Satyansh Singh, P. Yadav, Priyanshu Mishra, Asgar Shameem, Deepak Yadav
The process of drug development is very expensive process due to high costs of R&D and human clinical tests. At present a new approach is being tried to understand how disease and infection are controlled at the molecular and physiological level and to target specific entities based on the knowledge. The drugs discoveries are based on molecular biological targets and improve the therapy for disease, wide ranging dosages of the compounds are introduced to the cell line or animal in order to obtain preliminary efficacy and pharmacokinetic information. The process of drug discovery involves the identification of candidates, synthesis, characterization, screening & assay for therapeutic efficacy. Once a compound has shown its value in these tests, it will begin the process of drug development prior to clinical trials.
{"title":"Drug Discovery","authors":"Satyansh Singh, P. Yadav, Priyanshu Mishra, Asgar Shameem, Deepak Yadav","doi":"10.33513/ppps/2001-20","DOIUrl":"https://doi.org/10.33513/ppps/2001-20","url":null,"abstract":"The process of drug development is very expensive process due to high costs of R&D and human clinical tests. At present a new approach is being tried to understand how disease and infection are controlled at the molecular and physiological level and to target specific entities based on the knowledge. The drugs discoveries are based on molecular biological targets and improve the therapy for disease, wide ranging dosages of the compounds are introduced to the cell line or animal in order to obtain preliminary efficacy and pharmacokinetic information. The process of drug discovery involves the identification of candidates, synthesis, characterization, screening & assay for therapeutic efficacy. Once a compound has shown its value in these tests, it will begin the process of drug development prior to clinical trials.","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"5 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2020-05-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"116945667","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}
Piperacillin/Tazobactam otherwise known as Zosyn is a broad-spectrum combination antibiotic used to treat severe infections. It combines the high antibiotic activity of piperacillin with β-lactamase inhibitor properties of tazobactam that helps to restore the susceptibility of bacteria to the antibiotic and prevents resistance. Despite this interesting pharmacological profile, Zosyn is given intravenously because of its poor oral
{"title":"Formulation and Comparative Characterization of Methylcellulose, Carbomer and Petrolatum Gels for Topical and Transdermal Delivery of Zosyn (Piperacillin/Tazobactam) Antibiotics","authors":"K. Yeboah, Ocimum Scientific Publishers Pty Ltd","doi":"10.33513/ppps/2001-19","DOIUrl":"https://doi.org/10.33513/ppps/2001-19","url":null,"abstract":"Piperacillin/Tazobactam otherwise known as Zosyn is a broad-spectrum combination antibiotic used to treat severe infections. It combines the high antibiotic activity of piperacillin with β-lactamase inhibitor properties of tazobactam that helps to restore the susceptibility of bacteria to the antibiotic and prevents resistance. Despite this interesting pharmacological profile, Zosyn is given intravenously because of its poor oral","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"56 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2020-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123772578","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}
Correspondence should be addressed to Antoine Al-Achi, USA E-mail: alachi@campbell.edu Since ancient times botanicals that affected moods and produced a feeling of relaxation have been used as sleep aids (for insomnia), to overcome anxiety, and to induce stillness [1]. A list of these plants, along with their chemical composition, is found in table 1. Specific therapeutic applications of psychoactive botanicals include their use for insomnia, as anti-depressive agents, to induce an anxiolytic action, as a treatment for headaches and migraines, to control menopausal symptoms associated with mood issues, and for various neurodegenerative diseases, among others (Table 2). Copyright
{"title":"Psychoactive Botanicals and Their Constituents: A Brief Review","authors":"Ocimum Scientific Publishers Pty Ltd","doi":"10.33513/ppps/1901-18","DOIUrl":"https://doi.org/10.33513/ppps/1901-18","url":null,"abstract":"Correspondence should be addressed to Antoine Al-Achi, USA E-mail: alachi@campbell.edu Since ancient times botanicals that affected moods and produced a feeling of relaxation have been used as sleep aids (for insomnia), to overcome anxiety, and to induce stillness [1]. A list of these plants, along with their chemical composition, is found in table 1. Specific therapeutic applications of psychoactive botanicals include their use for insomnia, as anti-depressive agents, to induce an anxiolytic action, as a treatment for headaches and migraines, to control menopausal symptoms associated with mood issues, and for various neurodegenerative diseases, among others (Table 2). Copyright","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"61 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"125886586","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}
