prepared using dry compression (F1) and wet granulation (F2). The prepared formulas were evaluated for hardness, friability and disintegration. Thereafter, monophasic and biphasic dissolution systems were used to compare the dissolution profiles of the prepared formulas with a commercially available tablet. The results of the physical properties of the prepared tablets were within acceptable values. Moreover, there were insignificant differences (P>0.05) between generic product and the prepared formulations. The similarity and difference factors were > 58 and <10, respectively. On the other hand, the biphasic dissolution system results showed significant difference regarding dissolution profiles for all items under investigation. In conclusion, biphasic dissolution system could be a viable tool in assessment in-vitro drug performance as a result of its good discriminatory power.
{"title":"The predictive power of biphasic dissolution approach using Class IV model drug","authors":"Mohammed Abdulzahra Hussein, Mohanad Naji Sahib","doi":"10.32947/ajps.v23i2.1024","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1024","url":null,"abstract":"This study was aimed to evaluate biphasic dissolution system and its applicability to discriminate between different formulas. Two different tablet formulas of furosemide were prepared using dry compression (F1) and wet granulation (F2). The prepared formulas were evaluated for hardness, \u0000friability and disintegration. Thereafter, monophasic and biphasic dissolution systems were used to compare the dissolution profiles of the prepared formulas with a commercially available tablet. The results of the physical properties of the prepared tablets were within acceptable values. Moreover, there were insignificant differences (P>0.05) between generic product and the prepared formulations. The similarity and difference factors were > 58 and <10, respectively. On the other hand, the biphasic dissolution system results showed significant difference regarding dissolution profiles for all items under investigation. In conclusion, biphasic dissolution system could be a viable tool in assessment in-vitro drug performance as a result of its good discriminatory power. ","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87678898","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 : 2023-05-23DOI: 10.32947/ajps.v23i2.1022
Mohammed Ridha Jawad, Ghaith Ali Jasim
Background: Benign prostatic hyperplasia [BPH] is the urologic condition that affects elderly men the most frequently Benign prostatic hyperplasia. Benign prostatic hyperplasia must be distinguished from lower urinary tract symptoms and benign prostatic enlargement. which refers to an enlarged prostate, benign prostatic hyperplasia is a purely histological term the development, maintenance, and secretory activity of the prostate and other sex-accessory tissues are stimulated by the presence of certain hormones and growth factors. the pathophysiology of Benign prostatic hyperplasia is significantly influenced by the activity of the enzyme 5α-reductase. It's important to remember that 5-αreductase is responsible for creating Dihydrotestosterone a stronger androgen. Pterostilbene Mostly found in blueberries and grapes and pterostilbene substance with a number of biological properties including anticancer properties. pterostilbene is a lipid-soluble molecule that exists in both cis and trans forms with the latter being more prevalent. The conventional medication for Benign prostatic hyperplasia utilized in this trial was finasteride which inhibits the 5α-reductase enzyme and lowers the amount of Dihydrotestosterone. Methods: Forty-eight male rats were divided into six groups; the control group consisted of eight rats who received subcutaneous injections of oil vehicle for a period of 42 days. The induction group consisted of eight rats who received subcutaneous injections of testosterone propionate for a period of fourteen days. The finasteride group consisted of eight rats who received finasteride 0.44 mg/kg by oral gavage for a period of twenty-eight days following the induction of Benign prostatic hyperplasia and Pterostilbene 200 group included 8 rats were given pterostilbene 200mg/kg by oral gavage for 28 days after 14 days of Benign prostatic hyperplasia induction. pterostilbene 100 group included 8 rats were given a pterostilbene 100mg/kg per day kg by oral gavage for 28 days after 14 days of induction Benign prostatic hyperplasia dose and the resveratrol group included 8 rats were given a resveratrol 100mg/kg per day kg by oral gavage for 28 days after 14 days of induction Benign prostatic hyperplasia After twenty-eight days. Results: Histological section of prostate Pterostilbene 200 were similar those in control negative revealed numerous variable sizes alveoli that filled with homogenous eosinophilic secretion, had normal epithelial and stromal tissue. Conclusion: Pterostilbene have a potent anti-proliferative effect by decrease the hyperplastic nodules for prostate and return epithelial cell to normal and have a very good scavenging activity for free radical [very good as antioxidant] in compare with Vitamin c and resveratrol. Aim of study: evaluate the effect of Pterostilbene as Anti proliferative on Benign prostatic hyperplasia and assess the antioxidant activity for Pterostilbene by DPPH Assay.
