SYNTHESIS AND COMPARISON OF PEG-IBUPROFEN AND PEG-KETOPROFEN PRODRUGS BY IN VITRO AND IN VIVO EVALUATION

Abstract

Pain is an unpleasant sensation experienced by all individuals and classified as acute and chronic pain. NSAID’s were most widely used for treatment of Analgesia and Inflammation. Ibuprofen, Ketoprofen, Polyethylene glycol 1500 & PEG 6000 were used as drug carriers and Glycine was used as spacer to link the drugs through ester linkage. Ibuprofen and Ketoprofen belong to propionic acid derivatives of Anti-inflammatory drugs and are non-selective COX inhibitors. PEG 1500/PEG6000-Ibuprofen/Ketoprofen and PEG 1500/PEG 6000-Glycine-Ibuprofen/Ketoprofen were synthesized and are subjected to In Vitro dissolution studies which revealed that the drug release was higher at 7.2 pH rather than at 1.2 pH. The results of In Vivo evaluation studies of both synthesized prodrugs revealed that these prodrugs retained their Analgesic activity by hot plate method and acetic acid method, Anti-inflammatory activity by paw edema method and cotton pellet method. Both the prodrugs had exhibited good ulcer protective activity when compared to parent drugs. Keywords: Prodrugs, Polyethylene Glycol 1500, Poly Ethylene Glycol 6000, Ibuprofen, Ketoprofen.