Inclusion complex can enhance the drug solubility, stability, and masking smell. Cyclodextrin (CD) is a commonly used host molecule for inclusion, with three main types of CD, exist, α, β, and γ. They are classified based on their chemical structure. The derivative of β-CD, (Hydroxypropyl-βCyclodextrin; HP-β-CD), is widely used in pharmaceutical formulations. HP-β-CD works by a dynamic equilibrium process for inclusion. Nifedipine is a Class II drug (Biopharmaceutical Classification System) that has poor solubility in water, and high permeability through the cellular membrane. The Phase-solubility profile of nifedipine/HP-β-CD complex showed an AL type (according to Higuchi and Connors' method) indicating a complex ratio of 1:1. The objective of this study was to investigate the pH effect on the inclusion process of nifedipine/HP-β-CD. The results of this study showed that ionization pH conditions improved nifedipine solubility in water to a limited extent however it was not as efficient as the unionization pH conditions since unionization conditions produced higher Complexation Efficiency (CE) and the stability constant (K1:1) value. Therefore, maintaining the drug in a unionized form is perhaps a more efficient way of producing inclusion complex with HP-β-CD. In order to characterize the inclusion complex thus formed between the drug and HP-β-CD, a solvent evaporation method was used to prepare the complex which was compared to a physical mixture, pure drug, and pure HP-β-CD. Significant differences were found to exist between the inclusion complex and all the other groups based on the TGADSC, ATR, and PXRD analysis.
{"title":"Investigation on Complexation Efficiency of Hp-β-Cd/ Nifedipine Complex: pH Effect","authors":"Ocimum Scientific Publishers Pty Ltd","doi":"10.33513/ppps/1901-15","DOIUrl":"https://doi.org/10.33513/ppps/1901-15","url":null,"abstract":"Inclusion complex can enhance the drug solubility, stability, and masking smell. Cyclodextrin (CD) is a commonly used host molecule for inclusion, with three main types of CD, exist, α, β, and γ. They are classified based on their chemical structure. The derivative of β-CD, (Hydroxypropyl-βCyclodextrin; HP-β-CD), is widely used in pharmaceutical formulations. HP-β-CD works by a dynamic equilibrium process for inclusion. Nifedipine is a Class II drug (Biopharmaceutical Classification System) that has poor solubility in water, and high permeability through the cellular membrane. The Phase-solubility profile of nifedipine/HP-β-CD complex showed an AL type (according to Higuchi and Connors' method) indicating a complex ratio of 1:1. The objective of this study was to investigate the pH effect on the inclusion process of nifedipine/HP-β-CD. The results of this study showed that ionization pH conditions improved nifedipine solubility in water to a limited extent however it was not as efficient as the unionization pH conditions since unionization conditions produced higher Complexation Efficiency (CE) and the stability constant (K1:1) value. Therefore, maintaining the drug in a unionized form is perhaps a more efficient way of producing inclusion complex with HP-β-CD. In order to characterize the inclusion complex thus formed between the drug and HP-β-CD, a solvent evaporation method was used to prepare the complex which was compared to a physical mixture, pure drug, and pure HP-β-CD. Significant differences were found to exist between the inclusion complex and all the other groups based on the TGADSC, ATR, and PXRD analysis.","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"129018510","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}
{"title":"Lithium as a Dietary Supplement","authors":"Ocimum Scientific Publishers Pty Ltd","doi":"10.33513/ppps/1901-16","DOIUrl":"https://doi.org/10.33513/ppps/1901-16","url":null,"abstract":"","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-09-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"120955293","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}
{"title":"Retrospective Evaluation of Doxycycline versus Azithromycin in Non-Intensive Care Unit Veterans Hospitalized with Community-Acquired Pneumonia","authors":"Ocimum Scientific Publishers Pty Ltd","doi":"10.33513/PPPS/1901-14","DOIUrl":"https://doi.org/10.33513/PPPS/1901-14","url":null,"abstract":"","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"29 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-08-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121552741","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}
{"title":"Preparation of Metronidazole Containing Film Dosage Forms from Sodium Alginate","authors":"Ocimum Scientific Publishers Pty Ltd","doi":"10.33513/PPPS/1901-13","DOIUrl":"https://doi.org/10.33513/PPPS/1901-13","url":null,"abstract":"","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128625019","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}
{"title":"Cardiovascular Outcomes in Patients Over 75 Years of Age Taking a Statin For Primary Prevention","authors":"Ocimum Scientific Publishers Pty Ltd","doi":"10.33513/PPPS/1901-12","DOIUrl":"https://doi.org/10.33513/PPPS/1901-12","url":null,"abstract":"","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"70 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114067892","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}
Solid dosage forms, such as tablets, are widespread in practice. This is due to the ease of administration and capability of mass production by the pharmaceutical industry. Tablet formulation consists of the active ingredient along with fillers that serve various functions in the product. Tablets are prepared on machines known as presses. Material to be compacted is ready by either dry or wet methods. The United States Pharmacopeia lists tests to be performed on the finished products. A description of tablets, their characteristics, preparation, and quality control tests applied to them is the subject of this brief review.
