Pub Date : 2016-01-01DOI: 10.21767/2321-547X.1000003
D. Sen, Jalpa Patel
Prodrug is a substance which after administration is metabolized into a pharmacologically active drug. Actually prodrug has least medicinal value in in-vitro/in-vivo but after biotransformation by metabolism in invivo it releases the active medicament. A drug is a substance which is a chemical entity, has definite structural skeleton, obtained by natural or synthetic or semisynthetic source, which can fit on bioreceptor platform having controlling capacity to control over the biochemical malfunction. Every drug is xenobiotic because it is coming from outer source (xeno) and active in biological unit (biotic). Prodrug is the precursor of drug which is made by derivatization of the same to enhance the bioavailability by pharmacokinetics, lipid solubility by partition coefficient and increase the physicochemical and biochemical parameters by pharmacodynamics. Ibuprofen, Diclofenac and Paracetamol have been taken as NSAID (Non-Steroidal Anti Inflammatory Drug) and three prodrugs have been synthesized by reacting with acid chloride of ibuprofen and diclofenac with paracetamol to get prodrug of ester linkage and acid chloride of ibuprofen has been reacted with diclofenac to get prodrug of amide linkage. All three prodrugs showed different logP values and molecular weights according to the solubility parameters and electronegativity: logP profile: Prodrug-C>Prodrug-B>prodrug-A; molecular weight profile: Prodrug-C>Prodrug-B>prodrug-A.
{"title":"Logarithmic Partition Coefficient ComparisonStudy and Molecular Weight of SynthesizedProdrugs of Ibuprofen+Paracetamol, DiclofenacSodium+Paracetamol and Ibuprofen+DiclofenacSodium","authors":"D. Sen, Jalpa Patel","doi":"10.21767/2321-547X.1000003","DOIUrl":"https://doi.org/10.21767/2321-547X.1000003","url":null,"abstract":"Prodrug is a substance which after administration is metabolized into a pharmacologically active drug. Actually prodrug has least medicinal value in in-vitro/in-vivo but after biotransformation by metabolism in invivo it releases the active medicament. A drug is a substance which is a chemical entity, has definite structural skeleton, obtained by natural or synthetic or semisynthetic source, which can fit on bioreceptor platform having controlling capacity to control over the biochemical malfunction. Every drug is xenobiotic because it is coming from outer source (xeno) and active in biological unit (biotic). Prodrug is the precursor of drug which is made by derivatization of the same to enhance the bioavailability by pharmacokinetics, lipid solubility by partition coefficient and increase the physicochemical and biochemical parameters by pharmacodynamics. Ibuprofen, Diclofenac and Paracetamol have been taken as NSAID (Non-Steroidal Anti Inflammatory Drug) and three prodrugs have been synthesized by reacting with acid chloride of ibuprofen and diclofenac with paracetamol to get prodrug of ester linkage and acid chloride of ibuprofen has been reacted with diclofenac to get prodrug of amide linkage. All three prodrugs showed different logP values and molecular weights according to the solubility parameters and electronegativity: logP profile: Prodrug-C>Prodrug-B>prodrug-A; molecular weight profile: Prodrug-C>Prodrug-B>prodrug-A.","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"59 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91538058","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 : 2016-01-01DOI: 10.21767/2321-547X.1000005
A. Nagappa, G. Agarwal, Vinuth Chikkamath, S. Agarwal, R. Rani, P. K. Karar
Acyclovir sodium is an antiviral drug used to treat herpes, chicken pox and herpes skin infections. Acyclovir sodium potential as an antiviral drug is limited by its low oral bioavailability (20-30%) with short half life (2-3hours) with poor plasma protein binding. There is an opportunity to utilize Acyclovir sodium as an antiviral drug by enhancing the bioavailability by formulation technology. In this paper solid microparticle (o/w) of Acyclovir was prepared by melt dispersion technique. The characterization of drug using scanning electron microscopy, FT-IR, particle size, percentage yield, drug loading capacity, hausner’s ratio and carr’s index, bulk density and tapped density. In vitro drug release studies using phosphate buffer has shown as formulation F5 sustained release for 17hrs.
{"title":"Formulation And Evaluation Of Acyclovir Sodium Solid Lipid Microparticles","authors":"A. Nagappa, G. Agarwal, Vinuth Chikkamath, S. Agarwal, R. Rani, P. K. Karar","doi":"10.21767/2321-547X.1000005","DOIUrl":"https://doi.org/10.21767/2321-547X.1000005","url":null,"abstract":"Acyclovir sodium is an antiviral drug used to treat herpes, chicken pox and herpes skin infections. Acyclovir sodium potential as an antiviral drug is limited by its low oral bioavailability (20-30%) with short half life (2-3hours) with poor plasma protein binding. There is an opportunity to utilize Acyclovir sodium as an antiviral drug by enhancing the bioavailability by formulation technology. In this paper solid microparticle (o/w) of Acyclovir was prepared by melt dispersion technique. The characterization of drug using scanning electron microscopy, FT-IR, particle size, percentage yield, drug loading capacity, hausner’s ratio and carr’s index, bulk density and tapped density. In vitro drug release studies using phosphate buffer has shown as formulation F5 sustained release for 17hrs.","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83613603","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 : 2016-01-01DOI: 10.21767/2321-547X.1000002
N. L. Prasanthi, M. Sudhir, N. Jyothi, V. S. Vajrapriya
The investigation of drug polymorphism is an essential step in any formulation. While formulating a drug product physiochemical stability, solubility and bioavailability of active ingredient are prominent are factors. The Study of polymorphism is necessarily predominant acquire comprehensive knowledge on rapid absorption of low solubility drugs in systemic circulation. In order to increase the effective surface area of the drug substances by turning them into different shapes, the empowerment of dissolution rate and bioavailability by employing recrystallization technique is very important. Since most of the drugs are examined through oral route practice, the size and shape of the crystal play a key note is their dissolution rate, as proved by Noyes Whitney, through his equation. In this an crystal view point the writer makes an effort to prove the importance of polymorphism in pharmaceuticals and how it shows its impact on pharmaceutical properties like solubility, dissolution rate, bioavailability, etc. of drug substances.
