68 results about "Cefprozil" patented technology

The invention relates to a cefprozil submicron emulsion solid preparation and new application thereof in the preparation of medicine for treating acute plasma cell mastitis. The cefprozil submicron emulsion granule comprises cefprozil, yolk lecithin, poloxamer 188 and deoxysodium cholate with the weight ratio of 1:2.3-14:1.2-8:0.8-10.

The invention relates to a preparation method of a medicinal preparation taking cefprozil as a main ingredient, and in particular relates to a preparation method of a cefprozil dispersible tablet with higher bioavailability. The method comprises the following steps of: taking the cefprozil in a therapeutic dose as a main active medicine ingredient; micronizing the cefprozil; adding an additive in proper quantity into the cefprozil to be pelletized by using a dry method; and pressing a pellet into the tablet. The cefprozil dispersible tablet comprises the following ingredients in parts by weight: 250+/-5 parts of the cefprozil, 180+/-20 parts of microcrystalline cellulose, 100+/-10 parts of micronized lactose or pregelatinized starch, 30+/-3 parts of hydroxypropyl cellulose; 5+/-2 parts of lauryl sodium sulfate, 2.5+/-1 parts of magnesium stearat and 2.5+/-1 parts of stevioside, wherein the micronized cefprozil is in the shape of powder with the particle diameter of 60 to 150 mu m. The method provided by the invention has the advantages that the production process is simple; and the prepared cefprozil dispersible tablet is high in dissolution rate and stable in quality.

The invention relates to a cefprozil suspension pharmaceutical composition, in particular to a suspension pharmaceutical composition containing cefprozil and xanthan gum. The cefprozil and the xanthan gum are uniformly mixed according to a certain proportion, pharmaceutic adjuvants, such as appropriate amount of disintegrating agent, diluent, flavoring agent, deodorant or lubricant and the like, are added in the mixture, then, the mixture is prepared into standard suspension in a manner of dry granulation or directly filling dry powder. The xanthan gum used as a suspending aid is less in dosage and excellent in adding suspension, the stability of the basic remedy is excellent, and simultaneously, the composition is free from solubilizer and preservative, so that the problem that the existing cefprozil suspension is long in dispersion time in water and low in safety, and has various accessories; and the compliance for taking the composition by a patient is further improved while the effectiveness and the safety of clinical application are ensured.

The invention relates to the field of medicine, and in particular relates to a cefprozil compound, and dispersible tablets, a dry suspension and a preparation method thereof. The cefprozil compound is a crystal, and an X-ray powder diffraction diagram obtained by Cu-K alpha ray measurement is shown in figure 1. Through experimental detection, the cefprozil dispersible tablets and the dry suspension have the advantages of superior stability and quite good smell and taste, and are quite suitable for clinical application.

The invention discloses a recovery method of cefprozil. The method comprises the steps of dripping dimethylformamide and acetone in a cefprozil refined mother solution to obtain the crude cefprozil; adding the crude cefprozil into a mixed solvent, adjusting the pH value of the solution with hydrochloric acid, activated carbon fading, and adjusting the pH value of stronger ammonia water; and finally cooling crystallization, suction filtration and drying to obtain the end product of cefprozil. The recovery method has the advantages that 95% of cefprozil can be extracted from the mother solution, so that the wastewater treatment pressure is greatly reduced, and the end product meets the pharmacopeia standards after recovery and treatment; and in addition, the recovery method is simple and convenient to operate, and dimethylformamide, acetone and isopropanol can be recycled and utilized.

The present invention relates to an improved process for the preparation of 3-propenyl cephalosporin DMF solvate, more particularly, the present invention relates to an improved process for the preparation of cefprozil DMF solvate of the formula (I), which is useful for the preparation of cefprozil of the formula (XIV).

The invention relates to a cefprozil liposome, a preparation method thereof and a dry suspension containing the cefprozil liposome. The cefprozil liposome comprises cefprozil, hydrogenated soya bean lecithin, hydrogenated yolk lecithin, cholesterol and vitamin E in the weight ratio of 1:(1.25-5):(1.25-5):(2.5-10):(0.1-3). The dry suspension containing the cefprozil liposome not only conforms to the requirements of Chinese pharmacopoeia, but also has the advantages of more stable storage at normal temperature, rapider effect taking and obviously increased bioavailability compared with common cefprozil medicine compositions.

