41results about How to "Low therapeutic dose" patented technology

The invention belongs to the field of bio-pharmaceutical products, which provides a chemical modification method for recombinate human rh-Endostatin ('rh-ES' is called for short) through the way of using mPEG-propionaldehyde to be combined on the fixed point of free amino of N-terminal amino acid of rh-ES. Mono-PEG-rhES is the output material, its purity meet the requirements of biological products. It plays a key role in the hydrolysis resistance of trypsin and chymotrypsin, it can be used as long-acting formulations for its stability for pH and temperature and there is a great perspective in the clinical treatment of cancer.

The invention relates to the field of medicine, and discloses meloxicam tablets for dogs and cats and a preparation method for the meloxicam tablets. The preparation method mainly comprises: a mixing step, a granulation step, a drying step, a granulation straightening step, a granule mixing step and a tabletting step. The meloxicam tablets consist of the following components in percentage by mass: 0.1 to 0.6 percent of meloxicam, 50 to 70 percent of lactose, 20 to 40 percent of microcrystalline cellulose, 3 to 5 percent of hydroxypropyl cellulose, 0.4 to 0.6 percent of sodium citrate, 1 to 5 percent of cross-linked polyvinylpyrrolidone, 4 to 8 percent of polyvinylpyrrolidone (PVP) K30, 0.2 to 0.8 percent of aspartame and 0.60 to 2 percent of magnesium stearate. The meloxicam tablets have small irritation on the intestines and stomach of the dogs and the cats, and are favorable for the absorption of active ingredients.

The invention discloses a gamboges acid nanometer particle preparation and is prepared by the components of raw material gamboges acid 0.05 to 1.5 percent, polylactic acid 0.05 to 1.5 percent, surfactant 0.1 to 1.5 percent, organic solvent 33 to 50 percent and the allowance of water with the following steps: dissolving the polylactic acid into the organic solvent and dispersing the gamboges acid in the mixed solution of the polylactic acid and the organic solvent; the preparation is obtained by adding the mixed solution with the gamboges acid into water phase with the surfactant, stirring magnetically for 4 hours, vacuum distillation and filtering with a 0.22Mum micro-porous filtering film after the organic solvent and part of water are distillated. The drug with a clear system, the particle size between 10 to 100nm and good dispersion and stability can significantly solubilize drugs, has a targeting effect for reticuloendothelial cells and concentrate at lesion sites, thus improving the curing effect of the drug and reduces the side effect of the drug. Additionally, the drug has a slowly releasing effect, can maintain constant plasma concentration or pharmacologic effect for a long time and improve drug bioavailability.

The invention aims to provide a method for preparing a docetaxel long-circulating liposome. The method comprises the following steps of: dissolving docetaxel and carrier materials such as phospholipid, cholesterol and the like together in an organic solvent; forming a film through rotary evaporation in a 40 to 70 DEG C water bath; adding buffer solution which contains a surfactant and performing refrigeration at the temperature of below 4 DEG C for 10 to 60 minutes to fully hydrate the film; and then mixing or stirring to obtain the docetaxel liposome. The liposome of 70 to 500nm is prepared from the docetaxel and can be prepared into docetaxel long-circulating liposome frozen powder for injection by lyophilization.

The invention provides a preparing method of a compound brucea javanicaseed oil liposome freeze-dried powder, and belongs to the technical field of traditional Chinese medicine preparation. The preparing method is characterized by comprising the following steps: 1) weighing soybean phospholipids, cholesterol, vitamin E and brucea javanicaseed oil, dissolving by ethanol, and taking as an oil phase; 2) measuring a toad venom aqueous extract, adding mannitol and sucrose, and adding distilled water to as an aqueous phase; 3) injecting the oil phase into the aqueous phase, and extruding by a micropore filter membrane to obtain a suspension; 4) filling a penicillin bottle with the suspension, carrying out freeze drying, and thus obtaining the compound brucea javanicaseed oil liposome freeze-dried powder. The preparation method of the compound brucea javanicaseed oil liposome freeze-dried powder adopts the brucea javanicaseed oil and toad venom for combined application, the average encapsulation rate of the prepared liposome freeze-dried powder is 91.90%, the average content of indole alkaloids is 5.19*10<-3> mg.g<-1>, the average content of oleic acid is 79.08 mg.g<-1>, the average content of linoleic acid is 50.41 mg.g<-1>, the antitumor effect is good, and toxic and side effects are small.

The invention provides a niobium tungstate compound for resisting hepatitis virus, which has the function of resisting the hepatitis virus and the chemical formula of AmBr (X (NbO2) 3W9O37). nH2O, wherein A is alkali metal ion Li, Na, K or Cs; B is hydrogen cation H+, ammonium ion NH4+ or amino acid cation; X is Si, Ge or P; and m=0-7, r=0-7 and n=0-20. The niobium tungstate compound is taken as active ingredient which is assisted by carrier or auxiliary material that is pharmaceutically acceptable, thus being used for preparing oral preparation or injection medicine applied to treating hepatitis. Compared with the existing medicine which is applied to treating hepatitis clinically, the niobium tungstate compound has the advantages of better liver target, low effective therapeutic dose, higher therapeutic index and lower toxicity, thus being an antiviral compound which has higher efficiency and is safer.

