WO2015056897A1

WO2015056897A1 - Intestine cleansing composition

Info

Publication number: WO2015056897A1
Application number: PCT/KR2014/008893
Authority: WO
Inventors: 강윤식; 신정윤; 강현석; 강현이
Original assignee: 강윤식; 신정윤; 강현석; 강현이
Priority date: 2013-10-17
Filing date: 2014-09-24
Publication date: 2015-04-23

Abstract

The present invention relates to an intestine cleansing composition comprising: a particular sugar alcohol, such as Xylitol or Sorbitol, as a first cleansing ingredient; ascorbic acid or a mixture of ascorbic acid and ascorbic acid salt as a second cleansing ingredient; picosulphate as a third ingredient; and a water-soluble solvent, wherein, with respect to the total composition, the content of the first cleansing ingredient is 10-500 g/L, the content of the second cleansing ingredient is 1-100 mg/L, the content of the third cleansing ingredient is 15-500 g/L, and the water-soluble solvent volume is 0.1-1.0 L, the intestine cleansing composition having a superb intestine cleansing ability, easier administration and improved safety, and thus can be used for intestinal cleansing for: colonoscopy, endoscopic surgeries and such; intestinal cleansing prior to abdominal surgeries; intestinal treatment prior to anal surgery, such as for hemorrhoids; and treating and alleviating diseases such as chronic and acute constipation.

Description

Intestinal cleansing composition

Technical Field

The present invention relates to an intestinal cleansing composition, and more specifically, by containing a high concentration of specific sugar alcohols and ascorbic acid in laxative phycosulfate, the overall dosage is reduced, and the intestinal cleanability is further improved, It relates to a novel intestinal cleansing composition also ensured safety.

Background Art

Colorectal cancer is the third most common cancer worldwide, according to a report by the World Cancer Research Fund International.In 2012, it is estimated that 1.4 million new colorectal cancer patients worldwide, and by 2035 It is estimated that 2.4 million new colorectal cancer patients will occur each year. Colonoscopy is essential to diagnose such colon cancer. Furthermore, colonoscopy is very important because colonic polyps, which can be called precursor lesions of colon cancer, can be blocked at the time of colonoscopy.

To ensure accurate colonoscopy, it is essential to clean the intestines in advance. Even if you fast for several days, the bowels will always remain in your colon, so you should clean your colon by artificial means before the test. To this end, methods for washing the intestine by taking a cleaning liquid consisting of laxative ingredients have begun to be developed. The ideal intestinal cleanser needs to have strong cleaning power, ease of taking and safety.

First, strong cleaning power is accurate colonoscopy. It is a necessary condition for inspection. If there are still many residues remaining after intestinal lavage, accurate examination is difficult, and because of poor visibility, the risk of complications such as intestinal perforation increases.In some cases, the intestinal lavage process must be repeated. May be rejected or avoided. Therefore, predictable successful detergency is the most important condition.

Second, is the ease of taking the uncomfortable symptoms such as nausea sick _i flicker eu vomiting, abdominal pain, according to taste, taking the dose determines whether Chapter cleaner. No matter how good your bowel cleansers can be, if you're having a hard time taking them, you won't be able to successfully complete your dose. In addition, the unpleasant memory of bowel lavage may manifest as a rejection of the retest. In many cases, rumors of the difficulty of taking may interfere with the activation of colonoscopy, which may harm the public health.

Third, safety requirements should minimize temporary disability and not cause irreversible chronic disability at all.

In the early days, it was suggested to drink a large amount of a solution such as an aqueous solution of sodium chloride up to 7-12 L as an intestinal cleanser, but this cleanser was accompanied by a great deal of pain and difficulty.

Since the introduction of intestinal lavage taking 2L of 10% Mannitol, a type of sugar alcohol, was highly anticipated. However, intestinal surgery or therapeutic colonoscopy was performed in patients who underwent mannitol intestine. Mannier's use was discontinued as a gas explosion incident was reported. In addition, consumption-intestinal cleansing is also contraindicated in most medical developed countries, such as the United States and Europe, due to similar risks.

In the 1980s, polyethylene glycol (PEG) was developed, and the intestinal rinsing method was prepared using 4L solution. PEG preparations are the most used bowel cleansers to date.

The main problem with PEG preparations is that the dosage reaches 41 _^ and the disgusting taste of PEG preparations makes them very difficult to take. Because of this difficulty in taking, there is a widespread negative perception of the bowel cleansing process, which eventually leads people to fear or avoid colonoscopy.

Thus, efforts to reduce the amount of PEG preparations consumed have been attempted at various angles. Prepackages of irritant laxatives, such as bisacryl tablets, should be taken 6-12 hours prior to the PEG solution, combined with magnesium citrate (Citromag ^® ) solution, or ascorbic acid (additional name Moviprep®) This can be used to reduce the dose of PEG diluent to 3L. In the case of this intestinal lavage of Moviprep ^® series, ascorbic acid and sodium ascorbate were added to compensate for the detergency that was enjoyed, but the total amount of PEG contained in the intestinal rinse was 200 g and 4L of colic acid was taken. The PEG content is only 15.3% less than the 236g contained in. Eventually, the PEG concentration is 1/7 times, despite the decrease in the total amount of dilute liquor to drink, the situation is more complaining of discomfort than taking 4L of colic acid. In addition to these dosage difficulties, PEG preparations are also not satisfactory. Several studies have shown that 70% of the intestinal lavage levels were adequate for colonoscopy after intestinal lavage using PEG. Such poor cleaning results of PEG formulations have been confirmed in several papers. An example is a study in Korea that showed that 47.1% of people with intestinal lavage with the PEG formulation, Colyte, had solid stool residues left in their large intestines that interfered with endoscopic examination. <"Before colonoscopy Treatment Comparison of 4L Polyethylene Glycol Monotherapy with 2L Polyethylene Glycol and Sodium Phosphate Solution (90mL) ", Bundang Seoul National University Hospital, Seoul National University College of Medicine, College of Medicine, Liver Research Institute Lee, Jung-Won et al., 56, 299-306, 2010 >.

There is a phycosulfate formulation containing citrate magnesium as an intestinal cleanser developed to solve the difficulty of taking such a PEG formulation. This preparation has a significant improvement in taste, and unlike the PEG preparation, there is little benefit from taking it. For this reason, phycosulfate preparations are most commonly used in Europe, but the biggest problem with phycosulfate preparations is their relatively poor bowel cleansing power. Ferring's Prepopik ^® (sodium picosulfate, magnesium oxide, and anhydrous citric acid), approved by the US FDA, has a recommended total dosage of 2.22 L, and practical experience shows that the cleaning performance is relatively inferior to PEG solution. It is.

As a result, in many cases, a total of 3.5 liters of Picolight ^® , the same ingredient as Prepopik ^® , is taken at 1.5 times the recommended dose.

In addition, phycosulfate-containing intestinal cleansers do not contain electrolytes, resulting in rare cases of hyponatremia and hypokalemia due to high doses, but serious side effects such as convulsions have been reported. Magnesium can cause hypermagnesemia, which is contraindicated in people with renal impairment.

