12 results about "FUDOSTEINE" patented technology

The invention relates to a method for determining the content of sorbitol and glycerol as auxiliary materials in a fudosteine oral solution, which has the advantages of high sensitivity, strong specificity, good accuracy and simple and rapid operation, can reduce the difficulty of preparation development, reduce the workload of prescription development, shorten the research and development time and further improve the BE passing rate, and has practical significance.

The invention relates to a method for determining the content of vanillin and ethyl vanillin which are auxiliary materials in a fudosteine oral solution, which is simple to operate, has good sensitivity, specificity and accuracy, provides an effective prescription analysis method for drug development, and has practical application value.

The invention discloses a fudosteine tablet with high stability and a preparation process thereof, and belongs to the technical field of pharmaceutical preparations. The fudosteine tablet comprises fudosteine as an active component, and is supplemented with a composite filler, an antioxidant protective agent, a disintegrating agent, a lubricant and a coating material, wherein the antioxidant protective agent is a synergistic combination of disodium ethylenediaminetetraacetate, disodium succinate and trehalose, and the coating material selects a specific combination to construct a preparation protective barrier. The preparation process sequentially comprises the steps of premixing under nitrogen protection, dry granulation, total mixing, tabletting and coating. A synergistic protection system of moisture absorption resistance, oxidation resistance and preparation protection is constructed, the long-term stability of the fudosteine tablet in a complex storage environment is remarkably improved, and the safety and effectiveness of clinical medication are guaranteed.

The application provides a preparation method of fudosteine tablets and belongs to the technical field of pharmaceutical preparations. The application provides a preparation method of fudosteine tablets, which adopts water as a lubricant, and solves the existing problem of poor fluidity in the granulation process by wet granulation under the formula of the application, and the obtained tablets and the original preparation have good dissolution consistency. The fudosteine tablets prepared by the technical scheme of the application have a significantly smaller rest angle relative to the raw material, and the water content is less than or equal to 2%. The fudosteine tablets prepared by the technical scheme of the application have good fluidity and good compressibility, and the appearance is a smooth white to white-like round tablet, which improves the compressibility of the product and the product pass rate, reduces dust and reduces the production risk. The preparation process of the technical scheme of the application is smooth, the shape of the prepared fudosteine tablets is good, and the dissolution behavior conforms to the in-vivo absorption process of the drug.

The invention discloses a fudosteine analogue as well as a preparation method and application thereof, and belongs to the technical fields of organic synthesis and medicines, in an alkaline aqueous solution, L-cysteine hydrochloride monohydrate reacts with chloro compounds with different substitutions to generate corresponding fudosteine analogues with different sulfydryl substitutions; the fudosteine is modified through a simple synthesis method, in-vitro activity tests prove that the obtained fudosteine analogues can show higher anti-inflammatory activity than the fudosteine by down-regulating mRNA expression of TNF-alpha, IL-1beta and IL-6, the compounds are expected to become lead compounds of anti-inflammatory drugs, and the fudosteine analogues can be used for preparing anti-inflammatory drugs. The stimulation of sulfydryl to gastrointestinal tracts is expected to be reduced, and the stability or targeting property is enhanced; the preparation method has the advantages of simple steps, mild reaction conditions, high yield and the like.

The invention relates to a method for determining the content of malic acid serving as an auxiliary material in a fudosteine oral solution, which is high in sensitivity, strong in specificity, good in accuracy, simple, convenient and rapid to operate, capable of reducing preparation development difficulty, reducing workload of prescription development, shortening research and development time and further improving the BE passing rate, and has practical significance.

Disclosed is a pharmaceutical composition containing Fudosteine, comprising the following components: a pharmaceutically active ingredient, a pH adjuster, and water. The concentration of Fudosteine in the composition ranges from 20 mg / mL to 200 mg / mL, and the pH value is between 3.0 and 6.0. The pharmaceutically active ingredient is one or more of Fudosteine, a pharmaceutically acceptable salt thereof, and a hydrate thereof. The pharmaceutical composition containing Fudosteine does not comprise an antioxidant, a surfactant, and a metal chelating agent, and can be prepared into an atomized inhalation preparation.

