JPS6163618A - Cathartic - Google Patents

Abstract

PURPOSE:A cathartic to evacuate efficiently the bowels by a carbonic acid gas of lactose decomposition product without causing side effects, comprising lactose with specific particle diameters and a mold such as lactic acid bacteria, etc. to mulfiply by the use of lactose as a nutrition source. CONSTITUTION:A cathartic comprising lactose having particle diameters capable of passing through at least 150-250mum mesh as a main agent, and a mold (e.g., lactic acid bacteria, Lactobacillus bifidus, etc.) to multiply by the use of lactose as a nutrition source. The cathartic uses about 20-50g lactose as an amount for one dose, it is dissolved in about 200cc water or warm water, and processed into preferably at least 1.5-10.7CS viscosity. In an existing cathartic, undissolved lactose is deposited in the stomach, and causes side effects such as nausea, vomiting feeling, but the cathartic has the fittest particle diameters determined from solubility of lactose, good circulation from the stomach to the intestine, and can evolve efficiently a carbonic acid gas, etc. by fermentation in the intestine.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a laxative containing lactose as a main ingredient and coexisting with fungi that grow using lactose as a nutrient source, such as lactic acid bacteria, vifidobacteria, and yeast.
By appropriately taking a laxative containing lactose with a particle size that can pass through a mesh of ~250 μm and coexisting with lactic acid bacteria, the lactose component is decomposed in the intestines, and the lactose decomposition product, lactic acid. This invention relates to a laxative that promotes defecation by utilizing the solid wall stimulating effect of acetic acid or carbon dioxide gas.

In general, laxatives have medicinal ingredients that come into contact with the intestinal wall or are absorbed by the intestinal wall and stimulate the intestinal nerves through a biochemical reaction, promoting intestinal function and promoting defecation. Taking laxatives can cause abdominal pain, and long-term use can become habit-forming and paralyze the nerves in the intestines, resulting in the laxatives becoming ineffective unless the dosage is gradually increased. There were concerns that the need for laxatives could further exacerbate chronic constipation, resulting in severe constipation, and that side effects of the medicine could have an adverse effect on users.

In addition, with the recent spread of meat-eating and the lack of vegetable fiber, the number of patients with chronic constipation has increased, and fecal impaction in the intestines has come to be seen as the cause of various diseases and even cancer. There was a need for a laxative or a defecation stimulant that would not cause any side effects.

Therefore, as previously described in Japanese Unexamined Patent Publication No. 58-8018 (Japanese Patent Application No. 56-106684), the present inventor has developed a method that uses lactose as the main ingredient, and adds lactic acid bacteria, other fungi, or drugs and supplements. He proposed a laxative that treats constipation by taking a certain amount of powder containing certain additives along with water on an empty stomach, and also removes fecal impaction and cures the patient's condition.

However, it has been found that some patients experience a feeling of gastric distension, nausea, or even vomiting after taking the laxative.

Therefore, upon careful investigation of the above cases, it was found that many of the target patients had chronic illnesses such as gastric ptosis or weak stomach, and when the inside of the stomach was examined after taking the laxatives, lactose was found to be undissolved. It has been found that this lactose is deposited at the bottom of the stomach and begins to ferment over time, causing a feeling of nausea and vomiting.

This symptom is especially noticeable in patients with severe gastroptosis or weak stomach, and since these patients have a weak constitution, their gastrointestinal function is also weak, and 1, Y accumulates in the intestines. The 1j1 production effect of dregs is also weak, so if you feel queasy for a long time, you will suffer from vomiting.

In view of the current situation, the present invention has solved the above-mentioned conventional difficulties as a result of intensive research.The gist of the present invention is to use lactose as the main ingredient, which consists of granules that can pass through a mesh of at least 150 to 250 μm. , this and the number of lactic acid bacteria,
This is due to the coexistence of fungi such as Vifidobacteria and yeast that grow using lactose as a nutritional source.

