JPH03284620A - Composition for cleaning intestine - Google Patents

Abstract

PURPOSE:To obtain the title composition exhibiting excellently cleaning effects, having ready administration, not fermenting with bacteria in the intestine, not having a bad influence on diagnosis, comprising erythritol and/or xylitol and a specific electrolyte in a specific ratio. CONSTITUTION:A composition which comprises erythritol and/or xylitol and an electrolyte selected from the group consisting of sodium sulfate, potassium chloride, sodium chloride and sodium hydrogen carbonate in a composition shown by the table, especially, based on 1l composition, 8-30g erythritol and/or xylitol, 40-135mEq Na<+>, 7-13mEq K<+>, 24-46mEq Cl<->, 14-26mEq HCO and 0-85mEq SiO and becomes the above-mentioned composition in a solution state or in dissolution. The composition is suitable for treatment of constipation and pretreatment for roentgenologic examination of enema, endoscopy of intestinum crassum or operation of intestinum crassum.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention is a composition for intestinal cleansing, specifically used for treatment of constipation, enema X-ray examination, colonoscopy, pretreatment for colon surgery, etc. The present invention relates to a composition for intestinal cleansing.

Conventional techniques and their problems Conventionally, pretreatments for enema X-ray examinations, colonoscopies, colonic surgeries, etc. have mainly been based on the Brownj method, i.e., low-residue, low-fat dietary restriction, salt laxatives, and contact laxatives. Either administering laxatives or using the so-called dry method without enema.
However, the Brown method is difficult to swallow and causes sudden diarrhea, making it difficult for the elderly and infirm to tolerate. Therefore, it had serious drawbacks, such as not being accepted in patients with heart failure or renal impairment, and radiologically it was difficult to clean the hemicolon, and residues tended to remain. .

Recently, in place of the above-mentioned Brown method, research and development has been carried out on a non-absorbable, non-secretory intestinal cleansing agent containing polyethylene glycol as the main component and electrolytes added thereto.This is already commercially available in the United States (product name :Golyley, Colyte
) has been done. Research is also being conducted to improve the above-mentioned commercially available products [see Japanese Patent Publication No. 500523/1983] (
Hereinafter, these products will be referred to as rPEG-ELSJ). Since these detergents are non-absorbable and non-secretory, they have the advantage that they can be administered to patients with heart failure, renal failure, and the like. However, the cleaning effect of the PEG-ELS is only approximately the same as that of the purgative used in the Brown method, and is still not fully satisfactory. Moreover, PEG
-ELS has the disadvantage that bubbles generated during administration can cause misdiagnosis, and there are also problems with taste, odor, etc. Also, polyethylene glycol has low solubility, so it is difficult to dissolve a certain amount to have a certain effect. This requires a large amount of water, which makes it difficult to take.Additionally, polyethylene glycol may cause side effects such as inflammation in the intestinal mucosa and anus in some patients.

The present inventors have conducted extensive research with the aim of researching and developing a new intestinal cleansing agent that eliminates and corrects the various drawbacks found in the above-mentioned PEG-ELS, is easier to apply, and has excellent cleaning effects. . In the process, erythritol and/or
Or, surprisingly, a composition containing xylitol as the main ingredient and a predetermined amount of a specific electrolyte component exhibits an excellent cleaning effect and is superior to conventional cleaning products in terms of taste, odor, etc. We found that it is superior to drugs, does not produce bubbles or disappears quickly if bubbles do occur, does not ferment with intestinal bacteria like mannitol, and has no adverse effect on diagnosis at all. The present invention has now been completed.

Means for Solving the Problems, That is, the present invention provides a composition for intestinal cleansing which is in liquid form and contains components in the following composition range, and the above-mentioned composition which is in the form of a ready-to-use dissolving agent which, when dissolved, has components in the following composition range. The present invention relates to the intestinal cleansing composition described above, which uses an electrolyte selected from the group consisting of sodium sulfate, potassium chloride, sodium chloride, and sodium hydrogen carbonate.

Na+35-150 mEq/A' +5-20 mEq/A'CA'-20-50mEq/A' HCO3-0-30 mEq/A'SO4'
0 to 100 mEq/10 The composition for intestinal cleansing of the present invention exhibits an excellent cleansing effect based on having the above-mentioned specific composition, is easy to take in terms of taste, odor, etc., and does not generate bubbles. It has the excellent feature that it either does not exist or disappears quickly even if it occurs, and is hardly fermented by intestinal bacteria, so it has no adverse effect on diagnosis at all.

Erythritol used in the present invention is a type of tetrose alcohol that has about 80% of the sweetness of sucrose, and has the structure of the following formula (1).

H20H C0H HCOH (1) H20H Moreover, xylitol is a type of pentose alcohol having almost the same sweetness as sucrose, and has the structure of the following formula (2).