Picosulfate-containing intestinal cleansers developed to address the difficulty of taking these most commonly used PEG preparations have improved dosage compliance, but have poor intestinal cleansing ability, and as a result still take large amounts of 2.3-3.5L. In addition, the situation has problems such as electrolyte abnormalities and side effects of hypermagnesemia.

Efforts to overcome these limitations of existing bowel cleansers remain unresolved, resulting in reliable bowel cleansing, Easy to take, there is an urgent need for the development of a new intestinal cleansing composition with minimal side effects.

[Start of invention]

The present invention is to solve the problems of the prior art as described above, the object of the present invention, while having both the ease of taking through the improvement of taste and safety for the human body is still up to 70% It is to provide a novel bowel cleansing composition with excellent cleansing power that greatly enhances the provision of adequate bowel preparation.

Another object of the present invention is to provide a novel bowel cleansing composition which can be economically mass produced and commercialized.

The bowel cleansing composition according to the present invention is composed of xylitol, consumption, glycerol, erytholi, tri, arabi, ribi, manny, galacta, fusi, eidi, and inoji as first cleaning components. At least one sugar alcohol selected from blemy, isomalt, malty, lacty, maltotri, maltotegra, and polyglyci; Ascorbic acid or a mixture of ascorbic acid and ascorbic acid as a second cleaning component; Picosulfate as a third cleaning component; And a water-soluble solvent, wherein the content of the first cleaning component is 10 g / L to 500 g / L based on the total composition, the content of the second cleaning component is 15 g / L to 500 g / L based on the total composition, and the third The content of the cleaning component is lmg / L to 100mg / L, and the capacity of the water-soluble solvent is 0.1L to 1.0L.

Intestinal cleansing composition according to the present invention by using a specific concentration of sugar alcohol, ascorbic acid, and picosulfate, while improving the taste and at the same time exhibited a superior bowel cleansing power than conventional bowel cleansing. In addition, the bowel cleansing composition according to the present invention greatly reduced the dose, thereby greatly improving the ease of taking and mildness. The bowel cleansing composition according to the present invention minimizes discomfort such as discomfort, abdominal pain and vomiting in the course of taking, thereby improving discomfort symptoms, and by containing bicarbonates such as sodium bicarbonate and potassium bicarbonate, It can prevent electrolyte abnormalities such as hyponatremia and hypokalemia, which can occur in detergents, and because it does not contain magnesium, it can be safely used in patients with kidney disorders without serious side effects due to hypermagnesemia. In addition, in the present invention, by using a combination of sugar alcohol and ascorbic acid in a certain concentration, it has excellent cleaning and antimicrobial activity compared to the dosage, eliminating the risk of the generation of flammable gas that may occur in the intestine after intestinal lavage, To ensure safety.

In particular, the most difficult reason for the intestinal cleansing from the patient's point of view is the inconvenience of large doses, poor detergent taste, abdominal pain, vomiting, etc. In the case of intestinal cleansers containing picosulfate, the poor symptoms of taking Due to the poor cleaning ability, many hospitals still have the inconvenience of taking a large amount of solution, totaling 3.51 _^ . The present invention contains sugar alcohol and ascorbic acid as a specific content instead of magnesium citrate, which is used in addition to the conventional picosulfate preparation, to increase intestinal cleansing and reduce the total dose including water to 2L or less, the purity of the dose Was raised. By solving these problems, the pain of the taking process was much more resolved. Nevertheless, the intestinal cleansing effect was improved even more, and by using certain sugar alcohols together with ascorbic acid, the risk of intestinal combustible gas generation could be eliminated as much as possible. It is very meaningful in that respect.

As described above, the bowel cleansing composition according to the present invention makes the bowel cleansing process much easier and safer, thereby greatly contributing to the activation of colorectal endoscopy, and as a result, early detection of colorectal cancer as well as resection of colorectal polyps. Maximize the prevention effect of colon like. In addition, the intestinal cleansing composition according to the present invention can be utilized for the treatment of constipation, etc. and symptom relief. According to the production method according to the present invention, it is possible to economically mass-produce and commercialize the intestinal cleansing composition.

[Brief Description of Drawings]

1 and 2 are photographs showing the results of culturing intestinal bacteria with respect to the composition for enteric cleaning according to one embodiment and comparative reference example of the present invention for each test organization.

Figure 3 is a photograph for showing the intestinal cleanliness after taking the intestinal cleansing composition according to one embodiment and comparative examples of the present invention.

4A and 4B are graphs showing the results of investigations on the ratio of clean bowel cleansing and unstable bowel cleansing after taking the bowel cleansing composition according to one embodiment and comparative examples of the present invention.

5 is a photograph showing a state in which a lot of bubbles occurred in the intestine after taking the intestinal cleansing composition prepared according to the prior art of the present invention.

BEST MODE FOR CARRYING OUT THE INVENTION

Hereinafter, with reference to the drawings attached to the present specification with respect to the present invention It explains in detail.

Intestinal cleansing composition according to the present invention, Xylitol, consumption (Sorbitol), glycerol (Glycerol), erythritol, Thritol (Threitol), Arabido (Arabitol) Ribitol, Mannitol, Galactitol, Fucitol, Iditol, Inositol, Volemitol, Isomalt At least one sugar alcohol selected from Maltitol, Lactitol, Maltotriitol, Maltote gradol, and Polyglycitol; Ascorbic acid or a mixture of ascorbic acid and ascorbic acid as a second cleaning component; Picosulfate as a third cleaning component; And a water-soluble solvent, wherein the content of the first cleaning component is 10 g / L to 500 g / L based on the total composition, the content of the second cleaning component is 15 g / L to 500 g / L based on the total composition, and the third The content of the cleaning component is lmg / L to 100mg / L, and the capacity of the water-soluble solvent is 0.1L to 1.0L. The sugar alcohol used as the first cleaning component in the present invention is a cleaning component that functions as a laxative by using at a high concentration. The sugar alcohols used as the first cleaning ingredient in the present invention are Xyl, consumption, glycerol, erythri, thrice, arabic, riboni, mantle, galacti, fusi, and eidiol. It is at least one selected from Remyl, Isomalt, Malty, Lactitol, Maltotritle, Maltotegrai and Polyglycile. In one aspect of the present invention, the sugar alcohol as the first cleaning component may include, for example, a consumption or a mixture of xyllets or consumption and xyllets.

Concerning the safety of sugar alcohol, consumption was no longer used for intestinal cleansing with manny after one explosive incident occurred during colon polypectomy after consumption intestinal cleansing using manny other than manny. It has been considered a substance that should not be.

Ladas et al.'S review, however, found that the explosion was not limited to Mannier's or consumption frame, but also after intestinal lavage with PEG or phosphate. Ladas et al reported a total of 20 gas explosions involving intestinal lavage between 1952 and 2006. Of these, two of four accidents during colon polypectomy were PEG and one was phosphate. As a formulation, one case was confirmed to have undergone intestinal lavage with mannni <"Colonic gas explosion during therapeutic colonoscopy with electrocautery", Ladas SD, Karamanolis G, Ben-Soussan E., World J Gastroenterol, 13, 5295-8, 2007X The gastrointestinal gas explosion that occurs during the surgical or therapeutic endoscopy after intestinal lavage is believed to have caused an explosion accident by generating explosive hydrogen gas and methane gas by decomposing the sugar alcohol, mannitol, and consumption by these intestinal bacteria. For reference, the explosive concentrations of methane and hydrogen gas are 5–15 vol% and 4-75 vol%, respectively.

