Pub Date : 2020-10-26DOI: 10.14805/jphchem.2020.art119
D. Karaman, K. Yelekçi, S. Altuntas
The research of ligand-protein interactions with in silico molecular modeling studies on the atomic level gives an opportunity to be understood the pharmacokinetic metabolism of anti-depressant drug candidates. Monoamine oxidase (MAO) enzymes are important targets for the treatment of depressive disorder. MAOs have two isoforms as MAO-A and MAO-B being responsible for catalyzing of neurological amines. In this study a new series of coumarin derivatives were designed for selective and reversible inhibition of MAO-A enzyme. 3rd, 5th and 7th positions were selected to be placed of five different side groups. Docking procedures of each ligand in M series of these novel 125 compounds were executed with 10 runs by using AutoDock4.2 software. Docking results were analyzed via Discovery Studio 3.1 (Biovia Inc.). The most promising compounds were M118 and M123 according to selectivity index, SI (MAO-B/MAO-A)=180 fold and 209 fold and Ki values 7.25 nM and 12.01 nM, respectively. Overall, the current study provided significant knowledge for the development of new anti-depressant drugs.
配体-蛋白质相互作用的研究与硅分子模型在原子水平上的研究为了解抗抑郁候选药物的药代动力学代谢提供了机会。mao有两个同工异构体，分别是MAO-A和MAO-B，负责催化神经胺。选择第3、5、7个位置放置5个不同的边组。利用AutoDock4.2软件对这125个新化合物M系列中的每个配体进行10次对接。对接结果通过Discovery Studio 3.1 (Biovia Inc.)进行分析。总的来说，本研究为新型抗抑郁药物的开发提供了重要的知识。
{"title":"Are Coumarin Derivatives The New Keys in Depression Treatment? In silico Key-lock Fitting Analysis of Coumarin Derivatives with Monoamine Oxidase-A","authors":"D. Karaman, K. Yelekçi, S. Altuntas","doi":"10.14805/jphchem.2020.art119","DOIUrl":"https://doi.org/10.14805/jphchem.2020.art119","url":null,"abstract":"The research of ligand-protein interactions with in silico molecular modeling studies on the atomic level gives an opportunity to be understood the pharmacokinetic metabolism of anti-depressant drug candidates. Monoamine oxidase (MAO) enzymes are important targets for the treatment of depressive disorder. MAOs have two isoforms as MAO-A and MAO-B being responsible for catalyzing of neurological amines. In this study a new series of coumarin derivatives were designed for selective and reversible inhibition of MAO-A enzyme. 3rd, 5th and 7th positions were selected to be placed of five different side groups. Docking procedures of each ligand in M series of these novel 125 compounds were executed with 10 runs by using AutoDock4.2 software. Docking results were analyzed via Discovery Studio 3.1 (Biovia Inc.). The most promising compounds were M118 and M123 according to selectivity index, SI (MAO-B/MAO-A)=180 fold and 209 fold and Ki values 7.25 nM and 12.01 nM, respectively. Overall, the current study provided significant knowledge for the development of new anti-depressant drugs.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"312 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-10-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79695592","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-08-15DOI: 10.18231/j.ijpca.2020.015
Yamuna Choudhary, A. Goyal, R. Vaishnav
Process validation is an essential part for the safety and quality of the drug products. Validation act as guidance that is intended to assist manufacturers in understanding quality management system requirements concerning process validation. It is a fundamental component for assuring the quality system used by pharmaceutical industries. Process validation is the key element to ensure the identity, purity, safety, and efficacy of drug products. The process validation of Prasugrel Hydrochloride Tablet USP precisely focused on the aim and method of analysis. The emphasis will be on the practical inspectional requirement, rather than on a theoretical approach that does not reflect the practicalities encountered when validating actual production operations. The Process validation reduces product recalls and troubleshooting assignments which results in more economical manufacturing process and quality products. In this paper an overview is given on process validation with special reference to solid dosage form of Prasugrel Hydrochloride Tablet USP containing dose of 10 mg. Keywords: Prasugrel Hydrochloride, Process validation, Product recalls, Quality products.
