JPH0368010B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a laxative containing lactose as a main ingredient and fungi that grow using lactose as a nutritional source, such as lactic acid bacteria, Vifidus fungi, and yeast. The main ingredient is lactose, which is coexisting with lactic acid bacteria, and the lactose used is about 20 to 50 g per dose, and the viscosity when dissolved in water or hot water temperature is
By taking appropriate laxatives adjusted to 1.5 to 10.7 CS (centistokes, same hereinafter), the lactose component is broken down in the intestines, and the lactose decomposition products, lactic acid, acetic acid, and relates to a laxative that promotes defecation by utilizing the intestinal wall stimulating effect of carbon dioxide gas and the like. In general, laxatives have their medicinal ingredients in contact with the intestinal wall,
Or, since it is absorbed into the intestinal wall and stimulates the intestinal nerves through a biochemical reaction, promoting intestinal movement and promoting defecation, taking laxatives may cause abdominal pain. Also, if taken over a long period of time, it becomes addictive and the nerves in the intestines become paralyzed, and the laxative dose must be gradually increased to become effective, resulting in the need for even more nerve-stimulating laxatives, leading to chronic constipation. The situation was such that there were concerns that the drug could further exacerbate the problem, leading to severe constipation, and that the side effects of the drug could have an adverse effect on the user. 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. However, there was a need for a laxative or a defecation stimulant that does not cause 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 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 stomach bloating, nausea, and vomiting after taking the laxative. For this reason, when we carefully investigate the above case, we find that
Many of the target patients had chronic illnesses such as gastric ptosis or gastric weakness, and when the inside of the stomach was examined after taking the laxatives, lactose was deposited at the bottom of the stomach in an undissolved state, and this lactose remained undissolved for a long time. Along with this, fermentation began, and it was discovered that this effect caused feelings of nausea and vomiting. This symptom is particularly noticeable in patients with severe gastroptosis or weak stomach, and since the patient's constitution is so-called incompetent, the gastrointestinal function is also weak.
Therefore, the ability to expel gas accumulated in the intestines is weak,
This results in prolonged nausea and vomiting. In view of the current situation, the present invention has solved the above-mentioned conventional difficulties as a result of intensive research. This is made by coexisting with fungi that grow using lactose as a nutritional source, such as lactic acid bacteria, Vifidus fungi, and yeast, and uses about 20 to 50 g of the lactose as a single dose, and about 200 c.c. of water. Or, when dissolved in hot water, the viscosity of the solution is adjusted to be at least 1.5 to 10.7 CS. That is, the lactose constituting the laxative is made to have a particle size that can pass through 150 to 250 meshes, 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 fungi that grow using lactose as a nutritional source, such as lactic acid bacteria, Vifidus fungi, and yeast, to gradually dissolve the residual lactose particles in the intestines of patients who have taken this solution, and to cause fermentation after the dissolution. This solution is designed to efficiently generate carbon dioxide gas, etc., and when used, 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. It is adjusted to Hereinafter, to explain the present invention in detail, the laxative according to the present invention basically contains lactose, and in addition to this lactose, lactic acid bacteria, Vifidus fungi, yeast, etc.
Mainly utilizes the carbon dioxide gas generated during fermentation after ingestion in coexistence with fungi that grow using lactose as a nutritional source, and also stimulates the intestinal wall during the carbon dioxide generation period by the physical pressure of this carbon dioxide gas. 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 we will explain about lactose, which is the main component of the laxative component according to the present invention.Water or warm water for dissolving lactose is required for actual administration.
In addition, kale powder, glucomannan,
Since it is taken with a selective combination of dried chlorella powder, brown sugar, and various vitamins, it is difficult to determine the amount used, but in order to have a therapeutic effect as a laxative, at least It is necessary to ingest more than 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 properties, lactose has low solubility in water.
Even if you try to dissolve it by adding g, it is difficult to completely dissolve it. 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 through the high temperature treatment, and furthermore, an aqueous solution of completely dissolved lactose has a strong sweet taste, making it unsuitable for long-term administration. It is something. Therefore, in order to make laxatives based on lactose components applicable to many patients with various pathological conditions, the present inventor first considered the mode of action of lactose components in the intestines after taking the drug, and first The relationship between particle size and solubility in water was investigated, and the optimum particle size range was determined as follows. That is, 50 g of lactose powder each having a particle size that can pass through 100, 150, 200, 250, and 300 meshes was collected and poured into 200 c.c. of water at temperatures of 25°C and 40°C, respectively. After thorough stirring, 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】

