Composition for intestinal lavage with reduced dosage on the day of examination

Abstract

The present invention relates to a composition for intestinal lavage, and more specifically, to a composition for intestinal lavage with enhanced safety by reducing the dosage on the day of the examination for which intestinal lavage is required.

Description

Technical Field

[0001] The present invention relates to a composition for colon cleansing, and more specifically, to a composition for colon cleansing that significantly improves safety and convenience of administration by reducing the dosage on the day of the examination that requires colon cleansing.

Background Art

[0002] Colonoscopy is a very effective means of completely preventing colon cancer. However, the acceptance rate of colonoscopy is low worldwide, and one of the main reasons for the low acceptance rate is the difficulty of taking colon cleansing agents. Unfortunately, most colon cleansing agents have a large dosage reaching 2L to 4L, and most people dislike the taste and find it very difficult to take. In particular, all existing colon cleansing agents have inconvenience in the method of administration in that a very large amount of 1L to 2L of colon cleansing agent and water must be taken in a short time at dawn on the day of colonoscopy.

[0003] Furthermore, such a method of taking existing colon cleansing agents may also cause problems with the safety of the subject. First, two-thirds of the patients undergoing colonoscopy also undergo gastroscopy at the same time. In gastroscopy, fasting for at least 8 hours including water is recommended, which is in direct conflict with the method of taking colon cleansing agents for colonoscopy. Also, most endoscopies are performed under sedation anesthesia, but a mixed solution such as a colon cleansing agent requires fasting for at least 3 hours before sedation anesthesia ("Simple Sedation Therapy for Non-Anesthesia Pain Medicine Medical Staff", Min Doje, Department of Anesthesiology and Pain Medicine, Ansan Hospital, Korea University, 2020).

[0004] In order to further activate colonoscopy and maximize the prevention of the occurrence of colon cancer with a more accurate examination, there is a need for a new composition of colon cleansing agent that reduces the total dosage, improves the taste to enhance the convenience of administration, and in particular, significantly reduces the amount to be drunk at dawn on the day of the examination to enhance safety.

Prior Art Documents

Non-Patent Document

[0005]

Non-Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0006] Technical Problem An object of the present invention is to provide a composition for bowel cleansing that epochally reduces the dosage on the day of examination requiring bowel cleansing, shows an excellent bowel cleansing effect while enhancing safety.

Means for Solving the Problems

[0007] <Summary of the Invention> The present invention is a composition for bowel cleansing to be taken before an examination requiring bowel cleansing, the composition is taken separately on the day before and on the day of the examination, and the total dosage taken on the day of the examination is 700 mL or less, to provide a composition for bowel cleansing.

[0008] The present invention is also a bowel cleansing method including administering a composition for bowel cleansing to a human before an examination requiring bowel cleansing, the composition is administered separately on the day before and on the day of the examination, and the total dosage (or dosage) administered on the day of the examination is 700 mL or less, to provide a bowel cleansing method.

[0009] The present invention is also a composition for bowel cleansing for use in taking before an examination requiring bowel cleansing, the composition is taken separately on the day before and on the day of the examination, and the total dosage taken on the day of the examination is 700 mL or less, to provide a composition for bowel cleansing.

[0010] In one embodiment, the total dose taken or administered on the day of the examination may be 600 mL or less.

[0011] In one embodiment, the total dose taken or administered on the day of the examination may be 500 mL or less.

[0012] In one embodiment, the total dose taken or administered on the day of the examination may be 360, 400, 450, 480, 500, 568 or 600 mL.

[0013] In one embodiment, the total dose taken or administered on the day before and the day of the examination may be 1.0 L to 4.0 L, and it may be a composition for intestinal lavage.

[0014] In one embodiment, the composition for intestinal lavage is a preparation solution obtained by dissolving a composition in the form of a powder, granule, liquid preparation, tablet or capsule containing an active ingredient in a water-soluble solvent; and separately contains a water-soluble solvent. The composition for intestinal lavage is administered in such a manner that after taking or administering the preparation solution, a water-soluble solvent is separately taken or administered, and the manner may be repeated 2 to 4 times in total on the day before and the day of the examination.

[0015] In one embodiment, the composition for intestinal lavage may be in any form of a solution, suspension or emulsion.

[0016] In one embodiment, the composition for intestinal lavage As the first active ingredient, one or more sugar alcohols selected from xylitol, sorbitol, glycerol, erythritol, threitol, arabitol, ribitol, mannitol, galactitol, fucitol, iditol, inositol, volemitol, isomalt, maltitol, lactitol, maltotriitol, maltotetritol and polyglycitol; As the second active ingredient, ascorbic acid or a mixture of ascorbic acid and ascorbate; and An intestinal lavage composition containing a water-soluble solvent, The content of the first active ingredient is 10 g / L to 500 g / L based on the total composition, the content of the second active ingredient is 1 g / L to 300 g / L based on the total composition, and the content of the water-soluble solvent can be 1.0 L to 3.0 L.

[0017] In a specific embodiment, the intestinal lavage composition additionally contains sodium bicarbonate and / or potassium bicarbonate as a third active ingredient, and the content of the third active ingredient can be 0.5 g / L to 5 g / L based on the total composition.

[0018] In a more specific embodiment, the intestinal lavage composition contains 110 g of D-sorbitol; 15 g of ascorbic acid; 2.1 g of sodium bicarbonate; 0.9 g of potassium bicarbonate; and 1.0 L to 3.0 L of water and the water can be administered in the form of a solution in which the components are dissolved or administered alone.

