Synthesis and pharmacological evaluation of cyclodextrin conjugate prodrug of mefenamic acid
Department of Pharmaceutical Chemistry, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, Pune-411 038, India
S R Dhaneshwar Department of Pharmaceutical Chemistry, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, Pune-411 038 India E-mail: [email protected]
In the present investigation mefenamic acid prodrug of β-cyclodextrins was synthesized. The primary hydroxy group of β-cyclodextrins was used to block the acid group. The synthesis involved a series of protection and deprotection reaction. The ester was evaluated for stability in simulated gastric and intestinal fluid. The hydrolysis of cyclodextrin conjugate in colon is confirmed by the hydrolysis kinetics studies in rat faecal material. The ester was also evaluated for ulcerogenicity. Results of these studies established the primary aim of masking the ulcerogenic potential of free drug, by using 12-fold dose of the normal dose of mefenamic acid and equivalent doses of the ester.