H20H )(Co)I (HOCH(2) COH H20H The intestinal cleansing composition of the present invention contains the above-mentioned erythrol and/or
Alternatively, it is essential to contain xylitol in an amount of 5.0 to 35°Og, preferably 8 to 30g per 11, and based on this, the following excellent effects can be achieved. That is, both erythritol and xylitol are hardly absorbed in the gastrointestinal tract, and even if they are absorbed, they are excreted as they are, so they have no adverse effect on the human body. It is also hardly fermented by colonic bacteria. Therefore, they can be metabolized into gaseous products, such as hydrogen gas, which can cause an explosion during volipectomy surgery or cause discomfort such as flatulence, or be absorbed by the body, depending on the patient to whom they are applied. There is no risk of it being metabolized into other substances, and it also has the advantage of not having any adverse effects on the intestinal mucosa. In addition, erythritol and xylitol
It has the advantage that air bubbles are less likely to be generated due to the oscillation of the intestinal tract, and even if they do occur, they disappear quickly.

This solves a serious drawback that cannot be overcome with conventional intestinal cleansing agents using polyethylene glycol and is one of the causes of misdiagnosis due to its use.From this point of view, the intestinal cleansing composition of the present invention It can be said that this product is superior to conventional cleaning agents of this type.

It is essential that the composition of the present invention contains a predetermined amount of the specific electrolyte ion having the above-mentioned composition along with the above-mentioned erythritol and/or xylitol.

These formulations sufficiently replenish the net electrolytes lost from the patient's body when the composition of the present invention is applied to the patient;
This substantially prevents the loss of electrolytes from the living body, thereby maintaining the electrolyte balance of the tissue and making it possible to observe the tissue in a normal state.

The blending amount of the electrolyte ion is within the specific range described above, more preferably Na 40 to 135 mEQ/A! .

K+7~13 mEq/l, C11-24~46 m
It is important to select from Eq/II, HCO3-14 to 26 mEq/A' and HCO3-50420 to 85 mEq/A', thereby achieving the effects specific to the present invention.

Compounds capable of providing such electrolyte ions are not particularly limited, but are usually preferably selected from sodium sulfate, potassium chloride, sodium chloride, and sodium bicarbonate.

The composition of the present invention contains sweet and odorless erythrol and/or
Since it uses xylitol, it does not have an oily taste like commercial products that use polyethylene glycol, and when sodium sulfate or potassium sulfate is added, it does not increase the pungent or harsh taste derived from them. Rather, it has the effect of concealing such unpleasantness and has the advantage of ensuring ease of administration. In addition, when reducing the amount of sodium sulfate or potassium sulfate mentioned above, it is desirable to increase the amount of erythritol or xylitol to maintain the cleaning effect.

In order to further improve the ease of drinking, the composition of the present invention may contain, for example, a flavoring agent such as sodium saccharin, a suitable flavoring agent such as fruit essence, etc., as appropriate.

The composition of the present invention can be made into a liquid by, for example, mixing erythritol and/or xylitol in the predetermined amount range with the electrolyte mixture by adding enough water to make the solution 11 and other additive components as necessary. It can be prepared in any form. The liquid preparation is filled into a suitable filling container, such as a glass vial or a synthetic resin container, which is widely used, to produce a product.

The composition of the present invention may also be in the form of a concentrate, powder, or other form of a dissolving agent before use. Powder preparations can be prepared, for example, by pulverizing erythritol or xylitol and crystals of each electrolyte compound, and packaging the powder in suitable drug wrapping paper. The above-mentioned solubilizing agent can be prepared and applied by dissolving and diluting it with water so that the concentration for each dose is within the range of the above-mentioned liquid preparation.

When the composition of the present invention thus prepared is used for purposes such as intestinal cleansing, the amount to be applied can be appropriately determined depending on the patient to whom it is to be applied. The amount of squeezing varies from person to person, but generally it can be approximately 1000 to 3000 y/day once a day. The dosage rate is usually about 15 to 2
5zl! /minute (approximately 0.9 to 1.5117 hours), and the administration is usually orally, but is not limited thereto, and may also be administered, for example, nasally.

The composition of the present invention can also be used to treat constipation by taking or ingesting an appropriate amount with meals.

EXAMPLES Hereinafter, in order to explain the present invention in more detail, preparation examples of the intestinal cleansing composition of the present invention will be given as examples, and then experimental examples will be given to clarify the effects thereof.

Example 1 Erythritol (manufactured by Wako Tsumugi Pharmaceutical Co., Ltd.) and other components were dissolved in water in the amounts shown in Table 1 below, stirred, and mixed to prepare a liquid composition for intestinal cleansing of the present invention.

The osmotic pressure (osmolality) of the solution was measured by the degree of freezing point depression and was found to be 283 mosm/l.

Example 2 In the same manner as in Example 1, a composition for intestinal cleansing of the present invention having the composition shown in Table 2 below was prepared.

Table 2 The osmotic pressure of the above solution was determined in the same manner as in Example 1.
283 m05m/l Tea Tsuta.

Example 3 In the same manner as in Example 1, an intestinal cleansing composition of the present invention having the composition shown in Table 3 below was prepared.

Table 3 The osmotic pressure of the above solution was determined in the same manner as in Example 1.
It was 302 mosm/ /.

Example 4 In the same manner as in Example 1, a composition for intestinal cleansing of the present invention having the composition shown in Table 4 below was prepared.