However, hydrogen gas and methane gas were found to occur well when intestinal residues remained due to poor intestinal lavage, and not only mannni and consumption, but also other sugar alcohols, PEG or sugar alcohols. Intestinal gas explosion occurred after intestinal lavage using the formulation, suggesting that the cause of intestinal gas explosion is not only limited to the problem of using a specific intestinal cleanser, but also the state of intestinal lavage has a great effect. In other words, when many intestinal bacteria remain due to incomplete intestinal lavage, overly decomposed stool residues and sugar alcohols in the rinsing liquid are caused to generate hydrogen gas and methane gas above explosive concentrations.

Indeed, according to Nunes et al, Manniel's bowel cleansing effect was lower than that of PEG preparations, and according to the author's criteria, the suitability of bowel cleansing was only 75% compared to 90% of PEG preparations. preparation for colonoscopy using mannitol and polyethylene glycol-a prospective study ", Nunes BL, Belo SG, Pessoa MH, Lins Neto MA., Rev Bras Coloproctol, 28, 294--8, 2008.

From this fact, it is judged that unstable bowel cleansing has been affected by gas explosion accidents occurring after cleansing bowel using mantle and consumption in the past.

However, in the present invention, the sugar alcohol is used in combination with a specific content together with a second cleaning component such as ascorbic acid and a third cleaning component of picosulfate as the first cleaning component to have an excellent intestinal cleansing and antimicrobial activity compared to the dosage. The risk of explosion by one cleaning was eliminated and safety was ensured.

The content of the first cleaning component used in the present invention is in the range of 10 g / L to 500 g / L, 20 g / L to 200 g / L, 50 g / L to 150 g / L based on the total composition, but is not limited thereto. When the content of the first cleaning component is excessively high beyond the above range, generation of hydrogen gas and methane gas, which are combustible gases, may be increased. In addition, bowel cleansing may be incomplete when the content of the first cleansing component is out of the above range and the concentration is low.

Silver ascorbic acid used as the second cleaning ingredient in the present invention Water-soluble vitamin known as c is an essential vitamin that plays various roles in maintaining human health. Recently, as interest in ascorbic acid has increased, various kinds of health drinks including ascorbic acid have been released. By the way, the concentration of ascorbic acid contained in such health drinks and the like is prepared up to 10 mg / mL (ie, 10 g / L) or less.

However, in the present invention, ascorbic acid is a major cleaning component that functions as a laxative by being used at high concentrations, and also exhibits an antibacterial effect, thereby inhibiting the activity of intestinal bacteria and minimizing the generation of intestinal gas. To this end, the second cleaning component is formulated in a high content of 15 g / L to 500 g / L, 20 g / L to 300 g / L, or 30 g / L to 200 g / L, based on the total composition. If the content of the second cleaning ingredient is excessively high beyond the range of the above concentration, the acidity of the solution may be excessively increased to make it difficult to take it by excessively sour taste, and it may cause severe stomach irritation, causing nausea, nausea, vomiting, heartburn, etc. May cause. On the other hand, if the content of the second cleaning component is out of the range of the low concentration, the antibacterial effect is low, there is a risk of excessive generation of intestinal combustible gas.

The ascorbic acid salt used as the second cleaning component in the present invention is an alkali metal or alkaline earth metal salt of ascorbic acid. Alkali metals are for example sodium or potassium, and alkaline earth metals can be, for example, but not limited to. Ascorbic acid salts used in the present invention are sodium ascorbate or calcium ascorbate.

Ascorbic acid salts can lower the acidity of the solution compared with the case of ascorbic acid alone, and further increase the intestinal cleansing effect by suppressing the absorption of ascorbic acid, which is known to increase absorption as the acidity is higher. It may be 1 to 60: 40: second cleaning component is ascorbic case of ^"Broken acid and ascorbic acid salt mixture, and ascorbic acid to the ascorbic acid salt weight ratio is 99. If the mass ratio of ascorbic acid to ascorbic acid is out of the above range, excess sodium, calcium, potassium or magnesium may be absorbed by the human body, leading to electrolyte abnormalities or to hypercalcemia or hypermagnesemia.

Picosulfate used as the third cleaning component in the present invention is a component used as an irritant laxative. Phycosulfate is usually taken at 7.5 mg once or twice a day. The content of picosulfate as the third cleaning component used in the present invention may be 1 mg / L to 100 mg / L, 10 mg / L to 80 mg / L, or 15 mg / L to 70 mg / L based on the total composition.

Intestinal cleansing composition according to the present invention after intestinal gas removal or bowel cleaning It may further comprise a bubble forming inhibitor to remove the intestinal bubbles that occur frequently. In one aspect of the present invention, for example, simethicone may be used as the bubble formation inhibitor, but is not limited thereto.

In general, when a large amount of air bubbles are found during colonoscopy, simethicone diluent is made and injected into the intestine through a small channel of the endoscope insert, or a separately provided simethicone preparation is the last step in taking an intestinal cleanser. Use a separate dose from. However, when injecting the dimethicone diluent through the endoscope insertion pipe during the test, the range that the dimethicone diluent can be applied at a time is very limited. Therefore, when bubbles are formed over a wide range, there is a hassle of injecting dilution liquid more than a dozen times. In addition, even when the simethicone preparation is separately taken at the end of the intestinal cleansing process, the dosage is usually about 10 ml, and thus there is a limit to suppressing bubble generation throughout the large intestine.

In the present invention, by diluting the bubble formation inhibitor such as simethicone in the intestinal cleansing composition to solve this problem, it is very effective to suppress the bubble formation over all the parts of the large intestine in contact with the bowel cleansing liquid even at a small dose.

The content of the bubble-forming inhibitor used in the present invention, in one aspect, may be 100 mg / L to 2 g / L, 150 mg / L to 1.5 g / L, 200 mg / L to lg / L based on the total composition of simethicone, In the case of a bubble forming inhibitor other than ticon, it is not limited thereto. If the bubble formation inhibitor exceeds the upper limit of the above criteria, side effects such as abdominal pain, rash, facial or tongue edema or difficulty breathing may occur.

The water-soluble solvent used in the present invention may be, for example, water, carbonated water, alkaline ionized water, beverages and the like. In addition, as long as it can achieve the effect of the present invention as a beverage, there is no particular limitation on the kind, for example drip coffee, various juices, cola, cider, gin and tonic. In one aspect of the present invention, carbonated water or alkaline ionized water may be used as the water-soluble solvent. Carbonated water has a laxative effect on its own and is known to improve constipation in the elderly who suffer from chronic constipation. Alkaline ionized water can enhance the cleaning effect by neutralizing a part of the acidity of the bowel cleansing composition according to the present invention to lower the absorption of ascorbic acid.

The capacity of the water-soluble solvent may be 0.1L to l.OL, 0.1L to 0.9L, 0.2L to 0.8L, 0.3L to 0.7L, but is not limited thereto. If the volume of the solvent is less than 0.1L contained components may not be completely dissolved in the solvent, 1) if the amount is greater than the dosage may be less dose compliance.

