105 results about "Oseltamivir Phosphate" patented technology

The invention provides an oseltamivir phosphate dry suspension. The oseltamivir phosphate dry suspension comprises oseltamivir phosphate, filler not prone to reacting with the oseltamivir phosphate and other pharmaceutically acceptable accessories, wherein the filler is one or more of maltitol, xylitol and mannitol or is the composition of one or more of the maltitol, the xylitol and the mannitol and sorbitol, the content of the sorbitol in the whole composition is X, and X large than or equal to 0% and less than or equal to 75%. Meanwhile, the invention provides a preparation method of the oseltamivir phosphate dry suspension. Preferably, the preparation method is a step-by-step wet preparation method. The oseltamivir phosphate dry suspension is good in stability, low in cost, simple in preparation technology and capable of being produced in an industrial mode easily.

The invention relates to a purification method of Oseltamivir phosphate, and the method is to recrystallize an Oseltamivir phosphate crude product acquired by a non-sodium azide process with water, alcohol or an aqueous solution of alcohol for obtaining the Oseltamivir phosphate with the purity higher than 99.0 percent, the maximum single impurity less than 0.1 percent, and the total impurities less than 1.0 percent. The method has advantages of simple operation, high purity of products, stable quality and high overall yield, and is particularly applied to the industrialized production.

Novel processes for the preparation of the anti-viral agent, Oseltamivir Phosphate and novel intermediates prepared in such processes. The novel processes use as starting materials D-glucose or D-xylose in the preparation of Oseltamivir Phosphate.

The invention relates to the field of pharmaceutical preparations, and particularly relates to oseltamivir phosphate dry powder inhalations for treating influenza A and influenza B and a preparation method thereof. The oseltamivir phosphate dry powder inhalations are characterized in that the inhalations comprise oseltamivir phosphate and a co-atomizing agent in a weight ratio of (8:2)-(6:4). The oseltamivir phosphate dry powder inhalations provided by the invention have a simple preparation method, good fluidity, and good stability. After administration, the medicine can be metabolized to metabolites with anti-influenza virus activity, which can take an antibacterial effect and be used for preventing and treating influenza A and influenza B.

The invention provides an oseltamivir phosphate tablet and a preparation method thereof. The oseltamivir phosphate tablet contains sucralose, Aspartame or a mixture of sucralose and Aspartame as a sweetening agent, and also contains pharmaceutically acceptable auxiliary materials. The oseltamivir phosphate tablet has good mouthfeel and good stability and is convenient to carry and take. On the other hand, the invention also provides a preparation method of the oseltamivir phosphate tablet. The method is simple and low-cost, and is suitable for industrial production.

The invention relates to a high performance liquid chromatography method for separating and measuring oseltamivir phosphate and specific impurities of the oseltamivir phosphate. According to the highperformance liquid chromatography method for separating and measuring the oseltamivir phosphate and the specific impurities of the oseltamivir phosphate, octyl silane bonded silica gel columns are adopted, the mobile phase is 0.05 mol/L, the volume ratio of a monopotassium phosphate buffer solution to methyl alcohol to acetonitrile is 620 to 245 to 135, the column temperature is 48 DEG C-50 DEG C,the detection wave length is 207 nm, and the flow rate is 1.1-1.3 ml per minute; and three diastereoisomers of the oseltamivir phosphate, two isomerides (impurity C and impurity D), and a specific technology impurity A, a specific technology impurity B and a specific technology impurity C and the oseltamivir phosphate specific impurity I, the oseltamivir phosphate specific impurity II and the oseltamivir phosphate specific impurity III recorded in the 2015 version of 'Chinese Pharmacopoeia' can be separated totally at the same time by the high performance liquid chromatography method, the method is simple and exact, and is high in sensitivity, and is very important for the quality control over drug products.

The present invention discloses biosynthesis process of preparing shikimic acid and the recombinant colibacillus therefor. The biosynthesis process of preparing shikimic acid includes constituting vector including the polygene kit of shikimic acid metabolizing pathway rate-limiting enzyme, replacing the polygene kit for shiA gene, knocking out shikimate kinase isozyme with Red recombinant system, fermenting recombinant engineering bacteria to obtain shikimic acid, purifying shikimic acid and other steps. The process has high shikimic acid expressing yield and lowered shikimic acid producing cost, and can provide material for preparing Oseltamivir phosphate as influenza preventing and treating medicine.

