44 results about "Cefadroxil" patented technology

The present invention relates to dry cefadroxil suspension and its preparation process, belongs to the field of medicine technology, and is for raising the water solubility and bioavailability of cefadroxil. The dry cefadroxil suspension consists of cefadroxil and supplementary material comprising including agent, water soluble stuffing, distintegrating agent, suspension assistant and adhesive. The dry cefadroxil suspension has the features of high medicine solubility, high medicine bioavailability, high chemical stability, good taste, convenient taking, high patient's compliance, full absorption in gastrointestinal tract, less irritation to gastrointestinal tract of medicine, etc.

The invention relates to a cefadroxil tablet and a preparation method thereof, and belongs to the technical field of medicines. The cefadroxil tablet comprises the following components in parts by weight: 125-500 parts of cefadroxil, 35-60 parts of starch, 40-120 parts of 10% starch paste, 2-6 parts of magnesium stearate, and 3-12 parts of sodium carboxymethyl starch, wherein X-ray powder diffraction pattern of cefadroxil has characteristic peaks at 2theta of 4.27+ / -0.2 degree, 8.52+ / -0.2 degree and the like; and the differential scanning calorimetry pattern of cefadroxil has characteristic peaks at 189-190 DEG C. Compared with the prior art, the impurity content is not significantly changed under the conditions of high temperature, high humidity and strong light, and the stability is greatly improved; pharmacokinetic experiment results show that the bioavailability of the cefadroxil tablet is significantly improved compared with that of commercially available cefadroxil tablets.

The present invention discloses isolation of Penicillin Acylase (PA) from Achromobacter sp CCM 4824 expressed in recombinant strain E. coli BL21 CCM 7394 bearing the recombinant plasmid pKXIP1 and processing of PA into biocatalyst useful for the industrial synthesis of antibiotics. More particularly the invention discloses a synthesis of semi-synthetic [beta]-lactam antibiotics in the reaction mixture consisting of activated acyl-donor (D-p-hydroxyphenylglycine methyl ester or amide for Amoxicillin and Cefadroxil; D-phenylglycine methyl ester or amide for Ampicillin and Cephalexin) and nucleophile (6-APA or 7-ADCA) catalyzed by PA obtained from recombinant E. coli BL21 CCM 7394 as the biocatalyst.

The invention provides a cefadroxil tablet. The cefadroxil tablet is prepared by mixing and tabletting cefadroxil particles, micro-crystal cellulose and a lubricating agent. The cefadroxil particle comprises the following ingredients: 250 parts by weight of cefadroxil, 10 to 20 parts by weight of micro-crystal cellulose, 2 to 4 parts by weight of starch, and 4 to 6 parts by weight of carboxymethyl starch sodium. Compared with the prior art, the cefadroxil tablet adopts the carboxymethyl starch sodium as a disintegrating agent which is unique in swelling effect; moreover, the micro-crystal cellulose is respectively added in the granulating and tabletting process, so that the cefadroxil is more uniformly dispersed, a product tablet core has good disintegrating effect, the particles can be rapidly disintegrated, the dissolution rate of the product is high, and the disintegrating time is short. The experiment result shows that the dissolution rate of the cefadroxil tablet is 87 to 103 percent, and the disintegrating time is 4 to 6 minutes.

The invention discloses a synthetic method of cefadroxil. The synthetic method of cefadroxil comprises the following steps of: dissolving 7-aminodesacetoxycephalosporanic acid by adopting organic base at the temperature ranging from minus 10 DEG C to minus 50 DEG C to obtain 7-aminodesacetoxycephalosporanate; carrying out reaction on HPCDane salt and pivaloyl chloride at the temperature ranging from minus 20 DEG C to minus 70 DEG C to generate mixed anhydride and carrying out condensation reaction on the mixed anhydride and 7-aminodesacetoxycephalosporanate, extracting and regulating pH value of a water layer, then separating salt and regulating pH value, and crystallizing to obtain cefadroxil. By adopting the manner, the synthetic method of cefadroxil has the advantages that a process is simple, solvate does not need to be formed in a synthetic process, crystallization can be directly carried out in water, consumption of an organic solvent is reduced, production cost is reduced, yield of cefadroxil is high, various quality indexes are qualified, pharmacopeia standards are met, and implementation of industrial production can be facilitated.