That is, the lactose constituting the laxative is made to have a particle size that can pass through a mesh of 150 to 250 μm, and in the presence of water, the lactose of this particle size is prepared as a suspended liquid containing undissolved matter, and an appropriate amount of lactose is prepared. The solution is made to coexist with bacteria such as lactic acid bacteria, vifidobacteria, and yeasts that grow using lactose as a nutritional source, and in the intestines of patients who take this solution, the residual lactose particles are gradually dissolved, and fermentation occurs after the dissolution. This allows carbon dioxide gas to be generated efficiently.

When this solution is used, it is desirable that it has at least a certain viscosity, and this viscosity allows the medicinal ingredients in the solution to act in the intestines for a certain period of time.

To explain the present invention in detail below, the laxative according to the present invention basically contains lactose, and in this lactose, fungi such as lactic acid bacteria, vifidobacteria, and yeasts that grow using lactose as a nutritional source are combined. A laxative that primarily utilizes the carbon dioxide gas generated during fermentation after ingestion, and utilizes the physical pressure of this carbon dioxide gas and the intestinal wall stimulating effect during the carbon dioxide generation period. Therefore, the amount of its main ingredients, lactose and lactic acid bacteria, in a single dose is an important factor that determines the therapeutic effect.

From this point of view, first of all, we will explain about lactose, which is the main component of the laxative component according to the present invention.Water or warm water is required to dissolve the lactose when actually taking it, and it also depends on the taste, preference, or nutritional balance of the user. It is taken by selectively combining kale powder, glucomannan, chlorella dried rice, brown sugar, various vitamins, etc. in response to the requests of people, and it is difficult to determine the exact amount from the mouth. In order to have a therapeutic effect, at least as a laxative, it is necessary to ingest a certain amount of lactose, and it is usually desirable for adults to use this selectively within a range of about 20 to 50 g.

However, due to its nature, lactose has low solubility in water.
For example, 150 to 250 cc of water (about 1 cup of water)
Even if 20 to 50 g of lactose, which is required as a laxative, is added and attempted to be dissolved therein, it is difficult to dissolve it completely.

For this reason, it is conceivable to dissolve lactose using boiling water, but on the other hand, in the present invention, it is also therapeutically effective to use a mixture such as live lactic acid bacteria, which is one of the constituent elements. As this is an important point, it is not preferable to kill the viable bacteria by the high temperature treatment, and furthermore, a completely dissolved aqueous solution of lactose has a strong sweet taste, making it unsuitable for long-term administration. It is.

Therefore, in order to make laxatives based on lactose components applicable to many patients with various pathological conditions, the present inventor took into consideration the mode of action of lactose components in the intestines after taking them,
First, the relationship between the particle size of lactose and its solubility in water was investigated, and the optimum particle size range was determined as follows.

That is, 50 lactose powders each having a particle size that can pass through a mesh of 100, 150, 200, 250, and 300 μm are
g was collected and added to 200cc of water at temperatures of 25°C and 40°C.
After stirring thoroughly, the mixture was allowed to stand for 1 minute, the supernatant liquid was transferred, and the remaining lactose was dried and weighed. The results are shown in Table 1.

Table 1 From these results, the larger the particle size of the lactose powder is, the less it dissolves in large amounts of water and the amount of residual lactose increases, and the better it dissolves in finer portions of water, so the finer the particle size, the less the amount of residual lactose. However, in the case of the purgative which is treated with a suspended solution, which is the gist of the present invention, when the amount of residual lactose was about 50% or more or about 5% or less at the time of the above experiment, the laxative according to the present invention Since the appropriate suspension state is elegant,
From now on, in the present invention, at least the particle size of the lactose powder is intended to be that which passes through a mesh of 150 to 250 μm.

Note that this particle size range allows the use of particles that pass through a mesh of 130 to 270 μm, but each differs depending on the patient's medical condition and the effects after taking the drug. Therefore, in the present invention, the particle size range is 150 to 250 μm, which is the range in which the optimal action and effect can be achieved, based on patients who are generally considered to be taking laxatives.
This shows the amount that passes through the mesh.

