JPH0940561A - Purgative agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a purgative agent which contains magnesium oxide and a binder and a disintegrator which can develop the purgation, and can develop sufficient purgative action with a reduced dose and is readily drinkable. SOLUTION: This purgative agent contains (A) magnesium oxide, (B) a binder which can develop the purgation, for example, carboxymethyl-cellulose, (C) a disintegrator which can develop the purgation such as calcium carboxycellulose, carmellose, when necessary, (D) phenovalin or phenolphthalein as a colorant and (E) a flavor for refreshing the mouth. Preferably, this is preferably prepared in the form of tablets.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a laxative used for elimination of constipation symptoms or intestinal contents,
More specifically, it relates to a laxative which can be taken in a small amount, is easy to drink, and can exert a sufficient laxative effect.

[0002]

2. Description of the Related Art As a purgative, a tablet containing magnesium oxide or magnesium hydroxide as a main ingredient and a binder, a disintegrant and the like is known.

[0003]

In the conventional laxatives of this kind, in order to obtain a sufficient laxative effect, it is necessary to take a large amount of laxatives, so that the size of each grain of laxative is large. However, there was a problem that it was difficult to swallow the laxative. In order to eliminate this point, if the size of the cathartic is reduced to a level that makes it easy to swallow, it is necessary to drink a large number of cathartic, which is not practical.

[0004]

SUMMARY OF THE INVENTION It is therefore an object of the present invention to provide a laxative which can be swallowed in a small amount and can exert a laxative effect sufficiently.

[0005]

The present invention has been proposed to achieve the above object, and is characterized by having the following constitution. That is, according to the present invention, there is provided a cathartic agent comprising magnesium oxide, a binder capable of exerting a cathartic action, and a disintegrating agent capable of exerting a cathartic action. Further, according to the present invention, there is provided a cathartic in which the above-mentioned dosage form is a tablet. Further, according to the present invention, a cathartic agent in which the binder is sodium carboxymethyl cellulose and / or low-substituted hydroxypropyl cellulose (L-HPC) is provided. Further, according to the present invention, there is provided a cathartic agent in which the disintegrant is carboxymethylcellulose calcium and / or carmellose. Further, according to the present invention, there is provided a purgative containing phenovaline and / or phenolphthalein. Further, according to the present invention, there is provided a laxative containing a flavor of an oral cooling agent.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The most technical feature of the present invention is that a binder and a disintegrating agent to be added to magnesium oxide is capable of exerting a cathartic action. This allows the binder and the disintegrant to exert a cathartic action in addition to their respective functions. That is, the cathartic agent of the present invention, in addition to magnesium oxide, also exhibits a cathartic action as a binder and a disintegrant, so that the amount of magnesium oxide as the main drug can be reduced, and therefore, the cathartic required for one dose The amount of the agent can be suppressed. For this reason,
The size of each cathartic can be reduced, making it easier for users to take. Further, in the present invention, magnesium oxide having a larger amount of magnesium per unit weight than magnesium hydroxide is used as a main agent,
Also in this respect, the amount of the main drug, that is, the amount of magnesium oxide can be reduced.

It is speculated that the cathartic action in the present invention is caused by the fact that magnesium oxide reacts with gastric juice (hydrochloric acid) in the intestine to generate magnesium carbonate, thereby retaining water in the intestine. When magnesium oxide reacts with gastric juice, the cathartic agent is disintegrated by the action of the disintegrant, so magnesium oxide and gastric juice react efficiently and in a state where a large reaction amount is ensured. Is increased. Further, as described above, the disintegrating agent and the binder also exert a laxative action, and the laxative as a whole can fully exhibit the laxative action.

[0008] Magnesium oxide in the present invention is soft magnesium oxide, which is obtained by baking at a temperature lower than that of heavy magnesium oxide, has excellent reactivity with gastric acid, and after transfer to the intestine, magnesium carbonate. Next, the cathartic action can be effectively exhibited.

In the present invention, examples of the binder include sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, crystalline cellulose and the like. Among these, sodium carboxymethyl cellulose is
It is officially recognized as a laxative in the Pharmaceutical Affairs Law and is in compliance with the Pharmaceutical Affairs Law. As the binder, those exemplified above may be used alone or in combination of two or more kinds. Further, as the disintegrant, carboxymethylcellulose calcium, carmellose, low-substituted hydroxypropylcellulose and the like can be exemplified. Among them, carmellose is officially recognized as a laxative in the Pharmaceutical Affairs Law, and is consistent with the Pharmaceutical Affairs Law. Is. As the disintegrant, those exemplified above may be used alone or in combination of two or more kinds.