The invention belongs to the technical field of medicines, and particularly relates to a cefadroxil compound and pharmaceutical composition comprising the same. The cefadroxil compound is a cefadroxil hydrate with the molecular formula of C16H17N3O5S*3.5H2O, and the structural formula is shown in the specification. Various pharmaceutically-acceptable dosage forms can be prepared from the pharmaceutical composition comprising the cefadroxil compound, and chewable tablets and capsules are preferred. The cefadroxil compound has the advantage of capability of significantly improving the water solubility and the hygroscopicity of cefadroxil compounds.

The invention relates to a cefadroxil compound and a preparation method thereof. The preparation method comprises the following steps: 1) adding ethanol or ethyl ether into cefadroxil serving as a raw material, keeping the temperature below 30 DEG C, fiercely stirring, filtering, washing filter cake with ethanol or ethyl ether at a temperature of below 15 DEG C, drying under vacuum or in the air;2) placing the filter cake in ammonia water, mildly stirring, keeping pH value below 9, obtaining ammonia water solution of cefadroxil, and filtering out precipitate; 3) slowly adding hydrochloric acid at concentration of 1 to 3 mol / L into the ammonia water solution of cefadroxil, keeping the temperature between 30 and 60 DEG C, keeping the final pH between 4.0 and 6.0, keeping the pH value for 30 minutes to 5 hours till crystals precipitate slowly, lowering the temperature to a minimum value of 10 DEG C, standing, crystallizing, filtering under vacuum, drying and thus obtaining refined cefadroxil; and 4) returning crystallization mother solution in which crystals precipitate to the step 3). When the method disclosed by the invention is used, the purity of the cefadroxil is increased, thecontent of related matters is lowered obviously, the quality of preparation product is improved, and the toxic and side effects are reduced.

The invention provides a cefadroxil liposome solid preparation. The cefadroxil liposome solid preparation consists of the following components in part by weight: 125 parts of cefadroxil, 90 to 120 parts of phosphatidylinositol, 30 to 40 parts of dimyristoyl phosphatidylcholine, 50 to 70 parts of cholesterol and 300 to 500 parts of other auxiliary materials which are used commonly and pharmaceutically. The liposome solid preparation is high in entrapment rate, and has uniform grain sizes, and medicines can be kept for a long time in blood circulation; and the quality of the preparation products is improved, the toxic and side effects are reduced, the equipment of a preparation method is simple and is easy to operate, and the cefadroxil liposome solid preparation is suitable for large-scaleindustrial production.

The invention discloses a compound dispersible tablet, which contains active components of cefadroxil and ambroxol hydrochloride, and the pharmacologically-acceptable excipient. The compound dispersible tablet is used for curing the upper respiratory tract infection.

The invention belongs to the technical field of pharmaceutical preparations and particularly relates to cefadroxil dispersible tablets and a preparation method therefor. A prescription for the cefadroxil dispersible tablets per 10,000 tablets comprises the following ingredients by weight: 5,000g of cefadroxil, 1,000g-1,300g of filler, 500g-800g of disintegrant and 20g-100g of magnesium stearate. The preparation method comprises the steps of weighing the cefadroxil, the filler and the disintegrant according to prescription amounts, carrying out uniform mixing, then, adding the lubricant, i.e.,magnesium stearate, carrying out uniform mixing, then, carrying out tabletting by a tabletting machine, thereby obtaining the cefadroxil dispersible tablets. The cefadroxil dispersible tablets prepared by the preparation method are uniform in unit-time drug release, readily available in raw materials and controllable in quality. According to the preparation method, the cefadroxil dispersible tablets are produced by employing a mixed-powder direct-tabletting process, the process is simple, the quality is stable, the operation is easy, the method is applicable to large-scale production, and therisk of degradation of the cefadroxil is avoided.