[Table] From this result, the larger the particle size of lactose powder is, the less it dissolves in water and the amount of residual lactose increases; However, in the case of laxatives that are treated in suspension, which is the gist of the present invention, the amount of residual lactose was about 50% in the above experiment.
If the concentration is above 5% or below about 5%, it is difficult to obtain a suspension suitable for the laxative according to the present invention. Therefore, in the present invention, the particle size of the lactose powder is targeted at at least the amount that passes through 150 to 250 meshes. That is. Strictly speaking, this particle size range allows for the use of particles that pass through 130 to 270 meshes, but each differs depending on the patient's condition and the effects after taking the drug, and the inside of the human body is extremely complex. Because of the entanglement, it is difficult to necessarily limit the particle size range. Therefore, in the present invention, the particle size range is 150 to 250, which is the range that can achieve the optimal action and effect, based on the generally considered patients taking laxatives. This shows the amount that has passed through the mesh. On the other hand, the lactic acid bacteria coexisting with lactose include:
For example, a culture medium after fermentation of lactic acid bacteria such as Bacillus Vifidus, or natto fungi containing lactic acid bacteria, yeast, etc., is dried as it is to produce a semi-dry product or dry powder containing all of live bacteria, spores, and yeast; This can be used as a lactic acid bacteria enzyme, or as a live lactic acid bacteria, spores, or culture medium that does not contain natto fungi or yeast.
The species or two or more species are selectively used as lactic acid bacteria. Compositionally, the enzyme consisting of the above components includes live bacteria,
They can be divided into 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, and when taken as a laxative, they are As the enzyme enters the small intestine from the human stomach and is dissolved,
It is thought that first the enzyme begins its action, then the living bacteria are revived, and eventually the spores 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 familiar nutrient for bacteria. As a component of laxatives, it is better to have as much enzyme as possible, which is fast-acting, but since it works quantitatively, it is difficult to take enough to cause diarrhea, and most of the enzymes are living bacteria and spores. Since it is thought that the enzyme acts, several grams of the enzyme, for example 1 to 5 grams, in one dose is sufficient. By the way, one microorganism, such as lactic acid bacteria, can increase to about 100 million in one night, but you have to consider a considerable amount of attrition as it passes through the gastric fluid, reaches the intestine, and begins to multiply. For the reliability of the effect, it is desirable to use one containing 10 ⁵ to 10 ⁸ live bacteria or spores per gram of enzyme, and the types of lactic acid bacteria include Lactobacillus, Acidophilus,
L. Bulgaricus etc. may be used selectively. Therefore, as mentioned above, the laxative of the present invention has lactose as a main ingredient having a particle size that can pass through at least 150 to 25 meshes, and has this as a suspended solution, and contains lactic acid bacteria in this solution. It is made up of coexisting with fungi that grow using lactose as a nutritional source, such as lactose, Vifidus fungi, and yeast, so if this ingredient is delivered from the stomach of the user into the intestine, the lactose decomposition product will be absorbed into the intestine. It has a stimulating effect on the inner wall, promoting defecation, and also removes fecal impaction stuck in the intestine, thereby cleaning the intestine. When targeting the drug, it is necessary to devise ways to further enhance its efficacy for specific patients, and for this reason, it is necessary to develop products with unique properties that take into consideration the mode of action on the patient after taking the compounded ingredients. This is what we do. 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 dissolution 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 studied. First, a lactose suspension solution, which is the laxative of the present invention, was prepared under certain conditions and divided into several types, and sodium alginate was used as a viscosity additive in each solution, and the amount of sodium alginate was varied. A sample solution was prepared. That is, in a beaker containing 200 c.c. of hot water maintained at a water temperature of 40°C, add 50 g of lactose (of a particle size that can pass through 200 mesh), and for this amount of lactose,
After adding sodium alginate in varying amounts as shown in the table below (Table 2) and stirring thoroughly, let it stand for 1 minute, transfer the suspension at the top of the beaker to another container, and add a portion of it. The viscosity of the solution was measured by fractionation, 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] 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 residual amount of 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 has been shown that it is possible to prepare laxatives that can induce It was found that the added viscosity of the suspension-like solution, which leaves undissolved lactose, should be set in the range of 1.5 to 10.7 CS as shown in Table 2, taking into account the amount of residual lactose. did. 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. We administered a laxative of the following composition to 32 complaining patients as monitors, and investigated the treatment status after they were made to fast for 4 hours after taking the drug. ●Laxative composition (prescription) Lactose (100 mesh) 47g Lactobacillus and other enzymes 3g Brown rice germ powder 2g Water 200c.c. Lactose (150 mesh) 47g Lactobacillus and other enzymes 3g Brown rice germ powder 2g Water 200c. c. Lactose (200 mesh) 47g Enzyme containing lactic acid bacteria and others 3g Brown rice germ powder 2g Water 200c.c. c. Lactose (250 mesh) 47 g Enzyme containing lactic acid bacteria and others 3 g Brown rice germ powder 2 g Water 200 c.c. Lactose (300 mesh) 47 g Enzyme containing lactic acid bacteria and others 3 g Brown rice germ powder 2 g Water 200 c.c. are shown in Table 3.

