46 results about "Cefpodoxime Proxetil" patented technology

A pharmaceutical composition comprising a solid unit dosage form comprising: one or more of pharmaceutically active ingredients selected from valacyclovir, olanzapine, voriconazole, topotecan, artesunate, amodiaquine, guggulosterone, ramipril, telmisartan, tibolone, atorvastatin, simvastatin, amlodipine, ezetimibe, fenofibrate, tacrolimus, valgancyclovir, valsartan, clopidrogel, estradiol, trenbolone, efavirenz, metformin, pseudoephedrine, verapamil, felodipine, valproic acid/sodium valproate, mesalamine, hydrochlorothiazide, levosulpiride, nelfinavir, cefixime and cefpodoxime proxetil in combination with a water insoluble polymer and/or a water soluble polymer. Methods for making the pharmaceutical composition are also disclosed.

A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics

wherein

X is chlorine or bromine; R is hydrogen, C_1-4 alkyl group, an easily removable hydroxyl protective group, —CH₂COOR₅, or —C(CH₃)₂COOR₅, wherein R₅ is hydrogen or an easily hydrolysable ester group. The compound of formula (I) is prepared by reacting 4-halo-2-oxyimino-3-oxobutyric acid of formula (IV¹),

wherein X, R and R₅ are as defined above, with N,N-dimethylformiminium chloride chlorosulphate of formula (VII)

in an organic solvent at a temperature ranging from −30° C. to −15° C. The cephalosporins that may be prepared from the intermediate include cefdinir, cefditoren pivoxil, cefepime, cefetamet pivoxil, cefixime, cefmenoxime, cefodizime, cefoselis, cefotaxime, cefpirome, cefpodoxime proxetil, cefquinome, ceftazidime, cefteram pivoxil, ceftiofur, ceftizoxime, ceftriaxone and cefuzonam.

The invention relates to a cefpodoxime proxetil dry suspension composition and a preparation method thereof. The invention provides the cefpodoxime proxetil dry suspension composition, containing 100 parts by weight of the cefpodoxime proxetil and 20 to 500 parts by weight of the glyceryl behenate. The invention also provides the preparation method of the dry suspension composition. The dry suspension composition of the invention is capable of reducing bitterness of the cefpodoxime proxetil remarkably and improving compliance of a clinical patient, thereby being suitable for a child to take a drug.

The invention discloses a cefpodoxime proxetil submicron emulsion solid preparation and a novel application thereof, particularly a cefpodoxime proxetil solid preparation which is subjected to micro-emulsification and a novel application thereof. In the invention, the micro-emulsification technology is applied to process cefpodoxime proxetil raw materials so as to obtain a cefpodoxime proxetil submicron emulsion with excellent performance, the stability of the cefpodoxime proxetil is improved and the dissolution rate of the cefpodoxime proxetil preparation is obviously improved, so that the cefpodoxime proxetil submicron emulsion solid preparation has better bioavailability and can be used for preparing a medicament for treating osteomyelitis of jaws.

The invention specifically discloses a cefpodoxime proxetil taste-masking granule and a preparation method thereof, belonging to the field of medicinal preparations. The taste-masking granule is prepared through mixing of a coated cefpodoxime proxetil pellet and a taste-masking particle, wherein the coated cefpodoxime proxetil pellet is of a structure composed of three layers, i.e., a drug-loadedpellet, a separating layer and a smoothing layer from interior to exterior. The main objective of the invention is to overcome the problems that current commercially-available cefpodoxime proxetil products immediately produce unpleasant bitter taste when child patients take the products; the taste of the cefpodoxime proxetil products is bad, which leads to poor medication compliance of child patients; and the cefpodoxime proxetil products have to be dissolved in water before taking, which leads to inconvenience in administration. To improve the medication compliance of children, the inherent bitter taste of cefpodoxime proxetil is totally masked, and components like a sweetener applicable to children are increased, so the bitter taste of the chemical drug is eliminated and fragrant smell is increased; and thus, child patients easily accept the granule and are pleasant to the fragrant smell, so the medication compliance of children is improved. Besides improvement of the medication compliance of children, the granule provided by the invention also overcomes the problem of inconvenience in administration of children by adding special adjuvants which allow children to take the granulethrough direct swallowing without dissolving in water into a prescription.