The bowel cleansing composition of the present invention may further include ingredients for increasing the degree of obesity of the dose and for alleviating upper gastrointestinal symptoms such as nausea, nausea, and vomiting that are commonly observed during intestinal cleansing.

Since the bowel cleansing composition of the present invention containing a large amount of ascorbic acid may have difficulty in taking due to excessive acidity, it may include bicarbonates such as sodium bicarbonate and potassium bicarbonate as neutralizing ingredients. Can be.

The content of sodium bicarbonate can be used in the range of O.lg / L to 10 g / L based on the total composition. Beyond this range, due to excessive salty taste, the dose of ungwoomyeon drop, may cause hypernatremia. The content of potassium hydrogen carbonate may be 0.1 g / L to 20 g / L based on the total composition. Beyond this range, more potassium than the recommended daily intake can lead to hyperkalemia. Hyperkalemia can pose a risk, including heart failure. The bowel cleansing composition of the present invention further contains an extract or powder or concentrate of ginger, peppermint, chamomile, or the like as an aqueous solution for the purpose of improving the nausea, vomiting, and abdominal pain. It may contain more. These components function as gastrointestinal stabilizers and may be mixed in amounts of 5 g / L to 50 g / L based on the total bowel cleansing composition. If the content of these gastrointestinal stabilizer components is excessively high out of the above range, the bowel cleansing ability may be reduced by inhibiting bowel movement.

The bowel cleansing composition of the present invention may further contain known cleaning ingredients or auxiliary ingredients for enhancing the cleaning effect. Additional cleaning and cleaning enhancement components include, for example, citric acid, magnesium such as magnesium oxide, docuate sodium, senna extracts (such as sennoside), aloe extracts (such as aloe), garlic extracts (such as aalli and allicin), and pectin. (pectin), zinc such as zinc oxide, caffeine, and the like.

Citric acid is a natural ingredient contained in high concentrations such as gamgle and gives a sour taste and is used as a preservative of various drinks and foods. Citric acid is classified as a very safe substance and is recognized by the FDA and FAO / WHO as it is almost harmless even when taken in large doses. In the bowel cleansing composition of the present invention, citric acid may be included as an additional cleansing ingredient that functions as a laxative. The citric acid content used at this time is the whole composition Reference lg / L to 15g / L can be. Beyond this range, heartburn and strong sourness can reduce your dose.

In addition, the magnesium component is a substance having a function as a laxative. However, when taking an overdose of 3g or more at a time may cause side effects due to hypermagnesemia, so people with renal impairment should be used with caution.

Pectin and zinc can inhibit the intestinal absorption of ascorbic acid and increase its function as a laxative. The pectin content may be used in the range of O. lg / L to 2 g / L based on the total composition, and may not be dissolved when using a higher content. Zinc oxide can be used in the range of 10 mg / L to 400 mg / L based on the total composition, vomiting, nausea and the like may occur when ingested in excess of this range.

Caffeine can be used to counteract the lethargy that may appear in the intestinal cleansing process and to enhance the intestinal cleansing effect and is used in the range of 30 mg or less based on the total composition. Excessive overdose can lead to tachycardia, anxiety, and sleep disorders in sensitive people.

Docutate Sodium (10 mg / L to 400 mg / L range, can cause vomiting and abdominal pain when ingested in excess), Senna extract (sennoside, 10 mg / L to 50 mg / L range, can cause vomiting and abdominal pain when ingested), aloe Extract (ingestion of aloein 10mg / L to 50mg / L for long periods of time may cause intestinal deterioration), garlic extract (to use allinin and allicin in the range of 10mg / L to 5g / L, severe ingestion of stomach pain and vomiting ) Can also be used as an auxiliary laxative.

The bowel cleansing composition of the present invention may include a sweetener to improve the taste, and usable sweeteners include, for example, sucralose, maltodextrin, glucose, sucrose, and text. Rox (Dextrose), Saccharin (Saccharin), Aspartame (Spartame), Stevia (Stevia) and the like, but are not limited thereto. These sweeteners may be used in the range of 0.01 mg / L to 10 g / L based on the total bowel cleansing composition. Excessive use beyond this range can lead to unpleasant symptoms such as nausea and nausea.

Intestinal cleansing composition of the present invention may be added to the appropriate amount of edible fruit flavor in order to increase the dose. These fruit flavors may include strawberry flavor, orange flavor, apple flavor, grape flavor, lemon flavor, banana flavor, cherry flavor, and the like.

Enteric cleaning composition of the present invention to prevent the oxidation of ascorbic acid In order to add an appropriate amount of antioxidant. Such antioxidants include, for example, ferrulic acid, glycine, histidine amino acids, hyaluronic acid, tocope, and the like, but are not limited thereto.

In addition, the bowel cleansing composition of the present invention may further include an adsorbent for adsorbing trace iron and copper ions that may be contained in the water-soluble solvent. Such adsorbents include, for example, Versene CA chelating agent (Dow), but are not limited thereto.

The bowel cleansing composition according to the present invention may be one-part or two-part. In one aspect of the present invention, the bowel cleansing composition comprises a first cleansing component, a second cleansing component, and a third cleansing component, and, if necessary, all components of the bubble forming inhibitor, the gastrointestinal stabilizing agent 1, and other additives are water-soluble solvents. Can be packaged together in one component.

In another aspect of the present invention, the bowel cleansing composition may be packaged in two-part form. For example, the first cleaning component, the second cleaning component, and the third cleaning component are packaged together and the water-soluble solvent is packaged separately, or the second cleaning component and the water-soluble solvent are packaged together and the first cleaning component is A third cleaning component is packaged separately, or the first cleaning component, the third cleaning component and the water soluble solvent are packaged together and the second cleaning component is packaged separately, or the first cleaning component, the third cleaning component and the water soluble component A portion of the solvent is packaged together and a portion of the second cleaning component and the water-soluble solvent are packaged together, or the first cleaning component, the second cleaning component, the third cleaning component and a portion of the water-soluble solvent are packaged together and the water-soluble solvent is The remainder of the solvent may be packaged separately, but is not limited thereto. In addition, foam forming inhibitors, gastrointestinal stabilizers, and other additives may be combined in various two-part forms as needed.

A method of packaging and using the bowel cleansing composition of the present invention in the form of a high concentration liquid and a vehicle as a two-part type will be described. For example, after dissolving all components such as the first cleaning component, the second cleaning component, and the third cleaning component and, if necessary, the foaming inhibitor, the gastrointestinal stabilizer, and other additives in a minimum amount of a water-soluble solvent, It can be diluted in the beverage of choice by the user (the remaining volume as an aqueous solvent). In this case, the capacity of the water-soluble solvent to form a high concentration may be 0.05L to 0.2L, the amount of the beverage, the vehicle selected by the user may be the remaining capacity as a water-soluble solvent. If necessary, the solid components of the composition are packaged separately and a water-soluble solvent is After packaging, users can mix and use the whole ingredient at the time of taking it. In addition to this can be packaged in various forms, the form of the two-part composition is not limited to the above-described packaging method.

In preparing the bowel cleansing composition according to the present invention, the first cleansing component, the second cleansing component, and the third cleansing component and, if necessary, all of the components, such as a bubble formation inhibitor, a gastrointestinal stabilizer, and other additives, are simultaneously mixed with a water-soluble solvent. Alternatively, each component may be separately prepared and blended step by step.