[Table] In other words, the section regarding the presence or absence of non-compliance effects in Table 3 is as follows:
It was created based on the monitor's own reports of discomfort such as stomach bloating, vomiting, nausea, and stomach pain after taking the laxative. It was created with people who have been hit as strong, people who have had no time at all in the same way as weak, and people who have had no time at all as weak. From the results in Table 3, it can be seen that those with lactose of about 100 meshes have a too coarse particle size, those with 300 meshes have a large incompatibility effect because the particle size is too fine, and those with 150 to 250 meshes of lactose have an incompatibility effect. is getting smaller and the effect is getting bigger. In particular, the one with 200 mesh of lactose has the greatest effect, and when an appropriate amount of viscosity additive is added to it,
It can be seen that the effect is further enhanced. This effect is due to the particle size of lactose at the time of ingestion, i.e. 200
Lactose suspensions with a particle size that can pass through a mesh, or those to which an appropriate amount of viscosity additive is added, have very good circulation when being sent from the stomach to the intestines, and therefore, they can easily pass through the stomach. To rapidly pass undissolved lactose fine powder in suspension, eliminate any inconvenient effects in the stomach, and effectively perform the fermentation action associated with dissolution in the intestine due to its particle size. This is thought to be due to In addition, the monitor monitors the particle size of lactose during administration.
If the particle size is less than 150 mesh, it tends to leave particulate matter on the tongue, which is undesirable.However, if the particle size is more than 150 mesh, especially around 200 mesh, or around 250 mesh, this sensation will not occur at all. From the above, the particle size of lactose is 150 to 250.
A range that can pass through Metsuyu seems to be best. In the above experiment, the viscosity of each formulation was set to 1.5 CS for lactose and lactic acid bacteria, and 2.0 CS for the one containing sodium alginate. Lactic acid bacteria-based ingredients alone have limitations due to their properties.
To increase the viscosity above a certain value, it is necessary to add a viscosity additive, such as sodium alginate. For this reason, we investigated the most effective range of viscosity additive addition for lactose-based laxatives. 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 recipe Lactose (200 mesh) 47g Extract enzyme containing lactic acid bacteria and others 3g Brown rice germ powder 2g ●Amount of sodium alginate Sodium alginate 0.010-0.500g Water 200c.c. The results are shown in Table 4.

[Table] In other words, 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. This study investigated the effects after 4 hours of 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. Judging from this result, when adding sodium alginate in an amount in the range of 0.010 to 0.250 g in a solution containing lactose as the main ingredient in a suspended state, a remarkable effect can be achieved, but if the amount is more than a certain amount, for example 0.400 g or more, In this case, the effect gradually becomes weaker. The reason for this is that the higher the viscosity in the solution,
After taking the drug, it mixes with viscous substances such as digestive juices in the human body, further slowing down the dissolution of the medicinal ingredients.
This is thought to be due to the fact that yeast and other fungi that grow using lactose as a nutritional source are less likely to be affected, and the generation of lactose decomposition products such as lactic acid, acetic acid, and carbon dioxide gas is delayed. Therefore, in the laxative according to the present invention, the one-time dose of lactose that allows the particle size to pass through at least 150 to 250 meshes is about 20 to 50 g, and about 1 g of lactic acid bacteria, brown rice germ, etc. ~5g coexist and dissolved in water or hot water of around 200 c.c., the viscosity range of the solution is at least
It can be said that about 1.5 to 10.7 CS is optimal. As mentioned above, the laxative of the present invention has at least 150%
The main ingredient is lactose with a particle size that can pass through ~250 mesh, and this is made to coexist with fungi that grow using lactose as a nutritional source, such as lactic acid bacteria, Vifidus fungi, and yeast. about 20
~50g is used, and the viscosity of the solution is at least 1.5 when dissolved in around 200c.c. of water or hot water.
The laxative has been adjusted to have a CS of ~10.7 CS, so when a patient takes a certain amount of this laxative with water, fine particles such as lactose dissolve and decompose in the patient's intestine, and this decomposition reaction occurs. It is effective in treating constipation and fecal impaction in patients with various pathological conditions without any side effects such as abdominal pain or chronicity. It becomes applicable. 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 powder It can produce the same effect as the one with the shape. 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 prepare a laxative by adding a laxative component and to enhance the therapeutic effect by taking the laxative as appropriate.

Claims (1)

[Claims] 1 The main ingredient is lactose with a particle size that can pass through 150 to 250 mesh, and this is made to coexist with fungi that grow using lactose as a nutritional source, such as lactic acid bacteria, Vifidus fungi, and yeast, and the single dose of lactose is About 20 to 50 g is used as the amount, and the viscosity of the solution is 1.5 to 1.5 when dissolved in around 200 c.c. of water or hot water.
A laxative characterized by being adjusted to 10.7CS.