JP2007153833A - Oral administration composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an oral administration composition exhibiting an excellent administration feeling by improving the taste of a composition comprising glucuronolactone and glucuronic acid. <P>SOLUTION: The oral administration composition comprises (A) glucuronolactone and/or glucuronic acid and (B) one or two or more compounds selected from among maltol, ethylmaltol, ethylvanillin, 2,5-dimethyl-4-hydroxy-3(2H)-furanone, 3-hydroxy-4,5-dimethyl-2(5H)-furanone, ethyl 3-methyl-3-phenylglycidate, ethyl phenylglycidate, ethyl p-methyl-β-phenylglycidate, γ-octalactone, γ-nonalactone, γ-decalactone, γ-undecalactone, γ-dodecalactone, δ-octalactone, δ-nonalactone, δ-decalactone, δ-undecalactone, δ-dodecalactone, benzaldehyde, allyl hexylate, allyl cyclohexylpropionate, p-hydroxyphenylbutanone and menthol. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to an oral composition containing glucuronolactone and glucuronic acid.

  Glucuronolactone and glucuronic acid have been used to improve liver function, treat urticaria, eczema, poisoning rash, pregnancy prevention and pregnancy toxemia. In addition, it is a useful drug that is known to be effective as a preventive agent for alcoholic fatty liver caused by a large intake of alcohol or fat. However, since it exhibits an unpleasant taste, it is necessary to suppress this when preparing an oral preparation. In particular, in the case of liquids, gels, granules, chewable tablets, orally disintegrating tablets, where the taste of the preparation greatly affects the ingestion, this is an important solution.

Conventionally, for the problem of unpleasant taste of drugs, a method of masking by adding a large amount of a sweetener such as sucrose has been taken, but in glucuronolactone and glucuronic acid combination agents, it is not necessarily sufficient I can not say. Japanese Patent Application Laid-Open No. 2005-104960 (Patent Publication 1) proposes an internal liquid preparation in which a change in taste is prevented by incorporating glucuronolactone, hydrochloric acid and phosphoric acid, but it is not sufficient.
JP-A-2005-104960

    It is an object of the present invention to provide an oral composition having an excellent feeling of taking by improving the taste of a glucuronolactone or glucuronic acid combination agent exhibiting an unpleasant taste.

As a result of diligent research, the present inventors have found that the above-mentioned problems can be solved by blending a specific compound into an oral composition containing glucuronolactone and / or glucuronic acid. did. That is, the present invention
(1) (A) glucuronolactone and / or glucuronic acid, and (B) maltol, ethyl maltol, ethyl vanillin, 2,5-dimethyl-4-hydroxy-3 (2H) -furanone, 3-hydroxy-4, 5-dimethyl-2 (5H) -furanone, ethyl 3-methyl-3-phenylglycidate, ethyl phenylglycidate, ethyl p-methyl-β-phenylglycidate, γ-octalactone, γ-nonalactone, γ-decalactone, γ-undecalactone, γ-dodecalactone, δ-octalactone, δ-nonalactone, δ-decalactone, δ-undecalactone, δ-dodecalactone, benzaldehyde, allyl hexylate, allyl cyclohexylpropionate, An oral composition containing p-hydroxyphenylbutanone or one or more compounds selected from menthol.

  (2) The above (1) further containing an organic acid such as acetic acid, propionic acid, n-butyric acid, iso-butyric acid, 2-ethylbutyric acid, n-valeric acid, iso-valeric acid, caproic acid, capric acid, etc. Orally.

  (3) Aspartame, acesulfame potassium, achacha extract, licorice extract, saccharin, saccharin sodium, sucralose, stevia extract, neotame, thaumatin, dipotassium glycyrrhizinate, disodium glycyrrhizinate, trisodium glycyrrhizinate, monoammonium glycyrrhizinate aspartame (1) or (2), which contains a high-intensity sweetener such as acesulfame potassium, licorice, licorice, saccharin, sodium saccharin, dipotassium glycyrrhizinate, disodium glycyrrhizinate, trisodium glycyrrhizinate, monoammonium glycyrrhizinate Oral composition.

  (4) Oral composition as described in said (1)-(3) containing high molecular compounds, such as polyvinylpyrrolidone, polyvinyl alcohol, and a cellulose derivative (Hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxymethylcellulose).

  (5) The oral composition according to (1) to (4), which is liquid or gel.

  (6) Maltol, ethyl maltol, ethyl vanillin, 2,5-dimethyl-4-hydroxy-3 (2H) -furanone, 3-hydroxy-4,5-dimethyl-2 (5H) -furanone, 3-methyl-3 -Ethyl phenylglycidate, ethyl phenylglycidate, ethyl p-methyl-β-phenylglycidate, γ-octalactone, γ-nonalactone, γ-decalactone, γ-undecalactone, γ-dodecalactone, δ One or more selected from -octalactone, δ-nonalactone, δ-decalactone, δ-undecalactone, δ-dodecalactone, benzaldehyde, allyl hexylate, allyl cyclohexylpropionate, p-hydroxyphenylbutanone, menthol An unpleasant taste ameliorating agent for glucuronolactone and / or glucuronic acid, comprising the compound:

  By setting it as the said structure, the composition for oral administration in which the unpleasant taste peculiar to glucuronolactone and glucuronic acid was suppressed can be obtained.