[0019] In a more specific embodiment, the intestinal lavage composition contains 1.0 L to 1.5 L of water, or the total dosage taken on the day before and on the day of the examination is 10 L to 1.5 L, and the total dosage taken on the day of the examination can be 500 mL or less.

[0020] In a more specific embodiment, the intestinal lavage composition contains 1.28 L, 1.35 L or 1.44 L of water, or the total dosage taken on the day before and on the day of the examination is 1.28 L, 1.35 L or 1.44 L, and the total dosage administered on the day of the examination can be 360 mL, 460 mL or 480 mL.

[0021] In one embodiment, the composition for intestinal lavage is polyethylene glycol as the first active ingredient; ascorbic acid or a mixture of ascorbic acid and ascorbate as the second active ingredient; and a composition for intestinal lavage containing a water-soluble solvent, wherein the content of the first active ingredient is 10 g / L to 500 g / L based on the total composition, the content of the second active ingredient is 1 g / L to 300 g / L based on the total composition, and the content of the water-soluble solvent can be 1.0 to 3.0 L.

[0022] In a specific embodiment, the composition for intestinal lavage further contains at least one selected from the group consisting of sodium chloride, potassium chloride, and sodium sulfate as a third active ingredient, and the content of the third active ingredient can be 0.5 g / L to 50 g / L based on the total composition.

[0023] In a more specific embodiment, in the composition for intestinal lavage, the polyethylene glycol can have an average molecular weight of 3000 to 4000 Da.

[0024] In a more specific embodiment, the composition for intestinal lavage contains 200 g of polyethylene glycol 3350; 9.4 g of ascorbic acid; 11.8 g of sodium ascorbate; 15 g of anhydrous sodium sulfate; 5.382 g of sodium chloride; 2.030 g of potassium chloride; and 1.0 L to 3.0 L of water and the water can be administered in the form of a solution in which the components are dissolved or administered alone.

[0025] In a more specific embodiment, the composition for intestinal lavage Containing 3.0 L of water, or the total dosage taken on the day before and on the day of the examination is 3.0 L. The total dosage taken on the day of the examination may be 600 mL.

[0026] In a more specific embodiment, the composition for intestinal lavage is 140 g of polyethylene glycol 3350; 7.54 g of ascorbic acid; 48.11 g of sodium ascorbate; 9 g of anhydrous sodium sulfate; 5.2 g of sodium chloride; 2.2 g of potassium chloride; and 1.0 L to 3.0 L of water and the water may be administered in the form of a solution in which the above components are dissolved or may be administered alone.

[0027] In a more specific embodiment, the composition for intestinal lavage is Containing 2.0 L of water, or the total dosage taken on the day before and on the day of the examination is 2.0 L. The total dosage taken on the day of the examination may be 400 mL or 500 mL.

[0028] In a more specific embodiment, the composition for intestinal lavage is 160 g of polyethylene glycol 3350; 40.6 g of ascorbic acid; 9.4 g of sodium ascorbate; 18 g of anhydrous sodium sulfate; 2.7 g of sodium chloride; 1 g of potassium chloride; and 1.0 L to 3.0 L of water and the water may be administered in the form of a solution in which the above components are dissolved or may be administered alone.

[0029] In a more specific embodiment, the composition for intestinal lavage is Contains 2.0 L of water, or the total dosage taken on the day before and the day of the examination is 2.0 L, The total dosage taken on the day of the examination can be 400 mL.

[0030] In one embodiment, the composition for intestinal lavage Based on the total composition, Sodium picosulfate or its hydrate 0.001 g / L to 0.1 g / L; Magnesium oxide 0.5 g / L to 50 g / L; Citric acid 1 g / L to 50 g / L; and Water-soluble solvent 1.0 L to 3.0 L Can contain.

[0031] In a specific embodiment, the composition for intestinal lavage Sodium picosulfate hydrate 0.03 g; Magnesium oxide 10.5 g; Citric acid 36.0 g; and Water 1.0 L to 3.0 L And the water can be administered in the form of a solution in which the above components are dissolved, or can be administered alone.

[0032] In a more specific embodiment, the composition for intestinal lavage Contains 3.0 L of water, or the total dosage taken on the day before and the day of the examination is 3.0 L, The total dosage taken on the day of the examination can be 600 mL.

[0033] In one embodiment, the composition for intestinal lavage, based on the total composition, Polyethylene glycol 10 g / L to 500 g / L; Sorbitol 1 g / L to 300 g / L; Sodium picosulfate or its hydrate 0.001 g / L to 1 g / L; and Water-soluble solvent 1.0 L to 3.0 L Can be a composition containing.

[0034] In a specific embodiment, the composition for intestinal lavage is Polyethylene glycol 75 g / L; Sorbitol 27.3 g / L; Sodium picosulfate or its hydrate 0.005 g / L; and Water 1.0 L to 3.0 L and the water can be administered in the form of a solution in which the above components are dissolved or can be administered alone.

[0035] In a more specific embodiment, the composition for intestinal lavage contains 2.0 L of water, or the total dosage taken on the day before and on the day of the examination is 2.0 L, and the total dosage taken on the day of the examination can be 400 mL.

[0036] In one embodiment, the composition for intestinal lavage, based on the total composition, Sodium sulfate 5 g / L to 300 g / L; Potassium sulfate 0.1 g / L to 50 g / L; Magnesium sulfate 0.1 g / L to 50 g / L; and Water-soluble solvent 1.0 L to 3.0 L and may contain the same.

