31 results about "Ebastine" patented technology

The invention is directed to compositions comprising at least one nanoparticulate H1-histamine receptor antagonist, such as ebastine or a salt or derivative thereof, having improved dissolution rate providing a faster onset of drug availability. The nanoparticulate H1-histamine receptor antagonist particles, such as ebastine, have an effective average particle size of less than about 2000 nm and are useful in the treatment of seasonal and perennial allergic rhinitis and related diseases.

A tablet of Ebastine is prepared from Ebastine, hydroxypropyl cellulose, microcrystalline cellulose, lactose, and adhesive through superfine pulverizing, proportional mixing, granulating, sieving, mixing and tabletting.

A pharmaceutical composition useful in the treatment of sneezing, itching runny nose, nasal congestion, redness of the eye, tearing, itching of the ears or palate, shortness of breath, inflammation of the bronchial mucosa, reduced Forced Expiratory Volume In One Second (FEV1), coughs, rash, itchy skin, headaches, and aches and pains associated with seasonal allergic rhinitis, perennial allergic rhinitis, common colds, otitis, sinusitus, allergy, asthma, allergic asthma and/or inflammation, in a mammalian organism in need of such treatment. The composition comprises: i) an effective amount of at least one leukotriene antagonist selected from a) montelukast, b) 1-(((R)- (3-(2-(6,7- difluoro-2- quinolinyl)ethenyl) phenyl)-3-(2- (2-hydroxy-2- propyl)phenyl) thio)methylcyclopropaneacetic acid; c) 1-(((1(R)-3 (3-(2-(2,3- dichlorothieno[3, 2-b]pyridin-5-yl) -(E)-ethenyl)phenyl) -3-(2-(1-hydroxy-1- methylethyl) phenyl)propyl) thio)methyl) cyclopropaneacetic acid; d) pranlukast; or f) [2-[[2-(4-tert -butyl-2-thiazolyl) -5-benzofuranyl] oxymethyl]phenyl] acetic acid; or a pharmaceutically acceptable salt thereof; in admixture with ii) an effective amount of at least one antihistamine which is descarboethoxyloratidine, cetirizine, fexofenadine, ebastine, astemizole, norastemizole, epinastine, efletirizine or a pharmaceutically acceptable salt thereof.

The invention provides an ebastine oral liquid preparation. The ebastine oral liquid preparation is mainly prepared from, by mass, 8-12 parts of ebastine, 90-120 parts of solubilizer, 0.8-2 parts of aromatic, 650-800 parts of sweetening agent, 1-4 parts of preservative, 0.8-2 parts of antifoaming agent, 2,000-3,000 parts of latent solvent, pH modifier adjusting pH to be 4-5 and a proper amount of water. The preparing method comprises the steps that solubilizer, latent solvent and a part of pH modifier are mixed and then water is added and stirred until the mixture is dissolved, then, ebastine, sweetening agent, aromatic and preservative are added and continue to be stirred until all the materials are dissolved, antifoaming agent and water are added, the residual pH modifier is added to adjust the pH value to be 4-5, and filtering, quality detecting and filling are added. The ebastine oral liquid preparation is absorbed by the human body easily, and is convenient to carry, wide in target user range and convenient to use.

The invention relates to compositions in the form of matrices consisting of solid ebastine dispersions in nonionic surfactants having a HLB of between 10 and 20 and a melting point of between 30° C. and 70° C. The invention also relates to solid oral pharmaceutical forms of ebastine containing said matrices, particularly tablets, and having good solubility and bioavailability properties and improved stability.

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.

The preparation process of ebastine includes the following steps: 1. condensation of 4-chlorobutyryl chloride and tert-butyl benzene to produce 4-chloro-1-[4-(1,1-dimethylethyl) phenyl]-1-butanone as intermediate I; 2. condensation of the intermediate I and 4-hydroxypiperidine to produce 1-[4-(1,1-dimethylethyl) phenyl]-4-[4-hydroxyl-1-piperidino] -butane ketone as intermediate II; 3. reflux condensation of methylisobutyl ketone ortoluene, chloro diphenylmethane and the intermediate II in the presence one small amount of phenylacetyl peroxide as reaction initiator, and 4. adding 2N hydrochloric acid in the same volume as the reactant after finishing the reaction, shaking, eliminating organic layer, adding 2N sodium hydroxide solution to neutralize to pH9, stirring to separate solid matter, filtering, water washing to neutral and obtain the ebastine product. The present invention has the features of complete reaction, high yield and other advantages.

The invention provides an application of loratadine or ebastine in preparation of a medicine for preventing and/or treating COVID-19 inflammation. In-vivo and in-vitro experiments prove that the loratadine or the ebastine can reduce the inflammatory reaction caused by SARS-CoV-2spike protein by inhibiting mast cell degranulation and inhibit inflammatory factor storm, and has certain protection on tissue damage. Therefore, the combination of the loratadine or the ebastine and an antiviral drug has important clinical application value in the aspect of treating the severe infection of the COVID-19.

