83 results about "Fluticasone" patented technology

The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

The present invention provides ophthalmic formulations of fluticasone that provide a comfortable formulation when instilled in the eye and is effective in the treatment of allergic conjunctivitis and/or allergic conjunctivitis. The invention further provides methods of treating allergic conjunctivitis and/or allergic conjunctivitis in a subject in need of such treatment by topical application of the fluticasone formulations of the invention directly to the eye.

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.

Formulations have been developed to improve the solubility of corticosteroids such as fluticasone proprionate in a composition designed to achieve localized release of the drug in the small intestine and/or colon. In one embodiment, solid dispersions of fluticasone are prepared wherein the drug is blended with or coated onto a highly water soluble substrate such as nonpareil (sugar beads) then coated with a layer of polymer soluble in small intestinal fluid, then coated with an enteric coating. The inner polymer layer controls release of the drug, and the enteric coating, a pH sensitive polymer that is broken down in the ileum and colon, controls localized release of drug at various sites within the gastrointestinal tract. The multilayer pharmaceutical composition can be in the form of pellets, tablets compressed from pellets or pellets packed into capsules. The release profile of the drug can be manipulated by (1) altering size or shape (i.e., surface area) and solubility of the inert substrate; (2) the ratio of drug to polymer, the polymer composition and solubility, the porosity of the polymer; (3) the drug form (i.e., free base or salt, or which salt); and the thickness and/or surface area of the drug/polymer and/or enteric coating. In a preferred embodiment, the composition is administered orally. This may also be packaged to provide for an escalating or tapering dosage.

The invention discloses a process for preparing fluticasone diproprionate superfine particles, which comprises the following steps of: (1) preparing solution of fluticasone diproprionate; (2) connecting the solution of fluticasone diproprionate prepared by the step (1) with a solution pump; (3) feeding carbon dioxide; (4) rapidly spraying the solution of fluticasone diproprionate prepared by the step (1) into a crystallization kettle from a nozzle in a supercritical fluid anti-solvent equipment system with the solution pump; and (5) performing crystallization to separate the fluticasone diproprionate out. The fluticasone diproprionate superfine particles prepared by the process is characterized in that: the particles are white loose amorphous superfine particles of which an effective grain size d (0.5) is equal to 8.055mu m. The invention has the advantages that: the process for preparing the fluticasone diproprionate superfine particles by applying supercritical fluid crystallization technology is provided, is suitable for the fluticasone diproprionate superfine particles and improves the solubility and curative effect of the medicament.

The present invention relates to new technological process of converting carboxylic acid into thiocarboxylic acid, and is especially synthesis process of fluticasone acetate. The present invention prepares fluticasone acetate with medicinal level flumethasone as initial material and through one of six technological paths, and has the advantages of short reaction path, high yield, simple reaction condition, high product purity, low cost, etc.

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 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 present embodiments may relate to topically delivered compounded medications for the treatment of scar tissue, skin disorders, and/or other ailments. In one aspect, a transdermal cream or gel may provide for the effective administration of multiple medications simultaneously. Preferably, a silicone-based gel may be provided as a base composition and may have a non-zero percentage of silicone or silicone variant. The silicone-based gel may comprise cyclopentasiloxane, polysilicone-11, dimethicone, and C30-45 alkyl cetearyl dimethicone crosspolymer, and include several active ingredients, such as glucocorticoids, antihistamines, and nerve depressants. The silicone-based gel may include a combination of fluticasone, loratadine, and gabapentin. The concentrations of fluticasone and loratadine may be relatively low, while that of gabapentin moderately high. The silicone-based gel may also have one or more local anesthetics, such as prilocaine and/or lidocaine. The silicone-based gel may include additional active ingredients, such as NSAIDs, anticonvulsants, antidepressants, muscle relaxants, and/or other active ingredients.

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 invention provides a pharmaceutical composition preparation. The pharmaceutical composition preparation comprises an anticholinergic drug tiotropium or a hydrate thereof, a beta 2-receptor agonistarformoterol or a salt thereof, and an inhaled glucocorticoid fluticasone or an ester derivative thereof; tiotropium bromide acts on a muscarinic receptor on bronchial smooth muscles, the cholinergiceffect of acetylcholine released by the tail ends of parasympathetic nerves can be inhibited, and muscular tension is blocked; the arformoterol acts on a beta 2-receptor on an airway smooth muscle cell membrane, so that the release of degranulation and media of mast cells and basophils is reduced, the permeability of capillaries is reduced, and swinging of airway epithelial cilia is increased; the fluticasone is an effective anti-inflammatory drug, and when the three drugs are combined for use, the three mechanisms jointly exert the bronchus relaxing effect and the anti-inflammatory effect; the application range of the triple therapy is wider on the important clinical indexes of reducing acute exacerbation of patients suffering from chronic obstructive pulmonary disease, reducing total-cause mortality rate, improving the lung function of the patients suffering from chronic obstructive pulmonary disease, improving the living quality and the like.

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.

A pharmaceutical composition comprising: (A) at least one compound of formula (I): wherein X is O or S, preferably O R₆ is H, C_1-6alkyl, —(CH₂)pCOOH, —(CH₂)_pCOOC_1-6alkyl, —(CH₂)_pCONH₂, —(CH₂)_pCONHC_1-6alkyl, —(CH₂)_pCON(C_1-6alkyl)₂, R¹¹ is H or C_1-6 alkyl; each R₅ is —OC_1-10alkyl, —SC_1-10alkyl, —C_1-12alkyl, or OAr²; wherein Ar² is phenyl, optionally substituted with one or more halo; each p is 0 to 3; each z is 1 to 2; or a pharmaceutically acceptable salt, or a hydrate or solvate thereof; and (B) one or more corticosteroid partners, preferably selected from the group consisting of betamethasone, clobetasol, halometasone, dexamethasone, fluocortolone, desoximetasone, diflorasone, fluocinonide, flurandrenolide, halobetasol, amcinonide, halocinonide, triamcinolone, hydrocortisone, aclometasone, fluticasone, mometasone, clocortolone, fluocinolone, desonide, prednisone, prednisolone, and prednicarbate or a pharmaceutically acceptable salt, or a hydrate or solvate thereof, especially betamethasone or a pharmaceutically acceptable salt, or a hydrate or solvate thereof.

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 an inhalation medicinal composition prepared from eplerenone and glucocorticoid serving as active ingredients. The inhalation medicinal composition consists of eplerenone, glucocorticoid and one or more carriers suitable for inhalation administration. The glucocorticoid is one or more of ciclesonide, desonide, fluticasone propopnate, mometasone furoate, beclomethasone dipropionate, flunisolide, and triamcinolone acetonide and medicinal salts or esters thereof; the inhalation medicinal composition is preferably prepared into aerosol powder which consists of eplerenone, glucocorticoid and carrier micro powder; the average grain diameter of the eplerenone and glucocorticoid micro powder is 0.5 to 1.0 mu m; and the average grain diameter of the carrier micro powder is 20 to 45 mu m.

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.

A pharmaceutical composition comprises at least one antihistamine, at least one corticosteroid, and at least one pharmaceutical excipient, wherein the at least one antihistamine comprises ebastine or its pharmaceutically acceptable salt, solvate, ester or physiologically functional derivative thereof, and wherein the at least one corticosteroid comprises fluticasone or its pharmaceutically acceptable ester thereof.