3 results about "Parecoxib sodium" patented technology

The present invention belongs to the field of pharmaceutical chemistry, and particularly relates to a preparation method of parecoxib sodium intermediate; the method comprises the steps of: (a) adding the crude product of the compound of formula (II) and an alkaline substance into solvent A for recrystallization, and separating out solid B; (b) mixing solid B with solvent C and stirring, and separating to obtain solid D; (c) drying solid D to obtain the refined product of the compound of formula (II). The refining method of the compound of formula (II) provided by the present invention can significantly improve the purity of the crude product of the compound of formula (II) in a high-yield manner; it has the advantages of simple operation, easy control of parameter conditions, and low cost in large-scale industrial production. The present invention also relates to a method for preparing parecoxib sodium by a one-pot method from valdecoxib, which does not require the separate isolation of parecoxib, and the production process is simpler, which is conducive to large-scale industrial production.

The present application discloses a method for synthesizing a parecoxib sodium intermediate, which utilizes readily available α-phenylacetophenone, acetaldehyde, and hydroxylamine as raw materials to obtain an important intermediate, 5-methyl-3,4-diphenyl-4,5-oxazoline-5-ol, through an Adol reaction and electrooxidation conditions. The entire reaction process can be carried out under mild conditions without requiring harsh reaction conditions. In addition, each step has high reaction efficiency, the reaction process is simple and controllable, and the method has good industrialization prospects.

Provided in the present invention is a lyophilized Etoricoxib powder for injection. The lyophilized powder comprises: (A) 10-70% of Etoricoxib; (B) 0.1-10% of a wetting agent; and (C) 30-90% of a lyoprotectant, wherein the wetting agent is selected from at least one of oleic acid, oleate, cholic acid, or cholate. Further provided in the present invention are a method for preparing the lyophilized powder, a suspension containing the lyophilized powder, and use thereof. The lyophilized Etoricoxib powder for injection of the present invention has an appropriate particle size, maintains a stable particle size after reconstitution, and features good long-term storage stability. The prepared suspension can be quickly released to reach an effective therapeutic level after intravenous injection, has a long duration of action, and exhibits a better effect compared with parecoxib sodium, an analgesic injection commonly used in current clinical practice.