69 results about "Acipimox" patented technology

The invention relates to a preparation method of acipimox for treating hyperlipidemia, belonging to the field of medicines. The invention provides an acipimox synthesis process which is simple and easy to operate. The preparation method comprises steps of with 2, 5-dimethylpyrazine as a raw material, carrying out nitrogen oxidation, reaction with acetic anhydride and alkaline hydrolysis to obtain 2-hydroxymethyl-5-methylpyrazine; directly oxidizing a post-treatment fluid by using 2,2,6,6-tetramethyl-1-piperidinyloxy/sodium hypochlorite/potassium bromide to obtain 5-methylpyrazine-2-carboxylic acid, wherein the post-treatment fluid is not needed to be dried and concentrated; oxidizing 5-methylpyrazine-2-carboxylic acid by using hydrogen peroxide/sodium tungstate to obtain acipimox.

The invention relates to an osmotic pump controlled release pharmaceutical composition which contains two medicine active ingredients and is used for treating hyperlipoidemia and a preparation method thereof, the pharmaceutical composition has a nicotinic acids medicine such as acipimox and the other one estatina medicine such as atorvastatin; wherein, the nicotinic acids medicine such as acipimox is a controlled release part, and the estatina medicine such as atorvastatin is a quick release part; or both the acipimox and the atorvastatin are the controlled release part. The compound osmotic pump preparation of the invention has the advantages of comprehensive action, low toxicity and side effects and convenient use.

The invention provides a synthetic process for acipimox. The synthetic process comprises steps: firstly, 5-methylpyrazine-2-carboxylic acid and hydrogen peroxide are reacted under action of catalysts in an aqueous solution; secondly, an auxiliary agent is added into the solution obtained in the first step, and the auxiliary agent is one selected from sulfite, bisulfate, oxalic acid and oxalate; thirdly, active carbon is added in the solution obtained in the second step and filtering is carried out; fourthly, the solution obtained in the third step is subjected to cooling crystallization and drying, and an acipimox finshed product is obtained. The synthetic process can lower the crystallization frequency effectively, avoids recrystallization operation, raises the yield and lowers the production cost.

The invention provides a method for improving the synthesis process of Acipimox, which is characterized by carrying out one-pot method on the steps of oxidization, acidification, decarboxylation and oxidization after cyclizing methylglyoxal and o-phenylenediamine which are taken as the original raw materials to directly prepare Acipimox. The method dispenses with intermediate processing, thus greatly simplifying the process steps, and overcomes the defect that the intermediate is easy to oxidize slowly due to multi-step processing, simultaneously utilizes the catalyst for catalytic oxidation in the process of H2O2 oxidation so as to facilitate reaction, improves the reaction yield (66% of overall yield) and is more beneficial to industrial production.

The invention relates to a method for preparing lipid lowering medicament acipimox. Acipimox is prepared by synthetic reaction by using 5-methylpyrazine-2,3-dicarboxylic acid, water, acid, sodium tungstate and hydrogen peroxide as raw materials, wherein a mol ratio of 5-methylpyrazine-2,3-dicarboxylic acid, acid, hydrogen peroxide to sodium tungstate is 1:0.05-5:1-10:0.04-0.2. Acipimox is prepared by the method by one-step reaction, purity of the product exceeds 99.5% through once recrystallization, yield exceeds 80%, and the method is suitable for industrial batch production. The method has advantages of low cost of raw material, short synthetic route, simple technology, convenient operation, simple post-treatment, safety and environmental protection of the solvent, basic no pollution of the oxidizing agent, no need of organic solvent in the reaction process, greening, environmental protection, small pollution and wide market prospect, and the production cost is less than a half of that of the prior method.