The application discloses a detection method of a degradation impurity 3-methyl-1-propanol in a fudosteine oral solution, relates to the technical field of drug degradation product analysis, and solves the technical problem that a quantitative analysis method for the degradation product 3-methyl-1-propanol in the fudosteine oral solution is lacked in the prior art; the detection method is high-performance liquid chromatography, a chromatographic column with octadecylsilane bonded silica gel as a filling agent is used, an ultraviolet detector is used, an organic solvent aqueous solution is used as a mobile phase, and isocratic elution is used; wherein the organic solvent in the mobile phase is methanol or acetonitrile; the method is high in specificity, high in sensitivity, good in accuracy, can effectively determine the content of the 3-methyl-1-propanol in the fudosteine oral solution, and thus guarantees controllable quality of the fudosteine oral solution.

A fudosteine nebulization inhalation solution composition and use thereof. The fudosteine nebulization inhalation solution consists of fudosteine, a pH-adjusting agent and water. The droplet particle size of the composition is as follows: the D90 particle size is 7.0-10.0 μm, the D50 particle size is 2.8-4.5 μm, and the Dio particle size is 0.5-1.5 μm; and the percent deposition of the particles with the aerodynamic particle size of 1.4-5.4 μm in the fudosteine inhalation solution is not less than 50%. In addition, further provided is a drug assembly for use in conjunction with the nebulization inhalation solution, comprising the inhalation composition, and a nebulizer and a nebulizing cup with specific parameters. The fudosteine nebulization inhalation solution composition and the assembly thereof have the advantages of a small effective dose, acting fast, high drug delivery efficiency, and the like, and are particularly effective in treating tracheal and main bronchial diseases.

The present application provides a high-stability low-irritation fudosteine aerosol inhalation preparation without EDTA, which is composed of fudosteine, a pH regulator and water, the concentration of fudosteine in the preparation is 20-140 mg / mL, the pH is 3.5-4.0, and the pH regulator is an organic carboxylic acid. In addition, the present application also provides the use of the above-mentioned fudosteine aerosol inhalation preparation in the preparation of respiratory tract mucus dissolving agents. By adjusting the type of pH regulator, the fudosteine aerosol inhalation solution preparation not only effectively reduces the adverse reactions caused by the auxiliary material components, improves the drug safety, but also ensures that the fudosteine aerosol inhalation solution preparation has good preparation stability.

The invention relates to the technical field of biological pharmacy, and discloses a synthesis and preparation method of high-purity fudosteine and a product thereof, the synthesis and preparation method comprises the following steps: carrying out substitution reaction on L-cysteine and 3-chloro-1-propanol, adding ammonia water and dithiothreitol or mercaptoethanol in the reaction, adjusting the pH after the reaction is finished, then adding ethanol for crystallization, and carrying out hot pulping to obtain the high-purity fudosteine. Filtering at room temperature to obtain a high-purity fudosteine product; or dithiothreitol or mercaptoethanol is not added in the substitution reaction stage, after the substitution reaction is finished and the pH is adjusted, ethanol is used for crystallization and thermal pulping, then filtration is performed to obtain a fudosteine crude product, the crude product is dissolved in ethanol, dithiothreitol or mercaptoethanol is added for reaction, filtration is performed, and a filter cake is pulped by ethanol at room temperature and dried in vacuum to obtain a high-purity fudosteine product. The method provided by the invention is simple and convenient to operate, high in yield and low in production cost, high-risk operation links such as hot filtration are avoided, and a high-purity fudosteine product with the impurity content lower than 0.1% can be directly obtained without tedious recrystallization operation.

The invention discloses a fudosteine pharmaceutical composition as well as a preparation method and application thereof. The invention provides a fudosteine pharmaceutical composition. The fudosteine pharmaceutical composition comprises the following components: a pharmaceutical active ingredient, a pH regulator and water, in the composition, the concentration of fudosteine is 20 mg / ml to 200 mg / ml, and the pH value is 3.0 to 6.0; the active pharmaceutical ingredient is one or more of fudosteine, pharmaceutically acceptable salts thereof and hydrates thereof. The fudosteine composition is good in stability, small in irritation, small in effective dose, high in curative effect, good in patient medication compliance, high in production controllability, free of antioxidants and / or surfactants, lower in adverse reaction occurrence rate, better in safety and good in market prospect.