JPH11147840A - Sodium sulfate tablet having excellent shape retention - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a tablet being slightly influenced by moisture and wetting with water and having excellent shape retention during storage or in an environment of use, comprising a volatile medicinal effect component, etc. SOLUTION: An organic acid such as fumaric acid, etc., which has <=3% solubility in water at 20 deg.C and is solid at normal temperature or boric acid is formulated with sodium sulfate in the ratio of 3-70 wt.% based on sodium sulfate and molded under pressure.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention carries an evaporative medicinal ingredient and the like, and can maintain its shape for a long period of time without being affected by moisture or temporary wetness during storage and in use environment. It relates to sodium sulfate tablets.

[0002]

2. Description of the Related Art Conventionally, tablets comprising sodium sulfate and an organic acid have been disclosed in JP-A-62-33114 and JP-A-59-33114.
Although these are disclosed in, for example, Japanese Patent No. 50359, they are used by dissolving them in bath water or the like.

[0003]

SUMMARY OF THE INVENTION The present invention relates to a sodium sulfate tablet intended to evaporate a medicinal component into the atmosphere. The present invention relates to a sodium sulfate tablet which does not lose its shape due to moisture or temporary wetness. It is intended to provide.

[0004]

The present inventors have repeatedly studied sodium sulfate tablets having excellent shape retention during storage and use, and as a result, the solubility in water at 20 ° C. was 3%.
% Or less of a compound selected from the group consisting of organic acids and boric acid which are solid at room temperature of not more than 3% by weight of sodium sulfate or sodium sulfate containing a small amount of evaporative medicinal ingredient in an amount of 3 to 70% by weight. It has been found that the compounded and pressed tablet achieves the intended purpose, and the present invention has been completed.

[0005]

DESCRIPTION OF THE PREFERRED EMBODIMENTS In practicing the present invention, anhydrous sodium sulfate should be used, and a small amount of transpirable medicinal component and an organic acid or boric acid which has a solubility in water at 20 ° C. are solid at room temperature. It should be uniformly mixed and pressed. Tablets using organic acids that are solid at room temperature and have a solubility in water at 20 ° C. of more than 3% absorb moisture in the air, reduce their hardness, and disintegrate, so that they maintain long-term efficacy. Can not do it.
Representative organic acids used in the present invention include fumaric acid, adipic acid, azelaic acid, benzoic acid, phthalic acid and the like. These organic acids and boric acid can be used alone or in combination of two or more, and those having a powdery or granular shape are suitable for use.

One or more compounds selected from the group of organic acids and boric acid which are solid at ordinary temperature should be added in an amount of 3 to 70% by weight, preferably 5 to 30% by weight based on sodium sulfate. It is. If the amount of the organic acid or boric acid in the sodium sulfate tablet is less than 3% by weight, the desired bond strength cannot be obtained in the tablet, making it difficult to maintain the shape during storage and use.
If the amount is more than the weight%, it is not preferable in terms of economy.

The molding pressure at the time of tableting of a composition containing sodium sulfate, an organic acid, boric acid, etc. is desirably such that no deficiency occurs during the distribution process of the obtained tablet and the impact received during use, and usually 500 to 500. 1,000kg / c
A surface pressure of m ² should be applied. In the sodium sulfate tablet of the present invention, a coloring agent, a fragrance, and the like can be added in addition to the transpirable medicinal component in the pressure molding, and a small amount of a lubricant is added as necessary to improve the pressure moldability. Can be increased.

Although the reason why the sodium sulfate tablet of the present invention has excellent shape retention is not clear,
Organic acids and boric acids which are solid at room temperature and have a solubility in water of 20 ° C. of 3% or less have hydrophobic properties, which are considered to partially block hydrophilic sodium sulfate.

[0009]

The present invention will be specifically described below with reference to examples and comparative examples. In addition, the hardness measurement method of the tablet in these tests is a method in which a cylinder having a diameter of 5 mm is vertically applied to the center of a tablet placed on a flat plate, and the load applied to the cylinder when the tablet is broken is measured. Example 1 After uniformly mixing 90 parts by weight of anhydrous sodium sulfate and 10 parts by weight of fumaric acid, the surface pressure was 700 kg / c.
By applying a load of m ² , flat tablets with a diameter of 30 mm were obtained.
In order to evaluate the shape retention of the tablet, the product was heated at a temperature of 40.
The package was allowed to stand for 3 weeks without packaging in a room at 75 ° C. and a humidity of 75% RH, and the appearance and shape before and after the test were measured. The results were as shown in Table 1.

Example 2 A tablet was prepared by tableting under the same conditions as in Example 1 except that 10 parts by weight of adipic acid was used instead of fumaric acid, and a tablet was prepared in the same manner as described above. Was carried out, and the results of the test were as shown in Table 1.

Example 3 After uniformly mixing 80 parts by weight of anhydrous sodium sulfate and 20 parts by weight of benzoic acid, the mixture was subjected to tableting under the same conditions as in Example 1 to prepare a tablet, and its shape-retaining property was confirmed. When an evaluation test was performed, the results of the test were as shown in Table 1.

Example 4 Example 1 was obtained by uniformly mixing 80 parts by weight of anhydrous sodium sulfate and 20 parts by weight of boric acid.
A tablet was prepared by tableting under the same conditions as described above, and an evaluation test of the shape retention was performed. The test results were as shown in Table 1.

[0013]

[Table 1]

Comparative Example 1 99.9 Anhydrous sodium sulfate
Parts by weight and lubricant "magnesium stearate" 0.1
After uniformly mixing the parts by weight, tableting was performed under the same conditions as in Example 1 to prepare a tablet, and an evaluation test of shape retention was performed. The results of the test are as shown in Table 2. there were.

[0015]

[Table 2]

Example 5 70 parts by weight of anhydrous sodium sulfate, 20 parts by weight of fumaric acid, and 10 parts by weight of a powder obtained by premixing 5 parts by weight of a medicinal ingredient "pyrethroid insecticide" and 5 parts by weight of calcium silicate were uniformly mixed. After tableting was performed under the same conditions as in Example 1 to prepare a tablet, and an evaluation test of the shape retention was performed. The test results were as shown in Table 3.

Comparative Example 2 90 parts by weight of anhydrous sodium sulfate, 10 parts by weight of a powder obtained by premixing 5 parts by weight of a medicinal ingredient "pyrethroid insecticide" and 5 parts by weight of calcium silicate were uniformly mixed. A tablet was prepared by tableting under the same conditions as in Example 1 and an evaluation test of its shape retention was performed. The test results were as shown in Table 3.

[0018]

[Table 3]

[0019]

The tablet of sodium sulphate containing the solid organic acid and boric acid of the present invention is more effective than the tablet of sodium sulphate alone in powdering and stiffening of the tablet surface due to moisture during storage and use. It has little decrease and has good shape retention over a long period of time, and is recognized as being extremely useful as a carrier for a transpiring medicinal ingredient.

Claims (2)

[Claims] 1. One or two or more compounds selected from the group consisting of organic acids and boric acids which are solid at room temperature and have a solubility in water at 20 ° C. of 3% or less, are dissolved in sodium sulfate in an amount of 3 to 3%.
A sodium sulfate tablet excellent in shape retention characterized by being compounded at a ratio of 70% by weight and molded under pressure. 2. The sodium sulfate tablet according to claim 1, wherein a small amount of a transpiring medicinal ingredient is blended.