JP2003342186A - Oral liquid composition for rhinitis - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain an oral liquid formulation for allergic rhinitis easily taken and sufficiently stable by solving problems that Schizonepeta herb which is a crude drug conventionally used as a solid formulation gives precipitation when added to the liquid formulation in an effective amount, therefore, it is difficult to provide as a commercial product, and a liquid formulation mixed with a crude drug, Magnoliae Flos, in an effective amount is difficult to provide as a commercial product caused by its inherited unpleasant taste. <P>SOLUTION: The oral liquid formulation composition contains 0.08-1.7 W/V% Magnoliae Flos and 0.08-2.5 W/V% Schizonepeta herb based on the raw crude drug. <P>COPYRIGHT: (C)2004,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a composition effective for improving allergic diseases, particularly nasal inflammation.

[0002]

2. Description of the Related Art In recent years, the number of patients with allergic diseases such as hay fever continues to increase. Symptoms of these allergic diseases include sneezing, nasal discharge, stuffy nose, itching / congestion of eyes, and common eyes. Among these symptoms, the nasal inflammation not only causes great discomfort to the patient, but also interferes with nasal breathing, and oral breathing is likely to occur to compensate for it. Recently, it has been said that such mouth breathing easily causes various diseases such as a cold syndrome, and thus it is very important to suppress the nasal inflammation. Conventionally,
As internal medicines for improving such nasal inflammation, antihistamines, vasoconstrictors, parasympathetic nerve inhibitors, anti-inflammatory agents and the like are generally used. In addition, as herbal medicine ingredients, kayigae (sagebrush), shinyi (spicy sauce), saishin,
Showkyo and the like are known.

These components are usually taken as oral preparations, but most of them are solid preparations such as tablets and powders.

In recent years, allergic diseases have become younger, and allergic rhinitis has been affected by children and infants. However, since patients such as children, infants, or the elderly have poor swallowing ability, it is difficult to take solid agents such as tablets, which are commonly used as internal medicines.

On the other hand, although a method of directly administering a drug to the affected area of rhinitis by a nasal drop and a method of washing away allergens of the nasal mucosa with a nasal irrigant are temporarily effective, but the effect is insufficient in sustainability. It was difficult to use because it had to be used for.

[0006]

DISCLOSURE OF THE INVENTION The present inventors have conducted studies for the purpose of providing a therapeutic agent for allergic diseases, which is an oral solution that is easy to take even by patients with poor swallowing ability. Conventionally,
It has been found that it is difficult to provide the crude cabbage, which has been used as a solid formulation, as a commercial product because precipitation may occur when mixed in an effective amount in a liquid formulation. In addition, the liquid formulation containing an effective amount of herbal medicine Shini, due to its unique unpleasant taste,
After all, it turned out that it was difficult to provide it as a product.

An object of the present invention is to provide an oral solution for allergic rhinitis which is easy to drink and has sufficient stability.

[0008]

Means for Solving the Problems As a result of investigations for achieving the object, the present inventors have found that co-blending kaigai and shinny as the active ingredients at a specific concentration has a sufficient effect on nasal inflammation. The present invention has been completed based on the finding that a liquid preparation having no problem in terms of flavor and stability of the preparation can be obtained.

That is, the present invention is 0.08 in terms of the amount of the original drug.
It is a liquid composition for rhinitis which is characterized by containing ~ 1.7 W / V% of Shinyi and 0.08-2.5 W / V% of keikai.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION Shinyi used in the present invention refers to buds of Astragalus membranaceus, Kobushi or closely related plants thereof, and the concentration of the compound is 0.08 to 1.7 in terms of the amount of the active drug substance.
It is W / V%. If it is less than 0.08W / V%, the dose will be too large to fully develop the drug effect, and 1.7W / V%
This is because an unpleasant flavor will be produced if the content is exceeded.

The pearl oyster of the present invention refers to the ear of pearl oyster, and the compounding concentration thereof is 0.08-
It is 2.5 W / V%. If it is less than 0.08 W / V%, the dose will be increased in order to fully exhibit the drug effect, and 2.
This is because if the content exceeds 5 W / V%, precipitation may occur in the preparation.

The dose of the galenical component of the present invention varies depending on age, sex, and body weight. Usually, the daily dose for adults is 0.3 to 3.0 g in terms of the crude drug equivalent for Shini, and Kaigai for Kaigai. It is 0.3 to 3.0 g in terms of the amount of the original drug.

Any of the galenical ingredients used in the present invention can be used in the form of dry powder, extract or the like. Here, as the extract, a dry extract, a soft extract, a stream extract or the like can be used.

The liquid composition of the present invention is preferably further blended with chlorpheniramine maleate from the viewpoint of improving the nasal inflammation.

The liquid composition of the present invention has a pH of 3.5 to 5.0.
Is preferred. This is because if it is less than 3.5, precipitation tends to occur in the preparation, and if it exceeds 5.0, the antiseptic property becomes low and it becomes difficult to maintain the quality.

