46 results about "Fluticasone furoate" patented technology

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.

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 provides a single preparation and compound preparation using furoic acid fluticasone as main constituent. The weight ratio of furoic acid fluticasone in pharmaceuticals is 0.0001-50%. The pharmaceuticals can be made into jellies, supensoid agent, liquor and pulvis, and the like, which are administrated in a percutaneous way. The preparation is suitable for anaphylactic rhinitis, asthma and stubborn skin disease. The invention has the advantages of high healing rate, high safety and high promotional value.

The invention relates to a preparation method of fluticasone furoate, especially preparation and purification of an intermediate 6alpha, 9alpha-difluoro-17alpha-[(2-furylcarbonyl)oxy]-11beta-hydroxy-16alpha-methyl-3-oxo-androstane-1,4-diene-17beta-thiocarboxylic acid. The preparation method comprises the following steps: in the presence of alkali and alcoholic solvent, a compound as shown in the formula VIII is converted into a mixture containing the compound of formula II; the mixture containing the compound of formula II is mixed with an aqueous solution of inorganic base and an ester solvent; a water phase is separated; pH value of the water phase is regulated by the use of acid until a solid is precipitated out; and the solid is separated. The invention provides a preparation method capable of remarkably raising purity of fluticasone furoate. Safety of drug application is guaranteed.

This invention provides a dry powder inhaler comprising: a dry powder medicament comprising fluticasone propionate, salmeterol xinafoate and a lactose carrier; wherein, the delivered dose of fluticasone propionate per actuation is less than 100 μg; and wherein the dose provides a baseline-adjusted FEV1 in a patient of more than 150 mL within 30 minutes of receiving the dose. A method of treating a patient includes administering to a patient a dry powder medicament having fluticasone propionate, salmeterol xinafoate and a lactose carrier; wherein, the delivered dose of fluticasone propionate per actuation is less than 100 μg; and wherein the dose provides a baseline-adjusted FEV1 in a patient of more than 150 mL within 30 minutes of receiving the dose.

The present invention relates to aggregate particles comprising nanoparticulate drug particles. In particular, the present invention is directed to aggregate particles comprising nanoparticulate drug particles of umeclidinium bromide and optionally vilanterol trifenatate and / or fluticasone furoate. Aggregate particles of the present invention may further comprise nanoparticulate excipient particles and one or more binders. The invention also relates to powder compositions suitable for inhalation that comprise said aggregate particles, processes of producing said aggregate particles, and use of said powder compositions in the treatment of respiratory diseases, such as asthma and COPD.

The present invention is directed to pharmaceutical combination products comprising a muscarinic acetylcholine receptor antagonist, fluticasone propionate and salmeterol xinafoate, and to their use in the treatment of inflammatory or respiratory tract diseases.

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.

Provided is a dry powder for inhalation formulation comprising salmeterol xinafoate, fluticasone propionate and tiotropium bromide, as pharmaceutically active ingredients, and a carrier, and an inhalation formulation comprising same. The inventive dry powder inhalation formulation having good content uniformity and showing small changes in the aerodynamic size distribution in accordance with the flow rate changes can effectively deliver said pharmaceutically active ingredients to a target site upon administration, and thus can be useful in the prevention or treatment of respiratory diseases, particularly asthma and COPD.

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 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 provides a fluticasone furoate liposome and a preparation method thereof. The fluticasone furoate liposome comprises the components of phospholipid, sterol and fluticasone furoate, wherein the fluticasone furoate accounts for 0.01%-1%, the phospholipid accounts for 0.065%-0.196%, and the sterol accounts for 0.035%-0.104%. A preparation method of the fluticasone furoate liposome comprises the steps of (1) performing mixing and injecting; and (2) performing filtering and concentrating. The method is simple to operate, stable in technology and suitable for mass production.