{"title":"Biochemical and Histopathological evaluation of prostatic tissue under effect of Pterostilbene in benign prostatic hyperplasia rat model","authors":"Mohammed Ridha Jawad, Ghaith Ali Jasim","doi":"10.32947/ajps.v23i2.1022","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1022","url":null,"abstract":"Background: Benign prostatic hyperplasia [BPH] is the urologic condition that affects elderly men the most frequently Benign prostatic hyperplasia. Benign prostatic hyperplasia must be distinguished from \u0000lower urinary tract symptoms and benign prostatic enlargement. which refers to an enlarged prostate, benign prostatic hyperplasia is a purely histological term the development, maintenance, and secretory activity of the prostate and other sex-accessory tissues are stimulated by the presence of certain hormones and growth factors. the pathophysiology of Benign prostatic hyperplasia is significantly influenced by the activity of the enzyme 5α-reductase. It's important to remember that 5-αreductase is responsible for creating Dihydrotestosterone a stronger androgen. Pterostilbene Mostly found in blueberries and grapes and pterostilbene substance with a number of biological properties including anticancer properties. pterostilbene is a lipid-soluble molecule that exists in both cis and trans forms with the latter being more prevalent. The conventional medication for Benign prostatic hyperplasia utilized in this trial was finasteride which inhibits the 5α-reductase enzyme and lowers the amount of Dihydrotestosterone. \u0000Methods: Forty-eight male rats were divided into six groups; the control group consisted of eight rats who received subcutaneous injections of oil vehicle for a period of 42 days. The induction group consisted of eight rats who received subcutaneous injections of testosterone propionate for a period of fourteen days. The finasteride group consisted of eight rats who received finasteride 0.44 mg/kg by oral gavage for a period of twenty-eight days following the induction of Benign prostatic hyperplasia and Pterostilbene 200 group included 8 rats were given pterostilbene 200mg/kg by oral gavage for 28 days after 14 days of Benign prostatic hyperplasia induction. pterostilbene 100 group included 8 rats were given a pterostilbene 100mg/kg per day kg by oral gavage for 28 days after 14 days of induction Benign prostatic hyperplasia dose and the resveratrol group included 8 rats were given a resveratrol 100mg/kg per day kg by oral gavage for 28 days after 14 days of induction Benign prostatic hyperplasia After twenty-eight days. \u0000Results: Histological section of prostate Pterostilbene 200 were similar those in control negative revealed numerous variable sizes alveoli that filled with homogenous eosinophilic secretion, had normal epithelial and stromal tissue. \u0000Conclusion: Pterostilbene have a potent anti-proliferative effect by decrease the hyperplastic nodules for prostate and return epithelial cell to normal and have a very good scavenging activity for free radical [very good as antioxidant] in compare with Vitamin c and resveratrol. \u0000Aim of study: evaluate the effect of Pterostilbene as Anti proliferative on Benign prostatic hyperplasia and assess the antioxidant activity for Pterostilbene by DPPH Assay.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79101578","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 : 2023-05-23DOI: 10.32947/ajps.v23i2.1023
Marwan Imad Jihad, Monther Faisal Mahdi
Novel therapeutics are desperately needed for the difficult-to-treat and very lethal malignancy known as hepatocellular carcinoma (HCC). The first drug now authorized for the treatment of individuals with advanced HCC is sorafenib. To find novel Vascular Endothelial Growth Factor Receptor Inhibitors as prospective candidate therapeutics for HCC, an in-silico technique was used in this case. Docking investigations were conducted using the GOLD Suite (v. 5.7.1) from the Cambridge Crystallographic Data Centre (CCDC). The docking/scoring methods of CCDC were validated by reproducing the docking interactions and poses of Sorafenib. Based on their PLP fitness, compounds I–X and sorafenib were graded for their ability to inhibit VEGF. Compounds II, III and VIII among other ligands exhibit higher binding energies than the standard drug sorafenib that give PLP fitness value (80.4).
