JPH0639374B2 - Effervescent glycerin suppository - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to effervescent glycerin suppositories, and more specifically,
It relates to an effervescent glycerin suppository containing carbonate and / or bicarbonate, an acid and glycerin, which is particularly effective for treating constipation.

In recent years, the number of people who have so-called constipation symptoms tends to increase due to changes in eating habits and the effects of a stressful society. Inflammatory constipation, which is the most common type of constipation, is associated with complicated weakness of the motor function of the large intestine and weakness of the abdominal muscles, internal and external anal sphincter muscles, and diaphragm that are involved in the intestinal tract and defecation. It is often found in bedridden people, lack of exercise, and helplessness. In addition to digestive symptoms, people who have constipation symptoms are often socially associated with general symptoms such as dizziness, stiff neck, heavy head, easy sweating of headache, hot flashes, and palpitations.

Currently, the mainstream of constipation medications on the market are called stimulant laxatives, and there are types such as chemical compounds and Chinese herbs, but there are side effects such as abdominal pain and diarrhea due to over-effect, and those with habits. Not a few. Most commonly, glycerin preparations are used.
If you do not use 20 ml, the effect will not be obtained, and you will have to use a special container if you want to stain the underwear by leaking the drug solution from the rectum during use or inject it into the rectum, sometimes around the anus with a container Since there are problems such as causing damage to parts, improvements have been desired. Glycerin suppositories have been developed as one of the solutions, but the fact is that suppositories can be administered only at 1 to 3 g at a time and the effect cannot be sufficiently obtained.

The present inventor, as a result of diligent studies in view of such actual circumstances, by combining carbon dioxide and glycerin that significantly affect the peristalsis of the rectal ampulla and lower part, it is extremely useful for constipation treatment compared to conventional glycerin suppositories. It was found that a suppository having a remarkable effect can be obtained, and the present invention has been completed.

That is, the first invention of the present invention provides an effervescent glycerin suppository containing a carbonate and / or bicarbonate, an acid and glycerin.

Carbonate used in the effervescent glycerin suppository of the present invention and /
Or, as the bicarbonate, for example, sodium hydrogen carbonate, sodium carbonate, sodium sesquicarbonate, potassium carbonate,
Potassium hydrogen carbonate, ammonium carbonate and the like can be mentioned, but sodium hydrogen carbonate and sodium carbonate are particularly preferable.

Examples of the acid include citric acid, tartaric acid, malic acid, malonic acid, pyridonecarboxylic acid, succinic acid, maleic acid, glutamic acid, gluconodeltalactone, gluconic acid, lactic acid, fumaric acid, phosphoric acid, adipic acid, and citric acid. Sodium acid, sodium succinate, potassium hydrooxysuccinic acid, sodium fumarate, sodium phosphate, sodium dihydrogen phosphate, disodium hydrogen phosphate, sulfamic acid, and the like, but especially sodium dihydrogen phosphate. Is preferred. The content of acid is 1 with respect to the weight of the carbonate present in the effervescent glycerin suppository.
0 to 300% by weight, particularly 30 to 150% by weight are preferred.

It is more preferable to use the carbonate and / or bicarbonate and the acid that have been dried in advance.

By the way, the effervescent glycerin suppository of the present invention containing the above-mentioned carbonate and / or bicarbonate, acid and glycerin is excellent in its effect, but as a carbonate and / or bicarbonate and an acid, Even if an anhydride is used, both of them react with each other due to the presence of a slight amount of water to generate carbon dioxide, and therefore there is room for improvement in terms of stability over time.

Therefore, the present inventor has conducted diligent research to improve such stability, resulting in magnesium oxide as a stabilizer,
It was found that an effervescent glycerin suppository having good storage stability over time can be obtained by adding calcium oxide or sodium aluminate, and completed the second invention of the present invention.

That is, the second invention relates to a carbonate and / or a bicarbonate, an acid,
An effervescent glycerin suppository containing glycerin and a substance selected from the group consisting of magnesium oxide, calcium oxide and sodium aluminate.