For example, the method for preparing a bowel cleansing composition according to the present invention comprises the steps of: forming a first blend comprising sugar alcohol as the first cleansing component; Forming at least 12 blends of ascorbic acid or ascorbic acid with ascorbic acid as a second cleaning component; Forming a nearly 13 blend comprising picosulfate as a third cleaning component; Forming a fourth blend comprising a bubble forming inhibitor as needed; Forming a fifth blend comprising a gastrointestinal stabilizer as needed; And combining the first to fifth blends with a water-soluble solvent to form a bowel cleansing composition.

In another aspect of the present invention, the method for preparing the bowel cleansing composition according to the present invention comprises blending the first blend, the second blend, and the third blend with the fourth blend and the fifth blend as necessary in a water-soluble solvent. Prior to this, the method may further include pre-mixing the first to fifth blends in any combination.

In another aspect of the present invention, a method for producing a bowel cleansing composition according to the present invention includes, for example, the first blend, the second blend, and the third blend, and, if necessary, the fourth blend. It is possible to prepare a high concentrate form containing a fifth formulation and a part of a water-soluble solvent in advance, and to drink by adjusting to the specific concentration and content by diluting to various drinks as a vehicle at the time of taking. At this time, a beverage that can be selected by the user as a vehicle is not limited as long as it is a water-soluble solvent, and may be, for example, water, carbonated water, alkaline silver water, or beverage, and may be the same as or different from the water-soluble solvent in a high concentration liquid. In addition, as long as the effect of the present invention can be achieved as a beverage, there is no particular limitation on the kind thereof. Examples include drip coffee, various juices, cola, cider, gin and tonic.

In the method for preparing the bowel cleansing composition according to the present invention, a method of blending each component, in the case of solids, particle shape and size, pH, preparation temperature, stirring condition, packaging container, packaging material, vacuum packaging or gas substitution packaging, etc. The packaging method, etc. is the type, type, transportation, storage method, etc. Can be adjusted accordingly.

The method of taking the bowel cleansing composition according to the present invention takes into account the intestinal sensitivity of the subject. Begin taking 3-5 hours before colonoscopy and take 5-10 doses every 5-10 minutes, 50–lOOcc at a time, without limitation. In addition, the ingestion time of the intestinal cleansing composition according to the present invention may be taken over an hour to 1 hour and 30 minutes, for example, but if thirst is added, an appropriate amount of mineral water may be additionally added, but is not limited thereto.

Intestinal cleansing composition according to the present invention by containing a certain concentration of sugar alcohol, ascorbic acid and picosulfate, not only shows an improved intestinal cleansing power even at a significantly reduced dose, but also provides the convenience of taking in a very small dose, It does not contain disgusting ingredients, and does not cause or minimize discomfort symptoms such as nausea, vomiting and gas bloating, and is safe by inhibiting the production of intestinal flammable gas in the human body.

The production method according to the present invention is economically capable of mass production and commercialization of a high performance bowel cleansing composition.

Since the bowel cleansing composition of the present invention has the ease and safety of taking excellent cleansing power, not only bowel cleansing for colonoscopy, but also bowel cleansing, pretreatment such as hemorrhoids, chronic constipation or acute constipation It can be used for treatment and prevention. The present invention will be described in more detail with reference to the following Examples. However, the following examples are provided only for the purpose of illustration in order to help the understanding of the present invention is not limited to the scope and scope of the present invention.

Example 1

As a solvent, 45 g of Xyl, 25 g of ascorbic acid, 20 mg of picosulfate, 200 mg of simethicone, 200 mg of sodium bicarbonate, 1.4 g of potassium bicarbonate, and 20 mg of sucralose were prepared as a solvent to prepare a 150 ml high-concentrate solution. As an example, 350 ml of carbonated water was prepared to prepare a two-component bowel cleansing composition.

Mixing was performed by mixing all the powder form components at once and then pouring the solvent to dissolve. Care must be taken in the formulation because a large amount of carbonic acid (C0 ₂ ) gas generated by the neutralization reaction between acidic ascorbic acid and alkaline bicarbonate creates severe foaming. These bubbles were prepared in advance by diluting a 1:10 dilution of Gasocol® containing simethicone, a defoamer. If it mixes suitably, it can suppress well and a compounding process can be advanced smoothly. Since the simethicone raw material drug containing about 30% of silicon is insoluble in water at all, in this embodiment, a gasoline ^@ , which is a liquid medicine containing simethicone as a main component, was used as a substitute.

Comparative Reference Example 1 was prepared as a comparative sample for the solution of Example 1 for an in vitro experiment for confirming the safety of the sugar alcohol used as the first cleaning component in the present invention.

Comparative Reference Example 1 is 10 ml of a picoliteite solution, and the picoliteite solution is diluted in bottled water according to the recommended dosage method. The concentration of the active ingredient is the same as that used for intestinal lavage.

<Test Example 1: Safety experiments related to the generation of flammable gas (in vitro experiment)> Measurement of hydrogen gas and methane gas concentration

Regarding the safety test for intestinal flammable gas generation, it is not easy to collect appropriate samples from the subject during the colonoscopy or to measure the intestinal gas, and the results of limited examples confirmed in various conditions after the intestinal cleaning of each subject It is not valid to conclude that the difference according to each cleaning solution with only, indirectly to determine whether or not the risk of the composition prepared by Example 1 through in vitro experiments that can be carried out under the same conditions.

To this end, in each solution of Example 1, Comparative Reference Example 1, the control (bottled water), the solution obtained by diluting the stools obtained from five persons was mixed, stored in a 500 ml container, 20 ml, and stored at room temperature for 18 hours. Gas concentration in each container was measured. At this time, the diluted solution of the stool was taken from five different people, and each person's 3g side was diluted with 100 ml of bottled water to make five kinds of fecal lime solution.

The experimental method is described in detail as follows.

The stool dilution made from the stools collected from five people was divided into 10 ml each of three containers for each individual to make three containers containing the same stool limestone solution. Was prepared.

To each of the three vessels containing the same fecal lime solution of each person, 10 ml of the experimental solutions of Example 1, Comparative Reference Example 1 (picolite), and control group (bottled water) were added.

Combine the fecal diluent with each test solution, and then close the lid of the container. Tightly closed and stored at room temperature for 18 hours.

Thereafter, hydrogen and methane gas concentrations in each vessel were measured using a Geotech GA5000 gas meter (manufactured by Landtech, UK). The Geotech GA5000 gas meter can measure m0 gas in _V0 l% and hydrogen gas up to 0–100 ppm.

As a result of measuring the gas concentration in a total of 15 containers, the average of the measurement values of the hydrogen gas and methane gas concentration, which are combustible gases, is shown in the table below.

Table 1

As shown in the above table, the bowel cleansing composition of Example 1 was not detected at all, and the methane gas concentration was 0.13%, lower than that of the control, and lower than the bowel cleansing solution of the picosulfate formulation of Comparative Reference Example 1. That is, it can be confirmed that the bowel cleansing composition according to the present invention is the safest in relation to the intestinal combustible gas generation.