{"title":"Process validation of prasugrel hydrochloride tablet USP","authors":"Yamuna Choudhary, A. Goyal, R. Vaishnav","doi":"10.18231/j.ijpca.2020.015","DOIUrl":"https://doi.org/10.18231/j.ijpca.2020.015","url":null,"abstract":"Process validation is an essential part for the safety and quality of the drug products. Validation act as\u0000guidance that is intended to assist manufacturers in understanding quality management system requirements\u0000concerning process validation. It is a fundamental component for assuring the quality system used by\u0000pharmaceutical industries. Process validation is the key element to ensure the identity, purity, safety, and\u0000efficacy of drug products. The process validation of Prasugrel Hydrochloride Tablet USP precisely focused\u0000on the aim and method of analysis. The emphasis will be on the practical inspectional requirement, rather\u0000than on a theoretical approach that does not reflect the practicalities encountered when validating actual\u0000production operations. The Process validation reduces product recalls and troubleshooting assignments\u0000which results in more economical manufacturing process and quality products. In this paper an overview is\u0000given on process validation with special reference to solid dosage form of Prasugrel Hydrochloride Tablet\u0000USP containing dose of 10 mg.\u0000\u0000Keywords: Prasugrel Hydrochloride, Process validation, Product recalls, Quality products.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"1 1","pages":"98-103"},"PeriodicalIF":0.0,"publicationDate":"2020-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83116416","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-08-15DOI: 10.18231/j.ijpca.2020.009
A. S. Bisht, J. Negi, D. K. Sharma
Quinazoline is a compound with amalgamated heterocyclic system popular for their biological activities. Quinazoline is a compound made up six membered fused aromatic rings i,e a benzene ring with pyrimidine ring. Its chemical formula is C8H6N2O. It is yellow colour and found in the crystalline form. Molecular optimization of potentially lead compounds through a chemist is an needy and upcomming approach for the discovery of new pharmaceuticals. More than two combinations of pharmacophore and making them one moiety is a noval and popular procedure of exploitation of synthesis now a days and this cause an additive increment of biological activities with taking away of surplus side effects. Present communication studies about the structure origin, diversity and chemical modification with change in pharmacological activities of Quinazoline. Keywords: Quinazoline, Molecular modification, Pharmaceuticals, Pharmacological activity.
{"title":"Chemistry and activity of quinazoline moiety: A systematic review study","authors":"A. S. Bisht, J. Negi, D. K. Sharma","doi":"10.18231/j.ijpca.2020.009","DOIUrl":"https://doi.org/10.18231/j.ijpca.2020.009","url":null,"abstract":"Quinazoline is a compound with amalgamated heterocyclic system popular for their biological activities.\u0000Quinazoline is a compound made up six membered fused aromatic rings i,e a benzene ring with pyrimidine\u0000ring. Its chemical formula is C8H6N2O. It is yellow colour and found in the crystalline form. Molecular\u0000optimization of potentially lead compounds through a chemist is an needy and upcomming approach for the\u0000discovery of new pharmaceuticals. More than two combinations of pharmacophore and making them one\u0000moiety is a noval and popular procedure of exploitation of synthesis now a days and this cause an additive\u0000increment of biological activities with taking away of surplus side effects. Present communication studies\u0000about the structure origin, diversity and chemical modification with change in pharmacological activities\u0000of Quinazoline.\u0000\u0000Keywords: Quinazoline, Molecular modification, Pharmaceuticals, Pharmacological activity.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"41 1","pages":"61-65"},"PeriodicalIF":0.0,"publicationDate":"2020-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85564471","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-08-15DOI: 10.18231/j.ijpca.2020.012
Dalia Mohsen, K. A. Awam, Soheir A. A. Hagras, Mohammed H Fagir
As microbes are massively risky and have gotten to be safe to about all advertised anti-microbials. Withinthe period of anti-microbial resistance, antimicrobial of natural origin give an successful and cheap alternative for combating resistant strains of Gram negative microorganisms which induce pneumonia e.g. (P. aeruginosa) Pseudomonas aeruginosa and (K. pneumoniae) Klebsiella pneumoniae. Cefotaxime is an antimicrobial used in control and treatment of anaerobic bacteria which may be administered with Gentamicin within the treatment of blended contaminations caused by anaerobic and oxygen consuming living beings. Combination treatment has corresponding components of activity. Gentamicin is bactericidal aminoglycoside antibiotic used mainly against Gram negative bacteria. Allium sativum in garlic extract has been known to have inhibitory action & and valuable as helpful specialist against numerous pathological diseases. Expanding Multidrug resistance of pathogens strengths to discover elective strategies for treatment of irresistible infections. Methods: Ethical approval: Protocols were approved by the IRB of the Scientific Research Unit (SRU) at Inaya Medical College (IMC) RIYADH (KSA) Results: In-vitro and in-vivo antibacterial presented effect for combination of antibiotics and FGE for fourteen days. Indicated a significant (p homogenate. Our data showed that FGH combined antibiotics could protect the liver and kidney against the histopathological and histochemical changes by blocking oxidative damages in addition to restorement of the antioxidant enzymatic profile. Conclusion: FGE displayed the best effect on administration one hour before gentamicin and cefotaxime due to its anti-inflammatory and antioxidant effects. Moreover, the potential use of FGE as a prophylactic agent against multi drug resistant bacteria. Keywords: Pneumonia related infections, Gentamicin, Cefotaxime, Garlic, Histochemical and histopathological.