[0037] In a specific embodiment, the composition for intestinal lavage Anhydrous sodium sulfate 12.333 g / L; Potassium sulfate 2.206 g / L; Magnesium sulfate 1.128 g / L; and Water 1.0 L to 3.0 L and the water can be administered in the form of a solution in which the above components are dissolved or can be administered alone.

[0038] In a more specific embodiment, the composition for intestinal lavage Contains 2.838 L of water, or the total dosage taken on the day before and the day of the said examination is 2.838 L, The total dosage taken on the day of the said examination may be 568 mL.

[0039] Throughout the specification, when a part refers to a certain component as "including", this means that, unless otherwise stated to the contrary, it does not exclude other components, but may further include other components.

[0040] As used in this specification, the term "about" means within 10% of a given numerical value or range, preferably within 5%, more preferably within 1%.

[0041] The present invention relates to an intestinal lavage composition with enhanced safety by epoch-making reduction of the amount to be drunk in the early morning, for example, on the day of an examination requiring intestinal lavage. Specifically, the present invention relates to an intestinal lavage composition in which the total dosage (including all auxiliary solvents such as water) of the intestinal lavage composition taken on the day of the examination is about 700 mL or less, for example, about 200 to about 700 mL, preferably about 600 mL or less, more preferably about 500 mL.

[0042] In one embodiment, the present invention is an intestinal lavage composition to be taken before an examination requiring intestinal lavage, The composition is taken separately on the day before and the day of the said examination, The total dosage taken on the day of the said examination is 700 mL or less, and provides an intestinal lavage composition.

[0043] In another embodiment, the present invention is an intestinal lavage method including administering an intestinal lavage composition to a human before an examination requiring intestinal lavage, The composition is taken / administered separately on the day before and the day of the said examination, The total dosage / administered amount taken / administered on the day of the said examination is 700 mL or less, and provides an intestinal lavage method.

[0044] The total dosage or administration amount to be taken on the day of the examination is preferably 600 mL, more preferably 500 mL. For example, the administration amount can be about 300, about 310, about 320, about 330, about 340, about 350, about 360, about 370, about 380, about 390, about 400, about 410, about 420, about 430, about 440, about 450, about 460, about 470, about 480, about 490, about 500, about 510, about 520, about 530, about 540, about 550, about 560, about 570, about 580, about 590, about 600, about 610, about 620, about 630, about 640, about 650, about 660, about 670, about 680, about 690, about 700 mL. In one specific example, the total dosage to be taken on the day of the examination can be about 360, about 400, about 450, about 480, about 500, about 568 or about 600 mL. In this case, considering the numerical range of the term "about" as defined in this specification, all dosage amounts within 10% of the specific value, preferably within 5%, more preferably within 1% are also included.

[0045] The terms "dosage" or "administration amount" used in this specification can be used interchangeably, particularly when their meanings in terms of interpretation remain unchanged.

[0046] As used in this specification, the "examination requiring bowel cleansing" means an examination that requires emptying the inside of the intestinal tract as completely as possible in colonoscopy, X-ray examinations such as enterography, radiography, or bowel cleansing before surgery (for example, preoperative preparation for colon surgery, preoperative preparation for anal surgery such as hemorrhoids), etc., and includes without limitation any examination or procedure that requires bowel cleansing other than those listed above. In addition, treatment of diseases such as chronic constipation or acute constipation may also be included in some cases. In particular, the examination includes the case where gastroscopy is performed simultaneously with colonoscopy.

[0047] As used herein, the "composition for intestinal lavage" means a "purgative" or a substance that promotes defecation, and includes the category of laxative effects. By way of example, "intestinal lavage" includes not only defecation that completely empties the large intestine ("complete purgation") or strong defecation that almost completely empties it (stronger catharsis), but also mild defecation (mild catharsis) that causes diarrhea ("partial purgation, partial purgation"). As used herein, the "composition for intestinal lavage" comprehensively includes a composition used when washing the intestine or a composition used when manufacturing a pharmaceutical product for intestinal lavage. Similarly, as used herein, the "method for intestinal lavage" means a method for washing the intestine using the "composition for intestinal lavage".

[0048] In one embodiment, the composition of the present invention can be administered in the form of a preparation solution together with an auxiliary solvent such as water, or can be administered in that form as it is.

[0049] In another embodiment, the composition for intestinal lavage of the present invention can be understood to include a first part containing an active ingredient; and a second part containing a water-soluble solvent, for example, an auxiliary solvent such as water. In this case, the first part contains components that exhibit an intestinal lavage effect, and is understood to contain, in addition to the active ingredient that directly exhibits the intestinal lavage effect, any pharmaceutically acceptable excipient, etc. The first part is arbitrarily selected from any pharmaceutically acceptable form, for example, powder (powder), granule, liquid preparation, tablet, capsule, etc., and preferably can be in a form soluble in the second part, for example, powder, granule, or liquid preparation. When the first part is in the form of a tablet or capsule, etc., it can be dissolved in water or an auxiliary solution in the form of a preparation solution and taken, or can be taken separately in the form of a tablet or capsule together with water or an auxiliary solution, etc. In this case, the dosage of the solution of 700 mL or less according to the present invention will be determined by the amount of water or auxiliary solution taken together with the tablet or capsule, etc.

