Preparation for injection of diclofenac sodium capable of being used for intravenous injection and preparation thereof

Abstract

The invention provides an injection formulation of diclofenac sodium for intravenous injection and the preparation method, which is characterized in that the diclofenac sodium is included successfully with the inclusion material of propyl-Beta-cyclodextrin. The injection formulation has the advantages of improving the solubility of diclofenac sodium in the solution and reducing the adverse reaction in intravenous injection. The injection formulation exists in the form of injection, frozen powder, sterile powder and large-capacity infusion. The invention also describes the main technical parameters of adopting propyl- Beta -cyclodextrin to include the diclofenac sodium, such as inclusion method, the concentration of propyl-Beta-cyclodextrin, solution temperature in inclusion and inclusion time.

Description

technical field [0001] The invention relates to a preparation for intravenous injection of diclofenac sodium injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Diclofenac is a non-steroidal anti-inflammatory analgesic derived from phenylacetic acid. Its mechanism of action is to inhibit the activity of cyclooxygenase, thereby blocking the conversion of arachidonic acid to prostaglandins. At the same time, it can also promote the combination of arachidonic acid and triglyceride (triacylglycerol), reduce the concentration of free arachidonic acid in cells, and indirectly inhibit the synthesis of leukotrienes. Diclofenac is one of the most powerful non-steroidal anti-inflammatory drugs, and its inhibitory effect on prostaglandin synthesis is stronger than that of aspirin and indomethacin. It is mainly used for symptomatic treatment of fever and renal colic in various febrile diseases, severe rheumatoid arthri...

AI Technical Summary

Problems solved by technology

[0003] Diclofenac is often used in the form of medicinal salts, and its oral medicinal value has been recognized clinically, but compared with injections, its bioavailability and onset rate are not very satisfactory, and oral administration often causes some gastrointestinal reactions , so the injection of diclofenac is worthy of further research and development, because the solubility of diclofenac sodium (DS) in water is small (9 mg·mL-1, 25°C), which cannot meet the concentration requirements of the preparation, and the molecular structure of DS still contains easily oxidized groups. If it is made into an injection, the stability of the drug can be reduced, so finding a suitable solvent system and improving the stability of the preparation has become a key issue in research

At present, diclofenac sodium and potassium injections have been used clinically, but they are mainly injected into muscles and subcutaneously, and the effect is remarkable, but they are rarely injected into veins, because they are irritating to blood vessels, and long-term use can easily cause venous inflammation. technology can solve this problem