{"title":"A Review on Polymorphism PerpetuatesPharmaceuticals","authors":"N. L. Prasanthi, M. Sudhir, N. Jyothi, V. S. Vajrapriya","doi":"10.21767/2321-547X.1000002","DOIUrl":"https://doi.org/10.21767/2321-547X.1000002","url":null,"abstract":"The investigation of drug polymorphism is an essential step in any formulation. While formulating a drug product physiochemical stability, solubility and bioavailability of active ingredient are prominent are factors. The Study of polymorphism is necessarily predominant acquire comprehensive knowledge on rapid absorption of low solubility drugs in systemic circulation. In order to increase the effective surface area of the drug substances by turning them into different shapes, the empowerment of dissolution rate and bioavailability by employing recrystallization technique is very important. Since most of the drugs are examined through oral route practice, the size and shape of the crystal play a key note is their dissolution rate, as proved by Noyes Whitney, through his equation. In this an crystal view point the writer makes an effort to prove the importance of polymorphism in pharmaceuticals and how it shows its impact on pharmaceutical properties like solubility, dissolution rate, bioavailability, etc. of drug substances.","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88697545","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 : 2006-12-01DOI: 10.2165/00137696-200604040-00006
M. Robert, Y. Kalia
{"title":"New developments in topical antifungal therapy","authors":"M. Robert, Y. Kalia","doi":"10.2165/00137696-200604040-00006","DOIUrl":"https://doi.org/10.2165/00137696-200604040-00006","url":null,"abstract":"","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"29 1","pages":"231-247"},"PeriodicalIF":0.0,"publicationDate":"2006-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74139212","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 : 2006-12-01DOI: 10.2165/00137696-200604040-00004
Jin Zhang, Carryn H. Purdon, Eric W. Smith
{"title":"Solid lipid nanoparticles for topical drug delivery","authors":"Jin Zhang, Carryn H. Purdon, Eric W. Smith","doi":"10.2165/00137696-200604040-00004","DOIUrl":"https://doi.org/10.2165/00137696-200604040-00004","url":null,"abstract":"","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"45 1","pages":"215-220"},"PeriodicalIF":0.0,"publicationDate":"2006-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77271914","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 : 2006-12-01DOI: 10.2165/00137696-200604040-00003
Senshang Lin, Y. Chien
{"title":"Transdermal contraceptive patches","authors":"Senshang Lin, Y. Chien","doi":"10.2165/00137696-200604040-00003","DOIUrl":"https://doi.org/10.2165/00137696-200604040-00003","url":null,"abstract":"","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"35 1 1","pages":"201-213"},"PeriodicalIF":0.0,"publicationDate":"2006-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90089575","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 : 2006-12-01DOI: 10.2165/00137696-200604040-00008
A. Bernkop‐Schnürch, V. Grabovac
{"title":"Polymeric efflux pump inhibitors in oral drug delivery","authors":"A. Bernkop‐Schnürch, V. Grabovac","doi":"10.2165/00137696-200604040-00008","DOIUrl":"https://doi.org/10.2165/00137696-200604040-00008","url":null,"abstract":"","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"64 1","pages":"263-272"},"PeriodicalIF":0.0,"publicationDate":"2006-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81192820","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 : 2006-12-01DOI: 10.2165/00137696-200604040-00005
A. Banga
{"title":"New technologies to allow transdermal delivery of therapeutic proteins and small water-soluble drugs","authors":"A. Banga","doi":"10.2165/00137696-200604040-00005","DOIUrl":"https://doi.org/10.2165/00137696-200604040-00005","url":null,"abstract":"","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"26 1","pages":"221-230"},"PeriodicalIF":0.0,"publicationDate":"2006-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90532891","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 : 2006-12-01DOI: 10.2165/00137696-200604040-00007
G. Sandri, M. C. Bonferoni, F. Ferrari, S. Rossi, C. Caramella
{"title":"Differentiating factors between oral fast-dissolving technologies","authors":"G. Sandri, M. C. Bonferoni, F. Ferrari, S. Rossi, C. Caramella","doi":"10.2165/00137696-200604040-00007","DOIUrl":"https://doi.org/10.2165/00137696-200604040-00007","url":null,"abstract":"","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"1 1","pages":"249-262"},"PeriodicalIF":0.0,"publicationDate":"2006-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75881845","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 : 2006-12-01DOI: 10.2165/00137696-200604040-00002
Manmohan J. Singh, M. Ugozzoli, Elawati Soenawan, A. Pannu, E. Pushnova, J. Allen, D. O’hagan
{"title":"Extent of supercoiling in plasmid DNA vaccines","authors":"Manmohan J. Singh, M. Ugozzoli, Elawati Soenawan, A. Pannu, E. Pushnova, J. Allen, D. O’hagan","doi":"10.2165/00137696-200604040-00002","DOIUrl":"https://doi.org/10.2165/00137696-200604040-00002","url":null,"abstract":"","PeriodicalId":7704,"journal":{"name":"American Journal of Advanced Drug Delivery","volume":"31 1","pages":"195-199"},"PeriodicalIF":0.0,"publicationDate":"2006-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73629313","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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