67 results about "Cinepazide" patented technology

The invention relates to a method to synthesize maleic acid cinepazide. (2) reacts with 3,4,5- cinnamyl chloride, aquiring free alkali of cinepazide, the solvent is chosen from 5, add 6 and acquire the (7), the method for separating (1) is filtration. The invention uses safe solvent in the synthesis of (2), and the method of filtration and 8, making it suitable for industrialized production. The method uses the solvent with low toxicity and good safety, simplized productive condition and course, has high productivity and low cost.

The invention belongs to the pharmaceutical technical field, particularly relates to maleate cinepazide crystal form (including maleate cinepazide A crystal form and maleate cinepazide B crystal form) and preparation method thereof. The maleate cinepazide crystal form has characteristic peak at 9.0 plus or minus 0.2, 16.1 plus or minus 0.2, 19.8 plus or minus 0.2 and 21.7 plus or minus 0.2 in X-ray powder diffraction expressed by 2 THETA using Cu-Ka radiation. The maleate cinepazide crystal form has characteristic peak at 7.6 plus or minus 0.2, 19.7 plus or minus 0.2, and 22.9 plus or minus 0.2 in X-ray powder diffraction expressed by 2 THETA using Cu-Ka radiation.

The invention relates to a medicine composition with high safety, a preparation method and an application thereof. The medicine composition contains cinepazide or salt thereof which is acceptable in pharmacy and a structural compound which has the content not higher than 0.5% and is shown in the formula (III). The cinepazide medicine composition and a preparation thereof have better safety, effectiveness and stability and can effectively lower or avoid the adverse reactions of hemogram lowering and the like of a patient caused by the cinepazide. Furthermore, the invention also separates, purifies and characterizes a novel cinepazide nitrogen oxide, researches the novel cinepazide nitrogen oxide fully and discovers that the toxicity of the compound is far greater than that of the cinepazide and the compound has an insecticidal activity which is different from that of the cinepazide. Meanwhile, the research discovers that the cinepazide nitrogen oxide can cause the leukopenia of animals, even influences the formation and the differentiation of granular cells and is possibly a main reason of the adverse reactions of the hemogram lowering and the like of the patient caused by the cinepazide.

The invention relates to a preparation method of cinepazide maleate. Preparation of chloroacetylpyrrolidine; Preparation of 1-[(1-tetrahydropyrrolecarbonyl)methyl]piperazine; Preparation of 3,4,5-trimethoxycinnamoyl chloride; 1-[(1-Pyrrolidinecarbonyl ) methyl]-4-(3,4,5-trimethoxycinnamoyl)piperazine; 1-[(1-pyrrolidinecarbonyl)methyl]-4-(3,4,5-trimethoxy Preparation of base cinnamoyl) piperazine maleate; purification of cinepazide maleate and preparation of stable crystal form; characterized in that: the solvent used in the preparation step of cinepazide maleate stable crystal form One or any combination of chloroform and acetone. The product prepared by the preparation method of cinepazide maleate has a melting point of 170-175°C. The product prepared by the method for preparing cinepazide maleate provided by the invention has high melting point and stable crystal form, and is suitable for industrial scale production.

The invention relates to a cinepazide maleate injection and a preparation method thereof. Every 1000ml injection contains 30-45g of cinepazide maleate, 5-23g of mannite, 0.5g-1.5g of disodium hydrogen phosphate used for regulating the pH value, and the rest of water used for injection. The preparation method comprises: under the condition of keeping out of the sun, the mannite is added to and dissolved in the water which accounts for 80% of the total quantity, the cinepazide maleate is then added into the mannite aqueous solution to be stirred and dissolved, the pH value of the mixed solutionis regulated by the solution with 4% of the disodium hydrogen phosphate, and the water used for injection is added until the total quantity is achieved. The invention selects the mannite with high safety as stabilizing agent, and the operation which is kept out of the sun is adopted in the preparation process of the product, so that the content of the cis isomer of the cinepazide maleate is more effectively reduced, and the stability as well as the safety of clinical medication can be improved.