[0050] The second part can be used without limitation as long as it is a co-solvent capable of dissolving the first part, and preferably a water-soluble solvent such as water, carbonated water, alkaline ionized water, or beverages can be used, and water may be particularly used. Furthermore, as long as the beverage can achieve the effects of the present invention, there is no particular limitation on its type. For example, drip coffee, various juices, cola, cider, gin and tonic, etc. can also be used as needed.

[0051] The second part can dissolve the first part and be administered as a liquid preparation, and can be administered separately as the second part alone. In this specification, a liquid preparation in which the first part is dissolved in the second part, that is, a solution obtained by well mixing the active ingredient and / or other excipients according to the content and then adding an appropriate amount of a co-solvent such as water and mixing is sometimes referred to as a "prepared solution".

[0052] In a specific example, the composition for intestinal lavage of the present invention is a composition (the first part) in the form of a powder, granule, or liquid preparation containing an active ingredient and a pharmaceutically acceptable excipient, dissolved in a co-solvent such as a water-soluble solvent to form a liquid preparation (prepared solution); and separately, a co-solvent such as a water-soluble solvent can be included. At this time, the composition for intestinal lavage can be administered in such a manner that after taking the prepared solution in the form of the liquid preparation, a water-soluble solvent is taken separately.

[0053] Thereby, the composition for intestinal lavage of the present invention, particularly the "prepared solution" or the liquid preparation, can be in the form of a solution, suspension, or emulsion. However, although the composition for intestinal lavage of the present invention is administered in such a manner that a water-soluble solvent is taken separately from the prepared solution, in some cases, the prepared solution and the water-soluble solvent taken separately as a whole can be collectively referred to simply as a solution, suspension, or emulsion.

[0054] The composition for intestinal lavage of the present invention can be administered with the total dose taken all at once (non-divided administration) or divided and taken at multiple time points (divided administration). Specifically, non-divided administration means administering on the same day (i.e., divided), for example, it can be taken over several hours on the night before the examination or at dawn on the day of the examination. Specifically, a part of the total dose can be taken, and after a certain period of time, for example, after 0.5 to 3 hours, the remainder can be taken. Divided administration means administering in two days, the day before the examination and the day of the examination. For example, it means taking a part at night before the examination and taking the remainder in the morning on the day of the examination.

[0055] In one embodiment, the composition of the present invention can be taken two or more times on the day before the examination and / or on the day of the examination, preferably divided into two times, namely, on the night before the examination and at dawn on the day of the examination. The number of times of taking "two or more times" in this specification is based on the taking of the preparation solution. For example, if a certain amount of the preparation solution is taken on the night before the examination and then water is taken separately, this is regarded as one time of taking. In another example, after taking a certain amount of the preparation solution on the night before the examination and then taking water separately (the first time of taking), after a certain period of time has passed (for example, after 30 minutes, 1 hour or 1.5 hours, etc.), the above process is repeated, and after taking a certain amount of the preparation solution and then taking water separately (the second time of taking), each separate time of taking is regarded as a total of two times of taking. However, taking a certain amount of the preparation solution determined as the first dose in several portions (for example, it is difficult for the taker to take it all at once and takes it while taking breaks at 5 - 10 minute intervals) is regarded as included in one time of taking.

[0056] In one specific example, the composition of the present invention is administered by a method of taking the above-mentioned preparation solution (liquid preparation) and then taking a water-soluble solvent separately. The above method may be repeated a total of two to four times on the day before the examination and the day of the examination. However, the statement "taking a water-soluble solvent separately" includes not only taking the water-soluble solvent after completely taking the liquid preparation, but also taking the water-soluble solvent during the taking of the liquid preparation.

[0057] The amount of the auxiliary solvent such as the preparation solution or water can be appropriately selected by those skilled in the art. However, the total amount of the solution taken on the day of the examination (for example, several hours before the examination, such as 3 hours before, 2 hours before or 1 hour before), including the preparation solution and the auxiliary solvent such as water, is about 700 mL or less, for example, about 200 mL to about 700 mL, preferably about 600 mL or less, more preferably about 500 mL or less.

[0058] On the other hand, the total dosage of the composition for intestinal lavage of the present invention can be any value from about 1.0 L to about 5.0 L, for example, from about 1.0 L to about 4.0 L, specifically, from about 1.0 L to about 3.0 L. In one specific example, the total dosage can be about 1.0 L, about 1.28 L, about 1.35 L, about 1.44 L, about 2.0 L, about 2.838 L, about 3.0 L, etc. At this time, the total dosage can refer to the dosage taken on the day before and the day of the examination. Therefore, the composition for intestinal lavage of the present invention can have a total dosage taken on the day before and the day of the examination of the above values, for example, from about 1.0 L to about 4.0 L.

[0059] In one embodiment, the composition for intestinal lavage of the present invention may contain one or more of the following components as active ingredients.

[0060] · Polyethylene glycol (PEG), for example, PEG having a number average molecular weight of 1,000 to 10,000, preferably PEG having a number average molecular weight of 2,000 to 6,000, more preferably PEG having a number average molecular weight of 3,000 to 5,000, specifically, polyethylene glycol 3350; · Ascorbic acid or its salts, for example, alkali metal (e.g., sodium or potassium) or alkaline earth metal salts (e.g., calcium) of ascorbic acid, and as a specific example, sodium ascorbate; · One or more sugar alcohols selected from xylitol, sorbitol (e.g., D-sorbitol), glycerol, erythritol, threitol, arabinitol, ribitol, mannitol, galactitol, fucitol, iditol, inositol, volemitol, isomalt, maltitol, lactitol, maltotriitol, maltotetritol, and polyglycitols; · Picolsulfate, for example, sodium picolsulfate or its hydrate; · Citric acid; · Magnesium oxide; · (Anhydrous) sodium sulfate; · Potassium sulfate; · (Anhydrous) magnesium sulfate; · Sodium chloride; · Anhydrous sodium hydrogen phosphate; · Sodium dihydrogen phosphate monohydrate; and · Potassium chloride.