{"title":"In vivo antimicrobial efficiency of garlic extract against pulmonary infections; Histopathological and Biochemical study","authors":"Dalia Mohsen, K. A. Awam, Soheir A. A. Hagras, Mohammed H Fagir","doi":"10.18231/j.ijpca.2020.012","DOIUrl":"https://doi.org/10.18231/j.ijpca.2020.012","url":null,"abstract":"As microbes are massively risky and have gotten to be safe to about all advertised anti-microbials.\u0000Withinthe period of anti-microbial resistance, antimicrobial of natural origin give an successful and cheap\u0000alternative for combating resistant strains of Gram negative microorganisms which induce pneumonia e.g.\u0000(P. aeruginosa) Pseudomonas aeruginosa and (K. pneumoniae) Klebsiella pneumoniae. Cefotaxime is\u0000an antimicrobial used in control and treatment of anaerobic bacteria which may be administered with\u0000Gentamicin within the treatment of blended contaminations caused by anaerobic and oxygen consuming\u0000living beings. Combination treatment has corresponding components of activity. Gentamicin is bactericidal\u0000aminoglycoside antibiotic used mainly against Gram negative bacteria. Allium sativum in garlic extract has\u0000been known to have inhibitory action & and valuable as helpful specialist against numerous pathological\u0000diseases. Expanding Multidrug resistance of pathogens strengths to discover elective strategies for\u0000treatment of irresistible infections.\u0000Methods: Ethical approval: Protocols were approved by the IRB of the Scientific Research Unit (SRU) at\u0000Inaya Medical College (IMC) RIYADH (KSA)\u0000Results: In-vitro and in-vivo antibacterial presented effect for combination of antibiotics and FGE for\u0000fourteen days. Indicated a significant (p \u0000homogenate. Our data showed that FGH combined antibiotics could protect the liver and kidney against\u0000the histopathological and histochemical changes by blocking oxidative damages in addition to restorement\u0000of the antioxidant enzymatic profile.\u0000Conclusion: FGE displayed the best effect on administration one hour before gentamicin and cefotaxime\u0000due to its anti-inflammatory and antioxidant effects. Moreover, the potential use of FGE as a prophylactic\u0000agent against multi drug resistant bacteria.\u0000\u0000Keywords: Pneumonia related infections, Gentamicin, Cefotaxime, Garlic, Histochemical and histopathological.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"40 1","pages":"74-83"},"PeriodicalIF":0.0,"publicationDate":"2020-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81154954","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-08-15DOI: 10.18231/j.ijpca.2020.010
Shripad Potadar, R. Kotnal
A new series new N’-(3-hydroxy-3,4-dihydroquinoxaline-2-carbonyl)-N-phenylcarbamimidic acid derivatives were designed and synthesized. The newly synthesized compounds were evaluated for their anti-tb activity. The structure of the synthesized compounds was confirmed by elemental analysis and spectral data (IR, 1H NMR and Mass). The data obtained from biological screening revealed that; synthesized compounds showed the good to moderate anti-tb activities. Keywords: Quinoxaline, Orthophenylenediamine, Alloxane and antimycobacterial.