    Hereinafter, the present invention will be described in detail.

    The oral composition of the present invention contains (A) glucuronolactone and / or glucuronic acid. Glucuronic acid may be an acid, a salt, or a mixture thereof. Examples of the salt include sodium salt and potassium salt. Preferably, when glucuronolactone / glucuronic acid (salt) = 1/99 to 99/1, particularly 10/90 to 50/50, the specific compound (B) described below has an unpleasant taste suppressing effect. Especially good.

    The content of glucuronolactone and / or glucuronic acid in the preparation is preferably 0.1 to 6.0 w / v% (g / 100 ml, hereinafter the same), and preferably 0.2 to 5.0 w / v%. Is particularly preferred.

    The specific compound (B) that suppresses the unpleasant taste of the component (A) in the oral composition of the present invention is maltol, ethyl maltol, ethyl vanillin, 2,5-dimethyl-4-hydroxy-3 (2H)- Furanone, 3-hydroxy-4,5-dimethyl-2 (5H) -furanone, ethyl 3-methyl-3-phenylglycidate, ethyl phenylglycidate, ethyl p-methyl-β-phenylglycidate, γ -Octalactone, γ-nonalactone, γ-decalactone, γ-undecalactone, γ-dodecalactone, δ-octalactone, δ-nonalactone, δ-decalactone, δ-undecalactone, δ-dodecalactone, benzaldehyde, hexyl It is a compound selected from allyl acid, allyl cyclohexylpropionate, p-hydroxyphenylbutanone, and menthol. These may be used alone or in combination of two or more. The content of the component (B) in the preparation is preferably 0.000001 to 1 w / v%, particularly preferably 0.000001 to 0.1 w / v%.

    When the glucuronolactone and / or glucuronic acid-containing oral composition of the present invention contains a sweetener, an organic acid, a polymer compound, and a polyhydric alcohol in addition to the component (B), the drug discomfort is further reduced. This is preferable because the taste is suppressed.

    Sweeteners include sucrose, liquid sugar, fructose, fructose glucose liquid, reduced maltose water candy, brown sugar, high fructose liquid sugar, glucose, powdered reduced maltose water candy, water candy, high glucose water candy, lactose, sucrose, Sugars such as purified sucrose, purified sucrose spherical granules, honey, purified honey, simple syrup; sugar alcohols such as erythritol, xylitol, D-sorbitol, D-sorbitol, maltitol, maltitol, maltose, D-mannitol, Aspartame, acesulfame potassium, amacha extract, licorice extract, saccharin, sodium saccharin, sucralose, stevia extract, neotame, thaumatin, dipotassium glycyrrhizinate, disodium glycyrrhizinate, trisodium glycyrrhizinate, monoammonium glycyrrhizinate aspartate High sweetness sweeteners that are at least 10 times the sweetness of sucrose, such as mussole, acesulfame potassium, licorice, saccharin, sodium saccharin, dipotassium glycyrrhizinate, disodium glycyrrhizinate, trisodium glycyrrhizinate, monoammonium glycyrrhizinate . These may be used alone or in combination of two or more. When at least one kind of high-intensity sweetener is used in the early sweetener, a particularly excellent unpleasant taste suppressing effect can be obtained. Sugar alcohols (particularly erythritol and xylitol) are also preferably used as the sweetener of the present invention.

    The content of the sweetening agent is preferably 1.0 to 75.0 w / v% for sugar / sugar alcohol, particularly 1.0 to 50.0 w / v%, and 0.001 to 7 for high-intensity sweetening agent. 0 w / v%, in particular 0.01 to 5.0 w / v%.

    As the organic acid, it is preferable to use a monovalent to divalent organic acid and / or an organic acid salt having 1 to 6 carbon atoms. Among them, in particular, one selected from acetic acid, propionic acid, n-butyric acid, iso-butyric acid, 2-ethylbutyric acid, n-valeric acid, iso-valeric acid, caproic acid, capric acid and / or a salt thereof, or It is preferable to contain two or more of 0.000001 to 0.1 w / v%, particularly 0.00001 to 0.01 w / v%. In addition to the preferred organic acids, it may further contain malic acid, citric acid, and / or their salts.

    The polymer compound is preferably a water-soluble polymer, and examples thereof include polyvinyl pyrrolidone, polyvinyl alcohol, and cellulose derivatives (water-soluble cellulose derivatives such as hydroxypropylcellulose, hydroxypropylmethylcellulose, and hydroxymethylcellulose).

