Application of citric acid in the preparation of parecoxib sodium freeze-dried preparation composition and its composition and preparation method

Abstract

The invention discloses the application of citric acid in the preparation of the parecoxib sodium freeze-dried preparation composition, the composition and the preparation method. A light-stable freeze-dried preparation composition of parecoxib sodium, comprising a pharmaceutically acceptable amount of parecoxib sodium, a pharmaceutically acceptable amount of a pH regulator, and a pharmaceutically acceptable amount of sodium phosphate salt, which can be pharmaceutically acceptable An acceptable amount of photostabilizer, the photostabilizer being citric acid. The citric acid of the present invention can be used as a photostabilizer in the preparation of the parecoxib sodium freeze-dried formulation composition, while providing a more stable parecoxib sodium freeze-dried formulation composition, which can prevent or Delaying the generation of impurities U and T of the parecoxib sodium freeze-dried preparation composition under conditions of exposure to light during production, storage, transportation, and clinical use can significantly improve product quality and clinical drug safety.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of citric acid in the preparation of parenteral administration liquid preparation parecoxib sodium freeze-dried preparation composition and its composition and preparation method. Specific cyclooxygenase-2 (COX-2) inhibitors for intravenous administration and intramuscular injection are mainly used clinically for the short-term treatment of postoperative pain, and can also be used for the treatment of moderate or severe postoperative acute pain. Background technique [0002] Parecoxib sodium is a water-soluble drug and is an active prodrug of Valdecoxib. It does not inhibit COX-1 and COX-2 by itself, but parecoxib sodium is rapidly hydrolyzed by liver enzymes after injection. Converted to valdecoxib N-{[4-(5-methyl-3-benisoxazole-4-yl)benzenesulfonamide] and propionic acid. Valdecoxib is a selective COX-2 inhibitor. At therapeutic concentrations, pa...

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Problems solved by technology

[0010] Inquiring literature information, most of the photodegradation impurities introduced mainly involve the conversion of sulfonamide (ammonia) and propionamide active functional groups, including oxidation, hydrolysis and other pathways, and the photodegradation pathway and photodegradation impurities of parecoxib sodium have not been investigated. Research

Moreover, up to now, there is no information on the photodegradation impurities of parecoxib sodium for in-depth research, and there is also no public report on the photodegradation impurities of parecoxib sodium formulations.

[0011] Patents CN201310412213.0, CN201410016516.5, CN02810765.9, etc. all disclose the formulation patents of the preparation, but none of them propose to solve the problem of how to solve the problem of photodegradation impurities on the product during the production, storage, transportation and clinical use of the parecoxib sodium preparation. Quality Impact and Clinical Safety Issues

[0012] From the analysis of the above patents, it can be seen that photodegradation impurities in preparations cannot be avoided. These invention defects obviously bring very high risks to product quality and clinical administration.

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