JPS6097914A - Enema - Google Patents

Abstract

PURPOSE:An enema having physical and chemical stability, having the same effect as that of glycerin enema, and low side effect such as a stomachache, etc., containing sodium citrate as a main component. CONSTITUTION:An enema containing sodium citrate, preferably trisodium citrate hydrate as a main component. An amount of it blended is preferably 10- 30wt%. An aqueous solution of sodium citrate is found to have the same effect as that of glycerin, and a few clinical demerits glycerin has. Namely, it has no side effect such as a stomachache, and there is sufficient time to open the bowels. The enema is an extremely useful enema which is inexpensive, easily handeable, and has improved long-term safety.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an enema containing citric acid (IJ) as a main component.

Conventionally, enema preparations include glycerin solutions and soap solutions, but in reality most of them are glycerin enema preparations. However, glycerin enemas have a disadvantage in that they are accompanied by side effects such as abdominal pain due to their mechanism of action, which is to stimulate the rectal mucosa with glycerin, thereby inducing peristalsis of the large intestine.

The present inventors conducted various studies with the intention of developing a new enema that eliminates the above-mentioned drawbacks, and as a result, we found that an aqueous sodium citrate solution has an effect equivalent to that of glycerin, and has fewer of the above-mentioned drawbacks. This discovery led to the completion of the present invention.

The present invention will be described in detail below.

Sodium citrate used in the present invention has the general formula Na5C6H,02·nH,, o(n-=o, 2+:L
s), Na2 HC6H507・nH2O (n=0.1
．． 2), NaH2C6H,07・nH2O (n=0.1
), among which trisodium citrate trihydrate is preferably used.

The blending amount of sodium citrate is preferably 5 to 50%.
Furthermore, 10 to 30 inches is desirable.

Although the enema in the present invention is an aqueous solution of sodium citrate, it is of course possible to add various additives to it. For example, preservatives such as benzoic acids, parabens, or sorbic acid, thickening agents such as CMC-Na, hydroxypropylcellulose, carboxyvinyl polymer, and other polymer thickeners, xanthan gum, carrageenan, locust bean gum, and other natural agents. Gummy substances, sugars such as sorbitol and mannitol, propylene glycol,
It is possible to use polyhydric alcohols such as 1.3-butylene glycol and polyethylene glycol.

In some cases, it is also possible to add small amounts of ingredients used in other enema preparations, such as glycerin, to enhance the effect.

In the method for producing an enema according to the present invention, a required amount of sodium citrate is weighed out, and purified water is added to dissolve it to obtain a predetermined concentration.

Test examples will be given below to provide a more specific explanation, but the present invention is not limited by the following test examples.

Test example (Formulation example A) Disodium citrate trihydrate 100f! - Total amount of purified water 1.000m/! Weigh out 10 oz of sodium citrate trihydrate, add purified water to it, stir and dissolve, and then add purified water to make a total volume of 1.000 ml.

(Formulation Example B) Trisodium citrate trihydrate Total amount with 200p purified water 1. OOOmj Citric acid Weigh out 20 of sodium citrate, add purified water to it, stir and dissolve, and then add purified water to make a total amount of 1,000 m#.

(Formulation Example C) Trisodium citrate trihydrate 2001 sorbic acid
500 - Weigh out 200 y of trisodium citrate trihydrate (total volume 1,000 with purified water), add warm purified water (40 to 50°C) and dissolve with stirring, then add 500 ml of sorbic acid. Stir to dissolve and add purified water to bring the total volume to 1. ooomz.

(Formulation Example D) Trisodium citrate trihydrate 400ii1-Sorbic acid 500m9 Total volume with purified water 1.000mJ Weigh out citric acid sodium citrate 4009-, and add hot purified water (40-50°C) to it. After stirring and dissolving, add 500 μl of sorbic acid, stir and dissolve, and add purified water to make a total volume of 1.000 mA.

The clinical efficacy of the sodium citrate enema thus formulated was compared with that of the glycerin enema.

The study was conducted in a double-blind manner. Since the effects of sodium citrate enema were equivalent among Formulation Examples A, B, C, and D, Formulation Example C, that is, 20% sodium citrate enema, was used as the test drug. The control drug was a 50% glycerin enema, and both doses were 6omi. The test subjects were obstetrics and gynecology patients who had constipation for three days or more or required preoperative enema treatment, and pregnant women were excluded.

The results are shown below.

Sodium citrate 7.9 minutes Glycerin 5.7 minutes (side effects) (Usefulness) Looking at the results, we found that sodium citrate was able to defecate comfortably and somewhat comfortably;
For example, in 20 cases of glycerin, the results were 79.2% and 83.3% of the total, respectively, and no difference in effectiveness was observed between the two. In addition, there are two cases of worsening when glycerin is used.
Examples were recognized.

The time required for defecation was 7.9 minutes for sodium citrate and 5.7 minutes for glycerin.

As for side effects, abdominal pain was felt in 2 cases with sodium citrate and 7 cases with glycerin (citric acid).
Umu tended to have fewer cases. No local irritation was observed in either case.

The overall evaluation of usefulness was 79.2 for sodium citrate in 19 cases and glycerin in 20 cases, respectively.
% and 83.3%, and no difference in usefulness was observed between the two.

As mentioned above, the results of the clinical trials show that the sodium citrate enema has the same effect and usefulness as the conventional glycerin enema, and does not pose any problem in actual clinical use. There are several conditions for evaluating the usefulness of enemas, but the most significant problem for patients was abdominal pain, which was seen with conventional glycerin enemas. This issue is particularly important for pregnant women and others who are at risk of threatened miscarriage. As is clear from the present clinical experiment, the sodium citrate enema is sufficient to improve this point. Furthermore, the fact that defecation time is slightly longer is also useful. In other words, when an enema is administered in a hospital, etc., a nurse or an attendant administers the procedure, and the patient then needs some time to go to the toilet, but with glycerin enemas, the urge to defecate occurs too quickly. Improvements in this point were pointed out. It can be said that sodium citrate enema is an improvement in this respect as well.

Furthermore, sodium citrate is cheaper than glycerin, and an aqueous solution of sodium citrate has no viscosity, so it is extremely easy to handle. This is also useful during clinical use.

Additionally, sodium citrate enemas have excellent long-term safety. From the above, the sodium citrate enema overcomes the clinical drawbacks of the conventional glycerin enema 4゛°' and has the same effect.
It is an extremely useful enema agent that is physicochemically stable.

Patent Applicant Sato Pharmaceutical Co., Ltd. Representative Patent Attorney 1) Representative Amended Procedures for Vaporization (Method) % Formula % 1. Indication of the Case Patent Application No. 1982-205858 2. Name of the Invention Enema 3. Person making the amendment Relationship to the case Name of patent applicant: Sato Pharmaceutical Co., Ltd. 4, Agent: 103 Address: Tokyo Tatemono Building, 1-9-9 Yaesu, Chuo-ku, Tokyo (Telephone: 271-8508) Date of amendment order: 1982 January 11th (59 bows, 31 shipments) 6. Statement of the subject of amendment 7. Engraving of the statement of contents of the amendment (no change in content)

Claims (2)

[Claims] (1) An enema characterized by containing sodium citrate as a main component. (2) The enema according to claim (1), wherein the sodium citrate is trisodium citrate trihydrate.