The invention discloses a vilanterol trifluoromethanesulfonate-containing pharmaceutical preparation, which comprises the following main active ingredients: long-acting beta2 receptor agonist vilanterol trifluoromethanesulfonate, glucocorticoid drug fluticasone furoate and long-acting anticholinergic drug aclidinium bromide, or physiologically acceptable salts of the fluticasone furoate and aclidinium bromide, thus composing a compound preparation. The vilanterol trifluoromethanesulfonate has the effect of continuously dilating blood vessels for 24 hours; the fluticasone furoate is fast-acting potent glucocorticoid, and the duration time of the drug is longer than that of other glucocorticoids; the aclidinium bromide is long-acting cholinergic receptor antagonist, and combines with beta2 receptor agonist so as to play roles of synergism and reduction of adverse drug reaction. The vilanterol trifluoromethanesulfonate, the fluticasone furoate and the aclidinium bromide are combined for use to prepare an inhalable compound preparation which can be taken once daily due to 24-hour acting. The vilanterol trifluoromethanesulfonate-containing pharmaceutical preparation can enhance the curative effect, solves the compliance problem of patients with coexisting chronic obstructive pulmonary disease and asthma, thus being appreciable in application prospects.

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.

The invention provides a pulsatile controlled-release tablet containing fluticasone furoate and vilanterol. The pulsatile controlled-release tablet can reach plasma concentration at midnight and early morning, so the purpose of chrono-chemotherapy is achieved. The pulsatile controlled-release tablet comprises a floating layer and a tablet core. The floating layer uses hydrophilic high molecules and fatty alcohol as adjuvant materials, so the floating layer can retain for a certain period of time in the stomach; when the tablet contacts with gastric juice, the surface of the floating layer hydrates to form gel, so the size of the tablet becomes larger; when the gel is smaller than the concentration of the gastric juice, the tablet is allowed to float above contents in the stomach; and the tablet core appears along with dissolution of the skeleton of the floating layer, so drugs are released from the tablet core.

The present invention relates to an improved process for the preparation of substituted Fluticasone derivatives. The invention also reveals the processes for the purification of Fluticasones and related intermediates to provide the highly pure product.

Described are processes for the preparation of monofluoromethylated organic biologically active compounds, such as Fluticasone Propionate and Fluticasone Furoate, in the presence of fluorodecarboxylating reagents such as XeF2 and BrF3.

Described is a process for the preparation of monofluoromethylated organic biologically active compounds using monofluoromethylated reagents. Fluticasone Propionate and Fluticasone Furoate can be prepared using, for example, S-monofluoromethyl-S-phenyl-2,3,4,5-tetramethylphenylsulfonium tetrafluoroborate as monofluoromethylating reagent instead of bromofluoromethane.

The invention relates to a preparation method of high-purity fluticasone furoate. The method comprises the steps as follows: adding a compound in formula III, an alcohol solvent and alkali to a reaction flask for an alcoholysis reaction to prepare a mixture of a compound in formula II, and performing after-treatment to prepare a solution of the compound in formula II; adding the solution of the compound in formula II, organic alkali and a fluoro-halogen methylation reagent to a reaction flask for a substitution reaction to prepare a crude product of a compound in formula I, and performing recrystallization to obtain a refined product of the compound in formula I. The target product is prepared by improving the after-tretament method of the compound in formula II and improving preparation methods of the compound in formula II to the compound in formula I, and the method is simple to operate, can effectively control methyl esters and oxidation impurities, is high in yield, high in purityand lower in cost, and can better meet the requirement of medicinal materials and the requirement of industrial enlargement.

A dermal medicine composition containing fluticasone propionate and a nitric oxide synthase (NOS) inhibitor comprises the fluticasone propionate used as an active ingredient, an amino acid derivative used as the NOS inhibitor, one type or a plurality of types of medicine auxiliary materials suitable for skins and the balance water.

The invention relates to an inhalation preparation containing calcitriol and fluticasone propionate and a preparation method thereof. The inhalation preparation comprises calcitriol, and fluticasone propionate as active components, and one or more of pharmaceutic adjuvants which are suitable for inhalation administration, a mass ratio of ciclesonide to calcitriol is 100-800:1, and the inhalation preparation is used for treating airway diseases of humans or mammals.

