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Abstract

Synthesis And Pharmacological Evaluation Of Mutual Prodrugs Of Some Nonsteroidal Antiinflammatory Drugs With Glucosamine

Author(s): B. C Ghodeswar, R. N Pophalikar, M. R Bhojani, Deepika Nagpal, Suneela S Dhaneshwar

Mutual prodrugs of ibuprofen and diclofenac with glucosamine were synthesized by reacting their acid chlorides with glucosamine with an aim to reduce gastrointestinal side effects possessed by these drugs. In vitro hydrolysis of these prodrugs in HCI buffer (pH 1.2) indicated that they were quite stable in gastric acid whereas in phosphate buffer (pH 7.4) undergo hydrolysis following first order kinetics, releasing free drug and glucosamine. These compounds were characterized by analytical and spectral data. The amides were evaluated for analgesic and antiinflammatory activity, Fruend's adjuvant-induced arthritis assay and ulcerogenic potential. They showed better to comparable analgesic and antiinflammatory activity with excellent antiarthritic activity and negligible ulcerogenicity.