{"title":"In silico Study of New Vascular Endothelial Growth Factor Receptor Inhibitors for The Treatment of Hepatocellular Carcinoma","authors":"Marwan Imad Jihad, Monther Faisal Mahdi","doi":"10.32947/ajps.v23i2.1023","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1023","url":null,"abstract":"Novel therapeutics are desperately needed for the difficult-to-treat and very lethal malignancy known as hepatocellular carcinoma (HCC). The first drug now authorized for the treatment of individuals with advanced HCC is sorafenib. To find novel Vascular Endothelial Growth Factor Receptor Inhibitors as prospective candidate therapeutics for HCC, an in-silico technique was used in this case. Docking investigations were conducted using the GOLD Suite (v. 5.7.1) from the Cambridge Crystallographic Data Centre (CCDC). The docking/scoring methods of CCDC were validated by reproducing the docking interactions and poses of Sorafenib. Based on their PLP fitness, compounds I–X and sorafenib were graded for their ability to inhibit VEGF. Compounds II, III and VIII among other ligands exhibit higher binding energies than the standard drug sorafenib that give PLP fitness value (80.4).","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75857090","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 : 2023-05-22DOI: 10.32947/ajps.v23i2.1015
Ali H. Farag, Wassan A. Abass, Hyder S. Qassem
Background: Chronic obstructive pulmonary disease (COPD) is a chronic inflammatory disorder of the airways associated with airway narrowing with airflow obstruction leading to difficulty in breathing impair daily activity and cause poor quality of life. Patients and methods: Fifty patients whom diagnosed with COPD are divided into two groups, 1st control group includes 25 patients assigned to receive conventional therapy of Formoterol fumarate 12 microgram inhaler twice daily, and 2nd interventional group also includes 25 patients assigned to receive conventional therapy with (300 mg/ 2 times daily) sublingual glutathione for two months. Saint George respiratory questionnaire (SGRQ) were measured before and after first and second months after treatment in both study groups. Aim of the study: This study was object to assess the changes in quality of life by using SGRQ following sublingual glutathione supplements therapy in COPD patients. Results and conclusion: After two months treatment , the mean values of SGRQ showed a significant increase compared to pre-treatment levels in both groups (P<0.01). There was highly significant improvement in SGRQ in both COPD patients groups after 2 months of treatment with much significant improvement in intervention group which may indicate the beneficial effects of adding glutathione sublingually administered supplements in COPD patients conventional therapeutic regiment.