The invention relates to the technical field of medicine and pharmacy and discloses a dry suspension of cefpodoxime proxetil composition and a preparation method thereof. The dry suspension of cefpodoxime proxetil composition is made from the following raw materials in parts by weight: 50 of cefpodoxime proxetil, 60 of sucrose, 71 of hydroxypropyl methylcellulose, 71 of xanthan gum and 200 of 95% ethanol. The 95% ethanol can serve as a pharmaceutical humectant for preventing drugs from caking and increasing dissolubility of drugs. The stability and safety of traditional Chinese medicines in the dry suspension of cefpodoxime proxetil composition are substantially not changed, to achieve safety and efficacy of medication. The trials show that the dry suspension of cefpodoxime proxetil composition has strong antimicrobial effect and good stability. The dry suspension of cefpodoxime proxetil composition can be widely applied to treatment of upper/lower respiratory infections, skin and soft tissue infections, urogenital system infections and pediatric infections.

The invention relates to a cefpodoxime proxetil compound of new route, which belongs to technology field of medicine. The steps comprise: (1) (Z) -2 - (2 - aminothiazole -4 - ethyl) -2 - methoxyimino aceticacid (AMAA in short) and p-nitrophenol react, 7-AMCA is added to the mixture and is stirred for reacting, the PH value is adjusted with hydrochloric acid to obtain the cefpodoxime acid; (2) PEG6000 is used as catalyst, the cefpodoxime acid reacts with 1 - iodine ethyl isopropyl carbonate to obtain the cefpodoxime proxetil. The advantages of the invention are as follows: the method has high yield, low cost, and obtained product of high purity; the content of delta2 isomer is low, and the invention is suitable for industrial production.

The present invention discloses one kind of soft cefpodoxime proxetil capsule and its preparation process. The medicine consists of medicine liquid and capsule shell, the medicine liquid contains cefpodoxime proxetil, matrix and stabilizer, and the capsule shell contains gelatin, glycerin, water, preservative and light screening agent. Compared with available cefpodoxime proxetil preparations, the present invention is even suitable for children and other people incapable of taking care of himself to take and has the advantages of high bioavailability, high stability, accurate content, etc.

The invention discloses a preparation method of cefpodoxime proxetil. In the method, a compound of formula II is used as an initial raw material, the intermediate compound of formula III is not separated during the process, and a crude product of cefpodoxime proxetil is synthesized by one step; and after that, a simple and easy recrystallization method is adopted for purifying the crude product of cefpodoxime proxetil to obtain cefpodoxime proxetil. In the preparation method disclosed by the invention, the yield is increased without reducing the quality, the obtained product has high purity, the synthesis path is simple, and the preparation method is suitable for industrial production.

A medication compound, which include cyclodextrin and cephalosporin ester's clathrate; this invention alao related to the method to produce it.

High-purity cefpodoxime propyl axetil can be prepared by a simple method comprising the step of reacting cefpodoxime salt with 1-iodoethyl isopropyl carbonate in an organic solvent in the presence of crown ether.

A stable taste masked, pharmaceutical composition comprising a plurality of coated, non-disintegrating discrete dosage units, said units comprising of a core comprising one or more cephalosporins such as cefuroxime axetil and cefpodoxime proxetil and one or more coating layers. Cefuroxime axetil is in α-crystalline and amorphous forms, where at least 30% of the Cefuroxime axetil is in the α-crystalline form, wherein the particle size distribution of the α-crystalline form being such that 100% of the particles have a particle size below 250μ. The ratio of the crystalline fraction to the amorphous fraction ranges from 0.3:0.7 to 0.99:0.01. The particle size of cefpodoxime proxetil is such that 90% of the particles are below 15μ. The process of preparation of coated, non-disintegrating pellets comprising the steps of reducing the particle size of the one or more cephalosporins, blending with the other excipients, wet granulation, extrusion, spheronization, drying and screening to obtain pellets, said pellets being further coated with one or more layers of film coating to achieve taste masking.

