53 results about "Faropenem" patented technology

The invention provides a method for preparing penicillenic antibiotics faropenem sodium Iwhich takes natural L-threonine as raw material, and method for preparing important intermediate II. The invention is characterized by high productivity, low cost, simple operation, easy post treatment and suitability for industrialization.

The invention particularly relates to a method for measuring the content of faropenem polymers in faropenem sodium raw materials and preparations by high-efficiency liquid chromatography, which belongs to the field of medicine analysis. The measuring method of the invention is gel chromatography. The high-efficiency liquid chromatogram is used for detection, and the chromatogram conditions are as follows: (1) the gel permeation chromatography has the exclusion molecular weight between 600 and 800 Daltons; (2) the mobile phases as two mobile phases, wherein the mobile phase A is a water phase solution with the pH value between 5.0 and 8.5 and the concentration between 0.01 and 0.2 mol/L, and the mobile phase B is water or a sodium dodecyl sulfate water solution or a glycin solution between 0.005 and 0.02 percent; (3) the column temperature is the room temperature; (4) the flowing rate is between 0.5 and 1.0 ml/min; and (5) the detection wavelength is between 210 and 300 nm. The method of the invention has the advantages of strong specificity, good repetitiveness and high automation degree, and the polymers in the faropenem sodium raw materials and the preparations can be accurately qualified.

The invention relates to a Faropenem sodium freeze-dried powder injection, which comprises only one composition: Faropenem sodium. Preferably, injection water is added into Faropenem sodium powder with the particle size of 75 to 100mum to be prepared into Faropenem sodium solution with concentration of 5-20 percent for drying, thus obtaining a finished product. The Faropenem sodium freeze-dried powder injection is simple and feasible in preparation process, beneficial to operation, and suitable for needs for large-scale industrial production.

The invention relates to a Faropenem sodium powder injection, which comprises only one composition: raw Faropenem sodium powder without any additive. As raw Faropenem sodium is solid powder and in isolating state, the oxidization and hydrolyzation are hard to carry out; in addition, as a current filling machine can be forcibly filled, the filling amount is stable. Particularly, when the humidity of a split charging workshop is controlled under 30 percent, the stability of the Faropenem sodium powder is better.

The invention belongs to the field of medicines and provides an orally disintegrating tablet containing faropenem sodium. The orally disintegrating tablet also contains mannitol and a lubricating agent. According to the orally disintegrating tablet, less auxiliary materials are used; the composition formula is simple; the orally disintegrating tablet which is prepared from powder through tabletting still has good fluidity; the obtained tablet is reliable in hardness and high in disintegrating speed; and the dissolution behavior of the main drug is excellent.

The invention provides a faropenem sodium granule and a preparation method thereof. The faropenem sodium granule contains faropenem sodium, polyvinyl alcohol, dextran and a sweetening agent. The faropenem sodium granule has the advantages of low polymer content, good stability and simple preparation technology.

The present invention is related to processes for the preparation of faropenem.

The invention relates to a preparation method of faropenem medoxomil, belonging to chemical synthesis technical field, which is characterized in that faropenem and 4-halogenated methyl radical-5-methyl-1, 3-dioxane cyclopentene-2-ketone, in alkali condition and solvent A, via phase transfer catalyst and reaction promoter containing iodine are synthesized to obtain faropenem medoxomil, or the inorganic salt of faropenem medoxomil and 4-halogenated methyl radical-5-methyl-1, 3-dioxane cyclopentene-2-ketone, in solvent B, via phase transfer catalyst and reaction promoter containing iodine are synthesized to obtain faropenem medoxomil. The method has simple operation, mild reaction and saved cost, while the synthesized faropenem medoxomil has high yield and purity.

The invention provides a process for synthesizing Faropenem from reaction by-products, which has the advantages of low cost, high yield, and easy realization of reaction conditions.

The invention discloses a synthetic method of faropenem sodium. The method uses (3R,4R)-3-[(R)-1-tert-butyldiemthylsilyloxyethyl]-4-[(R)-acetoxyl]azetidin-2-one (4-AA) as raw material and prepares the faropenem sodium through a five-step reaction. The method does not use a silver salt as a condensing agent, does not use 4-tetrahydrofuran-2-formic acid which is previously made into mercaptan acid, has simple and convenient operation, and is suitable for industrial production. The product purity and the total yield all exceed the prior art.

The invention discloses a purification method of a faropenem sodium hydrate, which comprises the following steps: 1) dissolving a faropenem sodium hydrate crude product in a lower alcohol solvent at -20-40 DEG C, adding active carbon for decoloration, filtering, 2) adding water into filtrate, performing decompression concentration and evaporation at 0-40 DEG C to remove the lower alcohol solvent, and 3) adding residual into a ketone insoluble solvent, stirring, crystallizing and filtering to form the pure faropenem sodium hydrate, wherein for the faropenem sodium hydrate crude product, the water content is 1g:(0.5-2mL). According to the method, the faropenem sodium hydrate crude product is dissolved in the lower alcohol solvent at the low temperature, a little water is added, and the lower alcohol solvent is evaporated off at the low temperature; the whole purification process is performed at the low temperature all the time, so that the crystallization yield is increased obviously and reaches above 90%; and residual products in a mother solution are fewer, so that the product cost is lowered.

The invention belongs to the field of pharmaceutical preparations, and relates to faropenem sodium particles and a preparation method thereof. The invention provides the faropenem sodium particles with a simple production process, stable and controllable quality and a safe and reliable curative effect. The particles contain the following components in percentages by weight: 5-20% of faropenem sodium, 75-95% of an excipient, and 0.3-1% of a desiccant. The stability of the faropenem sodium particles prepared by the method is greatly improved, the quality indicators of the substances, related tothe main components, such as related substances, polymers and moisture are well controlled, and the safety and shelf life standards of medication are improved.

The invention belongs to the technical field of medicines, and relates to a new application of faropenem, in particular to the new application of the faropenem in preparation of a medicine for initialtreatment of pathogen-positive pulmonary tuberculosis. Compared with an existing standard scheme, when being used for initial treatment of the pathogen-positive pulmonary tuberculosis, a pharmaceutical composition containing the faropenem is remarkable in effect, rapid in effect taking, small in side effect and high in safety, and effectively overcomes the defects that the tuberculosis treatmentis long in treatment course and high in toxic and side effects.

The invention discloses a preparation method of faropenem sodium, which comprises the following steps: mixing potassium carbonate, R-(+)-thiotetrahydrofuran-2-formic acid and (3R, 4R)-4-acetoxyl-3-[(R)-(tert-butyldimethylsiloxy) ethyl] azetidin-2-ketone, and reacting to obtain FPS-1; mixing the FPS-1, triethylamine and oxalyl chloride monoallyl ester, and carrying out a reaction so as to obtain FPS-2; mixing the FPS-2 with triethyl phosphite, and carrying out a reaction so as to obtain FPS-3; mixing the FPS-3 with tetrabutylammonium fluoride, and carrying out a reaction so as to obtain FPS-4; and mixing the FPS-4, triphenylphosphine, sodium isooctoate and tetrakis (triphenylphosphine) palladium, and reacting to obtain the faropenem sodium. According to the preparation method disclosed by the invention, high-purity and high-yield faropenem sodium can be obtained.