    The content of the polymer compound in the preparation is preferably 0.01 to 3.0 w / v%, particularly 0.05 to 1.0 w / v%.

    Examples of the polyhydric alcohol include glycerin, propylene glycol, and polyethylene glycol. The content of the polyhydric alcohol in the preparation is preferably 0.0001 to 5.0 w / v%, particularly 0.001 to 3.0 w / v%.

    The oral composition of the present invention can be used for liquid preparations such as solutions, suspensions and emulsions, gel preparations, granular preparations such as powders and granules, solid preparations such as chewable tablets and orally disintegrating tablets. However, liquid preparations and gel preparations are preferable because the effects of the present invention are remarkable.

    The oral composition of the present invention can contain various physiologically active ingredients in addition to the above-mentioned components as long as the effects of the present invention are not impaired. Examples of physiologically active ingredients include thiamine nitrate (vitamin B1), riboflavin sodium phosphate (vitamin B2), pyridoxine hydrochloride (vitamin B6), biotin (vitamin H), nicotinamide, cyanocobalamin (vitamin B12), ascorbic acid (vitamin C), water-soluble vitamins such as pantothenic acid and carnitine chloride; fat-soluble vitamins such as retinol (vitamin A) and tocopherol (vitamin E); herbal medicines such as tokuinin, toki, licorice; other, royal jelly, caffeine, chondroitin sulfate Sodium, iron and the like are preferable.

    Moreover, an appropriate additive component can be used for each preparation. Examples of the additive component include a pH adjusting agent (preferably pH: 1.5-6, particularly preferable pH: 2-4), an antiseptic, a solubilizing agent, a viscosity adjusting agent, a colorant, and a fragrance.

  The liquid for internal use according to the present invention can be adjusted by a conventional method, and the method is not particularly limited, but usually, each component is mixed with purified water of a specified amount or less, the volume is adjusted to a specified amount, and if necessary. Obtained by filtration and sterilization. When fat-soluble vitamins are included, they may be emulsified or solubilized with commonly used surfactants or solubilizers, or suspended using a dispersant.

  EXAMPLES Hereinafter, although an Example and a comparative example are given and this invention is demonstrated further more concretely, this invention is not limited to the following Example at all.

(Examples 1-22, Comparative Examples 1-2)
The liquid composition for internal use which mix | blended each component shown in Tables 1-3 was prepared by the conventional method. The unpleasant taste suppression effect is evaluated by 10 panelists who conduct sensory tests and evaluate the unpleasant taste and odorlessness and good drinking quality based on the following evaluation criteria, based on a 5-point score of 1 to 5 points. did. Each result is shown to Tables 2-4.
Evaluation criteria for the absence of unpleasant taste and odor and good drinking comfort: 5 points with no unpleasant taste and smell: 4 points: Almost unpleasant taste and smell: 3 points with good drinking comfort: Slightly unpleasant taste and smell, a little difficult to drink 2 points: Unpleasant taste and smell, difficult to drink 1 point: Very uncomfortable taste and smell, very difficult to drink

Claims (6)

(A) Glucuronolactone and / or glucuronic acid (B) maltol, ethyl maltol, ethyl vanillin, 2,5-dimethyl-4-hydroxy-3 (2H) -furanone, 3-hydroxy-4,5-dimethyl-2 (5H) -furanone, ethyl 3-methyl-3-phenylglycidate, ethyl phenylglycidate, ethyl p-methyl-β-phenylglycidate, γ-octalactone, γ-nonalactone, γ-decalactone, γ -Undecalactone, γ-dodecalactone, δ-octalactone, δ-nonalactone, δ-decalactone, δ-undecalactone, δ-dodecalactone, benzaldehyde, allyl hexylate, allyl cyclohexylpropionate, p-hydroxyphenylbutanone An oral composition comprising one or more compounds selected from menthol. 2. The oral composition according to claim 1, further comprising an organic acid. The oral composition according to claim 1 or 2, further comprising a high-intensity sweetener. Furthermore, the composition for oral administration of Claims 1-3 containing a high molecular compound. The composition for oral administration of Claims 1-4 which is a liquid agent or a gel agent. Maltol, ethyl maltol, ethyl vanillin, 2,5-dimethyl-4-hydroxy-3 (2H) -furanone, 3-hydroxy-4,5-dimethyl-2 (5H) -furanone, 3-methyl-3-phenylglycan Ethyl sidate, ethyl phenylglycidate, ethyl p-methyl-β-phenylglycidate, γ-octalactone, γ-nonalactone, γ-decalactone, γ-undecalactone, γ-dodecalactone, δ-octalactone , Δ-nonalactone, δ-decalactone, δ-undecalactone, δ-dodecalactone, benzaldehyde, allyl hexylate, allyl cyclohexylpropionate, p-hydroxyphenylbutanone, or menthol. An unpleasant taste improving agent for glucuronolactone and / or glucuronic acid, characterized by containing.