9 results about "Azelastine" patented technology

Disclosed are pharmaceutical compositions comprising azelastine or a pharmaceutically acceptable salt of azelastine and methylcobalamin. Also disclosed are methods of using the pharmaceutical compositions to treat patients suffering from Alzheimer's disease or Parkinson's disease.

This invention provides a pharmaceutical composition combining azelastine and methylcobalamin. [Solution] An orally administered pharmaceutical composition is provided, comprising azelastine or a pharmaceutically acceptable salt of azelastine, methylcobalamin, and one or more pharmaceutically acceptable excipients, wherein the pharmaceutical composition is formulated as a capsule, caplet, tablet, or pill configured for oral administration and absorption in the gastrointestinal tract, and the azelastine or a pharmaceutically acceptable salt of azelastine and methylcobalamin are present together in the pharmaceutical composition in a therapeutically effective daily dose for treating Alzheimer's disease or Parkinson's disease in human patients.

The invention belongs to the technical field of chemical synthesis of medicines, and particularly relates to a preparation process of azelastine hydrochloride, which comprises four steps of condensation reduction, hydrochloric acid hydrolysis, cyclization and hydrochloric acid salification. According to the method, the reaction efficiency, the product yield and the purity are improved, the production cost and the operation difficulty are reduced, and a stable, cost-controllable and repeatable preparation process is formed. The prepared azelastine hydrochloride is a long-acting anti-allergic drug, has dual effects of resisting histamine and inflammation, has high affinity to a receptor, effectively blocks histamine release of mast cells and basic granulocytes, has wide pharmacological effects on leukotriene, kinin, platelet activating factors and other inflammatory chemical mediators, and can be used for preparing an anti-allergic drug. Therefore, azelastine can effectively relieve typical symptoms of allergic conjunctivitis, such as pruritus, conjunctival congestion, lacrimation, conjunctival edema and the like.

Disclosed are pharmaceutical compositions comprising azelastine or a pharmaceutically acceptable salt of azelastine and a therapeutically active ingredient of donepezil or rivastigmine or galantamine or a pharmaceutically acceptable salt thereof. Also disclosed are methods of using the pharmaceutical compositions to treat patients with mental disorders, behavioral disorders, cognitive disorders.

The invention relates to a synthetic method of an aza-seven-membered ring nitrosamine impurity, which comprises the following steps: S1, condensing a compound I and a compound II in a solvent 1 to obtain a solution A containing a compound III; s2, a reducing agent is added into the solution A containing the compound III obtained in the S1 for a reduction reaction, after the reaction is completed, aftertreatment is conducted, and a compound IV is obtained; s3, hydrolyzing the compound IV obtained in S2 in an aqueous solution of strong acid, filtering after hydrolysis is completed, adjusting the pH value to 6.5-7.2, adding a compound V, heating, refluxing, condensing, dehydrating and cyclizing, and obtaining a solution B containing a compound VI after reaction is completed; and S4, concentrating the solvent in the solution B containing the compound VI obtained in the step S3 under reduced pressure, adding a solvent 2, filtering, adding a nitrosation reagent, and after the reaction is finished, performing column chromatography purification to obtain the target impurity. At present, no report related to synthesis of the nitrosamine impurity exists in the prior art, and the nitrosamine impurity synthesis method lays a foundation for quality control of azelastine.

This invention belongs to the field of biomedical technology and provides a mussel adhesive protein and azelastine hydrochloride nasal thermosensitive gel, its preparation and application. The mussel adhesive protein and azelastine hydrochloride nasal thermosensitive gel includes an active ingredient and pharmaceutically acceptable excipients. The active ingredient is recombinant mussel adhesive protein mefp-5 subtype and azelastine hydrochloride. The excipients include a thermosensitive polymer, which is mixed with the active ingredient to form a thermosensitive gel system. This invention solves the technical problem that existing single-drug formulations cannot simultaneously provide rapid symptom relief and long-term mucosal barrier repair for allergic rhinitis by combining recombinant mussel adhesive protein mefp-5 subtype with mucosal repair function with azelastine hydrochloride, which has rapid anti-allergic effects. Pharmacodynamic studies have confirmed that the two active ingredients exhibit a significant synergistic effect (CDI < 0.7) in improving allergy symptoms, inhibiting inflammatory responses, and repairing the mucosal barrier.

The application discloses application of a small-molecule drug azelastine in preparation of a medicine for treating sporotrichosis. The application takes abaA gene as a target for finding a new drug, performs batch molecular docking on a small-molecule database which has been approved by FDA and marketed, and screens out azelastine. The azelastine can inhibit Sporothrix globosa and Sporothrix schenckii, can also inhibit phase conversion of the Sporothrix globosa and the Sporothrix schenckii, and has a certain therapeutic effect on sporotrichosis, and is extremely likely to become a promising new drug for treating sporotrichosis. In the research process, it is also found that the small-molecule drug azelastine can have a broad-spectrum bacteriostatic effect. Since the drug is approved for marketing for treating other symptoms, compared with a new compound, a large amount of time and money cost for analyzing pharmacokinetics and pharmacology and toxicology is saved, and the azelastine has great potential as a new drug for treating sporotrichosis.

The application discloses a preparation method of an azelastine intermediate, relates to the technical field of medicines, and aims to solve the problems of a complex synthesis process and a low conversion rate of the azelastine intermediate. The application comprises the following steps: S1, reaction: mixing BBMZ, PD and an organic base according to a molar ratio of 1:1.0-2.0:0.8-1.2, and reacting at a temperature of 80-100 DEG C for 3-5 h; S2, dissolution: adding 1-3 times weight of an organic solvent into the reaction mixture to promote dissolution of a reaction product; S3, filtration: removing a by-product hydrochloride of the organic base by filtration; S4, crystallization: adding 0.5-2 times weight of water into the filtrate to stir and crystallize, and controlling a temperature range of 20-45 DEG C; S5, crystal growing: cooling the solution to 0-10 DEG C, and continuing to stir for not less than 1 h; S6, filtration and washing: sequentially washing the filter cake with an organic solvent and water; and S7, drying: drying the washed filter cake at a temperature of 20-30 DEG C by air blowing for 5-6 h to obtain a PDA product. The application not only improves production efficiency and product quality, but also remarkably reduces environmental influence, and has important industrial application value.

To provide novel antiviral treatments, pharmaceutical products, and chemicals that can be used to prevent viral infection and / or viral spread in subjects exposed to, infected with, or at risk of viral infection. [Solution] An azelastine compound in an antivirally effective amount for use as an antiviral substance in a pharmaceutical formulation.