On the other hand, examples of the lactic acid bacteria to coexist with lactose include:
The culture medium after fermentation of lactic acid bacteria such as Vifidobacterium or natto bacteria containing lactic acid bacteria, yeast, etc. is dried as it is to make a semi-dry product or dry powder containing all of live bacteria, spores, and yeast. It is used as a lactic acid bacterium enzyme, or alternatively, one or more types of live bacteria, spores, and culture media of lactic acid bacteria that do not contain natto fungi or yeast are selectively used as a lactic acid bacterium enzyme.

The enzymes made up of the above components can be classified into live bacteria, spores, enzymes, and culture media.Live bacteria enter a state of suspended animation during distribution as a product, but spores and enzymes can withstand dry conditions. Moreover, when taken as a laxative, it enters the small intestine from the stomach of the user and as the enzyme is dissolved, the enzyme first begins to act, followed by the revival of viable bacteria, and eventually spores. It is thought that they absorb water, sprout, and begin to multiply.

The culture medium is thought to act as a protective agent against the outside air during product distribution, and after consumption, it also acts as a trophic factor that is familiar to bacteria.

As a component of laxatives, it is better to have as many fast-acting enzymes as possible, but since they act quantitatively, it is difficult to take enough to produce a diarrheal effect, and live bacteria and spores account for most of the action. Therefore, several grams of the enzyme, for example 1 to 5 grams, per dose is sufficient.

By the way, one microorganism, such as lactic acid bacteria, can grow to about 100 million in one liquid, but it must be considered that a considerable amount of wastage is required for the microorganisms to pass through the gastric fluid, reach the intestines, and begin to multiply. For the reliability of the effect, it is desirable to use one containing 10 to 10 live bacteria or spores in 1 g of enzyme, and the types of lactic acid bacteria include Lactobacillus, Ac1d.
Ophilus, L., Bulgaricus, etc. may be selectively used.

Therefore, as mentioned above, the laxative of the present invention has lactose as a main ingredient having a particle size that can pass through a mesh of at least 150 to 250 μm, and has a suspension of this as a solution, and the number of lactic acid bacteria in this solution. , Vifidobacteria, yeast, and other fungi that grow using lactose as a nutritional source coexist, so if this ingredient is delivered from the stomach of the user into the intestine, the lactose decomposition product will be absorbed into the intestinal lining. In addition to stimulating defecation, it also removes fecal impaction stuck in the intestines and cleanses the intestines. If applicable,
It is necessary to devise ways to further develop the efficacy for specific patients, and for this reason, unique properties are added that take into account the mode of action on patients after taking the compounded ingredients.

That is, after taking the laxative according to the present invention, in order for the medicinal ingredient to exert the therapeutic effect in the intestine of the user, at least the suspended component must remain in the intestine for a certain period of time and undergo fermentation. It is desirable to sustain such reactions, and therefore, in the present invention, this objective is achieved by imparting a certain viscosity to the medicinal ingredient.

To be more specific, if the medicinal ingredients are given a certain viscosity, after taking the drug, the ingredients will not remain suspended at the bottom of the stomach, but will be rapidly transported from the stomach to the intestines. The duration of dissolution is extended or shortened depending on the set viscosity, so by setting the viscosity, the retention time and elution rate of the medicinal ingredient in the intestine can be controlled, making it suitable for patients with various pathological conditions. This makes it possible to perform treatments that are applicable to each patient.

For this reason, various conditions were set for the laxative component according to the present invention, which uses lactose as a main ingredient, and the added viscosity thereof was investigated.

First, - adjust the lactose suspension solution that is the main ingredient of the present invention under the main conditions and divide it into several types, use sodium alginate as a viscosity additive in each solution, and change the amount of sodium alginate. A test solution was prepared.

That is, in a beaker containing 200 cc of hot water maintained at a water temperature of 40°C, 50 g of lactose (with a particle size that can pass through a 200 μm mesh) is added, and for this amount of lactose, the following table (
After adding sodium alginate in varying amounts as shown in Table 2) and stirring thoroughly, leave it for 1 minute, transfer the suspension at the top of the beaker to another container, and collect a portion of it. The viscosity of the solution was measured, and the remaining liquid in the beaker was dried and the residue was weighed to determine the amount of residual lactose.