The invention relates to a high-performance liquid chromatography method for separating oseltamivir phosphate and oseltamivir phosphate SSR-isomers through the normal-phase chromatography method. Themethod is characterized in that the surface of silica gel is coated with cellulose-tris(3,5-dichlorophenyl carbamate) columns, a moving phase is a mixture of normal hexane, absolute ethyl alcohol, methanol, trifluoroacetic acid and diethylamine at a volume ratio of 90:8:2:0.4:0.2, the column temperature ranges from 30 DEG C to 40 DEG C, the detection wavelength is 240nm, and the flow velocity is 0.9-1.1ml per minute. The method has the advantages that the oseltamivir phosphate and the oseltamivir phosphate SSR-isomers can be separated; high simplicity, high accuracy and high sensitivity can beachieved; and the method can be used for SSR-isomer detection during oseltamivir phosphate production.

The invention discloses a method for preparing a tert-butylamine derivative, and relates to the field of drug synthesis. The method comprises the following steps: 1, preparing a magnesium-amine compound, namely, adding magnesium halide and tert-butylamine A into an aprotic solvent, and carrying out a mixing stirring reaction for 0.5-1.5 h at a temperature of 0-15 DEG C to prepare a mixed solutionA; 2, adding a compound B into the mixed solution A prepared in the step 1, and carrying out a stirring reaction for more than 8 hours to prepare a mixed solution B; and 3, supplementing tert-butylamine D into the mixed solution B prepared in the step 2, and carrying out a stirring reaction for 24-48h at a temperature of 50-70 DEG C to prepare a tert-butylamine derivative I. By controlling the preparation temperature of the compound, the addition mode of tert-butylamine and the time of the ring-opening reaction, the curing phenomenon in the reaction and the increase of by-products can be effectively controlled.

The invention provides a solid preparation of oseltamivir phosphate; the solid preparation contains oseltamivir phosphate and a diluent with the effective treatment or prevention amount, wherein the diluent is maltitol; and the solid preparation further contains an adhesive and a selectable sweetening agent and/or edible essence. The solid preparation has the characteristics of being steady in quality, safe, effective, good in patient compliance and wide in drug application crowd. The invention further provides a preparation method of the solid preparation of oseltamivir phosphate. The preparation method is simple and feasible and is applied to industrial production.

The invention discloses application of neuraminidase and neuraminidase inhibitors to preparation of medicines for inhibiting hepatic gluconeogenesis. Zanamivir and oseltamivir phosphate are effectiveinhibitors of the neuraminidase; the inhibition effect of coptisine on neuraminidase is also disclosed in the previous patent application of the applicant. The applicant also discovers that salvanic acid B is capable of inhibiting the activity of the neuraminidase in vitro and is used as an inhibitor of the neuraminidase. In-vivo test proves that the several neuraminidase inhibitors are capable ofeffectively inhibiting the activity of the neuraminidase in the liver and then inhibiting hepatic gluconeogenesis. Therefore, the neuraminidase and the neuraminidase inhibitors can be used for preparing the medicines for inhibiting hepatic gluconeogenesis and can also be used for treating diabetes, obesity and non-alcoholic fatty liver disease.

Use of Neul sialidase inhibitors for the treatment of cancer as a monotherapy or in combination with known chemotherapeutics. Preferably, Neul sialidase inhibitors are oseltamivir phosphate or 2-deoxy-2,3-dehydro-N-acetylneuraminic acid (DANA) or analogues thereof.

The invention discloses a neuraminidase inhibitor and a preparation method thereof. The preparation method comprises the following steps: with oseltamivir phosphate and biphenyl aldehyde substances as raw materials, carrying out a reaction with a reducing agent under the action of a catalyst so as to obtain the neuraminidase inhibitor, wherein the catalyst is acetic acid. The invention has the following beneficial effects: by adopting a one-pot method, a final product with high purity and high yield can be obtained; meanwhile, practicability and effectiveness in economy and environmental friendliness are realized.

The present invention discloses an economic, simple, azide and aziridine complexity free process for the synthesis of osletamivir phosphate (Tamiflu) by stereospecific amidoalkylation of imidazothiazolone from easily available L-cysteine via Ramberg-Backlund reaction and Sharpless-Reich protocol.