The invention relates to a method for synthesizing cefprozil through a green enzymatic method. The method includes following steps: S1, adding parent nucleus 7-APRA or hydrochloride thereof into a buffer solution, and adding D-para hydroxybenzene glycinate derivative and/or D-para hydroxybenzene glycine amide under the condition that pH is 5-8; S2, adding cefprozil synthetase into the S1, reacting at temperature of 15-30 DEG C and pH of 6.5-7.8 for 1-3h, separating out separation liquid after reaction finishes, and immobilizing cefprozil synthetase to obtain a cefprozil crude product; S3, subjecting the crude product obtained in the S2 to acidolysis dissolved clarification, filtering and re-crystallizing to obtain cefprozil. Raw materials are cheap and easy to obtain, reaction is simple, hydrolysis activity of penicillin acylase can be effectively inhibited, and production cost is low; compared with conventional chemical synthesis methods, the method is simple and convenient to operate and low in cost, synthesis period is shortened, production efficiency is improved, total yield is high, controllability is high, and needs on industrial production are met.

The invention relates to a method for preparing cefprozil in a pH responsive regenerative double aqueous phase system. The method comprises (1) preparing two double-aqueous phase systems, (2) orderly adding 7-APRA, D-p-hydroxyphenylglycine methyl ester hydrochloride into the systems, adjusting solution pH to 5.00-6.50 and controlling a solution temperature in a range of 10-30 DEG C, (3) adding immobilized penicillin acylase into the solution obtained by the step (2), and (4) standing the mixed solution, removing the immobilized penicillin acylase, adjusting the pH of the reaction solution, recovering P<ADBA>/<PMDB> and P<ADB>/P<MDB> polymers of the double-aqueous phase systems, feeding the supernatant to a crystallization section, carrying out crystallization, and carrying out centrifugation, washing and drying to obtain a product. The method reduces a chemical synthesis cost, improves a low product conversion rate of the monohydrolase catalytic reaction, effectively improves a yield, simplifies the operation, reduces a cost and realizes easy recovery of the double-aqueous phase systems.

The invention relates to a synthesis method of cefprozil. The synthesis method comprises the following steps: under the existence of an enzyme, enabling parent nucleus 7-APRA and a D-4-hydroxyphenylglycine ester derivative to react with each other, and before the precipitation of cefprozil, adding cefprozil, with the purity greater than 99%, taken as a seed crystal, into a reaction system. According to the invention, the reaction efficiency is improved, the synthesis period is shortened, the conversion rate of 7-APRA is increased, and the purity of the obtained cefprozil is improved; the method is an enzymatic method, and the enzymatic catalysis is only required, water is taken as a solvent, and any organic solvent is not required during the reaction process, so that the environment friendliness is achieved, the route is simple, the product yield is high, and the purity is high.

The invention relates to a method for preparing cefprozil mother nucleus 7-amino-3-acryl cephalosporanic acid. According to the method, 7-amino cephalosporanic acid is adopted as a starting raw material, silylation protection, phosphorusylide formation, wittig reaction and silylation protection group removing are sequentially performed to obtain a cefprozil mother nucleus crude product, and a cefprozil mother nucleus crude product refining post-treatment process is added, wherein the cefprozil mother nucleus crude product refining post-treatment process comprises: a, amine salt forming, b, decolorization treatment, and c, cefprozil mother nucleus refined product preparing. According to the present invention, the prepared cefprozil mother nucleus has characteristics of high purity, good crystalline form, good color and high yield, the ratio of the E isomer content to the Z type isomer content is optimal so as to ensure the improved quality of the cefprozil prepared at the latter stage, the cefprozil mother nucleus purity can achieve 99.7%, the 7-ADCA is less than or equal to 0.15%, the crystalline form is hexagonal columnar, separation is easy, the patina is not easily generated, the color is less than or equal to Y-4 and is basically bright white, the yield is high, the quality is good, and the mass yield is more than 65%.

The invention discloses cefprozil suspension. The cefprozil suspension is prepared through the following steps that 1, a diluent and microcrystalline cellulose & sodium carboxymethylcellulose are placed in a wet type granulator to be premixed; 2, cosolvent and wetting agents are added to conduct wet granulation; 3, whole grains are dried and marked as the material A; 4, cefprozil, suspending agents and wetting agents are mixed with the material A in an equivalent progressively-increasing mode, and the mixture is subpackaged after being evenly mixed, and the cefprozil suspension is obtained; the suspending agents are selected from one of xanthan gum or sodium carboxymethylcellulose or hydroxypropyl methyl cellulose; the weight proportion of the microcrystalline cellulose & sodium carboxymethylcellulose and suspending agents ranges from 2:1 to 8:1; the wetting agents are folic acid solutions with the concentration being 1 wt%. The cefprozil suspension is low in impurity content, high in dissolution rate, good in stability, even in main medicine spreading and simple in preparing process, no special equipment is needed, and the cefprozil suspension is capable of being suitable for industrialized mass production.