{"title":"Synthesis and Anti tubercular activity of some new N’-(3-hydroxy-3, 4-dihydroquinoxaline-2-carbonyl)-N-phenylcarbamimidic acid derivatives","authors":"Shripad Potadar, R. Kotnal","doi":"10.18231/j.ijpca.2020.010","DOIUrl":"https://doi.org/10.18231/j.ijpca.2020.010","url":null,"abstract":"A new series new N’-(3-hydroxy-3,4-dihydroquinoxaline-2-carbonyl)-N-phenylcarbamimidic acid\u0000derivatives were designed and synthesized. The newly synthesized compounds were evaluated for\u0000their anti-tb activity. The structure of the synthesized compounds was confirmed by elemental analysis\u0000and spectral data (IR, 1H NMR and Mass). The data obtained from biological screening revealed that;\u0000synthesized compounds showed the good to moderate anti-tb activities.\u0000\u0000Keywords: Quinoxaline, Orthophenylenediamine, Alloxane and antimycobacterial.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"530 1","pages":"66-68"},"PeriodicalIF":0.0,"publicationDate":"2020-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77099149","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-08-15DOI: 10.18231/j.ijpca.2020.011
D. A. Patil, G. Patil, Jitendra K. Sonawane, Z. Khan
The goal of this study is to carry out degradation studies of Levocetirizine market-available tablet brands. Forced degradation is the process which involves degradation of the drug products which can be studied to determine the molecule’s stability. Various brands of levocetirizine dihydrochloride (Okacet-L, LECOPE, Levocet, 1-AL) were used. It is an H1 receptor antagonist and is used in the treatment of persistent or seasonal allergic rhinitis and chronic idiopathic urticaria. As per ICH recommendations, this drug has been subject to various stress conditions during the study. In the presence of degradation products, an ultraviolet spectroscopic (UV) method for drug analysis has been developed. The pH 7.0 phosphate buffer was used as solvent. The amount of degraded drug was determined by taking the 230 nm absorbance. All products have been degraded under conditions of acidic, oxidation, photolytic and thermal degradation, and less degraded in alkaline conditions. In all conditions of degradation the tablet of brands Levocet and LECOPE showed less degradation than the brand name tablets Okacet-L and 1-AL. Keywords: Levocetirizine dihydrochloride, Degradation studies, Different brands, UV-spectrophotometer.
{"title":"Forced degradation study of different brands of levocetirizine dihydrochloride by UV-spectroscopy","authors":"D. A. Patil, G. Patil, Jitendra K. Sonawane, Z. Khan","doi":"10.18231/j.ijpca.2020.011","DOIUrl":"https://doi.org/10.18231/j.ijpca.2020.011","url":null,"abstract":"The goal of this study is to carry out degradation studies of Levocetirizine market-available tablet brands.\u0000Forced degradation is the process which involves degradation of the drug products which can be studied to\u0000determine the molecule’s stability. Various brands of levocetirizine dihydrochloride (Okacet-L, LECOPE,\u0000Levocet, 1-AL) were used. It is an H1 receptor antagonist and is used in the treatment of persistent or\u0000seasonal allergic rhinitis and chronic idiopathic urticaria. As per ICH recommendations, this drug has been\u0000subject to various stress conditions during the study. In the presence of degradation products, an ultraviolet\u0000spectroscopic (UV) method for drug analysis has been developed. The pH 7.0 phosphate buffer was used as\u0000solvent. The amount of degraded drug was determined by taking the 230 nm absorbance. All products have\u0000been degraded under conditions of acidic, oxidation, photolytic and thermal degradation, and less degraded\u0000in alkaline conditions. In all conditions of degradation the tablet of brands Levocet and LECOPE showed\u0000less degradation than the brand name tablets Okacet-L and 1-AL.\u0000\u0000Keywords: Levocetirizine dihydrochloride, Degradation studies, Different brands, UV-spectrophotometer.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"80 1","pages":"69-73"},"PeriodicalIF":0.0,"publicationDate":"2020-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90555031","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-08-15DOI: 10.18231/j.ijpca.2020.016
A. Shetti, Ravi Solabannavar, Veena P. Munavalli
Myocardial infarction is a crucial and commonly seen in the Indian population. The disease is prevalent in both rural and urban area. Timely detection, awareness of the myocardial infarction among the population especially rural Indians should be taken seriously. Here we discuss an unusual case of myocardial infarction. Keywords: Pain, Myocardial infarction, Angiography, Angioplasty.