The invention provides a cefpodoxime proxetil rapid-release solid preparation and a preparation method thereof. The cefpodoxime proxetil rapid-release solid preparation comprises cefpodoxime proxetil and a surfactant, wherein cefpodoxime proxetil accounts for 2.5-15wt% of the total preparation, and the surfactant accounts for 0.8-15.0wt% of the total preparation. The method for preparing the rapid-release solid preparation adopts wet granulation and specifically comprises the following steps: (1) dissolving cefpodoxime proxetil and the surfactant in absolute ethyl alcohol to obtain a mixture I; (2) after mixing a diluting agent with a disintegrating agent uniformly, slowly adding or spraying the mixture I and carrying out granulation and fluidized bed drying to obtain a mixture II; (3) adding a suspending aid, a flavoring agent and a lubricating agent to the mixture II and carrying out total mixing and subpackaging. The rapid-release solid preparation can be quickly dissolved out when meeting water and can not be gelated. Meanwhile, technology improvement is adopted, thus avoiding the processes of raw material grinding and micronization treatment; and special equipment, such as a dry type granulator, is unnecessary to be used, thus ensuring the product stability while simplifying the production operation.

A cefpodoxime proxetil flavored chewable tablet is prepared from, by weight, 10%-30% of cefpodoxime proxetil, 40%-75% of filler, 1%-10% of a disintegrating agent, 1%-5% of an adhesive, 10%-20% of corrigent and 2%-5% of Eudragit EPO. The Eudragit EPO is used as a granule coating material to realize fluidized bed coating of granules containing the cefpodoxime proxetil, bitter taste is effectively removed for canines chewing the cefpodoxime proxetil flavored chewable tablet, direct contact between the cefpodoxime proxetil and the corrigent is isolated, and stability of the cefpodoxime proxetil is improved evidently. In addition, the cefpodoxime proxetil flavored chewable tablet is high in content uniformly and quick in disintegration and dissolution, and high stability is guaranteed while palatability is improved.

The invention discloses cefpodoxime proxetil pellets and capsules and a preparation method thereof. The pellets are composed of the following raw materials: 55 to 70 percent of cefpodoxime proxetil, 10.5 to 30 percent of hydroxypropyl methyl cellulose, 6 to 12 percent of mannitol, 1 to 5 percent of diacetyl glycerin monoester, and 1 to 3 percent of talcum powder. The method is low in cost, simple in process, and applicable for industrial production. The prepared capsules are good in quality, and are free of gravel taste after taking. The cefpodoxime proxetil has good taste, flowability, and content uniformity so as to be well preserved for a long time.

A process for obtaining cefpodoxime proxetil of formula (I), of high purity conforming to pharmacopoeial specifications is disclosed. The process comprises addition of a solution of methanesulfonic acid in water to a solution of impure cefpodoxime proxetil of formula (I) in an organic solvent to form the corresponding cefpodoxime proxetil methanesulfonate of formula (II¹), followed by addition of a co-solvent and separation of the aqueous phase containing cefpodoxime proxetil methanesulfonate of formula (II¹) having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6 and subsequent neutralization of the methaneulfonate salt (II¹) with a base to give cefpodoxime proxetil (I) free of impurities and having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6, or, addition of impure cefpodoxime proxetil of formula (I) to a solution of methanesulfonic acid in water to form the corresponding solution of cefpodoxime proxetil methanesulfonate of formula (II¹) in water, followed by sequential addition of a first organic solvent and a co-solvent and separation of the aqueous phase containing cefpodoxime proxetil methanesulfonate of formula (II¹) having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6 and subsequent neutralization of the methaneulfonate salt (II¹) with a base to give cefpodoxime proxetil (I) free of impurities and having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6.

The invention belongs to the technical field of medicines, and in particular relates to a cefpodoxime proxetil compound as well as a preparation method and a medicinal composition thereof. The cefpodoxime proxetil compound has a chemical structural formula shown in a formula (I); and the cefpodoxime proxetil compound adopts an X-ray powder diffraction pattern which is obtained by Cu-Kalpha ray measurement and shown in a figure 1. The stability test shows that the humidity stability of the cefpodoxime proxetil compound is obviously superior to that of cefpodoxime proxetil in the prior art, the temperature and illumination stability of the cefpodoxime proxetil compound is also superior to that of cefpodoxime proxetil in the prior art, and the purity of the cefpodoxime proxetil compound is obviously higher than that of cefpodoxime proxetil in the prior art; and in addition, surprisingly, the cefpodoxime proxetil compound provided by the invention has good fluidity and is easy to subpackage.

