45 results about "Levocetirizine" patented technology

A solid oral dosage composition is provided comprising a prophilactically or therapeutically effective amount of an active pharmaceutical ingredient comprising levocetirizine or a pharmaceutically acceptable salt thereof, the solid oral dosage composition having a coating thereon capable of providing taste masking of the levocetirizine or pharmaceutically acceptable salt thereof.

The embodiments described herein include methods and formulations for treating viruses and diseases that are exacerbated by inflammatory responses in the body. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of levocetirizine and montelukast to a patient in need. The methods and formulations can comprise conventional and / or modified-release elements, providing for drug delivery to the patient.

The invention relates to a hydrochloric acid levocetirizine orally disintegrating tablet and a preparation method thereof. The hydrochloric acid levocetirizine orally disintegrating tablet is obtained by directly pressing principal medicine and accessories. The tablet of the invention can be dissolved fast in a mouth cavity and has no grit feeling and high biological availability, which takes effect fast and can have curative effect faster.

A resolution method of a levocetirizine chiral intermediates belongs to the technical field of fine organic chemical engineering. The method comprises the following specific steps: adding racemic 1-[(4-chlorophenyl)benzyl]piperazine and chiral ionic liquid in a reaction container to react at 10-100 DEG C for 1-10 hours, extracting with toluene for layering, adjusting the pH value of the aqueous phase with 10wt% of sodium hydroxide solution to 11-12, extracting with toluene again, and concentrating to crystallize after the post-treatment, thus obtaining the product. The chiral ionic liquid is used as the solvent and resolving agent, the technology is easy to operate, the efficiency is high, the yield of three wastes is low, the yield of the product is more than 34%, the melting range of the product is narrow, the melting point is 94-96 DEG C, the specific rotation [alpha] D is not more than -21.5 degrees (C1, toluene), the optical purity is not less than 99.0%, and the content is not less than 99.0%. The post-treatment is convenient, the ionic liquid can be used repeatedly and the resolution method is an economical, practical, green and environmentally friendly technology.

The embodiments described herein include methods and formulations for treating viruses and diseases that are exacerbated by inflammatory responses in the body. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of levocetirizine and montelukast to a patient in need. The methods and formulations can comprise conventional and / or modified-release elements, providing for drug delivery to the patient.

The invention relates to an H1-receptor-antagonist-containing inhalation preparation which contains an H1 receptor antagonist and one or more pharmaceutical auxiliary materials suitable for inhalation administration. The H1 receptor antagonist is one or more of loratadine, desloratadine, cetirizine, levocetirizine, astemizole, ketotifen, ebastine, fexofenadine, avastin, mequitazine, mizolastine and salts thereof, and preferably one or more of loratadine, desloratadine, cetirizine, levocetirizine, ebastine, mizolastine, avastin, mequitazine, ketotifen and hydrochlorides or fumarates thereof.

The invention relates to an oral anti-allergy compound pharmaceutical composition, which contains levocetirizine and mast cell membrane stabilizer. The dosage forms of the composition comprise tablet, capsule, suspending agent, dry suspending agent, oral solution, granule, and the like. The oral medicament is applied to the treatment of allergic diseases such as urticaria, eczema, dermatitis, allergic rhinitis, skin pruritus, and the like.

The present invention relates to a medicine levocetirizine hydrochloride preparation for external application. Said preparation is made up by using levocetirizine hydrochloride as active effective component and medicinal auxiliary material, and can be used for effectively curing various dermal allergic diseases.

The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof using diglycolic acid or derivatives thereof and new intermediates used in that process.

The present invention provides a compound of formula (IV) wherein R is Cl, Br, NO2, OH or OR', and R' is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (-)-1-[(4-chlorophenyl)-phenyl methyl] piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).

An exterior-applied levocetirizine hydrochloride for preventing and treating the anaphylaxia and inflammation without untoward effect is disclosed.

The invention relates to a levocetirizine preparation method and a levocetirizine dihydrochloride preparation method. Levocetirizine is prepared through a synthesis route shown in the specification, and levocetirizine dihydrochloride is prepared through hydrochlorinating the prepared levocetirizine to form a salt, and recrystallizing the salt. The preparation method which adopts cheap and easily available Pd-M / C to realize the catalytic oxidation of L-hydroxyzine as a catalyst in order to prepare levocetirizine realizes the high conversion rate of the substrate L-hydroxyzine and the high selectivity and high optical purity of the target product levocetirizine, and is an environmentally-friendly technology.

