JPH11269073A - Preparations containing copper chlorophyllin salts - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a preparation preventing staining of e.g. the oral cavity, tongue and easy to be administered by including a salt of copper chlorophylline and acid(s). SOLUTION: This preparation contains (A) a salt of copper chlorophylline, preferably potassium copper chlorophylline or sodium copper chlorophylline and (B) 0.1-10 pt(s).wt., per pt.wt. of the ingredient A, of acid(s), preferably, at least one acid selected from ascorbic acid, tartaric acid, citric acid, malic acid and the like. Furthermore, medicinal ingredient(s), e.g. antidiarrheal drug(s), drug(s) for controlling intestinal function, antiulcer drug(s) may be compounded in this preparation. It is preferable this preparation is used in the form of solid, particularly, e.g. chewable form, troche form.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a preparation containing a salt of copper chlorophyllin and an acid. More specifically, the present invention relates to a preparation containing a salt and an acid of copper chlorophyllin which does not cause coloring in the oral cavity even when taken.

[0002]

2. Description of the Related Art Chlorophyll, which is naturally present as chlorophyll in plants and the like, is a porphyrin-based pigment having one magnesium atom in the molecule and is known to have a unique dark green color. Chlorophyll is a fat-soluble substance, but can be converted to water-soluble chlorophyllin by hydrolysis with an alkali. Copper chlorophyllin is a compound obtained by replacing a magnesium atom in the molecule of chlorophyllin with a copper atom. Chlorophylline is effective as a medicine for preventing bad breath and treating wounds, and has been blended in many products. Also,
It is also known to be useful as a prophylactic / therapeutic agent for gastric ulcer, duodenal ulcer and gastritis based on mucosal protection, and is a very familiar pharmaceutical ingredient. For this reason, it is usually compounded in the form of a salt, such as potassium copper chlorophyllin, to give a dosage form that can be taken easily and easily, such as powders, granules and tablets.

[0003]

However, on the other hand, salts of copper chlorophyllin such as potassium copper chlorophyllin are substances showing a dark green color. There is a problem that the oral cavity and even the tongue are colored dark green. Since such coloring is so strong that it remains on the tongue and the like for a whole day, the dosing method has been limited to tablets and the like that do not dissolve in the oral cavity. However, in view of diversification of consumer needs and the like, a dosage form such as a chewable tablet in which a tablet or the like containing a salt of copper chlorophyllin is dissolved and taken in the mouth has been desired. An object of the present invention is to provide a preparation containing a salt of copper chlorophyllin, which prevents such coloring and is excellent in taking feeling.

[0004]

Means for Solving the Problems The present inventors have conducted intensive studies in view of the above circumstances, and as a result, it has been found that a preparation obtained by adding an acid generally used to a salt of copper chlorophyllin can be dissolved in the mouth even if dissolved in the mouth. The present inventors have found that the coloring of the oral cavity and tongue by the salt of the present invention is greatly reduced, and have completed the present invention.

That is, the present invention relates to a preparation containing a salt of a copper chlorophyllin and an acid. The present invention also relates to a method for preventing coloring in the oral cavity by a salt of copper chlorophyllin by adding an acid.

[0006] The salt of copper chlorophyllin in the present invention means that the carboxyl group of copper chlorophyllin forms a salt. Such salts specifically include, for example, salts with alkali metals such as potassium salt and sodium salt; salts with amines such as trimethylamine salt, triethylamine salt, procaine salt, pyridine salt and phenethylbenzylamine salt; hydrochloride, odor Salts with inorganic acids such as hydrochloride, hydroiodide, sulfate, nitrate, perchlorate, phosphate, carbonate, bicarbonate; alginate, aspartate, glutamate, And the like, preferably a salt with an alkali metal such as a potassium salt or a sodium salt; a salt with an amino acid such as alginate, aspartate, or glutamate, and more preferably potassium. Salts with alkali metals such as salts and sodium salts.

The acid in the present invention means any acid that can be compounded as a pharmaceutical excipient, and specifically, for example,
Inorganic acids such as hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, nitric acid, phosphoric acid, carbonic acid, bicarbonate; organic carboxylic acids such as acetic acid, malic acid, citric acid, maleic acid, tartaric acid, fumaric acid, ascorbic acid Acids; organic sulfonic acids such as methanesulfonic acid, trifluoromethanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, and toluenesulfonic acid;
Amino acids such as arginic acid, aspartic acid, glutamic acid and the like.

In the present invention, the weight ratio of the salt of copper chlorophyllin to the acid is usually 0.01 to 1 part by weight of the acid having the same meaning as defined above with respect to 1 part by weight of the salt of copper chlorophyllin. The acid having the same meaning as defined above is used in an amount of 0.05 to 1 part by weight, more preferably 0.05 to 0.75 part by weight, and even more preferably 0.1 to 0.3 part by weight, per part by weight of the salt.

