azelastine hydrochloride(CAS#79307-93-0)

Chemical Property:

Molecular Formula	C22H24ClN3O·HCl
Melting Point	219-221?C
Solubility	Soluble in water (25 mg/mL), DMSO (>10 mg/mL), and ethanol.
Appearance	Solid
Color	White
Storage Condition	-20°C Freezer
Sensitive	Sensitive to heat
Physical and Chemical Properties	For Azelastine Hydrochloride Nasal Spray, ie, acerbine (AZEP): This product is colorless or almost colorless clear liquid
Use	[Drug Name] Common name: Azelastine Hydrochloride Nasal Spray Chinese pinyin: Yansuandanzhuositing bifenwuji [ingredients] Azelastine hydrochloride. [Properties] This product is a colorless transparent liquid, high pressure valve, medicine is sprayed in a mist. [indications] seasonal allergic rhinitis (hay fever) and perennial allergic rhinitis [dosage] 1 spray/nostril, morning and evening, twice daily (equivalent to a 0, 56mg Azelastine hydrochloride dose per day) or as described. When spraying, keep the head upright before the symptoms disappear should adhere to the use of acerbine nasal spray, but continuous use is not more than 6 months. [adverse reactions] a small number of patients spray will produce nasal mucosa irritation, individual patients appear epistaxis. If the method of administration is incorrect, there will be bitter taste. [medication for pregnant and lactating women] Although the drug test in large doses in animals did not produce a malformed response to the drug, however, the drug is not recommended for women in the first 3 months of pregnancy. The use of this product is strictly prohibited for lactating mothers. [children's medication] children over 6 years old with adult dosage [drug interaction] found no interaction with other drugs. [overdose] animal tests have shown that excessive oral doses can cause symptoms of the central nervous system, once this situation occurs, it should be symptomatic treatment or supportive therapy, no specific antidote. [Pharmacology and Toxicology] Azelastine hydrochloride is a new structure of 2, 3 diazepinone derivatives, as a potential long-acting anti-allergic compounds, with H1 receptor antagonist characteristics. Animal experimental data show that high concentrations of Azelastine hydrochloride can prevent the synthesis and release of certain chemical mediators (eg, leukotrienes, histamine, serotonin) in allergic reactions. And can prevent the migration of I-CAMI of the upregulated and eosinophilic cells to exert a wide range of anti-inflammatory effects. No local or organ-specific toxic reactions were detected at the maximum dose permitted for nasal spray administration. [pharmacokinetics] repeated daily nasal spray of 0, 56mg Azelastine hydrochloride (equivalent to 1 spray/nostril, 2 times/day), the steady-state plasma concentration of Azelastine hydrochloride Cmax in healthy volunteers was 0, 27ng/ml, its active metabolite, N-Desmethyl azelastine, can be detected at or below the limit of quantification (0, 12ng/ml). [storage] sealed and kept in a cool place. [validity period] tentative 18 months

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azelastine hydrochloride(CAS#79307-93-0) Introduction

Azelastine hydrochloride
This product is (soil) 4-(4-chlorobenzyl)-2-(hexahydro-1-methyl-1 H-azazepine-4-yl)-l(2ff)-2,3-diazanaphthone hydrochloride. Calculated as a dry product, the content of C22H24C1N30•HCl shall not be less than 99.0%.

Characters
This product is white or off-white powder or crystalline powder; Odorless.
This product is slightly soluble in methanol, slightly soluble in water or ethanol, and soluble in glacial acetic acid.
Differential
take this product, add water to dissolve and dilute to make a solution containing about 30ug per 1ml, according to ultraviolet-visible spectrophotometry (General rule 0401), there is a maximum absorption at a wavelength of 286nm, and a minimum absorption at a wavelength of 264nm.
The infrared absorption spectrum of this product should be consistent with that of the reference substance (General rule 0402).
The aqueous solution of this product shows the reaction of chloride identification (1) (General rule 0301).
examine
optical rotation
take this product, weigh it accurately, add water to dissolve and quantitatively dilute it to make a solution containing about 5mg per love ml (if necessary, it can be dissolved by ultrasonic), and determine it according to law (General rule 0621), and the optical rotation is 0.01 ° to + 0.01 °.

acidity
take 50mg of this product, add 30ml of water to dissolve (if necessary, it can be dissolved by ultrasonic), and determine according to law (General rule 0631), the pH value should be 5.0 to 7.0.

Application

Azelastine hydrochloride (CAS 79307-93-0) is a second‑generation, selective histamine H1‑receptor antagonist belonging to the phthalazinone derivative class. As an active pharmaceutical ingredient (API), it is clinically indicated for the symptomatic treatment of seasonal and perennial allergic rhinitis (via intranasal spray, e.g., Astelin®, Optivar®) and allergic conjunctivitis (ophthalmic solution). It functions by competitively blocking H1 receptors on effector cells, thereby inhibiting histamine release and stabilizing mast cells to suppress the activation of multiple allergic inflammatory mediators, including leukotrienes, platelet‑activating factor, and IL‑6. Azelastine is also formulated in fixed‑dose combination with fluticasone propionate (Dymista®) for enhanced management of moderate‑to‑severe seasonal allergic rhinitis. In pharmaceutical R&D and quality control, azelastine hydrochloride is widely used as a certified reference material (CRM) for analytical method development (AMD), method validation (AMV), HPLC/GC calibration, impurity profiling (including genotoxic nitrosamine impurities), and forced degradation studies. Its chiral forms, (R)‑ and (S)-azelastine hydrochloride, are employed as enantiomeric reference standards for ANDA filings and commercial production. Xinchem offers custom synthesis, custom chemical synthesis, and contract manufacturing of high‑purity azelastine hydrochloride with flexible scaling from R&D to commercial tons. Contact us today for a competitive quote and reliable global supply.

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allergic rhinitis nasal spray