Table 4 The osmotic pressure of the above solution was determined in the same manner as in Example 1.
341 m05m/l.

Example 5 In the same manner as in Example 1, xylitol (manufactured by Eisai Co., Ltd.)
An intestinal cleansing composition of the present invention having the compositions shown in Table 5 below and other components was prepared.

Table 5 The osmotic pressure of the above solution was determined in the same manner as in Example 1.
283 mosm/I! Met.

Example 6 In the same manner as in Example 1, a composition for intestinal cleansing of the present invention having the composition shown in Table 6 below was prepared.

Table 6 The osmotic pressure of the above solution was determined in the same manner as in Example 1.
376 m05m/I! Met.

Example 7 In the same manner as in Example 1, a composition for intestinal cleansing of the present invention having the composition shown in Table 7 below was prepared.

Table 7 The osmotic pressure of the above solution was determined in the same manner as in Example 1.
283 mosm/l Teatsuta.

Example 8 In the same manner as in Example 1, a composition for intestinal cleansing of the present invention having the composition shown in Table 8 below was prepared.

Table 8 Example 10 In the same manner as in Example 1, a composition for intestinal cleansing of the present invention having the composition shown in Table 10 below was prepared.

Table 10 The osmotic pressure of the above solution was determined in the same manner as in Example 1.
It was 297 mos+n/l.

Example 9 In the same manner as in Example 1, a composition for intestinal cleansing of the present invention having the composition shown in Table 9 below was prepared.

Example 11 Erythritol powder 19.94g.

Na2SO411,38g5NaHCO33,36g,
2.92 g of NaCl and 1.50 g of KCl crystals were mixed, and the mixture was wrapped in drug wrapping paper to prepare a powder preparation for dissolution before use.

The above-mentioned ready-to-dissolve powder preparation can be prepared into a liquid preparation as follows. That is, put an appropriate amount of water into a bottle No. 21, add the above powder preparation to it, shake well to dissolve it completely, and then add water to make the total No. 21. In this way, single-dose solutions can be prepared.

Example 12 Erythritol 40.4g, NaHCO33.36g,
NaCl2.92g and KCI! Dissolve 1.50 g in water to make a total volume of 400xl and prepare the intestinal cleansing composition of the present invention in concentrated liquid form (erythritol concentration: 10.1%W).
/V) was prepared.

This concentrated solution can be prepared into a single-dose solution by diluting it with water to a total volume of 21.

Experimental Example 1 Cleaning Effect Test Cecalectomized rats (Wistar rats, body weight approximately 250 g, 8 rats per group) that were given free access to the diet were used as test animals. Cleansing compositions (invention group 1), compositions prepared in 2 to 8 (invention groups ■ to ■), commercially available intestinal cleansers (Table 11 below, comparative group ■), and Japanese Patent Application Publication No. 1983 -500523, the intestinal cleansing agent described in Example 3 (Table 12 below,
Comparison group ■) at a rate of 20xl/kg once each
It was orally administered 8 times at 0 minute intervals.

Table 11 Table 12 A non-administered rat group to which no detergent (composition) was administered was provided as a control group.

For each group of rats, the time from the end of administration to the excretion of watery stool and soft stool (time to completion of excretion) was measured, and this was used as an index of the immediate effectiveness of each detergent sample.

Two hours after the end of the above administration, the rats in each group were sacrificed under Nembutal anesthesia, and the contents of their digestive tracts (stomach to intestines) were washed out with physiological saline. Centrifuge the washing solution (300
After drying the residue at 60° C. for 5 days, each weight was measured to determine the dry weight of the gastrointestinal contents.

The results obtained are shown in Figure 1 (dry weight of gastrointestinal contents) and Figure 2 (time to watery stool excretion).

The plot in each figure shows the overall average value of each group of rats, and the main mark of the value in Figure 1 indicates that p<Q compared to the control group.
, 05, and this mark indicates p<Q, 01, respectively.

From FIG. 1 and FIG. 2, it can be seen that the composition of the present invention is superior to commercially available products in terms of intestinal cleansing effect and immediate effect.

[Brief explanation of drawings]

FIG. 1 is a graph showing the dry weight of the gastrointestinal contents in the gastrointestinal tract cleaning test according to Experimental Example 1 of the present invention, and FIG. 2 is a graph showing the time taken to excrete watery stool in the same test. (that's all)

Claims (3)

[Claims] (1) A composition for intestinal cleansing, which is characterized in that it contains components in the following composition range and is in a liquid form. Erythritol and/or xylitol: 5.0-35.0g/lNa
^+: 35-150mEq/l K^+: 5-20mEq/l Cl^-: 20-50mEq/l HCO_3^-: 0-30mEq/l SO_4^2^-: 0-100mEq/l (2) A composition for intestinal cleansing, which is in the form of a ready-to-use solubilizer that, when dissolved, becomes a component within the composition range described in claim (1). (3) The intestinal cleansing composition according to claim (1) or (2), which uses an electrolyte selected from the group consisting of sodium sulfate, potassium chloride, sodium chloride, and sodium hydrogen carbonate.