Pharmaceutical composition of levoketorolac and preparation method thereof

Abstract

The invention discloses a pharmaceutical composition of levoketorolac and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The pharmaceutical composition comprises the levoketorolac or pharmaceutically acceptable salts thereof, a stabilizer, a pH regulator and an excipient, preferably freeze-dried powder injection. After the freeze-dried powder injection prepared by the method disclosed by the invention is placed for 6 months under a long-term stability test condition, the optical purity of the active ingredients is greater than or equal to 95%; and after the freeze-dried powder injection is placed for 6 months under an accelerated stability test condition, the optical purity of the active component is greater than or equal to 90%. The freeze-dried powder injection has important application in preparation of non-steroidal anti-inflammatory drugs with the effects of easing pain, diminishing inflammation, relieving fever and the like.

Description

technical field [0001] The invention relates to a pharmaceutical composition of levoketorolac and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Ketorolac Tromethamine (Ketorolac Tromethamine) is a non-steroidal antipyretic and analgesic drug with a special structure of pyrrole acid derivatives. It was first developed and marketed by Syntex Corporation of the United States. It achieves analgesic, anti-inflammatory and antipyretic effects by inhibiting the synthesis of prostaglandins (PG), instead of acting on opioid receptors or stimulating the release of opioid peptides in the body. Ketorolac trometamol relieves toxic pain in a variety of muscles, soft tissues, and joints and is indicated for the short-term treatment of acute, more severe pain requiring opioid analgesics, usually for postoperative analgesia, not for mild Or chronic pain treatment, the drug is not addictive. In the standard anima...

AI Technical Summary

Problems solved by technology

In the long-term storage, with the inevitable volatility of ethanol, there are still white spots or crystallization, which affects the quality indicators such as visible foreign matter and insoluble particles, and there are safety hazards in clinical use.

In addition, when combined with cephalosporin antibiotics, disulfiram reactions may occur, resulting in a drop in blood pressure, rapid heartbeat, or partial changes in the electrocardiogram

Therefore, ketorolac tromethamine injection containing ethanol has potential safety hazards

[0005] Chinese patent CN101199514A improves the clarity of ketorolac tromethamine injection by adding 10% to 60% propylene glycol in the traditional prescription, and improves the white spots after sterilization. The use of propylene glycol solvent still cannot avoid the adverse stimulation caused by the current use of propylene glycol, which is not conducive to the popularization and application of drugs, and the related substances increase rapidly

[0013] Chinese patent CN108451909A reports, "Korolac trometamol is unstable to light, heat, acid, and alkali, and is prone to decarboxylation and oxidation to produce impurities, which affects the safety of clinical medication to a certain extent."

After literature review and experimental exploration, we found that it is difficult to maintain the chiral optical purity of the raw material in the preparation of levoketorolac

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