{"title":"Tablets: A Brief Overview","authors":"Ocimum Scientific Publishers Pty Ltd","doi":"10.33513/PPPS/1901-10","DOIUrl":"https://doi.org/10.33513/PPPS/1901-10","url":null,"abstract":"Solid dosage forms, such as tablets, are widespread in practice. This is due to the ease of administration and capability of mass production by the pharmaceutical industry. Tablet formulation consists of the active ingredient along with fillers that serve various functions in the product. Tablets are prepared on machines known as presses. Material to be compacted is ready by either dry or wet methods. The United States Pharmacopeia lists tests to be performed on the finished products. A description of tablets, their characteristics, preparation, and quality control tests applied to them is the subject of this brief review.","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"64 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114200828","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}
Janhvi Dureja, R. Chadha, Maninder, Karan, Akshita Jindal, K. Chadha
Objective: The present work reports the existence of polymorphism in metformin free base applying virtual and experimental approach. Methods: The experimental screening of various polymorphs of metformin free base has been coupled with virtual approach resulting in isolation of three distinct crystal phases from different solvents/ or solvent mixtures. The virtual screening of polymorphs was performed using Polymorph Predictor module of BIOVIA Material Studio (MS) software. A state-of-the-art approach was undertaken utilizing integrated molecular modeling and Monte Carlo simulation technology. The sophisticated tools were used to characterize the experimentally isolated forms such as Differential Scanning Calorimetry (DSC), Fourier Transform Infra-Red Spectroscopy (FTIR), Powder X Ray Diffraction (PXRD) and optical microscopy. Lattice energy landscape was examined to look for these observed forms. Crystal morphology study was conducted to analyse Morphologically Important (MI) facets. Results: A list of potential polymorphs of the drug molecule was generated with varied lattice constants using MS. Crystal energy landscape obtained from the study provided systematic energy ranking to the polymorphs. DSC of these forms exhibited endothermic peaks at 134.01, 111.24 and 79.84°C respectively indicating them to be different forms of metformin base. Structure determination from powder patterns showed that although all the forms, form I, II and III crystallize out in same triclinic space group, P-1 but they possessed different crystallographic parameters and hydrogen bonding patterns. The predicted results were quite complacent with experimental observations with respect to lattice parameters. The three observed forms have been found as local minima in the lattice energy landscape of potential polymorphs. Conclusion: The study explained the practical relevance of Crystal Structure Prediction (CSP) in studying the potential polymorphs of a drug molecule by successfully predicting various polymorphs of metformin free base. Out of all predicted polymorphs, three polymorphs were actually isolated experimentally. The information generated about the existence of multiple forms of metformin free base provides an opportunity to select and scale-up the desired crystal form well suited on bioavailability and stability grounds. The process can be escalated further to preclinical study, to emerge as an invaluable technology in future in increasing the efficiency of drug development process.