The invention belongs to the field of medicine processing, and relates to a dry suspension containing oseltamivir phosphate and a preparation method of the dry suspension. The dry suspension comprisesraw materials containing drug-containing particles and non-drug-containing particles, wherein the drug-containing particles are prepared from the following raw materials: oseltamivir phosphate, sorbitol, sodium benzoate, anhydrous sodium citrate, saccharin sodium and an ethanol aqueous solution; and the non-drug-containing particles are prepared from the following raw materials: sorbitol, titanium dioxide and an ethanol aqueous solution. According to the dry suspension and the preparation method, a twin-screw extrusion granulation technology is adopted to solve the problems that hydrophilic auxiliary materials in a prescription are easy to agglomerate in the preparation process, the content uniformity is unqualified through detection, a qualified preparation cannot be smoothly obtained, and by means of the preparation method, granulation is enabled to be easier during preparation, the process can be continuously operated, and the stability is better.

The invention discloses an influenza luciferase reporter virus-based animal model building method and application. In the method, a mouse is mainly infected with Gaussia luciferase gene-carrying recombinant influenza virus, and the infection degree of the mouse is evaluated by detecting the expression level of luciferase in a lung tissue of the mouse. The invention further discloses an influenza luciferase reporter virus technology-based method for screening and evaluating an anti-influenza drug. According to the method, anti-influenza drugs with prevention/treatment effects are screened by mainly detecting the influence of antiviral treatment on the expression level of the luciferase in the lung tissue of the mouse. Detection of positive drugs ribavirin and oseltamivir phosphate shows that the method disclosed by the invention has a wide application value in the aspect of screening, researching, developing and evaluating the novel anti-influenza drug.

The present invention provides a pharmaceutical composition comprising: one or more excipients selected from sugars and sugar alcohols in which equilibrium water content is 1% by weight or less at 25° C. and at 70% relative humidity; and oseltamivir phosphate, wherein an amount of each of glucose and mannose contained in the sugars and sugar alcohols as impurities is 0.01% by weight or less.

The invention discloses an analysis method for separating and detecting an oseltamivir phosphate intermediate and impurities thereof, belongs to the field of analytical chemistry, and particularly relates to an analysis method for carrying out gradient elution on the oseltamivir phosphate intermediate by taking pentafluorophenylsilane bonded silica gel as a filler, water-perchloric acid as a mobile phase A and acetonitrile-methanol as a mobile phase B. The method can realize effective separation and detection of the oseltamivir phosphate intermediate and the specific impurities thereof, has the characteristics of high detection sensitivity and accurate and reliable detection result, and provides a reliable reference method for quality research on separation and detection of the oseltamivir phosphate intermediate and the specific impurities thereof.

The invention provides an improved oseltamivir phosphate medicinal composition, which comprises an effective amount of oseltamivir phosphate for treating or preventing diseases, at least one beta cyclodextrin or cyclodextrin derivative and one or more optional pharmaceutically acceptable excipients. The invention also provides the application of a solid medicinal composition to the preparation of an oral liquid medicament. The invention further provides a liquid medicinal composition which comprises the medicinal composition and a water-containing medium. The medicinal composition has an excellent effect as specified in the specifications.

The invention provides an oseltamivir phosphate dispersible tablet and a preparation method thereof. The dispersible tablet is composed of the following components in percentage by weight: 30-50% of oseltamivir phosphate and 50-70% of medicinal excipient. The preparation method provided by the invention comprises the following steps: stirring and mixing oseltamivir phosphate and the proper auxiliary material, granulating, finishing, and tabletting to obtain the oseltamivir phosphate dispersible tablet. The dispersible tablet can be quickly disintegrated and uniformly dispersed in water, and is suitable for children, old people, bed-ridden patients and severely disabled patients; and the dispersible tablet can be prepared into a uniform dispersion solution, and the uniform dispersion solution can be measured by an appropriate measuring vessel to satisfy the application demands of children with different weights. The method is easy to implement and simple for preparation, is suitable for industrial production, and has great application value.

The invention provides a preparation method of an oseltamivir phosphate capsule. By controlling the adding manner and adding amount of a flow aid, the dissolution uniformity of medicines is effectively improved, and the effects of the change of the dissolution speed of the medicines on the effect taking time of the medicines are reduced.