{"title":"An unusual case of unstable angina - The timely intervention !!!","authors":"A. Shetti, Ravi Solabannavar, Veena P. Munavalli","doi":"10.18231/j.ijpca.2020.016","DOIUrl":"https://doi.org/10.18231/j.ijpca.2020.016","url":null,"abstract":"Myocardial infarction is a crucial and commonly seen in the Indian population. The disease is prevalent in\u0000both rural and urban area. Timely detection, awareness of the myocardial infarction among the population\u0000especially rural Indians should be taken seriously. Here we discuss an unusual case of myocardial infarction.\u0000\u0000Keywords: Pain, Myocardial infarction, Angiography, Angioplasty.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"14 1","pages":"104-106"},"PeriodicalIF":0.0,"publicationDate":"2020-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77799094","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-07-24DOI: 10.18231/j.ijpca.2020.014
D. Trivedi, A. Goyal
Dexketoprofen Trometamol is a NSAID, used as an analgesic and anti-inflammatory drug. It works by blocking the action of cyclo-oxygenase in the body. Conventional route of delivery has many drawbacks such as hepatic first-pass metabolism, reduced bioavailability, and fluctuating drug concentrations in the blood. These problems can be overcome by development of transdermal drug delivery system. The objective of this study was to develop and evaluate the transdermal patches of the drug Dexketoprofen Trometamol. The patches were prepared by solvent casting method using polymers; Ethyl cellulose, HPMC and ERS 100 in different ratios. The prepared formulations were uniform in their physical characteristics. The formulation F6, combination of polymer (HPMC: EC in ratio 4:1) showed maximum release of 85.77% in 24 hours. The resultant data was fitted in to zero, first, Higuchi and Peppas model. The results specify that Dexketoprofen Trometamol transdermal patch can be designed for obtaining better therapeutic benefits. Keywords: Transdermal drug delivery system, TDDS, Skin patches, Kinetics, NSAIDs, Analgesic, Invitro and exvivo drug release.
{"title":"Formulation and evaluation of transdermal patches containing dexketoprofen trometamol","authors":"D. Trivedi, A. Goyal","doi":"10.18231/j.ijpca.2020.014","DOIUrl":"https://doi.org/10.18231/j.ijpca.2020.014","url":null,"abstract":"Dexketoprofen Trometamol is a NSAID, used as an analgesic and anti-inflammatory drug. It works by\u0000blocking the action of cyclo-oxygenase in the body. Conventional route of delivery has many drawbacks\u0000such as hepatic first-pass metabolism, reduced bioavailability, and fluctuating drug concentrations in the\u0000blood. These problems can be overcome by development of transdermal drug delivery system. The objective\u0000of this study was to develop and evaluate the transdermal patches of the drug Dexketoprofen Trometamol.\u0000The patches were prepared by solvent casting method using polymers; Ethyl cellulose, HPMC and ERS\u0000100 in different ratios.\u0000The prepared formulations were uniform in their physical characteristics. The formulation F6, combination\u0000of polymer (HPMC: EC in ratio 4:1) showed maximum release of 85.77% in 24 hours. The resultant data\u0000was fitted in to zero, first, Higuchi and Peppas model. The results specify that Dexketoprofen Trometamol\u0000transdermal patch can be designed for obtaining better therapeutic benefits.\u0000\u0000Keywords: Transdermal drug delivery system, TDDS, Skin patches, Kinetics, NSAIDs, Analgesic, Invitro and exvivo drug release.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"60 1","pages":"87-97"},"PeriodicalIF":0.0,"publicationDate":"2020-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78168032","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-05-15DOI: 10.18231/j.ijpca.2020.005
Dinesh P Kawade, D. Chaple, P. Khedekar
A POCl3 catalyzed, efficient, one-step and solvent-free synthesis of novel thieno [2,3-d] pyrimidin-4(3H)-one derivatives from 2-amino-4,5-substitutedthiophene-3-carbonitrile has been developed using various aliphatic acid under both conventional heating and microwave irradiation techniques. The formation of compounds was confirmed via elemental analysis and spectroscopic techniques like FTIR, 1HNMR and mass spectroscopy. All synthesized compounds have been screened for their analgesic activity by using Eddy´s hot plate method. The synthesized compounds 2d, 2k and 2h showed good analgesic activity and compounds 2a, 2b, 2g and 2i showed moderate whereas remaining compounds possessed less analgesic activity compared with standard, Tramadol. Keywords: POCl3, Thieno[2,3-d]pyrimidin-4 (3H)-one, Analgesic activity, Eddy´s hot plate.
