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Title: Synthesis, hydrolysis and pharmacodynamic profiles of novel prodrugs of some non steroidal anti inflammatory drugs
Researcher: Rasheed, Arun
Guide(s): Ashokkumar, C K
Keywords: Prodrugs
Pharmaceutical Sciences
Upload Date: 19-Apr-2012
University: Jawaharlal Nehru Technological University
Completed Date: 24/11/ 2010
Abstract: Prodrugs are bio-reversible derivatives of drug molecules that undergo an enzymatic and chemical transformation in vivo to release the active parent drug, which exerts the desired pharmacological effects. The prodrug increases the usefulness of a potential drug. It provides possibilities to overcome various barriers to drug formulation and drug targeting such as poor aqueous solubility, chemical instability, insufficient oral absorption, rapid pre-systemic metabolism, inadequate brain penetration, gastric toxicity and local irritation. In the present research, use of amide prodrugs to temporarily mask the acidic group of non steroidal anti inflammatory drugs (NSAIDs) has been proposed as an innovative and novel approach to decrease the gastrointestinal toxicity due to direct contact effect. While conjugating NSAIDs with amino acids, the free carboxylic group of NSAIDs will be derivatized into corresponding esters or amides of amino acids, by altering the physical properties of parent drug with enzymes serving as the in vivo reconversion site (s). In the study, amide conjugates of NSAIDs such as Aceclofenac (AC), Mefenamic acid (MA) and Dexibuprofen (Dex) with various amino acid methyl esters were synthesized by Schottan Baumann technique using prodrug concept. The physicochemical characterization, analysis of hydrolytic behaviour in various simulated fluids and pharmacological evaluation of prodrugs were carried out with an expectation to get non toxic prodrugs with minimized GIT disturbance while maintaining the useful physicochemical and pharmacological properties.
Pagination: xxix, 248p.
Appears in Departments:Faculty of Pharmaceutical Sciences

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01_title.pdfAttached File59.6 kBAdobe PDFView/Open
02_declaration.pdf100.9 kBAdobe PDFView/Open
03_certificates.pdf102.69 kBAdobe PDFView/Open
04_acknowledgements.pdf101.06 kBAdobe PDFView/Open
05_abstract.pdf102.79 kBAdobe PDFView/Open
06_contents.pdf252.06 kBAdobe PDFView/Open
07_list of tables & figures.pdf210.04 kBAdobe PDFView/Open
08_list of abbreviations.pdf158.59 kBAdobe PDFView/Open
09_list of chemicals & instruments.pdf97.72 kBAdobe PDFView/Open
10_chapter 1.pdf404.6 kBAdobe PDFView/Open
11_chapter 2.pdf224.25 kBAdobe PDFView/Open
12_chapter 3.pdf194.94 kBAdobe PDFView/Open
13_chapter 4.pdf374.88 kBAdobe PDFView/Open
14_chapter 5.pdf5.17 MBAdobe PDFView/Open
15_chapter 6.pdf145.11 kBAdobe PDFView/Open
16_chapter 7.pdf119.58 kBAdobe PDFView/Open
17_references.pdf250.98 kBAdobe PDFView/Open
18_research publications.pdf163.68 kBAdobe PDFView/Open

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