Synthesis and Analgesic Properties of Prodrug Bipharmacophore Compounds Based on Pyridoxine and Ketorolac

Abstract

Prodrug bipharmacophore anti-inflammatory compounds based on pyridoxine and ketorolac were synthesized. A new laboratory method was developed to achieve > 98 % purity of these compounds, without the use of column chromatography. Compared to ketorolac tromethamine, which is the most potent non-opioid analgesic, both compounds exhibited lower toxicity (LD50 > 2000 mg/kg), while maintaining comparable analgesic efficacy in a model of acute thermal pain response.

Keywords

• pyridoxine
• ketorolac
• non-steroidal anti-inflammatory drugs (nsaids)
• analgesic activity
• safety