[0061] The composition for intestinal lavage of the present invention may additionally contain pharmaceutically acceptable excipients or additives suitable for intestinal lavage agents. The excipients or additives are not particularly limited as long as they are those commonly used in compositions for intestinal lavage.

[0062] For example, when the composition for intestinal lavage contains ascorbic acid as an active ingredient, since the acidity is high and it may be difficult to take due to excessive sour taste, bicarbonates such as sodium bicarbonate and potassium bicarbonate can be additionally included as components for neutralizing it.

[0063] Also, an appropriate amount of antioxidant can be added to the composition for intestinal lavage of the present invention to prevent the oxidation of ascorbic acid. Examples of such antioxidants include, but are not limited to, ferulic acid, amino acids such as glycine and histidine, hyaluronic acid, and tocopherol.

[0064] In addition, the composition for intestinal lavage of the present invention can contain a sweetener to improve the taste. Examples of usable sweeteners include, but are not limited to, Sucralose, Maltodextrin, Glucose, Sucrose, Dextrose, Saccharin, aspartame, Stevia, and the like.

[0065] In addition, the composition for intestinal lavage of the present invention can be added with an appropriate amount of edible fruit flavor to improve the compliance of taking. As these fruit flavors, the aroma of strawberry, orange, apple, grape, lemon, banana, cherry, etc. can be used.

[0066] In addition, the composition for intestinal lavage of the present invention can further contain an adsorbent for adsorbing trace amounts of iron ions and copper ions that may be contained in the water-soluble solvent. Examples of such adsorbents include, but are not limited to, Versene TM CA chelating agent (Dow).

[0067] Furthermore, the composition for intestinal lavage of the present invention can further contain a foam formation inhibitor to remove intestinal air bubbles that frequently occur after intestinal gas removal or intestinal lavage. In one aspect of the present invention, for example, simethicone can be used as the foam formation inhibitor, but it is not limited thereto. The simethicone used as the foam formation inhibitor in the present invention may be mixed with the composition for intestinal lavage in the form of a suspension. The usage method can follow the existing known methods.

[0068] The enteric cleansing composition of the present invention can further contain known cleansing components and auxiliary components for enhancing the cleansing effect. Examples of the additional cleansing components and cleansing-promoting auxiliary components include, but are not limited to, magnesium such as citric acid and magnesium oxide, sodium docusate, senna extract (such as sennoside), aloe extract (such as aloin), etc., and zinc such as pectin and zinc oxide, caffeine, etc.

[0069] The enteric cleansing composition of the present invention can be of the PEG-based, PSMC-based, oral sulfate-based, or sorbitol-based type.

[0070] [Table 1]

[0071] Specifically, the enteric cleansing composition of the present invention can contain the following active ingredients. Also in this case, the following composition can be taken in two or more divided doses on the day before or on the day of the examination. The amount of auxiliary solvents such as the preparation solution or water can be appropriately selected by those skilled in the art. However, the total solution intake amount on the day, including all the auxiliary solvents such as the preparation solution and water taken on the day of the examination (for example, a few hours before the examination), is about 700 mL or less, for example, about 200 mL to about 700 mL, preferably about 600 mL or less, and more preferably about 500 mL or less.

[0072] [Composition Example I]

[0073] 1) A composition containing polyethylene glycol 3350, ascorbic acid or sodium ascorbate, and anhydrous sodium sulfate (optionally containing potassium chloride, sodium chloride, and other additives) as active ingredients.

[0074] 2) A composition containing polyethylene glycol 3350 and sodium chloride as active ingredients.

[0075] 3) A composition containing D-sorbitol / mannitol; and ascorbic acid or sodium ascorbate as active ingredients.

[0076] 4) A composition containing disodium hydrogen phosphate anhydrous; and sodium dihydrogen phosphate monohydrate as active ingredients.

[0077] 5) A composition containing sodium picosulfate hydrate; magnesium oxide; and citric acid as active ingredients.

[0078] 6) A composition containing sodium sulfate anhydrous; and magnesium sulfate anhydrous (optionally containing potassium sulfate additionally) as active ingredients.

[0079] 7) A composition containing D-sorbitol; polyethylene glycol 3350; and sodium picosulfate hydrate as active ingredients.

[0080] 8) A composition containing D-sorbitol / mannitol; ascorbic acid or sodium ascorbate; sodium hydrogen carbonate; and potassium hydrogen carbonate as active ingredients.

[0081] In one specific embodiment, the composition for intestinal lavage of the present invention may contain active ingredients as follows.

[0082] [Composition Example II]

[0083] 1) A composition containing 100 - 400 g of polyethylene glycol 3350; 10 - 80 g of ascorbic acid or sodium ascorbate; and 5 - 40 g of sodium sulfate anhydrous (optionally containing 1 - 5 g of potassium chloride, 1 - 10 g of sodium chloride, and other additives additionally). The said composition is taken by dividing the total amount of the preparation solution of about 1 - 2 L and the total amount of water of about 1 L, but the total solution intake amount on the day of taking both the preparation solution and water on the day of the examination is about 700 mL or less, preferably about 600 mL or less, more preferably about 500 mL or less.