{"title":"Synthesis, physicochemical characterization and analgesic evaluation of some new thieno [2,3-D] Pyrimidin 4(3H) one derivatives","authors":"Dinesh P Kawade, D. Chaple, P. Khedekar","doi":"10.18231/j.ijpca.2020.005","DOIUrl":"https://doi.org/10.18231/j.ijpca.2020.005","url":null,"abstract":"A POCl3 catalyzed, efficient, one-step and solvent-free synthesis of novel thieno [2,3-d] pyrimidin-4(3H)-one derivatives from 2-amino-4,5-substitutedthiophene-3-carbonitrile has been developed using various aliphatic acid under both conventional heating and microwave irradiation techniques. The formation of compounds was confirmed via elemental analysis and spectroscopic techniques like FTIR, 1HNMR and mass spectroscopy. All synthesized compounds have been screened for their analgesic activity by using Eddy´s hot plate method. The synthesized compounds 2d, 2k and 2h showed good analgesic activity and compounds 2a, 2b, 2g and 2i showed moderate whereas remaining compounds possessed less analgesic activity compared with standard, Tramadol. \u0000\u0000Keywords: POCl3, Thieno[2,3-d]pyrimidin-4 (3H)-one, Analgesic activity, Eddy´s hot plate.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"28 1","pages":"32-38"},"PeriodicalIF":0.0,"publicationDate":"2020-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81446276","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-05-15DOI: 10.18231/j.ijpca.2020.004
Rahul Chaudhari, A. V. Ganorkar, Madhura P. Dixit, M. Umekar
The aim of the research work was to develop a method for comparative evaluation of dissolution profile of two different brands of Teneligliptin hydrobromide hydrate drug in its formulations containing using UV Spectrophotometer. Simple, precise and accurate UV-spectrophotometric method was developed for Teneligliptin hydrobromide hydrate using optimized dissolution parameters like as 900mL of Phosphate buffer pH 6.8 as a dissolution medium and paddle (type II) apparatus at a stirring rate of 100 rpm. The drug release was evaluated by UV spectrophotometric method using 243.2nm as detection wavelength. Developed method obeyed Beer’s-Lambert’s law in the concentration range of 0.5-25 ?g/mL, with correlation coefficient value less than 1. The percent drug amount released estimated by proposed method was nearly 100%, found to be in good agreement with label claim of marketed tablet formulation. The proposed method were validated as per ICH guidelines with respect to accuracy, precision, LOD, LOQ and found to be within limits. The proposed method can be adopted for routine quality control test for estimation of drug in formulation. Also the statistical data analysis of percent drug release of brand 1 and 2 were compared with preexisting dissolution data of literature by using F-test and t-test. Keywords: Teneligliptin hydrobromide, Spectrophotometric method.
{"title":"Comparative evaluation of dissolution profile of drug in its formulation by UV spectrophotometry","authors":"Rahul Chaudhari, A. V. Ganorkar, Madhura P. Dixit, M. Umekar","doi":"10.18231/j.ijpca.2020.004","DOIUrl":"https://doi.org/10.18231/j.ijpca.2020.004","url":null,"abstract":"The aim of the research work was to develop a method for comparative evaluation of dissolution profile of two different brands of Teneligliptin hydrobromide hydrate drug in its formulations containing using UV Spectrophotometer. Simple, precise and accurate UV-spectrophotometric method was developed for Teneligliptin hydrobromide hydrate using optimized dissolution parameters like as 900mL of Phosphate buffer pH 6.8 as a dissolution medium and paddle (type II) apparatus at a stirring rate of 100 rpm. The drug release was evaluated by UV spectrophotometric method using 243.2nm as detection wavelength. Developed method obeyed Beer’s-Lambert’s law in the concentration range of 0.5-25 ?g/mL, with correlation coefficient value less than 1. The percent drug amount released estimated by proposed method was nearly 100%, found to be in good agreement with label claim of marketed tablet formulation. The proposed method were validated as per ICH guidelines with respect to accuracy, precision, LOD, LOQ and found to be within limits. The proposed method can be adopted for routine quality control test for estimation of drug in formulation. Also the statistical data analysis of percent drug release of brand 1 and 2 were compared with preexisting dissolution data of literature by using F-test and t-test.\u0000\u0000Keywords: Teneligliptin hydrobromide, Spectrophotometric method.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"14 1","pages":"26-31"},"PeriodicalIF":0.0,"publicationDate":"2020-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82503297","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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