The invention provides a medicine composition comprising the cefpodoxime proxetil cyclodextrin inclusion compound. The basic composition comprises the cefpodoxime proxetil and the pharmacy-acceptable cyclodextrin; the cyclodextrin is chosen from one or a plurality of Beta -cyclodextrin, sulfobutyl- Beta -cyclodextrin, hydroxypropyl- Beta -cyclodextrin or hydroxypropyl-sulfobutyl- Beta -cyclodextrin. The invention has the advantages of increasing the solubility and stability of the medicine, meanwhile lower hemolysis irritability and higher activity. The invention also provides the preparation method of the medicine composition.

The invention discloses a cefpodoxime proxetil tablet. The cefpodoxime proxetil tablet comprises the following raw materials by weight: 30 to 50 parts of crude cefpodoxime proxetil, 10 to 20 parts ofan organic solvent A, 5 to 15 parts of an organic weakly-alkaline salt solution, 10 to 20 parts of active carbon, 5 to 10 parts of 1-iodoethyl isopropyl carbonate, 6 to 12 parts of an organic solventB, 2 to 8 parts of a filling agent, 2 to 6 parts of a disintegrating agent, 6 to 12 parts of an aqueous binder solution, 3 to 7 parts of Eudragit with a registered trademark of EPO, 1 to 7 parts of acorrigent, 2 to 9 parts of sodium alginate and 1 to 5 parts of isomaltitol. The cefpodoxime proxetil tablet provided by the invention is directly prepared by using the crude cefpodoxime proxetil, so the waste of the cefpodoxime proxetil tablet caused by crude cefpodoxime proxetil is avoided, and a plurality of unnecessary preparation steps can be reduced at the same time; meanwhile, the quality ofa clinical preparation is improved for better solidification of pills of master drug components, so medication safety is guaranteed; and the method provided by the invention has the advantages of simple process, convenient operation, low cost and applicability to large-scale production.

The invention discloses a medicine composition containing cefpodoxime proxetil. Meglumine is added into the composition to be used as a gelatin inhibitor; the gelation phenomenon of the solid preparation in an aqueous solution can be effectively inhibited; the dissolution-out performance of a solid preparation is effectively improved; the bioavailability is further improved. A flavoring agent of sodium glutamate is added in the composition to achieve the cooperated effect with meglumine, the problem of bitter taste of the particle preparation is solved. Through a dry process granulation process, the introduction of adverse factors such as moisture and high temperature is avoided; a preparation recipe is matched; the problems of hydrolysis or oxidization degradation of ester bonds, amido bonds, lactam bonds and primary amine groups in raw medicine molecules is solved. Experiments prove that the effect is good.

The invention provides a cefpodoxime proxetil composition freeze-dried powder injection for injection and relates to the field of medicines and medicine manufacturing technique. The cefpodoxime proxetil composition freeze-dried powder injection comprises the following raw materials: by weight, 1 part of cefpodoxime proxetil, 0.1-1.0 part of chitosan nanoparticles and 10-20 parts of water for injection. The invention has advantages as follows: 1) the composition can raise water solubility of cefpodoxime proxetil and shorten dissolution time of cefpodoxime proxetil and is beneficial to clinic application, and chitosan in the composition can be used as a cosolvent to replace beta-cyclodextrin so as to avoid renal toxicity and hemolytic activity of beta-cyclodextrin to human body; 2) the composition can remarkably enhance the antibacterial effect of cefpodoxime proxetil, can be used to reduce dosage of cefpodoxime proxetil in clinic and reduce adverse reaction of cefpodoxime proxetil, and in vitro experiments show that 0.1g of the cefpodoxime proxetil composition freeze-dried powder injection containing the chitosan nanoparticles has the same antibacterial efficacy with 0.2g of cefpodoxime proxetil without the chitosan nanoparticles; and 3) the chitosan nanoparticles can replace mannitol to be used as a freeze-drying skeleton agent of the freeze-dried powder injection so as to eliminate the active effect of mannitol on human body.