{"title":"Evaluation the Effect of Sublingual Glutathione on the Quality of Life in COPD Patient by Using Saint George respiratory questionnaire","authors":"Ali H. Farag, Wassan A. Abass, Hyder S. Qassem","doi":"10.32947/ajps.v23i2.1015","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1015","url":null,"abstract":"Background: Chronic obstructive pulmonary disease (COPD) is a chronic inflammatory disorder of the airways associated with airway narrowing with airflow obstruction leading to difficulty in breathing impair daily activity and cause poor quality of life. Patients and methods: Fifty patients whom diagnosed with COPD are divided into two groups, 1st control group includes 25 patients assigned to receive conventional therapy of Formoterol fumarate 12 microgram inhaler twice daily, and 2nd interventional group also includes 25 patients assigned to receive conventional therapy with (300 mg/ 2 times daily) sublingual glutathione for two months. Saint George respiratory questionnaire (SGRQ) were measured before and after first and second months after treatment in both study groups. Aim of the study: This study was object to assess the changes in quality of life by using SGRQ following sublingual glutathione supplements therapy in COPD patients. Results and conclusion: After two months treatment , the mean values of SGRQ showed a significant increase compared to pre-treatment levels in both groups (P<0.01). There was highly significant improvement in SGRQ in both COPD patients groups after 2 months of treatment with much significant improvement in intervention group which may indicate the beneficial effects of adding glutathione sublingually administered supplements in COPD patients conventional therapeutic regiment.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83389030","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 : 2023-05-22DOI: 10.32947/ajps.v23i2.1014
Haneen Hussein Farhood, Manal Khalid Abdulridha, Hameedah Hadi
Background; Due to the complicated etiology of cardiovascular illnesses, a thorough risk assessment is necessary for screening reasons. Many published studies relate the pregnancy complications and future cardiovascular disease (CVD) risk. Objective; Investigate the association between risk factors of the laboratory measures and adverse pregnancy outcomes (APOs) with level of cardiovascular disorders risk. Methods; Adult women were enrolled in a cross-sectional study, and they were divided into 2 groups according to whether they had a history of adverse pregnancy outcomes or not. Laboratory and clinical measurements were carried out, and The CVD risk was calculated according to Framingham risk score. Results; All women enrolled were over 40 years age, mostly obese, had predominantly A+ve and O+ve blood group phenotypes. As compared to the low risk category, women with a positive history of pregnancy-induced hypertension and preeclampsia were 7.5 times more likely to be in the intermediate group while those with a positive history of stillbirth were 17.2 times more likely to be in the high-risk group. Conclusion; With reference to the low risk category, a positive history of pregnancy-induced hypertension and preeclampsia was predictor for intermediate CVD risk, while a positive history of stillbirth was predictor for high CVD risk.
{"title":"The Association between Adverse Pregnancy Outcomes and Laboratory Measures as Risk for Cardiovascular Disorders","authors":"Haneen Hussein Farhood, Manal Khalid Abdulridha, Hameedah Hadi","doi":"10.32947/ajps.v23i2.1014","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1014","url":null,"abstract":"Background; Due to the complicated etiology of cardiovascular illnesses, a thorough risk assessment is necessary for screening reasons. Many published studies relate the pregnancy complications and future cardiovascular disease (CVD) risk. Objective; Investigate the association between risk factors of the laboratory measures and adverse pregnancy outcomes (APOs) with level of cardiovascular disorders risk. Methods; Adult women were enrolled in a cross-sectional study, and they were divided into 2 groups according to whether they had a history of adverse pregnancy outcomes or not. Laboratory and clinical measurements were carried out, and The CVD risk was calculated according to Framingham risk score. Results; All women enrolled were over 40 years age, mostly obese, had predominantly A+ve and O+ve blood group phenotypes. As compared to the low risk category, women with a positive history of pregnancy-induced hypertension and preeclampsia were 7.5 times more likely to be in the intermediate group while those with a positive history of stillbirth were 17.2 times more likely to be in the high-risk group. Conclusion; With reference to the low risk category, a positive history of pregnancy-induced hypertension and preeclampsia was predictor for intermediate CVD risk, while a positive history of stillbirth was predictor for high CVD risk.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91451234","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 : 2023-05-22DOI: 10.32947/ajps.v23i2.1017
Sa`ad H. Mohammed, Manaf Muwafak Ahmed, Ruaa Allawy Hasan
Background: - Neonatal jaundice is a frequent condition at newborns, particularly in the first few days after delivery, and it has to be treated well to prevent complications that might have significant, long-lasting complications. Objective: - To assess the outcome of newborn jaundice at the central teaching Hospital of pediatrics in Baghdad using different modality of treatments. Patients and Methods: - A retrospective study is done depending on the medical data of infants have jaundice who were admitted to the neonate units of the central teaching hospital within the period of a year, from May 1st 2020 to May 1st 2021. Blood grouping and total serum bilirubin measurements were taken in each case. Phototherapy, strong phototherapy, and exchange transfusion were utilized to treat the newborn jaundice, depending on its severity. Results: Total neonates admitted from 1st may2020 to1st may 2021 in neonate unit were 2508 and 855 [34%] have jaundice. the male: female rati0 is [1.6:1], males 516[60.3%], females 339[39.6%]. The Physiol0gical jaundice is the often-frequent cause 285[33.3%] patients. The Prematurity seen in 171[20%] patient and the ABO incompatibility seen in 128[1.3%] and the Rh incompatibility 17[2%] patient, the sepsis found in 16[2%] case and the other causes of hyperbilirubinemia seen in 238[27.8%] patient. the Phototherapy is the most frequent kind of management used in 513[55%] and intensive phototherapy is applied for 342[40.3%] patients and just 59[7%] of patients treated with exchange transfusion particularly patients with ABO incompatibility 25 [42%] also Rh incompatibility 34 [57.6%] Good decline in TSB level and not require the exchange transfusion is 812 [95%] of patients. Majority of infants 849 [99.55%] discharge with clinical improvement and only 17 [0.3%] of infant’s patients develops kernicterus and 8 patients is dying [0.1%] Conclusion: Moderate to severe hyperbilirubinemia is still often treated with phototherapy. Intensive phototherapy is beneficial in lowering T.S.B levels, minimizing the need for exchange transfusions, and shortening hospital stays in patients with newborn hyperbilirubinemia.