The invention relates to an anti-infection oral medicinal preparation and discloses a cefprozil medicinal composition. The cefprozil medicinal composition comprises cefprozil serving as an active ingredient, at least one filling agent, at least one disintegrating agent, at least one lubricating agent, 1 to 10 weight percent of pregelatinized starch and 0.5 to 2 weight percent of hydroxypropyl methylcellulose. The invention also relates to a preparation method for the preparation and application of the preparation to treatment for upper respiratory tract infection, lower respiratory tract infection and skin and skin soft tissue infection.

The invention relates to a method for recycling methanol in the preparation of a cefprozil intermediate. The method comprises the following steps: (1) reacting GCLE used as an initial raw material with sodium iodide and triphenylphosphine to generate intermediate phosphorus onium salt, and carrying out Witing reaction on phosphorus onium salt and acetaldehyde to generate GPRE; (2) after the Witing reaction is finished, carrying out reduced pressure distillation to remove dichloromethane, and then dropwise adding methanol and water to precipitate the GPRE; (3) carrying out suction filtration on a reaction liquid, wherein a filter cake is the GPRE, filter liquor is mother liquor and contains methanol and the water; (4) transferring the mother liquor to an evaporator, and evaporating and recovering methanol (which contains the water); (5) measuring the water ratio of recovered methanol; and (6) adding recovered methanol to the step (2) in proportion to continue a subsequent step. The method disclosed by the invention can be used for mainly solving the problem of recycling of methanol, obtaining preferable yield and product quality, solving the problem of pollution of a large amount of organic waste liquor, reducing the cefprozil production cost and realizing the maximization of economic benefits.

The invention discloses a cefprozil mother liquor application technique, comprising the steps of (1) adding saturated FeCl3 solution into cefprozil mother liquor to adjust pH; (2) after cefprozil synthetic reaction is over, adding the cefprozil mother liquor treated in step (1) into the reaction liquid, raising the temperature, stirring at a controlled temperature, allowing standing, and dividingthe liquid; (3) cooling an aqueous layer divided from step (2) to below -5 DEG C, adding dimethylformamide at a controlled temperature, adding acetone washing liquid, stirring, filtering, and collecting filtrate; (4) cooling the filtrate, dropwise adding liquid ammonia to adjust pH, cooling, stirring, filtering, collecting filter cake, washing with dimethylformamide, washing with acetone, and drying in the vacuum to obtain crude cefprozil; and (5) refining the crude cefprozil. The cefprozil mother liquor application technique is simple and convenient to perform, usage of dimethylformamide andacetone is greatly reduced, and the cefprozil mother liquor application technique has significant economic and environmental benefits.

The invention provides a method for detecting zymoprotein residues in cefprozil prepared by an enzymatic method. The method is characterized by comprising the following steps: preparing a Coomassie brilliant blue G-250 dye solution and a standard protein stock solution; preparing a standard curve solution by taking a sodium bicarbonate solution as a solvent; preparing a blank solution by taking asodium bicarbonate solution as a solvent; preparing a test sample determination solution by taking a sodium bicarbonate solution as a solvent; drawing an absorbance-protein concentration standard curve through blank solution correction by using an ultraviolet spectrophotometer; and calculating the residual content of zymoprotein contained in the test sample according to the absorbance value read by the test sample determination solution. Sodium bicarbonate is ingeniously selected as a solvent, cefprozil can be dissolved, zymoprotein can be fully dissolved, the residual quantity of zymoproteinin a cefprozil product prepared through an enzymatic method can be effectively measured, the medication safety of medicine is improved, and the detection method is easy to operate, high in accuracy and good in reproducibility and reliability.

The invention relates to a preparation method of cefprozil. A synthesis method comprises the following steps: taking 7-ACA (7-aminocephalosporanic acid) as a starting raw material; after carrying outsilylation protection, carrying out a series of reactions including iodination and the like to generate a compound 2; taking the compound 2 to react with methyl D-(-)-4-hydroxy-phenylglycinate under the catalysis of immobilized penicillin acylase to generate a compound 1, so as to obtain a target product cefprozil. The preparation method provided by the invention has the advantages of moderate reaction conditions, environmental friendliness, high conversion ratio, simple technology and high cis-isomer content.

The invention relates to a cefprozil liposome and a preparation method thereof as well as a capsule containing the cefprozil liposome. The cefprozil liposome comprises cefprozil, hydrogenated yolk lecithin, soyabean lecithin, cholesterol and vitamin E, wherein the weight ratio of the cefprozil to the hydrogenated yolk lecithin to the soyabean lecithin to the cholesterol and to the vitamin E is 1:(1.25-5):(1.25-5):(2.5-10):(0.1-3). The cefprozil capsule not only meets the Chinese pharmacopoeia requirement but also has the advantages of higher dissolution rate, faster action of medicament effect and obvious improvement of bioavailability compared with those of a common cefprozil pharmaceutical composition.