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Synthesis of nimesulide conjugates, in vitro and in vivo evaluation | Abstract

Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

ISSN: 0975-413X
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Abstract

Synthesis of nimesulide conjugates, in vitro and in vivo evaluation

Author(s): Durgaprasad Kemisetti*, Sarangapani Manda, Naga Kishore Rapaka and Jithan AV

In this study nimesulide drug conjugates were synthesized using polyethylene glycol 1500 and 6000, covalently bonded through ester and amidic linkages. Major complications of nimesulide included upper G.I tract irritation and it is used with an Antihistaminic drug. Hence to overcome the complications PEG 1500-Nimesulide, PEG 1500- Glycine-Nimesulide, PEG 6000-Nimesulide, PEG 6000-Glycine-Nimesulide were synthesized. The prodrugs synthesized were characterized by I.R, N.M.R, in vitro dissolution, in vivo anti inflammatory activity and ulcer protecting activity. I.R and N.M.R confirmed the structure of prodrugs. In vitro dissolution study revealed that the release of drug from drug conjugates was high at pH 7.2 as compared to pH 1.2. In vivo anti inflammatory activity was retained after conjugation of drug with polymers. Ulcer protecting activity was compared with standard nimesulide. Drug conjugates had more ulcer protecting activity.


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