{"title":"Evaluate of newborn with jaundice at central teaching hospital of pediatrics in Baghdad : descriptive study","authors":"Sa`ad H. Mohammed, Manaf Muwafak Ahmed, Ruaa Allawy Hasan","doi":"10.32947/ajps.v23i2.1017","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1017","url":null,"abstract":"Background: - Neonatal jaundice is a frequent condition at newborns, particularly in the first few days after delivery, and it has to be treated well to prevent complications that might have significant, long-lasting complications. \u0000Objective: - To assess the outcome of newborn jaundice at the central teaching Hospital of pediatrics in Baghdad using different modality of treatments. \u0000Patients and Methods: - A retrospective study is done depending on the medical data of infants have jaundice who were admitted to the neonate units of the central teaching hospital within the period of a year, from May 1st 2020 to May 1st 2021. Blood grouping and total serum bilirubin measurements were taken in each case. Phototherapy, strong phototherapy, and exchange transfusion were utilized to treat the newborn jaundice, depending on its severity. \u0000Results: Total neonates admitted from 1st may2020 to1st may 2021 in neonate unit were 2508 and 855 [34%] have jaundice. the male: female rati0 is [1.6:1], males 516[60.3%], females 339[39.6%]. The Physiol0gical jaundice is the often-frequent cause 285[33.3%] patients. The Prematurity seen in 171[20%] patient and the ABO incompatibility seen in 128[1.3%] and the Rh incompatibility 17[2%] patient, the sepsis found in 16[2%] case and the other causes of hyperbilirubinemia seen in 238[27.8%] patient. the Phototherapy is the most frequent kind of management used in 513[55%] and intensive phototherapy is applied for 342[40.3%] patients and just 59[7%] of patients treated with exchange transfusion particularly patients with ABO incompatibility 25 [42%] also Rh incompatibility 34 [57.6%] Good decline in TSB level and not require the exchange transfusion is 812 [95%] of patients. Majority of infants 849 [99.55%] discharge with clinical improvement and only 17 [0.3%] of infant’s patients develops kernicterus and 8 patients is dying [0.1%] \u0000Conclusion: Moderate to severe hyperbilirubinemia is still often treated with phototherapy. Intensive phototherapy is beneficial in lowering T.S.B levels, minimizing the need for exchange transfusions, and shortening hospital stays in patients with newborn hyperbilirubinemia.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78801571","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 : 2023-05-22DOI: 10.32947/ajps.v23i2.1019
Ameera A Radhi, Iman S Jaafar, Noor S Jaafar, Sarah M Faisal
Cocrystallization is an emerging approach for improving physico-chemical characteristics of an active pharmaceutical ingredient (API) for instance dissolution rate, solubility, stability in addition to mechanical properties without affecting their therapeutic activity. It is of great importance when other approaches like salt or polymorph formation do not encounter the estimated targets. In this review article, an outline of pharmaceutical cocrystals will be presented, with highlighting on factors affecting cocrystallization which include ∆pKa, donors and acceptors hydrogen bonds, molecular recognition point, synthon forming functional groups flexibility, dicarboxylic acid coformers carbon chain length and solvent effect, as well as and the methods for cocrystal preparation. Additionally, cocrystal characterization, dissolution pattern as well as the commercially available products were discussed.