Disclosed is a capsule formulation for preventing or treating allergic rhinitis and asthma, which comprises two separate layers of: (1) a Montelukast layer comprising montelukast or a pharmaceutically acceptable salt thereof; and (2) a Levocetirizine layer comprising levocetirizine or a pharmaceutically acceptable salt thereof; and a method for the preparation thereof. The capsule formulation according to the present invention can completely separate two active ingredients, thereby minimizing the reactivity between them and improving product stability against aging effects, and thus, can optimize the therapeutic effects.

The present invention belongs to the field of pharmaceutical technology, and discloses one kind of orally taken compound levo-cetirizine pseudoephedrine preparation. The preparation has activity similar to that of compound cetirizine pseudoephedrine preparation and is single optical isomer with half reduced dosage and thus long effect and reduced side effect. The preparation may be taken by adult and children. The preparation process is also provided.

The invention relates to naringin composition and a preparation thereof. The pharmaceutical composition is characterized by comprising naringin and levocetirizine hydrochloride, wherein preferably, the naringin is in a range of 27.5-275 mg, and the levocetirizine hydrochloride is in a range of 1.25-12.5 mg; the preferable mass ratio of the naringin to the levocetirizine hydrochloride is 20:1. Tests prove that the pharmaceutical composition has good curative effects on coughs and excessive phlegm caused by various reasons and the cough variant asthma, and the efficacy of the composition is obviously superior to the efficacy of the independently-used naringin or the independently-used levocetirizine hydrochloride.

The present invention relates to one new kind of medicine composition containing levocetirizine (or its pharmaceutically acceptable salt) and pseudoepherine (or its pharmaceutically acceptable salt). The medicine composition is pressed into double layer including the first layer containing levocetirizine (or its pharmaceutically acceptable salt) in the amount for resisting allergy effectively and the second layer containing pseudoepherine (or its pharmaceutically acceptable salt) in the amount as effective decongestant for nose. The medicine composition is used in treating seasonal and perennial allergic rhinitis.

An exterior-applied levocetirizine hydrochloride for preventing and treating the anaphylaxia and inflammation without untoward effect is disclosed.

An oral complex composition which comprises (i) a core comprising a swellable hydrogel-forming agent and pseudoephedrine, or a pharmaceutically acceptable salt thereof; (ii) a first coating layer encasing the core which comprises a water-soluble substance; and (iii) a second coating layer deposited on the first coating layer which comprises levocetirizine or a pharmaceutically acceptable salt thereof together with polyvinylalcohol, povidone, polyvinylalcohol-polyethyleneglycol graft copolymer or a mixture thereof, has an improved levocetirizine releasing rate and does not show a delayed release behavior even after a long storage period. Accordingly, the inventive oral complex composition is useful for treating perennial or seasonal allergic diseases including nasal obstruction, sneezing, and rhinorrhea.

The disclosure provides a semi-solid composition, comprising a gelling component in a sufficient amount to provide a cohesive gelled product, an anti-histamine composition, comprising an antihistamine, and a complexing agent, wherein the complexing agent is capable of interacting with the antihistamine and forming an antihistamine complex. In one embodiment, the antihistamine comprises diphenhydramine, cetirizine, levocetirizine, loratadine, desloratadine, fexofenadine, azelastine, bilastine, rupatadine, or a derivative, salt or a combination thereof.

An oral complex composition which comprises (i) a core comprising a swellable hydrogel-forming agent and pseudoephedrine, or a pharmaceutically acceptable salt thereof; (ii) a first coating layer encasing the core which comprises a water-soluble substance; and (iii) a second coating layer deposited on the first coating layer which comprises levocetirizine or a pharmaceutically acceptable salt thereof together with polyvinylalcohol, povidone, polyvinylalcohol-polyethyleneglycol graft copolymer or a mixture thereof, has an improved levocetirizine releasing rate and does not show a delayed release behavior even after a long storage period. Accordingly, the inventive oral complex composition is useful for treating perennial or seasonal allergic diseases including nasal obstruction, sneezing, and rhinorrhea.