When the liquid composition of the present invention is provided as a product, it is necessary to add a preservative in order to maintain its quality. However, in the present invention in which a galenical component is blended, it is easy to putrefaction, so that selection of a preservative becomes important. Therefore, as a result of investigations by the present inventors, benzoic acid and para-oxybenzoic acid ester were simultaneously mixed as a preservative, the total amount thereof was 0.06 W / V% or more of the entire preparation, and the content of para-oxybenzoic acid ester was 0. It was also found that when it is 0.01 W / V% or more, it has excellent antiseptic properties.

Here, a salt or the like can be used as the benzoic acid. The paraoxybenzoic acid ester is preferably ethyl paraoxybenzoate, propyl paraoxybenzoate or butyl paraoxybenzoate, and particularly preferably ethyl paraoxybenzoate.

In the liquid composition for rhinitis of the present invention, it is preferable to add a strawberry type flavor to further improve the flavor.

The liquid composition for rhinitis of the present invention comprises a compounding agent usually used for pharmaceutical liquids, for example, a stabilizer, an emulsifier, other medicinal ingredients, vitamins, etc., if necessary, to prepare a liquid agent. It can be manufactured.

[0020]

INDUSTRIAL APPLICABILITY The present invention has made it possible to provide a liquid formulation for rhinitis which has a good flavor and stability of the preparation and has an excellent effect.

[0021]

The present invention will be described in more detail with reference to Examples and Test Examples. Example 1 A liquid formulation for rhinitis was produced by a conventional method with the following formulation. d-Chlorpheniramine maleate 0.0067w / v% Kaigai Extract (raw drug equivalent) 0.42w / v% Shinyi Extract (raw drug equivalent) 0.42w / v% Sucrose 36.67w / v% D-sorbitol liquid (70%) 6.67 w / v% Benzoic acid 0.060w / v% Ethyl paraoxybenzoate 0.012w / v% Ethanol 1.2v / v% Lactic acid Appropriate amount (pH3.5) Caramel 0.02w / v% Strawberry flavor Micro-purified water Appropriate amount

Example 2 A liquid formulation for rhinitis was produced by a conventional method with the following formulation. d-Chlorpheniramine maleate 0.0067w / v% Kaigai Extract (raw drug equivalent) 1.67w / v% Shinyi Extract (raw drug equivalent) 1.67w / v% Sucrose 36.67w / v% D-sorbitol solution (70%) 6.67w / v% Benzoic acid 0.083w / v% Sodium benzoate 0.042w / v% Ethyl paraoxybenzoate 0.02w / v% Ethanol 1.2v / v% Lactic acid suitable amount (pH 3.9) Caramel 0.02w / v% Strawberry flavor Purified water Suitable amount

Test Example 1 Liquid formulations prepared by adjusting the formulation shown in the table below to pH 4.5 with a pH adjusting agent (lactic acid, sodium citrate: appropriate amount), at a temperature of 5 ° C., room temperature and 50 ° C. Was stored for 8 weeks, and the generation of precipitate was visually determined (-: no precipitation, ±: slightly precipitate expression, +: precipitate expression).

The results are shown in Table 1. In the table, “actual” indicates an example and “ratio” indicates a comparative example. The unit of numbers is w / v% unless otherwise specified.

[0025]

[Table 1] As is clear from the table, it was found that precipitates were generated when the content was outside the range of the present invention.

Test Example 2 The flavor of a liquid preparation prepared by adjusting the pH shown in the following table to pH 4.5 with a pH adjusting agent (lactic acid, sodium citrate: appropriate amount) was tested. The flavor test was quantified by 5 points out of 3 panelists (5: very delicious, 4: slightly delicious, 3: normal, 2: poor, 1: bad) and the average score is shown in the table.

[0027]

[Table 2] As is clear from the table, it was found that the flavor was insufficient when the amount of the cabbage was out of the range of the present invention.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 47/14 A61K 47/14 A61P 11/02 A61P 11/02 37/08 37/08 (72) Inventor Mitsuru Shimizu 119 Uenoda, Hino-cho, Gamo-gun, Shiga Prefecture F-term (reference) inside Hino Pharmaceutical Co., Ltd. AC03 MA07 MA08 MA16 MA52 NA03 NA09 NA10 ZA34 ZB13

Claims (5)

[Claims] 1. An orally administered liquid composition for rhinitis, which comprises 0.08 to 1.7 W / V% of Shiny ingredient and 0.08 to 2.5 W / V% of keikai in terms of a crude drug. 2. The oral solution composition for rhinitis according to claim 1, further comprising chlorpheniramine maleate. 3. The oral solution composition for rhinitis according to claim 1, which has a pH in the range of 3.5 to 5.0. 4. A benzoic acid and a paraoxybenzoic acid ester are simultaneously mixed as a preservative, and the total amount thereof is 0.06 W / V% or more of the whole preparation, and the paraoxybenzoic acid ester is 0.01 W / V%. The above is the oral liquid composition for rhinitis according to claim 1. 5. The liquid composition for rhinitis according to claim 1, which contains a strawberry flavor.