目的:应用虚拟和实验方法报道二甲双胍游离基基因多态性的存在。方法:实验筛选二甲双胍游离碱的各种多晶型，并结合虚拟方法，从不同的溶剂/或溶剂混合物中分离出三种不同的晶相。利用BIOVIA Material Studio (MS)软件的Polymorph Predictor模块对多态进行虚拟筛选。采用综合分子建模和蒙特卡罗模拟技术，采用了最先进的方法。利用先进的工具，如差示扫描量热法(DSC)、傅里叶变换红外光谱法(FTIR)、粉末X射线衍射(PXRD)和光学显微镜，对实验分离的形式进行了表征。为了寻找这些观察到的形式，研究了晶格能量图。晶体形态学研究分析了形态学重要面(MI)。结果:利用质谱法生成了具有不同晶格常数的药物分子的潜在多晶型序列，并对多晶型进行了系统的能量排序。这三种形式的DSC分别在134.01、111.24和79.84℃处出现吸热峰，表明它们是不同形式的二甲双胍碱。粉末形貌的结构测定表明，虽然形态1、形态2和形态3种在相同的三斜空间群P-1中结晶，但它们具有不同的结晶学参数和氢键模式。在晶格参数方面，预测结果与实验观测结果相当吻合。这三种观察到的形式被发现为潜在多晶的晶格能量景观的局部极小值。结论:本研究成功预测了二甲双胍游离碱的多种多态性，说明了晶体结构预测(CSP)在研究药物分子潜在多态性中的实际意义。在所有预测的多态性中，有三个多态性实际上是通过实验分离出来的。关于二甲双胍游离碱存在多种形式的信息为选择和扩大理想的晶体形式提供了机会，这种晶体形式非常适合生物利用度和稳定性。该过程可以进一步升级到临床前研究，成为未来提高药物开发过程效率的宝贵技术。
{"title":"A Study Showcasing Crystal Medley of Metformin Free Base: Virtual and Experimental Insights","authors":"Janhvi Dureja, R. Chadha, Maninder, Karan, Akshita Jindal, K. Chadha","doi":"10.33513/ppps/1801-07","DOIUrl":"https://doi.org/10.33513/ppps/1801-07","url":null,"abstract":"Objective: The present work reports the existence of polymorphism in metformin free base applying virtual and experimental approach. Methods: The experimental screening of various polymorphs of metformin free base has been coupled with virtual approach resulting in isolation of three distinct crystal phases from different solvents/ or solvent mixtures. The virtual screening of polymorphs was performed using Polymorph Predictor module of BIOVIA Material Studio (MS) software. A state-of-the-art approach was undertaken utilizing integrated molecular modeling and Monte Carlo simulation technology. The sophisticated tools were used to characterize the experimentally isolated forms such as Differential Scanning Calorimetry (DSC), Fourier Transform Infra-Red Spectroscopy (FTIR), Powder X Ray Diffraction (PXRD) and optical microscopy. Lattice energy landscape was examined to look for these observed forms. Crystal morphology study was conducted to analyse Morphologically Important (MI) facets. Results: A list of potential polymorphs of the drug molecule was generated with varied lattice constants using MS. Crystal energy landscape obtained from the study provided systematic energy ranking to the polymorphs. DSC of these forms exhibited endothermic peaks at 134.01, 111.24 and 79.84°C respectively indicating them to be different forms of metformin base. Structure determination from powder patterns showed that although all the forms, form I, II and III crystallize out in same triclinic space group, P-1 but they possessed different crystallographic parameters and hydrogen bonding patterns. The predicted results were quite complacent with experimental observations with respect to lattice parameters. The three observed forms have been found as local minima in the lattice energy landscape of potential polymorphs. Conclusion: The study explained the practical relevance of Crystal Structure Prediction (CSP) in studying the potential polymorphs of a drug molecule by successfully predicting various polymorphs of metformin free base. Out of all predicted polymorphs, three polymorphs were actually isolated experimentally. The information generated about the existence of multiple forms of metformin free base provides an opportunity to select and scale-up the desired crystal form well suited on bioavailability and stability grounds. The process can be escalated further to preclinical study, to emerge as an invaluable technology in future in increasing the efficiency of drug development process.","PeriodicalId":265635,"journal":{"name":"Journal of Pharmacy Practice and Pharmaceutical Sciences","volume":"115 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2019-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"124583487","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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