The invention discloses psoriasis eliminating powder for treating psoriasis. The psoriasis eliminating powder is prepared from, by weight, 143 parts of milkvetch roots, 143 parts of dark plum fruit, 71 parts of fructus chebulae, 71 parts of radix rehmanniae, 71 parts of fructus tribuli, 71 parts of radix sophorae flavescentis, 71 parts of cortex dictamni, 71 parts of fructus kochiae, 50 parts of periostracum cicada, 50 parts of rhizoma atractylodis, 50 parts of lumbricus, 50 parts of radix scutellariae, 14 parts of herba asari, 28 parts of radix bupleuri, 28 parts of licorice roots and 14 parts of ebastine. The bulk herbs are pulverized and then mixed with the ebastine, and the mixed powder is contained in capsules. According to the psoriasis eliminating powder, all the medicines cooperatively and jointly achieve the effects of treating skin tinea, allergy, eczema, pruritus and chilblain according to the differential treatment theory of traditional Chinese medicine by taking the effects of clearing heat, removing toxicity, dispelling wind, eliminating dampness, promoting blood circulation to remove meridian obstruction and improving the disease resistance and immunocompetence of the skin as a formulating principle. By means of clinical practice and application, the formula is free of irritation, allergenicity and adverse skin reactions and has the obvious treatment effect on the tinea, the eczema, the allergy, the pruritus and the chilblain to promote skin health. Total 180 cases of patients are observed, and the total effective rate is 96%.

The present invention is based on novel discoveries relating to ebastine, carebastine, and epinastine hydrochloride. Specifically, the present invention relates to the use of ebastine and carebastine as an inhibitor of (A) T cell proliferation, (B) Th2 type cytokine production, (C) inflammatory cytokine production, and (D) T cell migration. In addition, it relates to the use of epinastine hydrochloride as an inhibitor of (A) T cell proliferation, (B) Th2 type cytokine production, and (C) Th1 type cytokine production.

The invention relates to a method for detecting the content of bromodiphenyl methane in an ebastine medicine, which comprises the following steps of: 1, preparing a test solution by taking an ebastine raw material medicine and taking n-hexane as a solvent, and dissolving and diluting bromodiphenyl methane with n-hexane to prepare a reference solution; and 2, carrying out gas chromatographic analysis by taking a dimethyl polysiloxane column as a chromatographic column. According to the method for detecting the content of the bromodiphenyl methane in the ebastine medicine, gas chromatography is used for detection, and the method has the advantages of being good in specificity, high in sensitivity, good in repeatability and the like and can be widely used for detecting the content of the bromodiphenyl methane in the ebastine medicine.

The invention provides a preparation method of high-purity ebastine, which comprises the following steps: condensing 4-chloro-1-(4-tert-butylphenyl)-1-butanone serving as an initial raw material with 4-hydroxypiperidine to obtain 4-chloro-1-(4-(1, 1-dimethyl ethyl) phenyl-4-(4-hydroxy-1-piperidyl)-butanone), adding benzhydrol into methyl isobutyl ketone or methylbenzene serving as a solvent, and reacting at the temperature of 60-80 DEG C for 2-3 hours to obtain the high-purity ebastine. Ebastine is obtained through condensation, the obtained ebastine is purified through salification and then free, the purity of the obtained ebastine finished product is larger than 99.9%, the single impurity content is smaller than 0.1%, and the ebastine finished product meets the quality standard of ebastine pharmacopeia.

The invention provides a compound inhalation medicine of ciclesonide and an H1 receptor antagonist. The medicine comprises ciclesonide serving as an active component and one or more H1 receptor antagonists, and one or more medical auxiliaries for inhalation administration, wherein the H1 receptor antagonist is one or more of loratadine, desloratadine, cetirizine, levocetirizine, astemizole, ketotifen, ebastine, fexofenadine, acrivastine, mequitazine, mizolastine and salt thereof, and preferably one or more of loratadine, desloratadine, cetirizine, levocetirizine, ebastine, mizolastine, acrivastine, mequitazine, ketotifen and hydrochloride or fumarate thereof.

The invention discloses a preparation method of Ebastine and fumarate of the Ebastine. The preparation method comprises the following steps: 1) mixing 4-(diphenylmethoxy)-piperidine, 4'-tert-butyl-4-chlorobutyryl benzene, an acid-binding agent and a first solvent to carry out a synthetic reaction, adding a second solvent and water after the reaction is finished, and stirring the reaction productsfor layering to obtain an organic layer and an inorganic layer; and 2) concentrating and drying the organic layer, adding a third solvent or the third solvent and fumaric acid, filtering and drying the mixture to obtain 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(Diphenylmethoxy)-1-piperidinyl]-1-butanone or fumarate thereof. By applying the technical scheme, solvent-free or low-solvent synthesis has the advantages of solvent saving, cost reduction, environmental friendliness and the like.