Olopatadine hydrochloride nasal spray and preparation method thereof

A technology of olopatadine hydrochloride and nasal spray, applied in the field of medicine, can solve the problems of easy to produce bitter taste, influence on the stability of olopatadine, existence of ciliary toxicity, etc., to improve bioavailability, prolong residence time, improve The effect of stability

Active Publication Date: 2018-01-12
深圳大佛药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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 chlo

Method used

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  • Olopatadine hydrochloride nasal spray and preparation method thereof
  • Olopatadine hydrochloride nasal spray and preparation method thereof
  • Olopatadine hydrochloride nasal spray and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～3、 comparative example 1

[0029] Preparation of Examples 1-3, Comparative Examples 1-2 Olopatadine Hydrochloride Nasal Spray

[0030] formula:

[0031]

[0032]

[0033] Preparation:

[0034] S1: Take hydroxypropyl-β-cyclodextrin, add purified water to make a saturated solution, add olopatadine hydrochloride, and sonicate for 30 minutes at room temperature to obtain solution I;

[0035] S2: Take water-soluble chitosan, chitosan quaternary ammonium salt and osmotic pressure regulator, add appropriate amount of purified water to dissolve completely, and obtain solution II;

[0036] S3: Stir and mix the solution I described in step S1 and the solution II described in step S2, add purified water to adjust the solution volume to 80% of the final solution volume, add 6mol / L hydrochloric acid solution or 1mol / L sodium hydroxide solution to adjust pH , add buffer, add 6mol / L hydrochloric acid solution or 1mol / L sodium hydroxide solution to adjust pH, finally add purified water to make the solution volu...

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/335A61K47/40A61K47/36A61P11/02A61P37/08A61P17/00A61P17/04
Inventor 杨瑞雄肖仰
Owner 深圳大佛药业股份有限公司
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