99 results about "Fluticasone propionate" patented technology

Taught is a method for preparing S-fluoromethyl-6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioate (fluticasone propionate). The present method is simple, convenient, and mild, yields highly pure product, and is suitable for use commercially on a large scale.

An improved process for preparing fluticasone propionate, performed in the presence of water, is disclosed. Further disclosed is a process for preparing a fluticasone propionate that is highly suitable for administration by inhalation. Further disclosed are fluticasone propionate and a powdered fluticasone propionate prepared by these processes and pharmaceutical compositions for administration by inhalation containing same. A process of purifying a key intermediate in the synthesis of fluticasone propionate is also disclosed.

A solved three-dimensional crystal structure of a glucocorticord receptor (GR) α ligand binding domain polypeptide is disclosed, in the form of a crystalline glucocorticord receptor α ligand binding domain polypeptide in complex with the ligand fluticasone propionate (FP) and a peptide derived from the co-activator TIF2. The GR / FP / TIF2 structure includes an expanded binding pocket not seen in other GR structures. Methods of designing steroid and non-steroid modulators of the biological activity of GR and other nuclear receptors (NRs) are also disclosed. In another aspect of the present invention homology models of androgen receptor (AR), progesterone receptor (PR) and mineralcorticoid receptor (MR) are disclosed, as well as methods of forming homology models for other NRs. Methods of forming a soluble GR / FP / TIF2 complex are also disclosed.

Nasal pharmaceutical formulations comprising a drug substance having a specific particle size distribution profile are disclosed herein. Such profile provides increased bioavailability, increased efficacy or prolonged therapeutic effect of the drug substance when administered intranasally. The formulations of the present invention may comprise one or more corticosteroids having a specific particle size distribution profile. In a preferred embodiment, the corticosteroid is fluticasone or a pharmaceutically acceptable derivative thereof for the treatment of one or more symptoms of rhinitis. Preferably, the drug substance is fluticasone propionate. The formulations herein may be provided as an aqueous suspension suitable for inhalation via the intranasal route.

A fluticasone lotion having improved vasoconstrictor and anti-inflammatory activity and higher than expected potency. The fluticasone lotion contains 0.05 weight percent fluticasone propionate and an oil-in-water vehicle that includes excipients. The fluticasone lotion is unexpectedly efficacious while exhibiting an improved safety profile.

A method for treating respiratory disorders by administrating by inhalation an effective amount of a β2-receptor agonist, an acceptable amount of a corticosteriod, and HFA 134a, to a patient in need thereof, is disclosed. Preferably, the β2-receptor agonist is salmeterol or a physiologically acceptable salt thereof, and the corticosteriod is fluticasone propionate or a solvate thereof. The combination of salmeterol, fluticasone proprionate, and HFA 134a may lower the risk of cardiac arrhythmias, sudden death, or hypercorticism that are sometimes associated with the simultaneous administration of a β2-receptor agonist and an anti-inflammatory corticosteroid.

The invention involves methods and formulations for treating or preventing rhinosinusitis, including but not limited to, bacterial-induced, viral-induced and / or fungus-induced rhinosinusitis in mammals, and / or rhinosinusitis not induced by an infective agent, such as bacteria, fungus or virus. In one embodiment, the formulation of the present invention comprises an anti-inflammatory agent (e.g. fluticasone propionate) having a specific particle size distribution profile. The formulation may also comprise an antifungal agent, antibiotic or antiviral agent.

The present invention relates to a composition for treating skin inflammation, along with skin rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, and a corticosteroid. It discloses a composition for treating skin inflammation, along with skin rejuvenation containing a) a biopolymer in the form of chitosan, b) an active pharmaceutical ingredient (API) composition in the form of fluticasone propionate, used in treating skin inflammation c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants and d) water. The active ingredients, namely chitosan, and a corticosteroid in the form of fluticasone propionate, are incorporated in cream base for use in treating skin inflammation due to allergy & itching & wounds on human skin involving contacting human skin with the above identified composition.

The invention relates to a lipidosome medical composition which uses fluticasone propionate as an active component, and a cyst diameter of lipidosome is smaller than 800 nm. The composition comprises 0.025 percent to 0.2 percent of fluticasone propionate as the active component, 0.5 percent to 6 percent of phospholipid, 0 percent to 1 percent of lipophilic additive, 0.01 percent to 1 percent of antioxidant which is used for preserving the medical composition, a pH buffering agent which is used for retaining the pH value from 5 to 7.5, 3 percent to 15 percent of humectant, 20 percent to 30 percent of oil phrase component, 0.01 percent to 0.1 percent of antimicrobial preservative and the balanced of water. The fluticasone propionate lipidosome cream is used for treating skin diseases of human beings or animals.

The present invention describes novel and improved dosage forms containing fluticasone propionate for the treatment of conditions associated with inflammation of the esophagus.

