41 results about "Cefpiramide" patented technology

The present invention relates to a method of using a superfine pulverizing technology to prepare sterile powder for injection (powder injection) of chemical medicine and the prepared medicine powder injection. Invert sugar, clindamycin phosphate, cefpiramide sodium, cefepime hydrochloride, latamoxef sodium or cefmetazole sodium are preferable as the chemical medicine.

The stable cephalosporin powder for injection is mixture of bacteria-free cefpiramide and cosolvent in the weight ratio of 1 to 0.1-0.5. The cosolvent is sodium carbonate, arginine or sodium hydroxide. Compared with available cefpiramide injection, the cephalosporin powder for injection has the features of ever high stability, less impurity content and longer preservation period.

The invention relates to a cefpiramide sodium powder injection composition which contains cefpiramide crystals and anhydrous sodium carbonate, wherein the mass ratio of the cefpiramide crystals to the anhydrous sodium carbonate is (1:0.17)-(1:0.2); and in the X-ray powder diffraction, the main peaks of the cefpiramide crystals are displayed at the diffraction angles of 7.25 degrees + / -0.1 degree,10.04 degrees+ / -0.1 degree, 11.51 degrees+ / -0.1 degree, 12.04 degrees+ / -0.1 degree, 15.67 degrees+ / -0.1 degree, 17.65 degrees+ / -0.1 degree, 19.28 degrees+ / -0.1 degree, 22.52 degrees+ / -0.1 degree and 22.84 degrees+ / -0.1 degree. According to the invention, the water solubility of the cefpiramide crystals is improved to certain extent; when the cefpiramide crystals together with the anhydrous sodiumcarbonate are prepared into sterile powder injection, the amount of anhydrous sodium carbonate is greatly reduced, and the dissolution speed of the powder injection is high, that is to say, the powder injection can be completely dissolved in a short time, thereby being convenient for clinical use.

The invention provides a method for preparing cefpiramide acid. The method provided by the invention adopts (6R,R7)-3-[(1-methyl-1H-tetrazolyl-5-yl)thiomethyl]-7-amino-8-oxo-5-thia-1-azabicyclo-[4.2.0]octyl-2-alkenyl-2-carboxylic acid as a trimethylchlorosilicyl protective agent. The method provided by the invention is simple to operate, obviously enhances the product purity and yield, and can easily implement industrial production.

The invention relates to a cefpiramide sodium compound of a new way. The target product, i.e. cefpiramide sodium compound, is prepared by dissolving triphosgene, D-alpha-(6-methyl-4-hydroxy niacinamide)-p-hydroxy phenylacetic acid and triphenylphosphine oxide into an organic solvent, mixing and reacting the D-alpha-(6-methyl-4-hydroxy niacinamide)-p-hydroxy phenylacetic acid with the triphenylphosphine oxide, and then dripping reaction liquid into an aqueous 7-TMCA solution for reaction.

The invention discloses a method for refining cefpiramide acid, and belongs to the technical field of medicines. The method comprises the following steps: A, putting crude cefpiramide acid into a solvent 1, adding a transaminating agent, stirring and dissolving the mixture to clarification, so as to obtain a cefpiramide salt solution; B, adding a decolorizing agent into the cefpiramide salt solution, filtering and collecting filtrate; C, controlling the filtrate temperature to be 10-20 DEG C, adding a dissolution agent, filtering and collecting a solid crystal; D, putting the solid crystal into a solvent 2, controlling the temperature to be 10-15 DEG C, adding an acidic reagent to adjust the pH value to 2.0-3.0, adding a seed crystal, crystallizing, filtering and collecting the solid crystal of cefpiramide acid and mother liquor; and E, washing the solid crystal of cefpiramide acid and drying to obtain refined cefpiramide acid. The cefpiramide acid prepared with the method is high in purity, few in impurities and low in color grade; and the refining method provided by the invention has the advantages of being simple in process, environmentally friendly, and suitable for large-scaleindustrial production, saving energy, and the like.

The invention discloses a cefpiramide drug combination, which consists of the following effective ingredients in part by weight: 500 to 2000 parts of cefpiramide or pharmaceutically acceptable salt thereof (by cefpiramide), 100 to 200 parts of lidocaine, 20 to 100 parts of reduced glutathione and 50 to 100 parts of aspirin-DL-lysine. The drug combination cannot cause adverse reactions, and has a high curative effect, and moreover, the preparation method is simple and environment-friendly.

The invention discloses a preparation method of cefpiramide sodium, which belongs to the field of chemical pharmacy, and comprises the steps of preparing cefpiramide salt by using cefpiramide as raw material, forming salt and crystallizing, drying, and using gas to drive the atomized cefpiramide before drying. Purging with water for injection; the invention can reduce the solvent residue in the product, and the prepared cefpiramide sodium has the advantages of high purity and good stability, the preparation method is simple, energy-saving and environment-friendly, and is suitable for large-scale industrial production.

The invention discloses a method for crystallizing and producing cefpiramide sodium crystals. The method comprises the steps that: (a) cefpiramide acid and an transamination agent are dissolved in a solvent I, wherein the transamination agent is any one selected from triethylamine, diisopropylamine, and isopropylamine; and a temperature is controlled, and the materials are stirred until completely dissolved; (b) a salt-forming agent is added into a solvent II, wherein when the salt-forming agent is sodium ethylhexanoate, the solvent II is an acetone solvent, and when the salt-forming agent is sodium hydroxide, the solvent II is any one or a mixture of two selected from methanol and tetrahydrofuran; and the materials are stirred until completely dissolved; (c) the salt-forming agent solution is uniformly added into the solution of cefpiramide amine salt; the temperature is controlled, and crystal seeds are added; curing crystallization is carried out; acetone is added into the crystallization system for regulating the pH value of the crystallization system and for carrying out solvent-out crystallization; and filtering, washing, and drying are carried out, such that the cefpiramide sodium crystals are obtained. The method provided by the invention has the advantages of simple operation, uniform crystals, high purity, low impurity content, good stability, easy storage, and the like.