The invention particularly relates to application of 2-phenylpyrazole [1,5-a] pyrimidine compounds serving as a tumor drug resistance reversal agent. Aiming at the problem of cancer chemotherapy resistance, the invention provides compounds having an inhibiting effect on the ATP-binding cassette sub-family G member 2 (ABCG2), and the compounds are used for improving the drug resistance of tumor cells. According to the application, a series of 2-phenylpyrazole [1,5-a] pyrimidine compounds are obtained by study, so that the ABCG2 in drug resistance-type tumor cells can be in a resting state, pumping out of a substrate is blocked, and the drug resistance of tumors is reversed, and the therapeutic dose is safe and non-toxic. Based on the result of the study, the compounds can be combined with other ABCG2 drug resistance related antitumor drugs for treatment; and the 2-phenylpyrazole [1,5-a] pyrimidine compounds have good clinical medication significance.

The invention belongs to the field of biomedicines and relates to an anti-hyperlipidemia protein vaccine aiming at PCSK9 (Proprotein convertase subtilisin/kexin type 9). Aiming at solving the technical problems, the anti-hyperlipidemia protein vaccine which has good performances and takes the PCSK9 as a target is researched and developed. The protein vaccine aiming at the PCSK9, which is prepared by the invention, can be used for remarkably lowering the level of blood lipid of serum and has remarkable immunogenicity and good safety; a preparation method is simple and feasible and is low in cost. The protein vaccine aiming at the PCSK9 can be used for preventing and treating hyperlipidemia diseases and can realize treatment effect without the need of completely blocking the PCSK9; a condition that individuals is intolerant to complete blocking of the PCSK9 is avoided and the anti-hyperlipidemia protein vaccine has a better application prospect.

The invention discloses a hydroxyl camptothecin flexible liposome and a preparation method thereof. The method comprises the following steps of: dissolving hydroxyl camptothecin and carrier materials, such as phospholipid, cholesterol and the like, in an organic solvent; forming the mixture into a membrane in water bath through rotary evaporation; and adding buffer solution which contains chitosan into the membrane to form the hydroxyl camptothecin flexible liposome. The hydroxyl camptothecin flexible liposome is relatively lower in toxicity, relatively longer in residence time in a body, high in stability in a solution phase and smalllow in particle size, and the particle size of the liposome is not obviously changed after the liposome is lyophilized.

The invention discloses a tumor ECM degrading and/or inhibiting agent and a complete set kit and application thereof. The tumor ECM degrading and/or inhibiting agent comprises at least two kinds of ananti-hyaluronidase agent, an anti-collagen agent, and an anti-tissue agent. The tumor ECM degrading and/or inhibiting agent can effectively degrade or restrain generation of a tumor extracellular matrix in a broadspectrum manner, and the tumor penetrability is improved, so that drugs can effectively enter tumors to be in contact with and kill tumor cells, and improve the medication effect. The combination manner can be applied in an intratumoral injection manner, so that the applying concentration of single components can be reduced, and the side effect is low. The complete set kit can increase the medication effect, the medicament dose can be reduced, and dosage required for achieving the same effect by an antitumor intratumoral injection manner is lower than that used for venous or other nonintratumoral injection, the antitumor dosage is reduced, and besides, the antitumous effects are increased.

The invention belongs to the field of biological medicines, and relates to a mutant protein vaccine aiming at tumor necrosis factor alpha (TNF-alpha) and applications of the mutant protein vaccine. The invention aims at providing the protein vaccine which is good in property and takes TNF-alpha as the target spot. According to the scheme, by immunizing the TNF-alpha mutant protein vaccine, the biological activity of the TNF-alpha mutant protein vaccine is inhibited, the cross immunologic reaction is generated in vivo, the biological functions of TNF-alpha are neutralized, and the autoimmune diseases and inflammatory diseases are inhibited. The protein vaccine aiming at TNF-alpha can be used for treating the autoimmune diseases and the inflammatory diseases and preventing the relapse of the autoimmune diseases and the inflammatory diseases.

In the present invention, a new combination is disclosed comprising (i) 5-aminosalicylic acid (5-ASA) or a derivative thereof, or a pharmacologically acceptable salt thereof, and (ii) a group D vitamin, a derivative thereof, a metabolite or analogue, for use in the prevention and/or treatment of colorectal cancer (CRC). A further aspect of the invention is directed to pharmaceutical compositions comprising said combination together with at least one physiologically acceptable excipient and the use thereof in the prevention and/or in the treatment of the colorectal cancer.

The invention belongs to the technical field of medicines, and relates to an application of 3, 5-dinitrophenyl-pyrazolo [3, 4-d] [1,3] oxazine as a tumor drug resistance reversal agent. Researches show that 1-phenyl-6-(3, 5-dinitrophenyl)-pyrazolo[3, 4-d] [1, 3] oxazine-4(1H)-ketone can significantly improve the sensitivity of tumor cells to antitumor drugs and reverse the drug resistance of the tumor cells, and the treatment dosage is safe and non-toxic, so that the compound has potential to become a novel tumor drug resistance reversal agent. Based on the research results, the compound can be used for adjuvant therapy of a chemotherapy regimen and can be matched with other anti-tumor drugs for common medication, and has good clinical medication significance.

The invention relates to a polymer thermosensitive liposome loaded with yeast glucan and carnosic acid and a preparation method thereof. The polymer thermosensitive liposome comprises the following raw materials by weight: 5-15 parts of the yeast glucan, 5-10 parts of the carnosic acid, 4-10 parts of polylysine, 25-80 parts of phospholipid, 2-5 parts of tocopherol and 50-160 parts of cholesterol.The two drugs are respectively encapsulated in different positions of a lipid bilayer by membrane dispersion technology, and prescription technology and physicochemical properties are optimized and investigated to prepare a nanostructured carrier with excellent properties, and the polymer thermosensitive liposome can reverse multidrug resistance of cancer cells.