The results are shown in Table 2.

Table 2 As can be seen from the results in Table 2, as the amount of sodium alginate added as a viscosity additive increases, the viscosity of the solution increases, but on the other hand, the amount of residual lactose tends to decrease.

This is thought to be due to the solubility product of lactose changing with the addition of sodium alginate, and based on this effect, it is possible to suit the various patients by controlling the lactose component and the amount of sodium alginate as appropriate. It turns out that there is only one laxative preparation that can be used to cure the disease.

Then, the additional viscosity of the solution that leaves undissolved lactose as a suspended solution is determined by taking into consideration the amount of residual lactose,
As shown in Table 2, it has been found that it is sufficient to set the temperature in the range of 1.5 to 10.7C5.

Furthermore, based on these experimental results, in order to confirm the effectiveness in actual use, we conducted a study on patients receiving conventional treatment who experience discomfort such as stomach bloating, vomiting, and stomach pain, especially after taking laxatives. A laxative with the following composition was administered to 32 complaining patients as monitors.
We investigated the treatment status after the patient was fasted for 4 hours after taking the drug.

・Laxative composition (prescription) ■Lactose (100 μIn mesh) 47g Lactobacillus and other enzymes containing 38 brown rice germ rice
2g water 20
0cc■Lactose (150μm mesh 1)
47g Enzyme containing lactic acid bacteria and others 3g brown rice germ rice 2g water
200cc■ Lactose (200μm mesh) 47g Enzyme containing lactic acid bacteria and others 3g Brown rice germ rice
28 water
200cc ■ Lactose (2001tm Metshu)
47g・Sodium alginate 0.025g
3g of brown rice germ rice containing milk bacteria and others
2g water
200cc ■ Lactose (250μm mesh)
478 Enzyme containing lactic acid bacteria and others 3g brown rice germ rice
2g water
200cc ■ Lactose (300μm mesh) 4
7g Enzyme containing lactic acid bacteria and others 3g - Brown rice germ rice 2g water
200cc The results are shown in Table 3.

Table 3 In other words, the section on the presence or absence of incompatible effects in Table 3 was created based on the monitors' own reports of discomfort such as stomach distension, vomiting, nausea, and stomach pain after taking laxatives. In terms of the strength of the effect, those who had a bowel movement within 2 hours after taking the drug were classified as strong, those who had a bowel movement after 4 hours were similarly classified as medium, and those who had no effect at all were classified as weak.

Furthermore, from the results in Table 3, it can be seen that the particle size of lactose with a 100 μm mesh is too coarse, and that the particle size of the 300 μm mesh is too fine, resulting in a large incompatibility effect.
The one with a lactose mesh of 150 to 250 μm has less incompatibility and has a greater effect.

In particular, the lactose 200 μm mesh has the greatest effect, and when an appropriate amount of a viscosity additive is added thereto, the effect is further enhanced.

This effect is due to the particle size of lactose when taken, that is, a lactose suspension with a particle size that can pass through a 200 μm mesh, or a suspension containing an appropriate amount of viscosity additive, when sent from the stomach to the intestines. It has very good distribution properties, and therefore, it rapidly passes through the stomach as a suspension of insoluble lactose fine powder, eliminating any undesirable effects in the stomach, and due to its particle size, it passes through the intestine. This is thought to be due to the fact that the fermentation effect accompanying the dissolution etc. of

In addition, the monitor indicates that the particle size of lactose is 150μ when taking the drug.
A mesh of 150 μm or more tends to leave particulate matter on the tongue, which is undesirable.
In particular, it is said that the particle size of 200 μm mesh or around 250 μm mesh did not cause this sensation at all, so it seems that the best lactose particle size is in the range of 15G to 250 μm.

