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Ibuprofenamine hydrochloride is a novel transdermal nonsteroidal anti-inflammatory drug (NSAID) currently under clinical development for the treatment of rheumatoid arthritis and osteoarthritis. Developed as a topical spray, it is designed to deliver the active moiety across the skin to provide localized anti-inflammatory and analgesic effects while potentially minimizing systemic side effects associated with oral NSAIDs. In clinical studies, it has been shown to be metabolized or dissociated into ibuprofen, which acts as a non-selective inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes, thereby inhibiting prostaglandin synthesis. Phase I trials conducted by Beijing Hospital have evaluated its safety, tolerability, and pharmacokinetics in healthy volunteers, demonstrating a dose-proportional increase in exposure and good skin tolerability.
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