{"title":"Pharmaceutical cocrystal and their role in improving solid state properties of active pharmaceutical ingredients","authors":"Ameera A Radhi, Iman S Jaafar, Noor S Jaafar, Sarah M Faisal","doi":"10.32947/ajps.v23i2.1019","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1019","url":null,"abstract":"Cocrystallization is an emerging approach for improving physico-chemical characteristics of an active pharmaceutical ingredient (API) for instance dissolution rate, solubility, stability in addition to mechanical \u0000properties without affecting their therapeutic activity. It is of great importance when other approaches like salt or polymorph formation do not encounter the estimated targets. \u0000In this review article, an outline of pharmaceutical cocrystals will be presented, with highlighting on factors affecting cocrystallization which include ∆pKa, donors and acceptors hydrogen bonds, molecular recognition point, synthon forming functional groups flexibility, dicarboxylic acid coformers carbon chain length and solvent effect, as well as and the methods for cocrystal preparation. Additionally, cocrystal characterization, dissolution pattern as well as the commercially available products were discussed.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83543345","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 : 2023-05-22DOI: 10.32947/ajps.v23i2.1018
Omar Mustafa Alghulami, Ghaith A. Jasim, Suzan Yousif Jasim**
Rheumatoid arthritis is an immune-mediated condition that affects synovial joints. Synovial tissue, cartilage, bone, and less frequently extra-articular structures which in turn experience inflammatory changes. Paclitaxel's semi-synthetic equivalent, docetaxel, is an anti-neoplastic drug. Methotrexate is a treatment for early RA and may have a mildly negative impact on peptidyl arginine deiminase type 4 fluorescence test. However, 30% of patients fail to complete treatment within the first year due to resistance or side effects. The synovial membrane of Rheumatoid arthritis patient infiltrated with macrophages and neutrophils that express peptidyl arginine deiminase type 4 which their effect in rheumatoid arthritis pathogenesis lies in the generation of citrullinated neoepitopes that are Anti cyclic citrullinated peptide antibodies-targeted. The purpose of this study: was to assess the anti-inflammatory effects of docetaxel and methotrexate on the joint structure. Methods: Five groups of eight rats were formed from the 40 male Wister rats. Complete Freund’s adjuvant was injected subcutaneously into rats to induce the disease. The first group is control group which was the only group consists of (healthy untreated) rats. Second group was received complete Freund’s adjuvant. 0.5ml of ordinary saline was intraperitoneally administered to both the control and induction groups. Based on a preliminary experiment, the third group was given intraperitoneally 1 mg/kg/on alternative day docetaxel. The fourth group was given intraperitoneally 1 mg/kg/week of Methotrexate. Fifth group was given a half dose of both Methotrexate and docetaxel concurrently. Arthritis index was measured and Knee joint was histopathological examined. Results: significant Arthritis Index decrease in docetaxel group (p≤0.05). Significant lowering Histometric scoring (p≤0.05) in docetaxel, and Methotrexate group (cellular hyperplasia, formation of granulation tissue, infiltration of leukocytes, destroying of cartilage and intensity of erosion & Articular cartilage thickness) level in rats induced arthritis. Conclusion: This study showed that docetaxel may have anti-arthritic effects through their significant lowering Histometric scoring(p≤0.05).