Culture test

After the gas concentration measurement, the mixed solution contained in each container,

To the two inspection institutions of the Seoul National Institute of Medical Sciences (SCL) and the Green Cross Medical Foundation Laboratory, which have been certified as the outstanding laboratory of the Korean Diagnostic Medical Association (SCL). After incubation in the medium for 48 hours, the colony count of each container was measured.

The average number of strains grown for each experimental solution is shown in the table below. In addition, the intestinal bacteria culture results for Example 1, Comparative Reference Example 1 and the control in Figures 1 and 2 are shown for each test institution.

Table 2

(Unit 10 ⁵ CFU / ml) The strain number measurement result confirms more clearly the antimicrobial effect of the bowel cleansing composition according to the present invention. Specifically, in Example 1, as a result of culturing all five stool dilutions, not only Comparative Reference Example 1 using picolite, but also fewer strains than the control group. That is, in the case of Example 1, it can be seen that the bacteria capable of generating combustible gases such as hydrogen gas and methane gas are substantially suppressed. Although these results are the result of in vitro in vitro experiments, it is confirmed that the bowel cleansing composition according to the present invention is safer than any conventional bowel cleansers in relation to intestinal combustible gas generation.

On the other hand, in the case of Comparative Reference Example 1 using picorite, it was confirmed that the number of cultured strains was increased than that of the natural control group. This has not been a problem yet, but it appears to suggest the use of this type of enteric cleaner is a risk of promoting flammable gas generation. This fact shows that the intestinal cleansers according to the present invention are very safe with respect to the generation of flammable gases even though they contain sugar alcohols.

Therefore, on the basis of these results, it can be seen that the composition of Example 1 containing xylitol, ascorbic acid, and physulfate as a main component is a very safe composition with respect to intestinal bacterial growth and consequent intestinal flammable gas generation risk. The result of this excellent antimicrobial effect suggests that when the bowel cleansing composition according to the present invention is used as a laxative for pre- bowel treatment, it can make a great contribution to reducing the incidence of post-operative infection. For reference, during bowel surgery, contamination due to intestinal contents may occur, and therefore, antibiotics are pre-administered before surgery to prevent infection at the surgical site. However, when the intestinal treatment with the bowel cleansing composition according to the present invention, the bacteria in the intestinal contents are suppressed, thereby reducing the possibility of infection even when contamination due to the intestinal contents occurs.

This effect is more effective in the bowel cleansing composition according to the present invention, considering that the conventional bowel cleansing liquid is not only used for bowel cleansing before colonoscopy, but also as a causative agent for bowel treatment before colorectal surgery. It can be increased. From the above two in vitro safety experiments, a novel The bowel cleansing composition has the lowest risk by minimizing the generation of hydrogen gas and methane gas, which are combustible gases, and inhibiting bacterial growth, compared to other bowel cleansers.

Comparative Examples 1 and 2 were prepared for comparative experiments on the ease of taking the intestinal cleansing composition according to the present invention, the effect of cleaning each bowel, and safety.

Specifically, the intestinal three compositions in which the conventional commercial enteric cleaner picolite and coolprep were mixed with water in the recommended blending amounts were prepared as Comparative Examples 1 and 2, respectively. The kind of each enteric detergent given in Comparative Examples 1 and 2 and the amount of water blended are shown in Table 3 below.

Table 3

Clap: 56.402 g of serving content per package, manufactured by Taejun Pharmaceutical Co., Ltd. The cleaning performance analysis and dose compliance of the bowel cleansing compositions prepared in Example 1 and Comparative Examples 1 and 2 were performed.

Specifically, Comparative Example 1 for each colonoscopy subject was cited.

Intestinal cleansing power, ease of ingestion, and safety were tested through 63 subjects, 49 in Comparative Example 2, and 161 in Example 1. Example 1 and Comparative Examples 1 and 2, the specific taking method is as follows.

Dosing method of Example 1 starts 5 hours before the scheduled time of the test

In principle, 500 ml of enteric lavage solution was taken five times every 30 minutes, one half cup of 100 mK5 sip paper cups at a time. After drinking 100 ml of intestinal lavage solution, an additional 200 ml of drinking water was added every 15 minutes. This took a total of 120 minutes to take the cleaner.

Comparative Example 1, namely, 2.3L of picolite, was drank at 150 ml of water by drinking one packet provided 5 hours before the test day at 7:00 p.m. on the day before the test, followed by additional drinking of 1 L of water over 1 hour. I took it one more time in the same way before.

Comparative Example 2, that is, 3L of Cleprep, 1L of the preparation solution at 7 pm the day before the test The method was taken for 1 hour (250 ml every 15 minutes), and drinking 1 L of the preparation solution again for 1 hour 5 hours before the test day. After the evening and the day after drinking the dilution solution, they were asked to drink another 500 mL of water.

Intestinal cleansing power was examined by two items: ① intestinal cleanliness and ② bubble volume.

Cabinet cleanliness

Intestinal cleanliness is determined by the surgeon based on the criteria shown in Table 4 and FIG. 3, based on the criteria of Excellence, Good, Fair, Poor and Fail. Evaluation was divided into stages. Intestinal cleanliness evaluation was conducted by blind test without any information about the bowel cleansing composition that the patient drank for the fair evaluation without exposing it to the surgeon performing the colonoscopy. Table 4

Table 4 and the evaluation results of the intestinal cleanliness according to Figure 3 and the criteria are shown in Table 5 below.

Table 5

Intestinal cleanliness (%)

Sample number O number

Excellent Normal Poor Inspectability Example 1 36.7 55.7 5.7 1.9 0

Comparative Example 1

15.9 41.3 22.1 15.9 4.8

(Picolite)

Comparative Example 2 (Cool Wrap) 16.3 51 22.5 10.2 0 In addition, the results are classified into 'clean bowel cleansing', which is suitable for intestinal endoscopy, and 'unstable bowel cleansing,' which is insufficient or impossible to perform an accurate test, and is shown in FIGS. 4A and 4B. 'Clean bowel cleansing' includes excellent and excellent condition. 'Fouled bowel cleansing' usually includes inadequate and untestable condition.

As shown in Table 5, FIG. 4A and FIG. 4B, the clean bowel cleansing rate of Example 1 was the best at 92.4%, and the clean cleansing rate of Comparative Example 1 was only 57.2%. It became. In Comparative Example 2, the ratio of clean bowel washing was 67.3%. These results are in part consistent with the content of foreign papers which reported that the intestinal cleanliness of PEG and phosphate preparations was 70 to 75% <"(： 0101 03 (： 0 preparation”, ASGE technology committee, GASTROINTESTINAL ENDOSCOPY, 69 (No. 7): 1201-1209, 2009>.

By the way, unclear cleaning power as in Comparative Examples 1 and 2 makes accurate intestinal endoscopy impossible, which causes a serious problem in reality. In other words, enteroscopic examination is usually performed every 4-5 years. If the result of intestinal endoscopy performed after a difficult bowel cleaning is inaccurate and no polyp or early colon cancer is found, The disease may be left untreated for 4 to 5 years until the test, which can lead to polyps that develop into cancer or early colon cancer into advanced colon cancer.

