JP3324264B2 - Nasal rinse - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention
/ Nasal cleaning agent comprising a W-type emulsion, after spraying from a nasal drop container, forms an oil film layer in the nasal cavity, keeps the pH of the surface of the nasal mucosa in a weakly acidic state, and controls invasion of allergens such as pollen. Related to cleaning agents.

[0002]

2. Description of the Related Art In recent years, as the number of hay fever patients increases, the demand for a nasal irrigant for the purpose of washing the nasal cavity of pollen and the like that has entered the nasal cavity has rapidly increased. Generally, the extraction of allergen from pollen particles is performed in an alkaline solution. The pH in the nasal cavity of a nasal allergy patient is said to be 7.8 to 8.5. Considering the mechanism of onset of allergy, for example, pollen particles that have entered the nasal cavity elute the protein that causes allergies under alkaline conditions, penetrate into the living body through the nasal mucosa, and cause allergic symptoms (sneezing , Runny nose, nasal congestion).

[0003] Conventional nasal irrigants mainly have a neutral or alkaline pH. The purpose of this is to extract and wash away allergens from pollen particles by increasing the pH. However, the conventional nasal lavage has an insufficient action of washing out allergens, so that there is a disadvantage that allergens are caused by residual allergens. An object of the present invention is to provide a nasal cleanser highly effective against hay fever and the like in such a situation.

[0004]

Means for Solving the Problems As a result of intensive studies, the present inventors have found that by keeping the pH in the nasal cavity weakly acidic, the elution of allergen from pollen particles that have entered the nasal cavity can be suppressed, and the nasal mucosa can be further suppressed. It has been found that the above object can be achieved by suppressing the transfer of the allergen substance into the nasal mucosa by forming an oil film on the surface of the nasal mucosa, and completed the present invention. That is, the present invention is a nasal rinse comprising an O / W emulsion having a pH of 3.5 to 5.5.

In the present invention, in order to prepare an O / W emulsion, an oil component (1 to 50, preferably 20
-40% by weight), a surfactant (0.05-5.0, preferably 0.1-3.0% by weight) and water. As the oil component, any of a liquid, a solid, and a semi-solid may be used if it is insoluble in water, for example, jojoba oil,
Examples include sasanqua oil, avocado oil, soybean oil, olive oil, safflower oil, evening primrose oil, corn oil, higher polyhydric alcohols, fatty acids, medium-chain fatty acid triglycerides, fatty acid esters, and squalene. this house,
An oil component (soy oil, medium-chain fatty acid triglyceride, etc.) that is dispersed by a surfactant, lecithin, or the like is preferable. As the surfactant, a nonionic surfactant,
Any of a cationic surfactant, an anionic surfactant, an amphoteric surfactant and an amphipathic substance may be used, but a nonionic surfactant or an amphiphile usually used for a nasal washing agent from the viewpoint of safety. Substances are preferred. For example, sorbitan fatty acid ester, glycerin fatty acid ester, polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, N-acylmethyltaurine salt, imidazolium betaine, phospholipid (natural phosphorus Examples thereof include lipids, synthetic phospholipids, and phospholipids obtained by hydrogenating natural phospholipids, such as lecithin. One of these may be used alone, or two or more of them may be used in combination.

To adjust the pH of the preparation to 3.5 to 5.5, a pH adjuster is used. Examples of the pH adjuster include hydrochloric acid, phosphate buffer and the like.

[0007] The nasal rinse of the present invention can be used in addition to oil components, surfactants and pH adjusters, as well as substances commonly used for nasal drops, such as local anesthetics (dibucaine hydrochloride, lidocaine, lidocaine hydrochloride, procaine hydrochloride, etc.). Disinfectants (such as hibitene, benzalkonium chloride, and decalinium chloride), anti-inflammatory agents (such as glycyrrhizic acid and vitamin C), thickeners (such as polyvinylpyrrolidone, methylcellulose, and hydroxypropylcellulose), and isotonic agents (such as glycerin) , A stabilizer, a cooling agent and the like can be blended within a range that does not impair the effects of the present invention.

The nasal rinse of the present invention can be prepared, for example, as follows. That is, an aqueous phase containing a bactericide (such as benzethonium chloride) is added to an oil phase containing an oil component and a surfactant component, and the mixture is vigorously stirred. ~ 5.
Adjust to 5. At that time, a stable milky white O / W type emulsion can be obtained by preparing with a strong shear force such as a homomixer, manton goulin or an ultrasonic emulsifier.