The total dose of magnesium oxide, calcium oxide or sodium aluminate amounts to 0.5 to 15% by weight, in particular 0.5 to 10% by weight, based on the carbonate and / or bicarbonate and the mixture of acids. It is preferable to mix them as follows. If the blending amount is less than 0.1% by weight, the stabilizing effect is insufficient. The particle size of the stabilizer is not particularly limited, but is preferably 1000 μm or less, and particularly preferably 500 μm or less.

In the product of the present invention, carbonate and / or bicarbonate,
The mixture of the acid and / or the stabilizer is preferably blended in an amount of 20 to 90% by weight, particularly 30 to 80% by weight, based on glycerin.

The effervescent glycerin suppository of the present invention is prepared by thoroughly mixing a carbonate and / or bicarbonate, an acid and / or a stabilizer with concentrated glycerin and filling them into a soft gelatin capsule, or a carbonate and / or bicarbonate. A salt, an acid and / or a stabilizer are mixed well with a mixture of concentrated glycerin and one or more selected from the group consisting of stearic acid, sodium stearate, highly polymerized polyethylene glycol and highly polymerized polypropylene glycol. Then, the suppository mold is used to formulate.

Further, the effervescent glycerin suppository of the present invention may be blended with medicated soap, sodium hydroxide, liquid paraffin, lecithin, surfactant and the like to further enhance the effect.

The effervescent glycerin suppository of the present invention is one that exerts a physiological defecation promoting action by promoting peristaltic movement of the large intestine by the action of carbon dioxide and glycerin, and a gentle natural bowel movement can be obtained. In addition, it has sufficient effects with a small amount of drug compared to conventional products and is easy to use, so not only acute constipation, chronic constipation, postoperative constipation, but also elderly people, beds,
It can also be used by pregnant women.

Next, examples will be described.

Example 1 A suppository having the composition shown in Table 1 was produced.

That is, the ingredients ~ are thoroughly melted and mixed at 45 ° C, and 1g
It was formulated using a suppository template.

About the obtained suppository, when it was inserted into the rectum of a person who had no bowel movement for 3 days, the amount required to obtain bowel movement was examined after about 15 minutes. The results are shown in Table 1.

As is clear from the results in Table 1, the use of 1 g of the suppository of the present invention made it possible to obtain a bowel movement in a person who had no bowel movement for 3 days after about 15 minutes.

Further, when No. 1 suppository was hermetically packaged with a film laminated with aluminum and stored at a temperature of 40 ° C. and a humidity of 75% for 6 months, no abnormality was observed in this packaged product. On the other hand, the NO.4 suppository containing no magnesium oxide, when stored under the same conditions, the packaging container swelled after about two months, and the suppository became unusable.

Example 2 Composition: Concentrated glycerin 100 parts by weight Sodium carbonate 30 Disodium hydrogen phosphate 25 Calcium oxide 1 to 1 were mixed well at 40 ° C., and then filled into 500 mg soft gelatin capsules. When this product was inserted into the rectum of a person who had no bowel movement for 3 days, a bowel movement was obtained after about 10 minutes. Further, when this product was hermetically packaged with a film laminated with aluminum and stored at a temperature of 40 ° C. and a humidity of 75% for 6 months, no abnormality was observed in this packaged product. Use two of this product at a time.

Example 3 Composition: Concentrated glycerin 100 parts by weight Sodium stearate 7.5 Sodium hydroxide 1.3 Sodium hydrogen carbonate 35 Citric acid 30 Sodium aluminate 0.8-Well well mixed at 40 ° C. Used for formulation. When this product was inserted into the rectum of a person who had no bowel movement for 4 days, a bowel movement was obtained after about 10 minutes.

Further, when this product was hermetically packaged in a film laminated with aluminum and stored at a temperature of 40 ° C. and a humidity of 75% for 6 months, no abnormalities were observed in this packaged product.

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Claims (2)

[Claims] 1. An effervescent glycerin suppository containing a carbonate and / or bicarbonate, an acid and glycerin. 2. A foam containing carbonate and / or bicarbonate, an acid, glycerin, and a substance selected from the group consisting of magnesium oxide, calcium oxide and sodium aluminate in an amount that does not exert a laxative effect on its own. Glycerin suppository.