Olopatadine hydrochloride nasal spray and preparation method thereof

Abstract

The invention belongs to the technical field of medicines, and provides olopatadine hydrochloride nasal spray and a preparation method thereof. The nasal spray is prepared from olopatadine hydrochloride, water-soluble chitosan, chitosan quaternary ammonium salt, hydroxypropyl-beta-cyclodextrin, an osmotic pressure regulator, a buffer agent, a pH regulator and purified water. The olopatadine hydrochloride nasal spray prolongs residence time, in a nasal cavity, of olopatadine hydrochloride and improves bioavailability of the olopatadine hydrochloride. Besides, stability of the product is furtherimproved, bitter taste of the product is reduced, an occurrence rate of untoward effects such as epistaxis and a sore throat is reduced, thrill on nasal mucosa is low, side effect is small, and the safety of nasal cavity drug delivery is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an olopatadine hydrochloride nasal spray and a preparation method thereof. Background technique [0002] Olopatadine is a highly selective dibenzoxepin-2-acetic acid histamine H developed and marketed by Kyowa Hakko Co., Ltd. 1 Receptor inhibitors can inhibit the release of tachykinins and other chemical transmitters, such as histamine, arachidonic acid, thromboxane, leukotrienes, etc., and can be used to treat allergic rhinitis, urticaria, eczema, dermatitis, and prurigo , skin pruritus and other allergic diseases. Olopatadine is generally administered in the form of hydrochloride, and the commonly used dosage forms in clinical practice are tablets and eye drops. [0003] Nasal administration is convenient and easy, the patient can complete it independently, and is less restricted by the environment. After the drug is absorbed by the nasal cavity, it directly ente...

AI Technical Summary

Problems solved by technology

During the research and development of nasal pharmaceutical preparations, additives, absorption enhancers, preservatives and other excipients in the drug or preparations may have ciliary toxicity, which may irritate the nasal mucosa, limiting the research and application of nasal drug preparations

In addition, the drug stays in the nasal cavity for a short time and is quickly cleared by mucocilia after administration, which will affect the effectiveness of nasal administration to some extent

[0007] Existing olopatadine nasal spray, as disclosed in Chinese patent application CN 103830219 A, can be used to prepare nasal spray olopatadine composition and FDA approved olopatadine hydrochloride nasal spray Among them, the auxiliary material composition all includes bacteriostatic agent benzalkonium chloride and chelating agent edetate disodium, and both olopatadine and benzalkonium chloride are bitter substances, therefore, due to the scavenging effect of nasal cilia, olopatadine hydrochloride After the administration of nasal spray, it is easy to produce adverse reactions such as bitter taste; and studies have shown that edetate disodium has a significant impact on the stability of olopatadine

The paper "Pharmaceutical Research of New Antiallergic Drug Olopatadine Hydrochloride Nasal Spray" published by Xiao Xuecheng et al., Olopatadine Hydrochloride Nasal Spray Common (>1%) adverse reactions included bitter taste (12.8%), headache (4.4%), nosebleed (3.2%), sore throat (2.2%), postnasal drip (1.5%) and cough (1.4%), etc. , the existing olopatadine hydrochloride nasal spray is more irritating to the mucous membranes and has more side effects, and the prior art still lacks a kind of olopatadine hydrochloride nasal spray with strong stability and few side effects

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