A resolution method of a levocetirizine chiral intermediates belongs to the technical field of fine organic chemical engineering. The method comprises the following specific steps: adding racemic 1-[(4-chlorophenyl)benzyl]piperazine and chiral ionic liquid in a reaction container to react at 10-100 DEG C for 1-10 hours, extracting with toluene for layering, adjusting the pH value of the aqueous phase with 10wt% of sodium hydroxide solution to 11-12, extracting with toluene again, and concentrating to crystallize after the post-treatment, thus obtaining the product. The chiral ionic liquid is used as the solvent and resolving agent, the technology is easy to operate, the efficiency is high, the yield of three wastes is low, the yield of the product is more than 34%, the melting range of the product is narrow, the melting point is 94-96 DEG C, the specific rotation [alpha] D is not more than -21.5 degrees (C1, toluene), the optical purity is not less than 99.0%, and the content is not less than 99.0%. The post-treatment is convenient, the ionic liquid can be used repeatedly and the resolution method is an economical, practical, green and environmentally friendly technology.

The invention relates to a fluticasone and fluticasone ester / H1 receptor antagonist inhalant which contains fluticasone and fluticasone ester and one or more H1 receptor antagonists used as active components, and one or more pharmaceutical auxiliary materials suitable for inhalation administration. The H1 receptor antagonist is one or more of loratadine, desloratadine, cetirizine, levocetirizine, astemizole, ketotifen, ebastine, fexofenadine, avastin, mequitazine, mizolastine and salts thereof, and preferably one or more of loratadine, desloratadine, cetirizine, levocetirizine, ebastine, mizolastine, avastin, mequitazine, ketotifen and hydrochlorides or fumarates thereof.

The present invention relates to a pharmaceutical formulation for oral administration for preventing or treating allergic rhinitis or asthma, which comprises: (a) a first particle part comprising levocetirizine or a pharmaceutically acceptable salt thereof and an organic acid; and (b) a second particle part comprising montelukast or a pharmaceutically acceptable salt thereof. The pharmaceutical formulation according to the present invention comprises an organic acid as a stabilizing agent, which can effectively inhibit the production of levocetirizine and montelukast related substances, and thus, show good stability.

The invention provides a preparation method of levocetirizine. The method comprises the following steps of: the step 1, carrying out a cyclization reaction on (R)-4-chlorodiphenyl methylamine and tris(2-chloroethyl)amine to obtain a compound represented by a formula (I); 2, performing condensation reaction of the compound shown in the formula (I) and 2-ethyl glycolate to obtain a compound shown ina formula (II); and the step 3, converting the compound shown in the formula (II) into levocetirizine. According to the preparation method, (R)-4-chlorodiphenyl methylamine and tris(2-chloroethyl)amine are taken as the initial raw materials, and cyclization reaction, condensation reaction and hydrolysis reaction are carried out so as to obtain levocetirizine. The synthetic route provided by the invention is short, the yield is high, and experimental results show that the yield of the levocetirizine prepared by the method provided by the invention can reach 47%, and the purity can reach 99.7%.

The invention relates to the field of pharmaceutical preparations, in particular to a composition and a preparation method thereof, an oral liquid and a preparation method thereof. The preparation method of the composition is as follows: mixing montelukast sodium with the first water to obtain a montelukast sodium solution; mixing levocetirizine hydrochloride with the second water to adjust the pH value to 6.5-9 to obtain Levocetirizine hydrochloride solution; get montelukast sodium solution and levocetirizine hydrochloride solution to mix. The montelukast sodium in the oral liquid provided by the invention has high stability, does not contain organic solvents and surfactants, is convenient for children to take medicine, and has a simple preparation process.

The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof using diglycolic acid or derivatives thereof and new intermediates used in that process.

The present invention provides an antianaphylactic medicine solution preparation containing Levocetirizine. In 1000 ml of medicine composite solution 0.5-20g of zocetirizine or its pharmacal acceptable salt, 20-100 g of polyvinyl pyrrolidone, 5-50g of poloxamer and 10-250g of polyethylene glycol 400 are contained.

The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof using diglycolic acid or derivatives thereof and new intermediates used in that process.

The present invention describes a novel process for the preparation of levocetirizine and pharmaceutically acceptable acid addition salts thereof using diglycolic acid or derivatives thereof and new intermediates used in that process.

The present invention relates to one new kind of medicine composition containing levocetirizine (or its pharmaceutically acceptable salt) and pseudoepherine (or its pharmaceutically acceptable salt). The medicine composition is pressed into double layer including the first layer containing levocetirizine (or its pharmaceutically acceptable salt) in the amount for resisting allergy effectively andthe second layer containing pseudoepherine (or its pharmaceutically acceptable salt) in the amount as effective decongestant for nose. The medicine composition is used in treating seasonal and perennial allergic rhinitis.