The invention discloses a method for preparing an acipimox-ethylcellulose sustained release micro-capsule. The method comprises the following steps: (1) dissolving ethyl cellulose powder into a volatile organic solvent to obtain a solution a; (2) adding the acipimox powder to the solution a to obtain a solution b under an agitation state, wherein the mass ratio of the acipimox powder to the ethyl cellulose powder is (1:1) to (3:1); (3) dissolving an emulsifier sodium dodecyl benzene sulfonate into nonvolatile high boiling liquid at 30-35 DEG C to obtain a solution c, wherein the volume ratio of the nonvolatile high boiling liquid to the volatile organic solvent is (3:1) to (5:1), and the mass percent concentration of the sodium dodecyl benzene sulfonate in the solution c is 1-2%; and (4) adding the solution b to the solution c at 30-35 DEG C, agitating for 3-6 hours, then carrying out suction filtration, washing the solid by water, and naturally drying at room temperature. By adopting the method disclosed by the invention, the half-life period of the acipimox medicine can be prolonged, the bioavailability of the medicine is improved, and the medicine action time is prolonged.

The invention provides a new osmotic pump controlled-release pharmaceutical composition for treating hyperlipemia and a preparation method thereof, one of which is a nicotinic acid drug of acipimox, and the other is a statin drug of pitavastatin calcium; wherein, the acipimox is the controlled-release part, the pitavastatin calcium is the rapid-release part; or the acipimox and the pitavastatin calcium are both the controlled-release parts. A compound osmotic pump preparation has the advantages of comprehensive action, low toxicity and side effects and convenient use.

The invention discloses medicament for treating cardiac neurosis and a preparation method of the medicament. The medicament solves the problem that existing medicament is poor in effect on treatment of cardiac neurosis and has side effects. The medicament for treating cardiac neurosis comprises the following main materials of schisandra chinensis, manyprickle acanthopanax roots, albizzia julibrissin durazz, American ginseng, radix polygoni multiflori preparata, magnetit, fungus ganoderma lucidum, angelica sinensis, prepared dried rehmannia, fushen, agarwood and semen ziziphi spinosae. The medicine further comprises the following auxiliary materials of lumbrokinase, polypeptide, multivitamins, water-soluble dietary fibers, acipimox, phosphatidylcholine and honey. The medicament has the good curative effect on common cardiac neurosis in cardiovascular diseases, and has wide application prospect in the fields of treatment of palpitation, precardium area pains, dyspnea, panasthenia, anxiety, sinus arrhythmia and the like.

The invention relates to a production method of acipimox, wherein the production method comprises the following specific steps: under cooling and stirring, dissolving 78 g of maleic anhydride in 60 ml of a chloroform solution, adding 40 ml of a 30% hydrogen peroxide, 2 h later, adding 4.8 g of 5-methylpyrazine-2-carboxylic acid, keeping for 2 d at the temperature of 0-5 DEG C, filtering to remove maleic acid, concentrating to leave small volume, adding ethyl acetate, and filtering to obtain 1.1 g of acipimox with the melting point of 178-180 DEG C. According to the production method of acipimox, the manufacturing cost is low, and the production is convenient.

The invention relates to a composition capable of curing abnormal blood lipid. The composition capable of curing the abnormal blood lipid comprises ezetimibe, atorvastatin calcium and acipimox. The range of weight ratios of the ezetimibe, the atorvastatin calcium and the acipimox in the composition is 5-10: 5-80: 250-1000, preferably 10: 10-40: 250-750 and optimally, 10: 10-20; 500-750. The composition capable of curing the abnormal blood lipid is strong in blood lipid regulating effect, comprehensive in function and little in side effect.

The invention belongs to the field of pharmaceutical chemicals, and particularly relates to a preparation method of acipimox. The method for preparing acipimox comprises the following steps of adding5-methylpyrazine-2-carboxylic acid into purified water, adding concentrated hydrochloric acid for salifying, adding an oxidant, cooling and crystallizing to obtain the acipimox. The method has the advantages of simple reaction conditions, high selectivity in the nitrogen oxide formation process, avoiding of the use of a metal catalyst, simplification of the preparation process, effective improvement of the yield and the purity of the acipimox, and suitableness for industrial production.