In addition, in the above experiment, the viscosity of each formulation was determined by lactose,
The viscosity was set at 1 and 5C5 for lactic acid mycelia, and 2.0C5 for those with sodium alginate added, but there is a limit to the setting of this viscosity due to the properties of the lactose and lactic acid bacteria components. In order to increase the viscosity above a certain value, it is necessary to add a viscosity additive, for example, sodium alginate.

For this reason, G! I tried it.

The laxative composition (prescription) was based on the recipe shown in Table 3 above, and the amount of sodium alginate as a viscosity additive was varied as shown in Table 4 to prepare samples.

・Basic prescription lactose (200μm mesh) 47g lactic acid bacteria, enzyme containing the song 3g brown rice germ rice
2g Sodium alginate 0.010-0.500g Water
200cc The results are shown in Table 4.

That is, in this experiment, 35 patients who had been receiving conventional treatment were employed as monitors, and they were asked to take samples prepared by adding various amounts of sodium alginate to the basic prescription on an empty stomach before breakfast, and for 4 hours after taking the drug. This study investigated the effects after fasting.

In Table 4, the strength of the effect was determined as strong for those who had a bowel movement within 2 hours after taking the drug, moderate for after 4 hours, and weak for those who had no bowel movements at all.

Based on these results, in a suspension solution containing lactose as the main ingredient, the amount of sodium alginate should be 0.010 to 0.010.
When added in an amount of 0.250 g, a remarkable effect is exhibited, but when the amount is more than a certain amount, for example, 0.400 g or more, the effect gradually becomes weaker.

The reason for this is that the higher the viscosity of the i8 liquid, the more it mixes with viscous substances such as digestive juices in the human body after taking it, and the more the medicinal ingredients dissolve, the slower the dissolution of the medicinal ingredients. Fungi that proliferate using lactose as a nutritional source, such as Lactobacillus horni, Vifidus fungi, and I3, are less likely to be affected, and
It can be inferred that this is because the generation of lactic acid, acetic acid, carbon dioxide gas, etc., which are decomposition products of lactose, is delayed.

Therefore, in the laxative according to the present invention, the particle size is
A single dose of lactose that can pass through a mesh of at least 150 to 250 μm is about 20 to 50 g, and about 1 to 5 g of lactic acid bacteria, brown rice germ, etc. are coexisting therein, and the lactose is dissolved in about 200 cc of water or hot water. In this case, the optimum viscosity range of the solution can be said to be at least about 1.5 to 10.7 cs.

As mentioned above, the laxative of the present invention has at least 150 to 25
The main ingredient is lactose, which has a particle size that can pass through a 0 μm mesh, and it is made by coexisting with fungi such as lactic acid bacteria, vifidobacteria, and yeasts, which grow using lactose as a nutritional source. When a certain amount of the laxative is taken with water, fine particles such as lactose are dissolved and decomposed in the patient's intestine, and the carbon dioxide scum generated by this decomposition reaction effectively provides treatment.
Therefore, it can be applied to treat constipation and fecal impaction in patients with various pathological conditions without any side effects such as abdominal pain or chronicity.

In the above description of the present invention, the laxative component was mainly explained as a powder, but if it is processed into granules or tablets, dissolved in a solvent, and taken as a suspended solution, the above-mentioned laxative components can be obtained. It can produce the same effects as the powdered version.

Furthermore, within the scope of the present invention, the medicinal ingredient of the laxative of the present invention may be incorporated into a conventionally known laxative composition, or the medicinal ingredient of the laxative of the present invention may be incorporated into a composition based on the medicinal ingredient. It is also possible to create a laxative by adding a laxative component and to enhance the therapeutic effect by taking the laxative as appropriate.

Claims (2)

[Claims] (1) The main ingredient is lactose, which has a particle size that can pass through a mesh of at least 150 to 250 μm, and it is made by coexisting with fungi that grow using lactose as a nutritional source, such as lactic acid bacteria, vifidobacteria, and yeast. A laxative. (2) Use about 20 to 50 g of the lactose as a single dose, and adjust the viscosity of the solution to at least 1.5 to 10.7 CS when dissolved in water or hot water of around 200 c. A laxative according to claim 1.