[0084] 2) A composition containing 350 - 450 g of polyethylene glycol 3350 and 10 - 15 g of sodium chloride as active ingredients. The composition is taken by dividing the total amount of the preparation solution, about 4 L. The total solution intake amount on the day of the examination, combining both the preparation solution and water taken on the day of the examination, is 700 mL or less, preferably 600 mL or less, more preferably 500 mL or less.

[0085] 3) A composition containing 50 - 150 g of D-sorbitol and 5 - 30 g of ascorbic acid or sodium ascorbate as active ingredients. The composition is taken by dividing about 0.5 L of the preparation solution and about 1.0 L of water. The total solution intake amount on the day of the examination, combining both the preparation solution and water taken on the day of the examination, is 700 mL or less, preferably 600 mL or less, more preferably 500 mL or less.

[0086] 4) A composition containing 10 - 20 g of anhydrous sodium hydrogen phosphate and 30 - 50 g of sodium dihydrogen phosphate monohydrate as active ingredients. When the composition is in tablet form, it is taken by dividing it together with about 2 L of water. The total water intake amount on the day of the examination is 700 mL or less, preferably 600 mL or less, more preferably 500 mL or less.

[0087] 5) A composition containing 20 - 50 mg of sodium picosulfate hydrate, 5 - 15 g of magnesium oxide, and 30 - 50 g of citric acid as active ingredients. The composition is taken by dividing about 0.3 L - 0.4 L of the preparation solution and a total of 2 L of water. The total solution intake amount on the day of the examination, combining both the preparation solution and water taken on the day of the examination, is about 700 mL or less, preferably 600 mL or less, more preferably 500 mL or less.

[0088] 6) A composition containing 25 - 45 g of sodium sulfate anhydrous and 2 - 5 g of magnesium sulfate anhydrous (possibly containing 1 - 10 g of potassium sulfate additionally) as active ingredients. When the composition is in tablet form, it is taken divided together with about 2.5 - 3.0 L of water. When it is in powder form, it is taken divided together with about 0.9 - 1.0 L of the preparation solution and about 1.8 - 2.0 L of water. However, the total solution intake amount on the day of the examination, which is the sum of the preparation solution and water taken on the day of the examination, is 700 mL or less, preferably 600 mL or less, more preferably 500 mL or less.

[0089] 7) A composition containing 40 - 100 g of D-sorbitol, 100 - 300 g of polyethylene glycol 3350, and 5 - 20 mg of sodium picosulfate hydrate as active ingredients. The composition is taken divided together with about 1 L of the preparation solution and about 1 L of water. However, the total solution intake amount on the day of the examination, which is the sum of the preparation solution and water taken on the day of the examination, is 700 mL or less, preferably 600 mL or less, more preferably 500 mL or less.

[0090] 8) A composition containing 50 - 150 g of D-sorbitol; 10 - 20 g of ascorbic acid or sodium ascorbate; 1 - 5 g of sodium hydrogen carbonate; 0.5 - 1.5 g of potassium hydrogen carbonate as active ingredients. The composition is taken divided together with about 0.8 - 1.1 L of the preparation solution and about 0.3 - 0.5 L of water. However, the total solution intake amount on the day of the examination, which is the sum of the preparation solution and water taken on the day of the examination, is 700 mL or less, preferably 600 mL or less, more preferably 500 mL or less.

[0091] In a more specific embodiment, the composition for intestinal lavage of the present invention may contain active ingredients as follows. Also in this case, the following composition can be taken divided two or more times on the day before or the day of the examination. The amount of auxiliary solvents such as the preparation solution or water can be appropriately selected by those skilled in the art. However, the total solution intake amount on the day of the examination, which is the sum of all the auxiliary solvents such as the preparation solution and water taken on the day of the examination, is 700 mL or less, for example, 200 - 700 mL, preferably 600 mL or less, more preferably 500 mL or less.

[0092]

Table 2

[0093] In a more specific embodiment, the composition for intestinal lavage of the present invention may contain the following components. The following composition can be taken in divided doses two or more times on the day before or on the day of the examination. The amount of auxiliary solvents such as the preparation solution or water can be appropriately selected by those skilled in the art. However, the total solution intake amount on the day, which is the sum of the preparation solution and auxiliary solvents such as water taken on the day of the examination, is 700 mL or less, for example, 200 to 700 mL, preferably about 600 mL or less, and more preferably about 500 mL or less.

[0094]

Table 3

[0095] In one embodiment, the composition of the present invention can be packaged in separate packaging units according to the number of divisions or provided in the form of a kit in which each component is separately divided and packaged according to the convenience of taking. In particular, ascorbic acid can be packaged separately from other components according to its chemical properties. At this time, the kit can include an instruction that describes the method of taking or using mentioned throughout the specification of the present invention. In another embodiment, the composition for intestinal lavage of the present invention can be provided in the form of a kit in which the total dose is divided according to the number of doses and appropriately packaged. Specifically, the composition for intestinal lavage of the present invention can be provided by packaging the total dose at once, or by dividing and packaging the total dose into two or more portions.

[0096] In one embodiment, the composition for intestinal lavage of the present invention can package the first component, the second component, and, if necessary, all components of the third washing component, the bubble formation inhibitor, the gastrointestinal stabilizer, and other additives together with a water-soluble solvent in an integrated form (i.e., a liquid agent).