The invention discloses a method for measuring cefadroxil concentration in plasma through hygroplasm combination. A hygroplasm combination system is adopted for measurement. The method comprises the steps that firstly, a to-be-measured sample is taken, a certain quantity of mixed organic solvent is added for conducting extraction twice, and after pretreatment, through chromatographic column separation, a mass spectrometry detector is used for detection. The method is quick to use, accurate, high in sensitivity and easy and convenient to operate, and the basis is provided for plasma concentration measurement of cefadroxil. The linear range of a plasma standard curve is within 0.1-60 mug / mL, the within-run precision and between-run precision RSD are smaller than + / -15%, and the method is suitable for measurement of cefadroxil concentration in plasma.

A cefadroxil dry suspension and a preparation method thereof belong to the technical field of medicine and are used for solving the problems of improving the water solubility and bioavailability of cefadroxil. It consists of the main drug cefadroxil and auxiliary materials. The content of each main and auxiliary material in the total prescription by weight unit is as follows: cefadroxil 80-120, inclusion agent 16-60, water-soluble filler 440-520, disintegrant Solution 55-70, suspending agent 5-10, binder 30-45. The product of the invention has the characteristics of high drug solubility and bioavailability, good chemical stability, good taste, convenient taking, strong patient compliance and the like. The invention is made into a dry suspension dosage form, which can be widely distributed in the gastrointestinal tract, has more absorption points, more sufficient absorption, and reduces the local stimulation of the drug on the gastrointestinal tract.

The invention discloses a penicillin G acylation enzyme mutant, and application thereof in synthesis of cephalosporin antibiotics. An amino acid sequence of the penicillin G acylation enzyme mutant is shown in SEQ ID NO.1; a nucleotide sequence of an encoding gene is shown in SEQ ID NO.2. The invention also provides application of the penicillin G acylation enzyme mutant in synthesis of cefaclor. The invention provides a novel penicillin acylation enzyme mutant. Compared with the wild penicillin acylation enzyme mutant, the penicillin G acylation enzyme mutant has higher activity in synthesis of cephalosporin antibiotics, such as cefprozil, cefaclor or cefadroxil; especially when the penicillin G acylation enzyme mutant is used for catalyzing 7-ACCA and phenylglycine methyl ester to synthesize the cefaclor, the vitality is improved to 29.8U / mg from 1.2U / mg in the past, the synthesis and hydrolysis activity is almost consistent with that of the wild penicillin acylation enzyme mutant, the synthesis and hydrolysis ratio can be up to 1.7, and the yield of the cefaclor can be up to 71.5%.

The invention provides a cefadroxil tablet, which is prepared by compressing cefadroxil granules, microcrystalline cellulose and a lubricant after mixing; the cefadroxil granules include the following components: 250 parts by weight of cefadroxil; 10-20 parts by weight of crystalline cellulose; 2-4 parts by weight of starch; 4-6 parts by weight of sodium carboxymethyl starch. Compared with the prior art, the cefadroxil tablet provided by the invention uses sodium starch glycolate as a disintegrating agent, which has a unique swelling effect, and microcrystalline cellulose is added respectively in the granulation and tabletting process, so that the main drug The dispersion of cefadroxil is more uniform, so that not only the tablet core of the product has a better disintegration effect, but also the granules can disintegrate rapidly, and the product has a high dissolution rate and a short disintegration time limit. Experimental results show that the dissolution rate of the cefadroxil tablet provided by the invention is 87%-103%, and the disintegration time limit is 4min-6min.

The invention discloses a method for extracting and recycling penicillin sulfoxide. The method comprises the following steps that a, a penicillin sulfoxide solution is subjected to impurity separation through resin absorption; b, a penicillin sulfoxide desorption solution is obtained through resin desorption; c, a penicillin sulfoxide crystallization solution is obtained through the mechanical application of dissolution penicillin sulfoxide to the penicillin sulfoxide desorption solution or concentration of the penicillin sulfoxide desorption solution; d, the pH of the crystallization solution is adjusted with acid for crystallization, and the penicillin sulfoxide is obtained through filtration, washing and drying. The method can be used for extracting and recycling the penicillin sulfoxide from the low concentration penicillin sulfoxide solution, and therefore the yield of the penicillin sulfoxide is increased, the production cost is reduced, and environmental pollution is reduced. The quality of subsequent products like 7ADCA, cefradine, cefalexin and cefadroxil prepared from the penicillin sulfoxide produced through the technology is improved. Pharmaceutical compositions formed by cefradine, cefalexin, cefadroxil and a medically acceptable carrier can be utilized for treating respiratory tract infection like acute tonsillitis, angina, tympanitis, nasosinusitis, bronchitis and pneumonia, urinary tract infection, skin soft-tissue infection and the like caused by sensitive bacteria.

