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FABRICATION OF POTENTIAL MACROMOLECULAR PRODRUGS OF ASPIRIN AND DICLOFENAC WITH DEXTRAN
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نویسنده
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HUSSAIN MUHAMMAD AJAZ ,HASSAN ZAHID ,HASEEB MUHAMMAD TAHIR ,IQBAL MOHAMMAD SAEED ,SHER MUHAMMAD ,TAHIR MUHAMMAD NAWAZ ,TREMEL WOLFGUNG ,BASHIR SAJID ,AHMAD RIAZ
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منبع
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pakistan journal of pharmaceutical sciences - 2011 - دوره : 24 - شماره : 4 - صفحه:575 -581
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چکیده
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Aspirin and diclofenac conjugates with dextran were synthesized as potential macromolecular prodrugs under homogeneous reaction conditions by using 4-methyl-benzenesulfonyl chloride as an acylating agent in the presence of triethylamine as a base. highly pure conjugates with good yields were synthesized by this acylation method. all of the products were found soluble in aqueous medium as well as in dimethylsulfoxide and n,ndimethylacetamide. the uv/vis spectrophotometry has indicated the incorporation of drugs in conjugates and extent of substitution of drug onto dextran polymer. covalent attachment of the drug onto the drug carrier polymer (dextran) was verified by 1h nmr and fourier transform infrared (ftir) spectroscopic analysis. the prodrugs were analysed by powder x-ray diffraction (xrd) measurements. phase changes were noticed by powder xrd for all macromolecular prodrugs indicating the change of state of matter towards more crystallinity. therefore, fabricated macromolecular prodrugs are potential candidates to show better pharmacokinetic profile. all of the products were thoroughly characterized by using different spectroscopic techniques.
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کلیدواژه
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Acylation ,dextran ,NSAIDs ,macromolecular prodrugs ,polysaccharides ,X-ray diffraction.
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آدرس
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University of Sargodha, Department of Chemistry, Pakistan, University of Sargodha, Department of Pharmacy, Pakistan, University of Sargodha, Department of Pharmacy, Pakistan, GC University, Department of Chemistry, Pakistan, University of Sargodha, Department of Chemistry, Pakistan, Johannes Guttenberg University, Institute of Inorganic & Analytical Chemistry, Germany, Johannes Guttenberg University, Institute of Inorganic & Analytical Chemistry, Germany, University of Sargodha, Department of Pharmacy, Pakistan, GC University, Department of Physics, Pakistan
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Authors
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