Dexketoprofen trometamol injection and preparation method thereof

Abstract

The invention provides a dexketoprofen trometamol injection and a preparation method thereof. According to the injection, citric acid and sodium citrate are applied as pH (potential of Hydrogen) regulators; carboxymethyl chitosan and polysorbate 80 are applied as stabilizers; the photostability of dexketoprofen trometamol is effectively improved; meanwhile, the gastrointestinal irritation is decreased; the operation is simple and convenient, and the dexketoprofen trometamol injection is suitable for industrialized large-scale production.

Description

Technical field [0001] The invention belongs to the field of medical technology, and specifically relates to a dexketoprofen tromethamine injection and a preparation method thereof. Background technique [0002] Dexketoprofen tromethamine is a derivative of dexketoprofen, the single optical isomer of the 2-arylpropionic acid non-steroidal anti-inflammatory drugs (NASIDs) ketoprofen, and has strong antipyretic properties , analgesic and anti-inflammatory effects, better water solubility than dexketoprofen, higher activity than free acid, high bioavailability, better tolerance to patients, and beneficial to the treatment of acute sharp pain, so it has broad applications Clinical application prospects. Clinically suitable for mild to moderate pain of different causes, such as rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gouty arthritis joint pain, dysmenorrhea, toothache, postoperative pain, cancer pain, acute Various acute and chronic pains, such as sprains ...

AI Technical Summary

Problems solved by technology

Non-intravenous analgesic drugs often have slow onset of action, low bioavailability, and insignificant analgesic effects on patients, while intravenous injections can often directly reach the concentration required for drug action and have a faster onset of action

Some problems still exist in the present disclosed injection patent: patent ZL98122858.5 discloses a kind of dexketoprofen injection, adds sodium carbonate as solubilizing agent, but sodium carbonate meets acidic solution and can produce carbon dioxide, brings great harm to patient's blood injection Dangerous, and does not involve stability issues; patent ZL200710113179.1 discloses a ketorolac tromethamine injection, using propylene glycol as a solvent and solubilizer, the clarity is improved, but the organic solvent brings unsafe medication ; Patent ZL201210437623.6 discloses a kind of dexketoprofen injection, adopts basic amino acid as cosolvent, can improve the curative effect of injection, but the stability of injection is not disclosed; Patent ZL201210115129.8 discloses a kind of dexketoprofen for injection Ketoprofen trometamol temperature-sensitive hydrogel, including dexketoprofen trometamol and drug carrier, the carrier is chitosan and β-sodium glycerophosphate cross-linked to form a temperature-sensitive gel system, the drug has both Targeting and sustained release, but the temperature-sensitive hydrogel has a large volume change with temperature changes, and it is difficult to apply due to swelling in the blood

Simultaneously dexketoprofen trometamol sees unstable light, brings very big potential safety hazard to clinical medication, therefore reduces dexketoprofen tromethamine gastrointestinal irritation, improves its photostability and becomes a task Important research content

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