The invention discloses an indirect-competitive ELISA (Enzyme-linked Immunosorbent Assay) kit for detecting cephalosporin antibiotics in animal derived foods and application of the kit. The kit comprises an ELISA plate coated with a coating antigen, a cephalosporin antibiotic standard substance, a cephalosporin antibiotic general antibody, an enzyme labeled secondary antibody, a dilution buffer, a washing buffer, a substrate developing solution and a stop solution, wherein the cephalosporin antibiotic general antibody is capable of specifically identifying cefalexin, cefradine, cefadroxil, cefoperazone, cefazolin or cefotaxime and cannot identify penicillin sodium. According to the cephalosporin antibiotic general antibody prepared in the invention, the general antibody and most of cephalosporin antibiotics have high cross reaction rates, while hardly have any cross reaction for the analogue penicillin sodium containing a beta-lactam ring; and therefore, the general antibody has high specificity. The kit prepared by the general antibody has the advantages of high sensitivity, capability of detecting many types of drugs, low cost, simple operation and short detection time.

A method for preparing cefadroxil, comprising the steps of: adding a predetermined volume of ionic liquid and a phosphate buffer solution to form a co-solvent in a water-bath constant temperature reactor; adding D-HPGM and 7-ADCA of a predetermined molar ratio to the co-solvent and stirring it, the molar ratio of D-HPGM and 7-ADCA is 1:1~1:2.0; the concentration of 7-ADCA is 0.1~1.0mol / L; Magnetically immobilize penicillin G acylase, and keep stirring to make the magnetically immobilized penicillin G acylase fully contact with D-HPGM and 7-ADCA until the end of the reaction; The upper phosphate buffer solution of cefadroxil is layered with the lower ionic liquid, and the pH of the separated phosphate buffer solution is adjusted to 4.0-5.5, so that cefadroxil crystals are precipitated and dried.

An oral disintegrating tablet of dracefal contains dracefal and the medicinal excipient (water-soluble filler, disintegrant, lubricant, wetting agent, or adhesive). Its preparing process is also disclosed. Its advantages are high disintegrating speed, quickly taking its effect, less residue and low by-effect.

The invention relates to cefadroxil chewable tablets and a preparation method thereof. The cefadroxil chewable tablets provided by the invention comprise the following raw material components in parts by weight: 110-550 parts of cefadroxil, 240-1,050 parts of mannitol, 110-500 parts of sucrose, 15-90 parts of maltodextrin, 0.5-5 parts of aspartame, 10-70 parts of sweet orange powder essence, 0.5-5 parts of menthol, a proper amount of water and 3-25 parts of magnesium stearate. The cefadroxil chewable tablets provided by the invention have high absorption speed, no lingering bitterness and excellent mouthfeel.

The invention belongs to the technical field of pharmaceutical preparations, and provides a cefadroxil dispersion coated tablet and a preparation method thereof. The cefadroxil dispersion coated tablet is prepared from the following components in parts by weight: 250 parts of cefadroxil, 185 parts of microcrystalline cellulose, 25 parts of low-substituted hydroxypropyl cellulose, 37.5 parts of carboxymethyl starch sodium, 1.25 parts of magnesium stearate and 174.8 parts of ethanol. The coated tablet is a gastric-soluble type film coating, and the gastric-soluble type film coating is prepared from gastric-soluble type coating powder and purified water. The preparation method comprises the following steps: S1, weighing the raw material components in proportion; S2, preparing a cefadroxil tablet; S3, preparing a coating solution; and S4, performing coating. The cefadroxil coated tablet prepared by the preparation method provided by the invention adopts a water-soluble coating material, can be quickly dissolved out, has the advantage of quick effect, and meets the requirements that the antibiotic drug is quickly absorbed and the blood concentration reaches a peak value in a short time; and meanwhile, the coating treatment covers odor, so that poor compliance of a patient caused by oral disintegration is avoided, and the cefadroxil dispersion coated tablet is easy to orally take.