[0097] In another embodiment, the composition for intestinal lavage of the present invention can be provided in the form of a kit packaged in several packaging units. For example, when the first component and the second component are packaged together and the water-soluble solvent is packaged separately, when the second component and the water-soluble solvent are packaged together and the first cleaning component is packaged separately, when the first component and the water-soluble solvent are packaged together and the second cleaning component is packaged separately, when a part of the first cleaning component and the water-soluble solvent are packaged together and a part of the second component and the water-soluble solvent are packaged together, when the first component and the second component are packaged together with a part of the water-soluble solvent and the rest of the water-soluble solvent is packaged separately. Also, the water-soluble solvent can be a commercially available product (such as mineral water, carbonated water, etc.) and is not limited thereto. Furthermore, if necessary, a third cleaning component, a bubble formation inhibitor, a gastrointestinal stabilizer, and other additives can be formulated in various two-component forms.

[0098] For example, some examples of the composition of the present invention can be provided in the form of a kit packaged as follows.

[0099] [Table 4]

[0100] Needless to say, the above-mentioned composition can additionally contain the aforementioned excipients / additives.

[0101] In one embodiment, the present invention As the first active ingredient, one or more sugar alcohols selected from xylitol, sorbitol, glycerol, erythritol, threitol, arabinitol, ribitol, mannitol, galactitol, fucitol, iditol, inositol, volemitol, isomalt, maltitol, lactitol, maltotriitol, maltotetritol, and polyglycitol; As the second active ingredient, ascorbic acid or a mixture of ascorbic acid and ascorbate; and An enteric lavage composition containing a water-soluble solvent, The content of the first active ingredient is about 10 g / L to about 500 g / L, preferably about 30 g / L to about 300 g / L, more preferably about 50 g / L to about 100 g / L, and particularly preferably about 70 g / L to about 90 g / L based on the total composition; The content of the second active ingredient is about 1 g / L to about 300 g / L, preferably about 3 g / L to about 100 g / L, more preferably about 5 g / L to about 50 g / L, and particularly preferably about 10 g / L to about 15 g / L based on the total composition; The content of the water-soluble solvent is about 1.0 L to about 3.0 L, preferably about 1.0 L to about 1.5 L. Provided is an enteric lavage composition.

[0102] At this time, the enteric lavage composition can additionally contain sodium bicarbonate and / or potassium bicarbonate as a third active ingredient, The content of the third active ingredient is about 0.5 g / L to about 5 g / L, preferably about 1 g / L to about 3 g / L, and more preferably about 1.5 g / L to about 2.5 g / L based on the total composition.

[0103] The enteric lavage composition can additionally contain an appropriate amount of other fragrances. For example, the fragrance can be about 1.5 g / L to about 3.0 g / L based on the total composition.

[0104] In one specific example, the enteric lavage composition is D-sorbitol about 110 g; Ascorbic acid: about 15 g; Sodium hydrogen carbonate: about 2.1 g; Potassium hydrogen carbonate: about 0.9 g; and Water: about 1.0 L to about 3.0 L It can contain the above. The content (g) of each of the above components can be the content of the first part described above, i.e., the content of the active ingredient. At this time, the water can be administered in the form of a solution in which the above components are dissolved, or can be administered alone.

[0105] In another specific example, the composition can contain about 1.0 L to about 1.5 L of water, or the total dosage taken on the day of the test and the day before for the test can be about 1.0 L to about 1.5 L, provided that the total dosage taken on the day of the test is 500 mL or less.

[0106] In another specific example, the composition can contain about 1.28 L, about 1.35 L or about 1.44 L of water, or the total dosage taken on the day of the test and the day before for the test is about 1.28 L, about 1.35 L or about 1.44 L, and the total dosage taken on the day of the test is about 360 mL or about 500 mL. At this time, the "dosage" means the dosage when the composition is administered in the form of a liquid preparation. For example, when the liquid preparation is in the form of a solution, it means the total solution dosage.

[0107] In a more specific example, the composition, packaging method and dosage method of the first part of the intestinal lavage composition according to the present invention can be as follows.

[0108]

Table 5

[0109] The composition can additionally contain the following excipients.

[0110]

Table 6

[0111] The composition can additionally contain the following excipients.

[0112] [Table 7]

[0113] The composition can be dissolved in water or the like and taken in the form of a preparation solution with the following contents.

[0114] [Table 8]

[0115] The composition can be taken by dividing 960 mL of the total preparation solution and 480 mL of additional water in a ratio of "the day before the examination: 2:1 on the day of the examination". For example, the specific method of taking is as follows. (In the following example, the composition (for example, the first part) packaged in one pack is a powder, and when diluted and dissolved in water to produce a preparation solution, the content of the preparation solution is substantially the same as the content of the water for dissolution. Therefore, in the following example, the content of the water for dissolving one pack of the components is substantially the same as the content of the preparation solution. The same applies when a powder is used as the first part in a specific example of the present invention).

[0116] 1) On the day before the examination, take a preparation solution prepared by sufficiently diluting one pack in 320 mL of water, and then take another pack diluted in the same way. Then, drink an additional 320 mL of water. If the lips are dry or the throat is thirsty, an appropriate amount of additional water can be drunk (total 960 mL). 2) On the day of the examination, dilute one pack in 320 mL of water and take it, and then drink an additional 160 mL of water (total 480 mL).