In addition to intestinal cleanliness, there is an important factor for accurate intestinal endoscopy: the presence of bubbles (bubbles) in the large intestine. Almost all bowel cleansers tend to generate bubbles in the large intestine after bowel cleansing. Therefore, it is essential to prevent or eliminate these bubbles in order to look closely inside the intestine to find even small lesions. After taking the intestinal cleansing compositions of Examples 1 and Comparative Examples 1 and 2, the presence and absence of bubbles were observed, and the results are shown in Table 6 below. At this time, the degree of existence of bubbles was evaluated by dividing into three stages of none, a little, a lot. In addition, Figure 5 is a photograph showing a state in which a lot of bubbles in the intestine after taking the intestinal cleansing composition prepared according to Comparative Example 1. Table 6

As shown in the above results, in Example 1, no bubbles were generated in 92.8%, but in Comparative Examples 1 and 2, the ratio of no bubbles was only about one third, especially one of three persons. In more than one person, a large amount of bubbles were generated, which greatly disturbed the test. Bubbles can be washed off with medication during colonoscopy, but they require considerable effort and time because of the limited scope of washing at one time. In other words, the occurrence of excessive bubbles not only interferes with the smooth colonoscopy, but also causes missing small lesions. The bowel cleansing composition of Example 1 almost completely prevents the occurrence of air bubbles, shortens the inspection time and at the same time allows more time to observe the lesions, and also makes it easier to find small lesions due to the clear view. It can increase the diagnosis of disease.

Ease of taking was evaluated in four categories: ① taste of detergent, ② discomfort after taking, ③ whether to recommend to family, and ④ need for improvement.

Cleaner's Taste

The taste of the detergent is divided into three stages of very turtles, little turtles, alright, and subjectively judged the degree through a questionnaire, and obtained the percentage of the evaluation value is shown in Table 7 below.

Table 7

Intestinal cleansing composition (%)

Sample number

Very turtle little turtle passable

Example 1 0 4.9 95.1

Comparative Example 1

0 6.1 93.9

(Picolite)

Comparative Example 2 (Clep Prep) 14.3 53.1 32.6 As shown in the results, in Example 1, 95.1% of the taste of the detergent was good, and Comparative Example 1 was 93.9%, but Comparative Example 2 was only 32.6%.

Symptoms of discomfort after taking

'Discomfort symptoms after taking the questionnaire classified into four categories: abdominal pain, gas bloating, vomiting, thirst. Investigations were made to indicate the discomfort symptoms perceived by the patient himself, and the percentage of the evaluation value was obtained and shown in Table 8 below.

Table 8

As shown in Table 8, Example 1 can be seen that all of the items such as abdominal pain, gas distension, vomiting and thirst lower than or similar to the conventional intestinal detergents exhibited discomfort symptoms. In Comparative Example 2, the frequency of vomiting was quite high, which seems to be related to the disgusting taste of the PEG formulation.

Willing to recommend

The percentage of persons who answered negatively that they did not want to recommend by surveying whether the test subjects were willing to recommend to the family is shown in Table 9 below. Table 9

As shown in the above results, in the case of Comparative Example 2, the depreciation ratio was considerably high, at 53%.

On the other hand, Comparative Example 1 was relatively low as 7% of the non-recommended ratio was a little higher than Example 1. This can be seen as a result of the 2.3 L dose have.

Need for improvement

A survey was conducted on whether the intestinal cleansers that were taken needed to be improved, and the percentage of those who answered that there was a need for improvement was shown in Table 10 below.

Table 103

According to the above results, in the case of Example 1, it can be seen that the lowest rate of answers to the necessity of improvement shows the highest satisfaction. On the other hand, in Comparative Example 1, 7% and Comparative Example 2 answered that there is a need for improvement at 58%.

Comparison of preference between Example 1 and other detergents

Among the subjects using the bowel cleansing composition of Example 1, 89 patients with past bowel cleansing experience were surveyed whether the ease of taking was improved compared to the previous bowel cleansing experience, and the results are shown in Table 11 below. Indicated.

Table 11

As you can see from the above results, people who have taken other cleaners

About 78.7% said it was easier to take the bowel cleansing composition of Example 1, and no one was more difficult. This result can be said to be an indirect comparison between Comparative Examples 1 and 2, and Example 1, which is a conventional enteric cleaner, and it can be seen that the preference for Example 1 is very high.

Test Example 4: Safety (In Vivo Experiment)

The safety of each intestinal cleanser was determined by blood test. Ascorbic acid concentrations and other hematological tests were performed to evaluate.

Intestinal Gas Measurement

Examples of combustible gas generation In addition to confirming the safety of the intestinal cleansing composition according to the present invention by the above in vitro experiments, each of the ten people who were intestinal cleansing with the intestinal cleansing composition according to Example 1 Intestinal gas collected during colonoscopy was actually measured. As a result, the concentration of methane gas was 0.1 to 0.3 Vol%, and the concentration of hydrogen gas was 1 to 7 ppm. Therefore, it was directly confirmed that the gas concentration was 5% and 4,000 ppm, which is the lowest explosive concentration of these gases.

Blood Ascorbic Acid Concentration

After taking each intestinal cleansing composition, immediately before colonoscopy, blood was collected from the test subjects and asked to check the concentration of ascorbic acid in blood by SCL (Seoul Medical Research Institute), a laboratory that is equipped with ascorbic acid blood concentration measurement equipment. The average of is shown in Table 12 below.

Table 12

Reference values for blood ascorbic acid concentrations range from 2 to 20 pg / mL. In Comparative Example 3, in which 21.2 g of ascorbic acid is mixed and in Example 1 containing 25 g of ascorbic acid, it is foreseeable that the blood ascorbic acid concentration temporarily rises above the reference value. However, since ascorbic acid is water-soluble, it is known that blood ascorbic acid exceeding the reference value is excreted immediately through the kidneys, thereby normalizing blood levels.

Official data from the National Cancer Institute also shows that high levels of ascorbic acid are harmless to humans. page 1 / AllPages).

Since the 1970s, many studies have been conducted to determine whether a large amount of ascorbic acid is administered by intravenous injection for treatment of various cancers. There are many different opinions on the effectiveness of the treatment, The fact is that ascorbic acid can be safely administered intravenously up to 1.5 g / kg in healthy individuals, except in patients with G6PD deficiency, kidney disease or people with urinary tract stones <"Vitamin C pharmacokinetics: implications for oral and intravenous use", Padayatty SJ, Sun H, Wang Y, et al., Ann Intern Med 140 (7), 533-7, 2004; "Phase I clinical trial of iv ascorbic acid in advanced malignancy", Hoffer LJ, Levine M, Assouline S, et al., Ann Oncol 19 (11), 1969-74, 2008.

In addition, in the Phase I clinical study conducted in 2013, 15 g of ascorbic acid was injected intravenously over 4 minutes twice a week for 30 minutes to raise blood ascorbic acid concentration to at least 350 mg / dL (3,500 yg / mL). ， Very well tolerated and no serious side effects reported. <"Pharmacological ascorbate with gemcitabine for the control of metastatic and node-positive pancreatic cancer (PACMAN): results from a phase I clinical trial", Welsh JL, Wagner BA, van't Erve TJ, et al., Cancer Chemother Pharmacol 71 (3), 765-75, 2013

These are official data published on the US National Cancer Center's website, and it can be seen that high concentrations of blood ascorbic acid do not harm the human body at all. In addition, the above-mentioned ascorbic acid blood concentration of 3,500 g / mL is 175 times the upper limit of the reference value, and the average blood ascorbic acid concentration of 32.4 yg / mL measured after using the bowel cleansing composition of Example 1 in the present invention was 108. It is twice as much concentration. That is, it can be seen that increasing the ascorbic acid concentration after taking the intestinal cleansing composition of Example 1 does not cause any problem to the human body.