The invention relates to the field of medicinal preparation and relates to a compound pharmaceutical composition of iodine polymer and glucocorticosteroid for treating dermatitis. The pharmaceutical composition of the present invention comprises 0.01-5% of polyvinylpyrrolidone iodine, 0.01-10% of glucocorticosteroid, 0.001-0.5% of potassium iodate and the balance of pharmaceutically accepted carrier, wherein the glucocorticosteroid is fluticasone propionate or halometasone. Drug effect test has proved that the compound medicament can treat dermatitis by synergism; furtherly, addition of a certain proportion of potassium iodate overcomes unfavorable influences of drug effect decrease or auxiliary effect caused by medicament instability.

A method for treating respiratory disorders by administrating by inhalation an effective amount of a β2-receptor agonist, an acceptable amount of a corticosteroid, and HFA 134a, to a patient in need thereof, is disclosed. Preferably, the β2-receptor agonist is salmeterol or a physiologically acceptable salt thereof, and the corticosteroid is fluticasone propionate or a solvate thereor. The combination of salmeterol, fluticasone proprionate, and HFA 134a may lower the risk of cardiac arrhythmias, sudden death, or hypercorticism that are sometimes associated with the simultaneous administration of a β2-receptor agonist and an anti-inflammatory corticosteroid.

The invention provides a method for separating and detecting six cortical hormones in a skin-care cosmetic. The six cortical hormones, i.e. fluticasone propionate, triamcinolone acetonide, cortisone acetate, dexamethasone, hydrocortisone and prednisone, in the cosmetic are separated and detected by a reverse micro emulsion electrokinetic chromatography (MEEKC) with ionic liquid and beta-cyclodextrin as additives. Compared with a conventional MEEKC separation and detection method, the method has higher separation degree. An experiment result shows that the method is simple in sample treatment, low in using amount, economic, high in speed, and high in separation degree and sensitivity. Capillary electrophoretic detection on the cortical hormones in the cosmetic is realized by the method.

There is provided according to the invention a pharmaceutical aerosol formulation which comprises:(i) fluticasone propionate and(ii) a hydrofluoroalkane (HFA) propellant,characterised in that the fluticasone propionate is completely dissolved in the formulation. The invention also provided canisters containing the formulation and uses thereof.

In a metered dose inhaler, comprising a canister and metering valve, containing a suspension aerosol formulation comprising particles of formoterol fumarate dihydrate and fluticasone propionate suspended in an HFA propellant, a method of reducing deposition of particles on the surfaces of the canister and the metering valve, the method comprising the step of adding a wetting agent to the formulation.

The invention discloses a preparation method of fluticasone propionate particles having a D98 particle size smaller than 5 [mu]m. By utilization of a recrystallization method, a fluticasone propionate raw material is dissolved in a solvent to prepare a solution, and the solution is added into water containing a surfactant to precipitate the fluticasone propionate particles having the needed particle size. Compared with traditional methods, the preparation method provided by the invention has high yield, low production cost, no dependence on special equipment, and low energy consumption. The preparation method provided by the invention is free from duct generation. Reagents used in the preparation method are nontoxic, harmless and environmental friendly. Products have small particle sizes, narrow particle size distribution, high roundness and good fluidity, and are particularly suitable to be used as raw materials for medicinal preparations.

The invention discloses a highly pure S-fluoromethyl-6alpha,9alpha-difluoro-11beta-hydroxy-16alpha-methyl-17alpha-propionooxo-3-androsterone-1,4-diene-17beta-benzothiodiazole (fluticasone propionate) preparation method. The method is characterized in that various highly-pure intermediates of fluticasone propionate are prepared in order to obtain highly pure fluticasone propionate; and post-treatment and purification of the intermediates obtained in each step are carried out in order to obtain the highly pure fluticasone propionate. The method has the advantages of simple operation, high purity and low quantity of impurities, common and cheap reagents, and suitableness for the large-scale industrial production.

Novel crystalline forms II, III, IV, V, VI, VII and VIII of 6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-propionyloxyandrosta-1,4-diene-17β-carboxylic acid, a chemical intermediate useful in the preparation of fluticasone propionate, and novel methods of making these forms, substantially free of water, are disclosed.

The present invention relates to pharmaceutical products comprising fluticasone furoate for use in the treatment of COPD patients, particularly a subgroup of COPD patients that through analysis have been identified as possessing an eosinophil blood count of≧150 cells / W. The present invention is further directed to methods for treating a patient with COPD which methods include identifying a patient that will respond to treatment and administering a pharmaceutical product of the present invention comprising fluticasone furoate to said patient.

The invention provides a fluticasone propionate spraying agent with improved stability. According to the invention, it is found for the first time that a combined stabilizing agent can be formed by adding disodium edetate into conventional antiseptics--benzalkonium chloride and phenylethyl alcohol, which enables the fluticasone propionate spraying agent to have better stability compared with traditional preparations. After long-term storage, the spraying mode and a droplet distribution scope of the fluticasone propionate spraying agent basically maintain unchanged; the pH value of the preparation is maintained in a proper range without usage of a pH value adjusting agent, and the pH value basically maintains unchanged after long-term storage. The invention further provides a preparation method for the spraying agent.