Further, soft magnesium oxide is a main component which is excellent in acid reactivity, and it is preferable to add 50 to 95% by weight, and especially 80 to 95% by weight to one laxative. Further, the binder is preferably contained in 1 to 10% by weight, particularly 1 to 5% by weight in one cathartic, in order to obtain a good tablet which is necessary for good granule molding.
Further, the disintegrating agent is preferably contained in 5 to 20% by weight, and particularly preferably 5 to 10% by weight in one laxative, since magnesium oxide promotes reactivity with stomach acid in the stomach.

The technical features of another aspect of the present invention are as follows.
There is a point that the above purgative is blended with phenovaline or phenolphthalein, or phenovaline and phenolphthalein, whereby the purgative becomes pink and gives the user a favorable impression in the visual aspect. You can Moreover, since phenovaline and phenolphthalein can exert a laxative action as described above, the laxative action of the laxative can be improved.

In the present invention, the blending amount of phenovaline or phenolphthalein, or phenovaline and phenolphthalein is 0. It is preferable to add 0.01 to 1% by weight, particularly 0.01 to 0.05% by weight.

A technical feature of another embodiment of the present invention resides in that the above purgative agent is mixed with a flavor of a mouth-cooling agent, which allows the mouth to be filled with a flavor scent. Can make people feel refreshed.

In the present invention, examples of the mouth refreshing agent to be blended include nintan flavor, peppermint and the like. The flavor of the mouth-cooling agent is preferably 0.01 to 0.1% by weight, and more preferably 0.01 to 0.05% by weight, in one laxative.

[0015]

EFFECTS OF THE INVENTION According to the present invention, it is possible to provide a cathartic agent which is small in amount, easy to drink, and capable of sufficiently exerting cathartic action.

[0016]

EXAMPLES The present invention will be described below based on examples. Example 88% by weight of soft magnesium oxide in a tablet, 1% by weight of sodium carboxymethylcellulose of a fibrin system as a binder and 10% by weight of carboxymethylcellulose calcium as a disintegrant were mixed, and sieved with a wire mesh of 12 mesh. Then, the mixture is mixed again and stirred and granulated by using 100% alcohol as the associative solvent, and dried at 60 ° C. overnight.
After the dry granules were sized to 12 mesh or less, 1% by weight of magnesium stearate as a lubricant was added and mixed well, and then a laxative was prepared with a rotary tableting machine. The obtained tablet has a diameter of 8 mm, a weight of 335 mg, and a hardness of 13 kg.
/ Cm ² . Perform a disintegration test of the obtained laxative,
The results are shown in Table 1. The disintegration test was based on the pharmacopeia test. Further, a dissolution test of magnesium as magnesium oxide in artificial gastric juice was conducted, and the results are shown in Table 2.
This outflow test was carried out by putting artificial gastric juice into a disintegration tester, performing a disintegration test, withdrawing the test liquid at intervals shown in Table 2, and quantifying magnesium oxide. Each value shown in Table 2 is the elution% as magnesium oxide.

Comparative Example 1 A commercially available magnesium hydroxide tablet was subjected to a disintegration test under the same conditions as in Examples, and the results are shown in Table 1. Further, a dissolution test of magnesium as magnesium oxide against artificial gastric juice was performed under the same conditions as in the examples, and the results are shown in Table 2.

Comparative Example 2 Commercially available heavy magnesium oxide tablets were subjected to a disintegration test under the same conditions as in Examples, and the results are shown in Table 1. Further, a dissolution test of magnesium as magnesium oxide against artificial gastric juice was performed under the same conditions as in the examples, and the results are shown in Table 2.

[0019] From the above Table 1, it was revealed that the cathartic agent of the example had a very short disintegration time and was excellent in terms of disintegration. In the Examples, it is considered that one of the factors that the disintegration time is extremely short is that the effect of the disintegrant (carboxymethyl cellulose calcium) is exhibited. In Comparative Example 1 as well, the disintegration time is relatively short, but there is a problem in that the ratio of magnesium oxide to the total weight of the tablet is small and the effect as a laxative cannot be expected unless a large amount is taken.

[0020] From Table 2 above, it became clear that the cathartic agents of the examples had the best acid reactivity. This is because the synergistic effect of blending the soft magnesium oxide and the disintegrating agent is working.

Claims (6)

[Claims] 1. A cathartic agent comprising magnesium oxide, a binder capable of exerting a cathartic action, and a disintegrating agent capable of exerting a cathartic action. 2. The purgative according to claim 1, wherein the dosage form is a tablet. 3. The purgative according to claim 1 or 2, wherein the binder is sodium carboxymethyl cellulose and / or low-substituted hydroxypropyl cellulose (L-HPC). 4. The laxative according to any one of claims 1 to 3, wherein the disintegrant is carboxymethyl cellulose calcium and / or carmellose. 5. The laxative according to any one of claims 1 to 4, wherein phenovaline and / or phenolphthalein is blended. 6. The laxative according to any one of claims 1 to 5, which is blended with a flavor of an oral cooling agent.