For this reason, Moviprep®, the same ingredient as the product Kulprep (used in Comparative 2), which has been found to temporarily increase the concentration of ascorbic acid in the blood, seems to have been approved by the US FDA as an intestinal cleanser without any problems. ^'

Other blood chemical tests

Other blood chemistries include urea nitrogen (BUN), creatinine, and liver enzymes AST (( ⁾ T) and ALT, which measure magnesium levels, electrolyte levels, and kidney function. The concentration of (GPT) was measured and the results are shown in Tables 13 to 16 below. Blood was collected immediately before colonoscopy and measured according to a routine test at the Department of Diagnostic Laboratory, Joy Hospital. Table 13

Table 14

Table 15

As shown in the above results, the concentration of the electrolyte in all enteric detergents except for the magnesium concentration approaching the upper limit of 2.5 mg / dL (reference value 1.58 to 2.55 mg / dL) in the subject using the enteric cleaning composition of Comparative Example 1 Indicators No abnormalities were found in the test results of BUN and creatinine, liver enzymes AST and ALT.

The reason for the increase in magnesium blood concentration near the upper limit in the test subject using the bowel cleansing composition of Comparative Example 1 is that a large amount of magnesium oxide (10.5 g) is included in the picoliteite component.

In short, like other bowel cleansing agents, it was confirmed that the bowel cleansing composition according to Example 1 is a safe drug that does not cause abnormal conditions in blood chemistry. Industrial Applicability

Intestinal cleansing composition according to the present invention by using a certain concentration of sugar alcohol, ascorbic acid, and picosulfate in combination, while improving the taste at the same time exerted a superior bowel cleansing power compared to the existing three tablets. In addition, the bowel cleansing composition according to the present invention greatly reduced the dose, thereby greatly improving the ease of taking and wooseong. The bowel cleansing composition according to the present invention minimizes discomfort such as discomfort, abdominal pain and vomiting in the course of taking, thereby improving discomfort symptoms, and by including bicarbonate such as sodium bicarbonate and potassium bicarbonate, the existing picosulfate is included. It can prevent electrolyte abnormalities such as hyponatremia and hypokalemia, which can occur in intestinal cleansers, and do not contain magnesium, so it can be safely used in patients with kidney disorders without serious side effects due to hypermagnesemia.

Claims

【Scope of Claim】

【Claim 1】

As the first cleansing ingredient, xyly, sobittle, glycerol, erythri, thyri, arabitl, libirl, mannitl, galactyl, hussi, idyl, inogitl, bolemitl, isomalt, At least one sugar alcohol selected from maltyl, lactate, maltotri, maltotegra, and polyglycidyl; Ascorbic acid or a mixture of ascorbic acid and ascorbic acid salt as a second cleaning ingredient; Crab 3 Picosulfate as a cleaning ingredient; And a water-soluble solvent,

The content of the first cleaning component is 10 g/L to 500 g/L based on the entire composition, the content of the second cleaning component is 15 g/a to 500 g/L based on the entire composition, and the content of the third cleaning component is 10 g/L to 500 g/L based on the entire composition. A composition for bowel cleansing, characterized in that the standard is lmg/L to 100mg/L, and the volume of the water-soluble solvent is 0.1L to 1.0L.

【Claim 2】

According to clause 1,

A composition for bowel cleansing, wherein the composition further includes a bubble formation inhibitor, and the content of the bubble formation inhibitor is 100 mg/L to 2 g/L based on the total composition.

【Claim 3】

In paragraph 2,

A composition for bowel cleansing, wherein the foaming inhibitor is simethicone.

【Claim 4】

According to clause 1,

The composition further includes a bicarbonate selected from sodium bicarbonate and potassium bicarbonate, and if the content of the bicarbonate is sodium bicarbonate, it is 0. lg/L to 10 g/L based on the entire composition, and if it is potassium bicarbonate, the content of the bicarbonate is 0.1 g/L to 10 g/L based on the entire composition. A composition for bowel cleansing, characterized in that the standard is 0.lg/L to 20g/L.

【Claim 5】

In clause 1,

A composition for intestinal cleansing, wherein the composition further includes a gastrointestinal stabilizer selected from ginger, mint, and chamomile, and the content of the gastrointestinal stabilizer is 5 g/L to 50 g/L based on the total composition.

【Claim 6】

According to clause 1, A composition for intestinal cleansing, characterized in that the composition further contains a cleansing ingredient selected from citric acid, magnesium, docusate sodium, senna extract, aloe extract, garlic extract, pectin, zinc, and caffeine.

【Claim 7】

According to clause 1,

A composition for bowel cleansing, wherein the first cleansing ingredient is xylittle.

【Claim 8】

In clause 1,

A composition for bowel cleansing, characterized in that the first cleansing ingredient is soybean.

【Claim 9】

In paragraph 1,

A composition for bowel cleansing, characterized in that the first cleansing ingredient is a mixture of xylyl and sorghum.

[Claim 10]

In clause 1,

When the second cleansing ingredient is a mixture of ascorbic acid and ascorbic acid salt, the mass ratio of ascorbic acid to ascorbic acid salt is in the range of 99:1 to 60:40.

【Claim 11】

In clause 1,

A composition for bowel cleansing, wherein the water-soluble solvent is water, carbonated water, alkaline ionized water, or a beverage.

【Claim 12】

In clause 1,

A composition for bowel cleansing, characterized in that the water-soluble solvent is carbonated water.

【Claim 13】

In clause 1,

A composition for bowel cleansing, characterized in that the content of the first cleaning ingredient is 50 g/L to 150 g/L based on the total composition.

【Claim 14】

In clause 1,

A composition for bowel cleansing, characterized in that the content of the second cleaning ingredient is 30 g/L to 200 g/L based on the total composition.

[Claim 15]

In clause 1,

A composition for bowel cleansing, characterized in that the content of the third 'cleansing ^' component is 10 mg/L to 80 mg/L based on the total composition.

【Claim 16】

In clause 1,

A composition for bowel cleansing, characterized in that the volume of the water-soluble solvent is 0.3L to 0.7L.

[Claim 17]

According to any one of claims 1 to 16,

A composition for bowel cleansing, characterized in that the composition is a one-component type. 【Claim 18】

According to any one of claims 1 to 16,

A composition for bowel cleansing, characterized in that the composition is a two-component type. 【Claim 19】

In paragraph U8,

The composition is (i) packaged as a highly concentrated solution in which all ingredients are mixed in 0.05 L to 0.2 L out of the total volume of the water-soluble solvent, and (ii) the remaining volume excluding that used in the high concentrate out of the total volume of the water-soluble solvent. A composition for bowel cleansing, characterized in that it is a two-component type consisting of separately packaging.