Further, the preparation according to the present invention can be produced by mixing other medicinal ingredients with copper chlorophyllin salt. The other medicinal components are not particularly limited, and specifically include, for example, an antidepressant, an intestinal suppressant, an anti-ulcer agent, a stomachic digestive agent, an antacid, an antihistamine, an anxiolytic, an antiepileptic, an antipyretic analgesic and antiinflammatory, diuresis. Agents, antihypertensive agents, vasodilators, agents for hyperlipidemia, bronchodilators, vitamins, crude drugs, antibiotics, antiviral agents and the like.

The preparations according to the present invention are not particularly limited, such as solid preparations such as powders, granules, fine granules, pills and tablets; liquid preparations such as syrups and injections. Can be applied. Among them, a preferred dosage form is a solid preparation,
It is particularly suitable for preparations such as chewable tablets and lozenges which are chewed or dissolved in the mouth and taken.

For the preparation of these preparations, various additives commonly used can be blended. Examples of such additives include, in the case of solid preparations, excipients, binders, lubricants, coloring agents, flavoring agents, and the like.If necessary, absorption enhancers, surfactants, antioxidants, etc. Can also be used. In addition, as an additive that can be blended in the case of a liquid,
For example, surfactants, emulsifiers, suspending agents, preservatives, stabilizers, absorption enhancers, solubilizers, pH adjusters, preservatives,
And antioxidants.

The preparation according to the present invention can be produced by a usual preparation method in any case such as a solid preparation and a liquid preparation. For example, in the case of a solid preparation, a salt and an acid of copper chlorophyllin are added and mixed with an excipient such as lactose and mannitol as needed, and polyvinylpyrrolidone,
A binder such as hydroxypropylcellulose is added, and the mixture can be granulated by extrusion granulation, fluidized-bed granulation or spray-drying granulation and dried to obtain granules, which are then chewable by a usual method. Tablets and the like can also be used.

[0013]

The present invention will be described in more detail with reference to examples and test examples below, but it goes without saying that the present invention is not limited to these examples.

Example 1 Granules containing potassium copper chlorophyllin and citric acid
Agent magnesium hydroxide 60 g, precipitated calcium carbonate 110g, calcium hydrogen phosphate anhydrous 120 g, copper chlorophyllin potassium 9 g, purified sucrose 21g, lactose 121.2 g, aspartame 1g,
10 g of magnesium stearate and 9 g of anhydrous citric acid were stirred and mixed to obtain a powdery solid preparation. After drying such a powdered solid preparation, 0.8 g of 1-menthol is added, and the mixture is stirred and mixed.
462 g were obtained.

Example 2 A tube containing potassium copper chlorophyllin and citric acid
Able tablets 60 g magnesium hydroxide, precipitated calcium carbonate 110 g, anhydrous calcium hydrogen phosphate 120 g, copper chlorophyllin potassium 9 g, purified sucrose 21 g, lactose 121.2 g, aspartame 1 g,
9 g of citric anhydride was stirred and mixed to obtain a powdery solid preparation. After drying such a powdered solid preparation, magnesium stearate
10 g and 1 g of 1-menthol were added and mixed by stirring, and a chewable tablet was obtained by tableting.

Control Example A chewable tablet was produced in the same manner as in Example 2 except that citric anhydride was omitted from the formulation described in Example 2, and this was used as a control.

[0017]

[Test Example] Twenty test subjects dissolved one tablet obtained in each of the above Example 2 and the control example without chewing in the oral cavity on an empty stomach. The degree of coloring of the tongue was observed. Table 1 shows the results.

[0018]

[Table 1]

[0019]

Industrial Applicability The present invention is a preparation containing a salt of copper chlorophyllin and an acid. In particular, it effectively discolors the tongue and the oral cavity by the salt of copper chlorophyllin after dissolving in the oral cavity. It is excellent in that it can be prevented.

From the above effects, according to the present invention, it is possible to provide a preparation containing a salt of copper chlorophyllin, which can be easily taken at any time without regard to coloring.

Continued on the front page (51) Int.Cl. ⁶ Identification code FI A61K 47/12 A61K 47/12 Z

Claims (7)

[Claims] 1. A preparation comprising a salt of a copper chlorophyllin and an acid. 2. A solid preparation comprising a salt of copper chlorophyllin and an acid. 3. The preparation according to claim 1, wherein the salt of copper chlorophyllin is potassium copper chlorophyllin or sodium copper chlorophyllin. 4. The preparation according to any one of claims 1 to 3, wherein the acid is at least one acid selected from ascorbic acid, tartaric acid, citric acid, malic acid, hydrochloric acid and phosphoric acid. 5. The preparation according to claim 1, comprising 0.1 to 10 parts by weight of an acid per 1 part by weight of the salt of copper chlorophyllin. 6. A chewable tablet comprising a copper chlorophyllin salt and an acid. 7. A method for preventing tongue coloring by a salt of copper chlorophyllin by adding an acid.