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Research Paper Open Access
In the present investigation flurbiprofen prodrugs of Î± and Î³ cyclodextrins were synthesized. Here the primary hydroxy group of Î± and Î³ cyclodextrins were used to block the acid group. The synthesis involved a series of protection and deprotection reaction. The esters were evaluated for their stability in simulated gastric and intestinal fluid. The hydrolysis of cyclodextrin conjugates in colon is confirmed by the hydrolysis kinetics studies in rat faecal material. The esters were evaluated for their analgesic and antiinflammatory activities. The ulcerogenicity of the esters was also studied. The results of these studies revealed that the esters have comparable antiinflammatory and analgesic activity with the parent drug, flurbiprofen. The esters showed no ulcers even at a dose 12 times greater than normal dose.
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Author(s): Sheeba Varghese D Gupta Deepali Mhaske S S Kadam S R Dhaneshwar