{"title":"Histopathological evaluation of docetaxel effects in treatment of rheumatoid arthritis induced in rat model","authors":"Omar Mustafa Alghulami, Ghaith A. Jasim, Suzan Yousif Jasim**","doi":"10.32947/ajps.v23i2.1018","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1018","url":null,"abstract":"Rheumatoid arthritis is an immune-mediated condition that affects synovial joints. Synovial tissue, cartilage, bone, and less frequently extra-articular structures which in turn experience \u0000inflammatory changes. Paclitaxel's semi-synthetic equivalent, docetaxel, is an anti-neoplastic drug. Methotrexate is a treatment for early RA and may have a mildly negative impact on peptidyl arginine deiminase type 4 fluorescence test. However, 30% of patients fail to complete treatment within the first year due to resistance or side effects. The synovial membrane of Rheumatoid arthritis patient infiltrated with macrophages and neutrophils that express peptidyl arginine deiminase type 4 which their effect in rheumatoid arthritis pathogenesis lies in the generation of citrullinated neoepitopes that are Anti cyclic citrullinated peptide antibodies-targeted. \u0000The purpose of this study: was to assess the anti-inflammatory effects of docetaxel and methotrexate on the joint structure. \u0000Methods: Five groups of eight rats were formed from the 40 male Wister rats. Complete Freund’s adjuvant was injected subcutaneously into rats to induce the disease. The first group is control group which was the only group consists of (healthy untreated) rats. Second group was received complete Freund’s adjuvant. 0.5ml of ordinary saline was intraperitoneally administered to both the control and induction groups. Based on a preliminary experiment, the third group was given intraperitoneally 1 mg/kg/on alternative day docetaxel. The fourth group was given intraperitoneally 1 mg/kg/week of Methotrexate. Fifth group was given a half dose of both Methotrexate and docetaxel concurrently. Arthritis index was measured and Knee joint was histopathological examined. \u0000Results: significant Arthritis Index decrease in docetaxel group (p≤0.05). Significant lowering Histometric scoring (p≤0.05) in docetaxel, and Methotrexate group (cellular hyperplasia, formation of granulation tissue, infiltration of leukocytes, destroying of cartilage and intensity of erosion & Articular cartilage thickness) level in rats induced arthritis. Conclusion: This study showed that docetaxel may have anti-arthritic effects through their significant lowering Histometric scoring(p≤0.05).","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72561471","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 : 2023-05-22DOI: 10.32947/ajps.v23i2.1013
Ghufran salah ahmed, Khadim ali khadim2, Nabeel mudheher talib
Background:Chemotherapy-caused nausea and vomiting is a health problem in cancer patients. Olanzapine is used with serotonin receptor antagonists plus dexamethasone post Neurokinin 1 receptor antagonists as the antiemetic. Objective: The study aimed to determine the efficacy of (5 and 10) mg of olanzapine with antiemetic drugs against chemotherapy-induced nausea and vomiting. Methods: The study groups are Group S: received triple antiemetic therapy aprepitant at (1-3) day, dexamethasone at (1-4) day, and ondansetron only on the first day. Group O5: received olanzapine 5 mg with triple antiemetic therapy aprepitant (1-3) days, dexamethasone (1-4) day, ondansetron the first day, and olanzapine 5 mg (1-4) days. Group O10: received (olanzapine 10 mg with triple antiemetic therapy) aprepitant (1-3) days, dexamethasone (1-4) days, ondansetron day 1, and olanzapine 10 mg (1-4) days. The cancer was diagnosed by mamograph; the MAT score was used to control chemotherapy-caused nausea and vomiting. Results: Higher acute and delayed nausea was observed in group S than in groups O5 and O10. Overall, nausea control was increased in group S than in groups O5 and O10. There was no significant difference between the different study groups. Conclusion: Olanzapine 5 mg and 10 mg could treat nausea more than triple antiemetic in patients with nausea.
