45 results about "Tamoxifen Citrate" patented technology

The dispersive tamosxifen citrate tablet is prepared through mixing tamosxifen citrate powder of 25 micron below size, microcrystal cellulose, lactose, PVP, sodium dodecyl sulfate and partial sodium carboxymethyl cellulose; pelletizing the mixture into disintegrated pellets of 0.5 mm below size; adding magnesium stearate and the rest sodium carboxymethyl cellulose; and tabletting into the dispersive tablet. The dispersive tamosxifen citrate tablet can disintegrate fast within 2 min and has fast medicine digesting speed and high bioavailability.

The invention discloses a solid dispersion of tamoxifen citrate. The solid dispersion of tamoxifen citrate consists of tamoxifen citrate, polyethylene glycol-6,000 and a flow aid, wherein the weight ratio of the tamoxifen citrate to the polyethylene glycol-6,000 is 1:4.5-12.5; and the flow aid is micropowder silica gel or talcpowder, and the dosage of the flow aid is 0.5 to 3 percent based on the total weight of the tamoxifen citrate and the polyethylene glycol-6,000. The solid dispersion of tamoxifen citrate can be made into orally taken solid preparations with high bioavailability and good absorbability, such as common tablets, dispersible tables, sustained release tablets and capsules, can be conveniently prepared, and the dissolution of the tamoxifen citrate can stably reach over 90 percent; and the preparation method has the advantages of low cost, easy operation, no special requirement on equipment, suitability for mass production and the like, and establishes a good relationship between the disintegration, dispersion and release speed and the medical dissolution of the solid dispersion of tamoxifen citrate.

The present invention relates to a pharmaceutical product for administration to a patient, the product comprising 4′-cyano-α′,α′,α′-trifluoro-3-(4-fluorophenylsulphonyl)-2-hydroxy-2-methylpropiono-m-toluidide, or a pharmaceutically acceptable salt or solvate thereof, in solid dispersion with an enteric polymer having a pK_a from 3 to 6, the product further comprising an anti-oestrogen (eg, tamoxifen citrate) and/or an aromatase inhibitor (eg, anastrozole). The invention also relates to a pharmaceutical dose of the drug and anti-oestrogen/aromatase inhibitor provided by such a formulation. An advantage is the treating and/or preventing of at least one side effect selected from gynaecomastia, breast tenderness, hot flushes, impotence and reduction in libido, while increasing the bioavailability of the drug; reducing inter-patient variability in plasma concentrations of the 4′-cyano-α′,α′,α′-trifluoro-3-(4-fluorophenylsulphonyl)-2-hydroxy-2-methylpropiono-m-toluidide; enhancing the storage stability of the drug; and/or treating and/or reducing the risk of prostate cancer in a patient.

The invention relates to a preparation method of tamoxifen citrate polylactic acid-glycolic acid copolymer microspheres. The method comprises the following steps: 1) dissolving polylactic acid-glycolic acid copolymer (PLGA) in an organic solvent, adding tamoxifen citrate, and dissolving under ultrasonic action to obtain a solution as organic phase; 2) adding slowly the organic phase into aqueous solution of polyvinyl alcohol (PVA) as water phase under stirring, adding electrolytes, stirring at room temperature until the organic solvent volatilizes completely, centrifugating, washing, and freeze-drying to obtain tamoxifen citrate polylactic acid-glycolic acid copolymer microspheres. The microsphere has round shape, uniform particle size distribution (below 10 micrometers), high drug content (above 10%), high encapsulation rate (about 80%), and in vitro release characteristics of long-acting preparations; and is suitable for the use as implant for prevention and treatment of breast cancer.

The invention relates to tamoxifen citrate enteric coated particles which are prepared by the following steps: firstly, preparing tamoxifen citrate into inclusion compounds; and then, preparing the enteric coated particles.

The invention provides a preparation method of a tamoxifen citrate E isomer, which comprises the following steps: 1) with an intermediate for preparing tamoxifen citrate and having a structural formula as shown in the formula I as a raw material, performing a dehydration reaction in an acid condition in a mixed solution of water and organic solvent at certain proportion to obtain a mixture of an intermediate 1 with a structural formula as shown in the formula II and an intermediate 2 with a structural formula as shown in the formula III; 2) in an organic solvent of certain amount, enabling the intermediate 1 and the intermediate 2 to react with citric acid or hydrate thereof, and cooling for crystallization to obtain a mixture of Z-tamoxifen citrate with a structural formula as shown in the formula IV and E-tamoxifen citrate with a structural formula as shown in the formula V; and 3) in the water and organic solvent at certain proportion, performing twice recrystallization of the mixture of Z-tamoxifen citrate and E-tamoxifen citrate. The method provided by the invention can be used for preparing a high-purity tamoxifen citrate E isomer, provides an impurity reference substance for the National Institutes for Food and Drug Control, and solves the problem in E-isomer detection in a practical production process.

The invention relates to a tamoxifen citrate emplastrum and a preparation method thereof. A tamoxifen citrate micro emulsion is prepared into a transdermal emplastrum, and the transdermal emplastrum is divided into four layers: an anti-adhesion layer, a viscose layer, a back lining layer and a medicine storage layer. The tamoxifen citrate micro emulsion is used as a drug effect ingredient and comprises tamoxifen citrate used as an active ingredient, polysorbate 80 used as a surfactant, propylene glycol used as a cosurfactant, pure water or distilled water, and the like. Besides the drug effect ingredient, some non-polar polymers, a plasticizer, a tackifier, transdermal enhancer and an antioxidant are also added to the emplastrum. Compared with the traditional dosage forms such as tablets, solutions, oral cavity disintegrants, dispersants and external micro emulsion preparations, the tamoxifen citrate emplastrum has the prominent advantages of safety, low toxicity, convenient and simple use and accurate drug dosage.

The preparation process of high purity low type-E content Tamoxifen citrate includes dissolving Tamoxifen in dilute acid solution for refining and forming salt with citric acid; or dissolving Tamoxifen citrate in alcohol for refining, and can obtain Tamoxifen citrate with content of type-E Tamoxifen citrate isomer not higher than 0.05%. The process has the advantages of simple operation, short separation process and low cost.

The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.

The invention relates to tamoxifen citrate sustained-release tablets, the preparation method of which comprises the steps of preparing tamoxifen citrates into clathrate compounds and further preparing the clathrate compounds into sustained-release tablets.

The invention relates to tamoxifen citrate particles which are prepared by the following steps: firstly, preparing tamoxifen citrate into inclusion compounds; and then, preparing the particles.

The invention relates to tamoxifen citrate sustained-release granules, the preparation method of which comprises the steps of preparing tamoxifen citrates into clathrate compounds and further preparing the clathrate compounds into sustained-release granules.

The invention provides a preparation method of a tamoxifen citrate liposome. The preparation method comprises the steps of enabling tamoxifen citrate, phospholipid and cholesterol to dissolve in a solvent, and performing treatment by a gradient vacuum evaporation method to obtain a liposome film; and performing hydration on the liposome film, and performing filtration so as to obtain the tamoxifencitrate liposome. According to the preparation method, tamoxifen citrate is wrapped with phospholipid and cholesterol mediums to obtain the tamoxifen citrate liposome, so that the toxicity of medicines can be notably reduced, the solubility and the biological availability of the medicines can be improved, and the medicine action time can be prolonged; and besides, the tamoxifen citrate liposome which is obtained by a method for preparing the liposome film through gradient vacuum evaporation of the solvent is better in filming properties, moderate (150-200nm) and uniform in particle diameter,higher in entrapment efficiency (80% or above) and better in stability.