The invention relates to a method for synthesizing an intermediate of cephalosporins antibiotics cefpiramide, D-alpha-(6-methyl-4-hydroxy nicotinamido)-p-hydroxyphenyl acetic acid. The method comprises the steps of: reacting carboxyl group protected D-p-hydroxyphenyl glycine and anhydride or acyl chloride of 4-hydroxy-6-methylnicotinic acid to obtain acylated product, and hydrolyzing to remove the protecting group to obtain the target product D-alpha-(6-methyl-4-hydroxy nicotinamido)-p-hydroxyphenyl acetic acid. The method has the advantages of easy and feasible operation, and applicability to large scale production.

The invention belongs to the technical field of chemical synthesis, and particularly relates to a synthesis method of cefpiramide side chain acid. Pyridine-3-formic acid and methyl p-hydroxyphenylglycinate are used as raw materials, and the cefpiramide side chain acid is obtained through chlorination, acylation, hydrolysis and crystallization. The synthesis method of the cefpiramide side chain acid is simple to operate, easily available in raw materials and low in cost, adopts a dichloromethane and N, N-dimethylacetamide mixed solvent as a solvent, greatly improves the product yield and stability, has good economic benefits, and is convenient for large-scale industrial production.

The invention discloses cephalosporin nucleus derivative compound and cephaene onium salt compound prepared from the cephalosporin nucleus derivative compound, which are respectively intermediates for synthesizing cefpiramide sulfate, and a method for preparing the cefpiramide sulfate from the two intermediates, namely preparing 7beta-[2-(2-alkanol aminothiazol-5-yl)-2-methoxyimino acetamid]]-3-[3-alkanol amino-2-(2-alkanol oxy ethyl)-1-pyrazol onium]methyl-3-cephem-4-carboxylate (IV) by coupling 7beta-[2(2-alkanol aminothiazol-5-yl)-2-methoxyimino acetamid]]-3-(hydrocarbon sulfonate)-3-cephem-4-carboxylic acid (I) serving as a raw material with 5-alkanol amino-2-(2-alkanol oxy ethyl)-1-pyrazol, and then converting to obtain the cefpiramide sulfate. The method has the advantages of mild reaction conditions, short steps, cheap raw materials, industrial production, no special reagents, simple process and easy amplification.

The invention relates to a composite method for cefpiramide midbody D-alpha-(4-Hydroxy-6-methylnicotinamido) hydroxyphenylacetic acid, which includes the steps of using the acyl chloride of 4-hydroxy-6-methylnicotinic acid to directly acylate and esterify D-hydroxyphenylglycine, using water to remove the estersil of an acylation product and directly obtaining an objective product D-alpha-(4-Hydroxy-6-methylnicotinamido) hydroxyphenylacetic acid. Compared with the method of composing D-hydroxyphenylglycine into alkane ester or salt at first, the composite method for cefpiramide midbody D-alpha-(4-Hydroxy-6-methylnicotinamido) hydroxyphenylacetic acid simplifies the operation and is suitable for large-scale production.

The invention relates to a cefpiramide composite which is used for the cefpiramide powder-injection in the medicinal manufacture field. The invention discloses the following characteristic of the cefpiramide composite: the composite for the cefpiramide powder-injection which is prepare by the conventional production technology of powder-injection contains two or more of the following components: (a) sterile cefpiramide, (b) sterile sodium carbonate; and (c) sterile anhydrous glucose, dextrose monohydrate, sodium chloride, mannitol, sorbitol, anhydrous lactose or lactose monohydrate, wherein the weight ratio of the component (a) to the component (b) and the component (c) is 1:0.15-0.4:0.03-4.0. The invention has the advantages that the problem that the cefpiramide for injection on the market is difficult to dissolve, especially at a low temperature is solved; the operation of the nurse is easy; and the raw materials are accessible and the drug stability is good.

The invention relates to cefpiramide sodium micro-spheres and a preparing method thereof, belonging to the technical field of medicaments. A carrier material of each cefpiramide sodium micro-sphere is carboxy methyl chitosan while a slow release medicament of each cefpiramide sodium micro-sphere is cefpiramide sodium, wherein the content of the cefpiramide sodium is 5.3% to 5.5% of mass of the overall micro-sphere; each micro-sphere is 17.920 mum to 20.749 mum in average grain diameter and 2.799 in span of the grain diameter. The preparing method comprises the following step of: with biodegradable high molecular material, i.e., carboxy methyl chitosan as the carrier material, preparing highly water-soluble antibiotic-medicament, i.e., cefpiramide sodium into the slow release micro-sphere by using an emulsifying and dispersing-curing cross-linking method, wherein the micro-sphere is taken orally. The cefpiramide sodium micro-spheres disclosed by the invention can be used for reducing damage of intravenous drip to skins and mucous membranes of a patient, improving absorption of oral taking, and increasing bioavailability of the medicament; meanwhile, the cefpiramide sodium micro-sphere can be used for prolonging action time of the medicament, reducing dosage and improving compliance of the patient. The preparing method disclosed by the invention has the advantages of simpleness in operation, gentle conditions and strong controllability and is suitable for large-scale industrial production.