{"title":"Therapeutic study of the nausea and vomiting caused by chemotherapy medications by olanzapine to triple antiemetic therapy in Iraqi cancer patients","authors":"Ghufran salah ahmed, Khadim ali khadim2, Nabeel mudheher talib","doi":"10.32947/ajps.v23i2.1013","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1013","url":null,"abstract":"Background:Chemotherapy-caused nausea and vomiting is a health problem in cancer patients. Olanzapine is used with serotonin receptor antagonists plus dexamethasone post Neurokinin 1 receptor antagonists as the antiemetic. \u0000Objective: The study aimed to determine the efficacy of (5 and 10) mg of olanzapine with antiemetic drugs against chemotherapy-induced nausea and vomiting. \u0000Methods: The study groups are Group S: received triple antiemetic therapy aprepitant at (1-3) day, dexamethasone at (1-4) day, and ondansetron only on the first day. Group O5: received olanzapine 5 mg with triple antiemetic therapy aprepitant (1-3) days, dexamethasone (1-4) day, ondansetron the first day, and olanzapine 5 mg (1-4) days. Group O10: received (olanzapine 10 mg with triple antiemetic therapy) aprepitant (1-3) days, dexamethasone (1-4) days, ondansetron day 1, and olanzapine 10 mg (1-4) days. The cancer was diagnosed by mamograph; the MAT score was used to control chemotherapy-caused nausea and vomiting. \u0000Results: Higher acute and delayed nausea was observed in group S than in groups O5 and O10. Overall, nausea control was increased in group S than in groups O5 and O10. There was no significant difference between the different study groups. \u0000Conclusion: Olanzapine 5 mg and 10 mg could treat nausea more than triple antiemetic in patients with nausea.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74838299","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}
Novel 2-amino benzimidazole derivatives containing amide, azide and 1,2,3-triazole moieties have been synthesized. Compound 3 was synthesized by reaction of o-phenylenediamine with p-aminobenzoic acid. Compound 3 was converted into amide by treatment with chloroacetyl chloride to get compound 4. Compound 4 and sodium azide were combined to create compound which has an azide group. Compound 5 was converted into 1,2,3-triazole derivatives by treatment with acetylene derivatives. FTIR, 1H-NMR, and Mass spectra have been used to confirm the chemical structures of various substances. By using a technique called well diffusion agar, the final products were examined in vitro to predict activity against two kinds of gram-positive bacteria and two kinds of gram-negative bacteria as well as the antifungal activity against Candida albicans fungus. All the final products exhibited moderate to potent activity compared to Trimethoprim and Fluconazole as reference antibacterial and antifungal drugs respectively. Swiss ADME was also used to undertake ADME tests to determine the bioavailability, drug-likeness and topological polar surface area of the synthesized molecule. The results showed that every chemical tested was absorbed orally and followed the Lipinski rule.
{"title":"Synthesis, Characterization, ADME Study and Antimicrobial Evaluation of New 1,2,3-triazole Derivatives of 2-phenyl benzimidazole.","authors":"Asmaa Adnan Abdulnabi, Karima Fadhil Ali, Basma M.Abd Razik","doi":"10.32947/ajps.v23i2.1016","DOIUrl":"https://doi.org/10.32947/ajps.v23i2.1016","url":null,"abstract":"Novel 2-amino benzimidazole derivatives containing amide, azide and 1,2,3-triazole moieties have been synthesized. Compound 3 was synthesized by reaction of o-phenylenediamine with p-aminobenzoic acid. Compound 3 was converted into amide by treatment with chloroacetyl chloride to get compound 4. Compound 4 and sodium azide were combined to create compound which has an azide group. Compound 5 was converted into 1,2,3-triazole derivatives by treatment with acetylene derivatives. FTIR, 1H-NMR, and Mass spectra have been used to confirm the chemical structures of various substances. By using a technique called well diffusion agar, the final products were examined in vitro to predict activity against two kinds of gram-positive bacteria and two kinds of gram-negative bacteria as well as the antifungal activity against Candida albicans fungus. All the final products exhibited moderate to potent activity compared to Trimethoprim and Fluconazole as reference antibacterial and antifungal drugs respectively. Swiss ADME was also used to undertake ADME tests to determine the bioavailability, drug-likeness and topological polar surface area of the synthesized molecule. The results showed that every chemical tested was absorbed orally and followed the Lipinski rule.","PeriodicalId":7406,"journal":{"name":"Al Mustansiriyah Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88647805","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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