The invention relates to a nasal medicine composition enclosing fluticasone propionate by cyclodextrin, which contains the fluticasone propionate and one or more auxiliary material medicine compositions acceptable in pharmacy. The nasal medicine composition is characterized that the fluticasone propionate contained in the medicine composition and used as an active component is enclosed by the cyclodextrin and / or derivatives thereof. The medicine composition is used for treating the allergic rhinitis of human or mammals.

A transdermally-absorbed medicament used for skin and consisting of adjuvant-containing fluticasone propionate and adjuvant-containing water comprises: fluticasone propionate which is single packaged and water-insoluable, has a D90 particle size of 0.1 to 10 [mu]m, and contains one or a plurality of solid pharmaceutic adjuvants; and water which is single packaged and contains one or a plurality of water-soluable pharmaceutic adjuvants.

Method for preparing fluticasone furoate (6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-[(2-furoyl)oxy]-3-oxo-androsta-1,4-diene-17β-carbothioic acid S-fluoromethyl ester) by directly subjecting a compound of Formula III and a complex of a fluoromethylating reagent in presence of an organic base to a replacement reaction to obtain the target compound. Generation of impurities in a process via Compound IV is avoided; the method is simple with mild reaction conditions, suitable for industrial production, and yields products with purity of 98% by HPLC.

The invention provides a pulsatile controlled-release tablet containing fluticasone furoate and vilanterol. The pulsatile controlled-release tablet can reach plasma concentration at midnight and early morning, so the purpose of chrono-chemotherapy is achieved. The pulsatile controlled-release tablet comprises a floating layer and a tablet core. The floating layer uses hydrophilic high molecules and fatty alcohol as adjuvant materials, so the floating layer can retain for a certain period of time in the stomach; when the tablet contacts with gastric juice, the surface of the floating layer hydrates to form gel, so the size of the tablet becomes larger; when the gel is smaller than the concentration of the gastric juice, the tablet is allowed to float above contents in the stomach; and the tablet core appears along with dissolution of the skeleton of the floating layer, so drugs are released from the tablet core.

A method is provided for treating or preventing symptoms of asthma in a subject in need thereof by administering a corticosteroid pharmaceutical composition to a subject qualified for over-the-counter access to the corticosteroid pharmaceutical composition. In some embodiments, the corticosteroid pharmaceutical composition includes a class B corticosteroid, a glucocorticosteroid, budesonide, ciclesonide, fluticasone furoate, mometasone furoate, fluticasone propionate, or beclomethasone dipropionate.

Described herein are processes for the preparation of monofluoromethylated organic biologically active compounds, starting from protected intermediates and / or reagents to obtain compounds such as fluticasone propionate and fluticasone furoate, in presence of decarboxylating reagents XeF2 and BrF3, or using FCH2SH as a reagent.

The present invention is directed to a liposomal formulation having a lipid ingredient encapsulating fluticasone furoate, and a method for preparing the liposomal formulation. The liposome formulation comprises a lipid and a sterol. The method of preparing the liposomes comprises the steps of (1) mixing fluticasone furoate with lipid ingredients comprising a lipid and a sterol, (2) injecting the mixture into normal saline solution, and (3) ultrafiltering and concentrating the resulting solution. This preparation method can produce a liposome formulation having desirable properties and compositions, for example, the ratio of the lipid ingredient, the drug to lipid ratio, and the pH value, which is suitable for nebulization inhalation.

The invention provides a fluticasone furoate liposome and a preparation method thereof. The fluticasone furoate liposome comprises phospholipids, sterols and fluticasone furoate, wherein the amount of fluticasone furoate is 0.01% to 1%, and the amount of phospholipids is 0.065% %~0.196%, the amount of sterol is 0.035%~0.104%, the preparation method of the fluticasone furoate liposome comprises: (1) mixing and injecting (2) diafiltration concentration steps, the method of the present invention is simple to operate, and the process is stable , suitable for mass production.