30 results about "Bromfenac sodium" patented technology

The invention relates to an ophthalmic gel containing the active ingredient of bromfenac sodium hydrate and a preparation method thereof; the bromfenac sodium hydrate ophthalmic gel contains the active ingredient of bromfenac sodium hydrate, macromolecular hydrogel substrate, osmotic pressure regulator, bacteriostat, antioxidant, metal ion chelating agent, pH regulator and water for injection; the ophthalmic gel has convenient application and quick effect; particularly, the gel possesses certain viscosity and can stay in the eyes for a long time, thus overcoming the defect that eye drops can only stay in the eyes for a short time after being diluted by tears and achieving more effective therapeutic effect.

The invention relates to a preparation method of bromfenac sodium. The preparation method comprises the following steps of (a) reacting a compound represented by a formula (V) with an electrophilic substitutional reagent in the presence of N,N-dimethylformamide or dimethyl sulfoxide to obtain a compound represented by a formula (IV), (b) adding the compound represented by the formula (IV) into 2-methoxyethanol, adding phosphoric acid and carrying out acid hydrolysis to obtain a compound represented by a formula (III), (c) hydrolyzing the compound represented by the formula (III) with sodium hydroxide, extracting with dichloromethane and adding acetic acid to neutralize to obtain a compound represented by a formula (II) and (d) in the presence of an organic alcohol solvent, adding a sodium hydroxide solution, hydrolyzing the compound represented by the formula (II) to form a salt, adding the organic alcohol solvent, cooling and crystallizing to obtain bromfenac sodium. According to the preparation method disclosed by the invention, the reaction yield of the intermediate (IV) and the quality of the product are improved, high-purity bromfenac sodium can be obtained just by virtue of crystallizing with the organic alcohol solvent, the good environmental benefit is achieved and the generation of bromfenac sodium polymer impurity is reduced.

The invention discloses a method for synthesizing a standard substance of a degradation impurity of bromfenac sodium sesquihydrate. 7-(4-bromobenzoyl)indoline-2,3-diketone is adopted as a raw material and subjected to hydrolysis and refining to obtain a purified product of 2-(2-amino-3-(4-bromobenzoyl)phenyl)-2-oxo-acetic acid, and content calibration of the purified product is realized by conventional analysis means. The method is simple in process and short in preparation cycle, and calibrated product content is higher than 97.0%. The bromfenac sodium sesquihydrate impurity synthesized according to the method can be used as a standard substance of the impurity and applied to qualitative and quantitative research and detection of impurities in raw materials and preparation of bromfenac sodium sesquihydrate.

The invention belongs to the field of medicinal chemistry, and in particular relates to a preparation method of bromfenac sodium and an intermediate thereof. The method adopts a new solvent system to prepare the intermediate, avoids the generation of brick-red by-products, greatly reduces the impurity content in the intermediate, and improves the purity and yield of the intermediate.

The invention aims at providing a preparation method of bromfenac sodium sesquihydrate. The preparation method comprises the following steps: (1) adding bromfenac sodium and an antioxidant into a mixed solvent of water and an organic alcohol, heating, dissolving and adding a pH adjustor to adjust the pH to 7.0-10.5; (2) adding an anti-solvent into a solution obtained in the step (1), cooling the solution to 30 DEG C to 35 DEG C, adding bromfenac sodium monohydrate, bromfenac sodium sesquihydrate or a mixture thereof as a seed crystal, and stirring; and (3) cooling, crystallizing, collecting crystals and drying to obtain the bromfenac sodium sesquihydrate. The preparation method avoids use of ether agents and is mild in reaction condition and good in environmental benefit. The prepared bromfenac sodium sesquihydrate is high in purity.