Benzyl ester prodrug of ibuprofen: pharmacological and toxicological profile.
Prodrug approach is a promising way of overcoming gastrotoxicity associated with long term oral use of NSAIDs like ibuprofen. The candidature of benzyl ester prodrug of ibuprofen was examined to assess its ability to reduce gastrotoxicity without affecting pharmacological response. It gave highly promising activity profile in established animal models like carrageenan induced rat paw oedema and acetic acid induced writhing reflex assay. The effect of physicochemical properties like aqueous solubility, octanol-water partition coefficient, hydrolysis kinetics in human plasma and simulated gastric fluid, on activity profile has been investigated.
Bansal
A K
AK
College of Pharmacy, New Delhi, India.
Khar
R K
RK
Dubey
R
R
Sharma
A K
AK
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology* / Q000633:toxicity; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D007052:Ibuprofen / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D011355:Prodrugs / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D013276:Stomach Ulcer / Q000139:chemically induced
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011355:Prodrugs; D007052:Ibuprofen