The invention provides a method for recrystallizing fluticasone propionate. The method is characterized in that the fluticasone propionate is recrystallized in one or more solvents of alkylene oxide organic solvents and amide organic solvents to solve the impurity problem of the fluticasone propionate, so that related substances of the fluticasone propionate completely accord with the requirementof European Pharmacopoeia 2008 Edition EP6, namely total related substances are 1.2 percent maximally, impurities D and G are 0.3 percent maximally, impurities A, B, C, E, F, H and I are 0.2 percent maximally, and other unknown impurities are 0.1 percent maximally.

An inhalation drug composition with fluticasone propionate and a nitric oxide synthase (NOS) inhibitor comprises the fluticasone propionate which serves as an active ingredient, an amino acid derivative which serves as the NOS inhibitor and one or more drug auxiliary materials which suit to be inhaled.

The invention relates to a separate type water suspension medicament of fluticasone propionate containing auxiliary materials for treating skin disease, composed of separately packed fluticasone propionate and separately packed water, wherein the fluticasone propionate contains one or more kinds of pharmaceutical auxiliary materials for skin, is insoluble in water and has a D90 particle size of 0.1-10mu m.

The invention discloses a method for preparing fluticasone propionate suspension for inhalation. Sterile fluticasone propionate suspension is prepared in a way of treating fluticasone propionate and accessories respectively. A solution is prepared from the accessories, and is filtered and sterilized through a microporous filter membrane, and microbial load control over each accessory is not required, so that the cost is lowered.

A method of preparing a thioic acid intermediate of fluticasone propionate includes: treating a 17beta-[(N,N-dimethyl carbamoyl)thio]carbonyl compound in a solution including an alcohol and an alkali metal hydroxide, an alkaline-earth metal hydroxide, or a mixture thereof to cleave an amide from the 17beta-[(N,N-dimethyl carbamoyl)thio]carbonyl compound; treating the solution to separate an aqueous portion; and adding an acid to the aqueous portion to obtain the thioic acid intermediate of fluticasone propionate. A method of preparing fluticasone propionate includes preparing the thioic acid intermediate of fluticasone propionate, and alkylating the thioic acid intermediate of fluticasone propionate to prepare the fluticasone propionate.

The present invention relates to pharmaceutical formulations comprising an anti-inflammatory glucocorticoid compound of the androstane series and levocabastine, an H1 antagonist / anti-allergic, and also relates to therapeutic uses thereof, particularly for the treatment of inflammatory and allergic conditions, specifically rhinitis.

The invention relates to a preparation method of high-performance acrylic resin. According to the method, water, sodium dodecyl benzene sulfonate, fatty alcohol-polyoxyethylene ether and 2-acrylamide-2-methylpropanesulfonic acid are added; the temperature is raised; stirring is performed; monomers A are added; the emulsification is performed for 40min; when the temperature is raised to 70 DEG C, backflow water is introduced; when the temperature is raised to 85 DEG C, a potassium sulphate solution is added; the reaction is performed for 2h; then, fluticasone propionate is added; stirring and reaction are performed to obtain core layer emulsion; monomers B and a potassium peroxodisulfate solution are simultaneously dripped into the core layer emulsion; after the dripping is completed, stirring and reaction are performed; the temperature is lowered to 50 DEG C; the fatty alcohol-polyoxyethylene ether and the fatty alcohol-polyoxyethylene ether are added; the reaction time is 70 minutes; the reaction is performed for 1h at 70 DEG C; ammonia water is added for regulating the pH value to 7 to 8 to obtain the acrylic resin. The preparation method has the advantages that the abrasive resistance of the acrylic resin is greatly improved; the defect that a film formed by the acrylic resin emulsion becomes yellow is overcome.

The invention belongs to the medicine technical field, and relates to a pharmaceutical composition of a beta2 receptor agonist and steroid and application thereof, in particular to a pharmaceutical composition of tranditerol or salt thereof, or mabuterol or salt thereof, and fluticasone propionate and application thereof, wherein the mixture ratio of the tranditerol or the salt thereof to the mabuterol or the salt thereof to the fluticasone propionate is 10 to 1-1 to 10,000; and the composition can be a composition which can be atomized in respirable mode, and can be used for preparing an aerosol inhalant and an aerosol. The composition can be prepared into capsules and other formulations with other auxiliary materials after the composition is prepared into dried powder with pharmaceutically acceptable carriers. The composition can significantly improve pulmonary function, and can control obstructive or phlogistic airway diseases or slow down depravation of the diseases. The composition can be used for preparing medicaments for salving and treating the obstructive or phlogistic airway diseases.

The invention discloses a fluticasone propionate foaming agent composition, which contains fluticasone propionate serving as an active ingredient and one or more pharmaceutically acceptable auxiliary materials for a foaming agent, wherein the content of the fluticasone propionate serving as the active ingredient is 0.05 to 0.2 percent (weight / weight), and the volume expansion ratio of the foaming agent composition is 25 to 50.