[0009]

Industrial Applicability According to the present invention, it has become possible to provide a nasal washing agent having a high effect on hay fever and the like.

[0010]

The present invention will be described in more detail with reference to the following Examples and Test Examples. Test Example 1 (Expression test of nasal allergic symptoms by nasal washing) [Preparation of sample] Sample 1: 0.02% by weight of benzethonium chloride, 0.5% by weight of vitamin C, and 1.5% by weight of glycerin were dissolved in purified water. 20% by weight of Panassate 810 (trade name of medium-chain fatty acid triglyceride) and HCO-60 as a surfactant.
(Product name of polyoxyethylene hydrogenated castor oil 60)
A mixture of 2% by weight and 0.5% by weight of resinol S-10 (trade name of hydrogenated soybean lecithin) is stirred and mixed, emulsified, and an appropriate amount of dilute hydrochloric acid as a pH adjuster is used.
H4 and the total amount was 100 g. Sample 2: phosphate buffer (pH 7.8).

[Test Method] Interviews were conducted with 15 allergic rhinitis patients aged 23 to 42 to confirm that they had hay fever. The test period was two weeks. A: 8 people, B;
They were divided into two groups of seven, and for the first week, nasal washing was not performed, and follow-up of symptoms was performed only with nasal drops. Next one
In the week, the group A; the sample 1 and the group B; and the sample 2 were sprayed twice into both nasal passages at the time of getting up in the morning, after lunch, at home and before going to bed. The degree of allergic symptoms for one day was determined by self-report and filled out in a symptom progress report. Oral rhinitis medication was discontinued during the study period. Combined use of commercially available nasal drops was observed as needed for symptoms. At that time, the number of times of nasal use was described on the case card.

[Results] The results are shown in Tables 1 and 2. A
In the group, the symptoms of rhinitis were milder in the second week than in the group B. Also, the number of times of use of nasal drops was slightly reduced.

[0013]

[Table 1]

[0014]

[Table 2]

Example 1 Ingredients Compounding amount (% by weight) Benzethonium chloride 0.02 Panassate 810 30 Resinol S-10 0.5 Glycerin 2 1-Menthol 0.05 Dilute hydrochloric acid Appropriate amount (formulation pH 4.5) Purified water Total 100 g Benzethonium chloride And glycerin were dissolved in purified water, and HCO-60, Resinol S
A solution in which -10 and l-menthol were dissolved was stirred and mixed, emulsified, and diluted hydrochloric acid was used in an appropriate amount to adjust the pH of the preparation to 4 and the total amount to 100 g to prepare a nasal rinse.

Example 2 Ingredients Incorporation amount (% by weight) lidocaine 0.1 benzethonium chloride 0.02 panassate 810 10 HCO-60 0.2 resinol S-10 0.3 glycerin 1.5 hydroxymethylcellulose 0.02 phosphate buffer Liquid 100 g in total (formulation pH 3.5) A nasal rinse was prepared substantially in the same manner as in Example 1.

Example 3 Ingredients Content (% by weight) Cetylpyridinium chloride 0.02 Soybean oil 20 Tween 80 0.2 Resinol S-10 0.5 Glycerin 1.0 Dilute hydrochloric acid Appropriate amount (formulation pH 5.0) Purified water 100 g A nasal rinse was prepared substantially as in Example 1.

Example 4 Ingredients Compounding amount (% by weight) Dipotassium glycyrrhizinate 0.5 Benzethonium chloride 0.02 Panassate 810 10 HCO-60 0.2 Resinol S-10 0.3 Glycerin 1.5 Hydroxymethylcellulose 0.01 Suitable amount of diluted hydrochloric acid (preparation pH 4.0) Purified water 100 g In total, a nasal rinse was prepared substantially in the same manner as in Example 1.

Example 5 Ingredients Compounding amount (% by weight) Benzalkonium chloride 0.02 Panassate 810 30 Presome 0.5 Glycerin 1.5 Phosphate buffer 100 g in total (formulation pH 4.0) Substantially the same as Example 1. A nasal rinse was prepared in the same manner.

────────────────────────────────────────────────── ─── Continuation of front page (72) Fumio Urushizaki 3-24-1, Takada, Toshima-ku, Tokyo Inside Taisho Pharmaceutical Co., Ltd. (56) References JP-A-4-99729 (JP, A) JP-A-5 -70367 (JP, A) (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K 9/00-9/72

Claims (1)

(57) [Claims] 1. A nasal rinse comprising an O / W emulsion having a pH of 3.5 to 5.5 (excluding those containing parathyroid hormones or calcitonins).