[0117] As another method, it can be taken as follows.

[0118] 1) Take 720 mL of the preparation solution on the night before the colonoscopy examination and drink 360 mL of water (total 1080 mL). 2) Take 240 mL of the preparation solution on the morning of the day of colonoscopy and drink 120 mL of water (total 360 mL).

[0119] Or, 1) Take 320 mL of the preparation solution on the night before the colonoscopy and additionally drink 130 mL (total 900 mL). 2) Take 320 mL of the preparation solution on the morning of the day of colonoscopy and drink 130 mL of water (total 450 mL).

[0120] Or, 1) Take 320 mL of the preparation solution on the night before the colonoscopy and take 320 mL of the preparation solution again in the same way. Then, additionally drink 160 mL of water (total 800 mL). 2) Take 320 mL of the preparation solution on the morning of the day of colonoscopy and drink 160 mL of water (total 480 mL).

[0121] In one embodiment, the present invention is Polyethylene glycol as the first active ingredient; Ascorbic acid or a mixture of ascorbic acid and ascorbate as the second active ingredient; and An intestinal cleansing composition containing a water-soluble solvent, wherein the content of the first active ingredient is about 10 g / L to about 500 g / L, preferably about 30 g / L to about 300 g / L, more preferably about 50 g / L to about 200 g / L based on the total composition, the content of the second active ingredient is about 1 g / L to about 300 g / L, preferably about 3 g / L to about 100 g / L, more preferably about 5 g / L to about 60 g / L based on the total composition, the content of the water-soluble solvent is about 1.0 L to about 3.0 L, and provides an intestinal cleansing composition.

[0122] The intestinal lavage composition can additionally contain at least one selected from the group consisting of sodium chloride, potassium chloride, and sodium sulfate as a third active ingredient. For example, it can contain all of the three components. At this time, the content of the third active ingredient can be about 0.5 g / L to about 50 g / L based on the total composition, preferably about 3 g / L to about 30 g / L, and more preferably about 5 g / L to about 25 g / L.

[0123] The polyethylene glycol can have an average molecular weight of 3000 to 4000 Da, and preferably can be polyethylene glycol 3350.

[0124] In one specific example, the intestinal lavage composition Polyethylene glycol 3350 about 200 g; Ascorbic acid about 9.4 g; Sodium ascorbate about 11.8 g; Sodium sulfate anhydrous about 15 g; Sodium chloride about 5.382 g; Potassium chloride about 2.030 g; and Water about 1.0 L to about 3.0 L can be included. The content (g) of each component can be the content of the first part described above, that is, the content of the active ingredient. At this time, the water can be administered in the form of a solution in which the components are dissolved, or can be administered alone.

[0125] In a more specific example, the composition can contain about 3.0 L of water, or the total dosage taken on the day of the examination and the day before for examination can be about 3.0 L, and the total dosage taken on the day of the examination can be about 600 mL.

[0126] In a more specific example, the composition, packaging method, and administration method of the first part of the intestinal lavage composition according to the present invention can be as follows.

[0127]

Table 9

[0128] 1) Take 1.6 L of the preparation solution on the night before the colonoscopy and drink 800 mL of water. 2) Take 400 mL of the preparation solution in the morning on the day of the colonoscopy and drink 200 mL of water (total 600 mL).

[0129] In another specific example, the intestinal cleansing composition is Polyethylene glycol 3350 about 140 g; Ascorbic acid about 7.54 g; Sodium ascorbate about 48.11 g; Sodium sulfate anhydrous about 9 g; Sodium chloride about 5.2 g; Potassium chloride about 2.2 g; and Water about 1.0 L to about 3.0 L can be included. The content (g) of each of the above components can be the content of the first part described above, i.e., the content of the active ingredient. At this time, the water can be administered in the form of a solution in which the above components are dissolved, or can be administered alone.

[0130] In a more specific example, the composition can contain about 2.0 L of water, or the total dosage taken on the day of the examination and the day before for the examination can be about 2.0 L, and the total dosage taken on the day of the examination can be about 400 mL or about 500 mL.

[0131] In a more specific example, among the intestinal cleansing compositions according to the present invention, the composition, packaging method and administration method of the first part can be as follows.

[0132]

Table 10

[0133] 1) Take 750 mL of the preparation solution on the night before the colonoscopy and drink 750 mL of water. 2) Take 250 mL of the preparation solution on the morning of the day of the colonoscopy and drink 250 mL (total 500 mL) of water.

[0134] Or; 1) Take 800 mL of the preparation solution on the night before the colonoscopy and drink 200 mL of water. 2) Take 200 mL of the preparation solution on the morning of the day of the colonoscopy and drink 200 mL of water (total 400 mL).

[0135] In another specific example, the intestinal cleansing composition is Polyethylene glycol 3350 about 160 g; Ascorbic acid about 40.6 g; Sodium ascorbate about 9.4 g; Sodium sulfate anhydrous about 18 g; Sodium chloride about 2.7 g; Potassium chloride about 1 g; and Water about 1.0 L to about 3.0 L can be included. The content (g) of each component can be the content of the first part described above, that is, the content of the active ingredient. At this time, the water can be administered in the form of a solution in which the components are dissolved or can be administered alone.

[0136] In a more specific example, the composition may contain about 2.0 L of water, or the total dosage taken on the day of the examination and the day before for the examination may be about 2.0 L, and the total dosage taken on the day of the examination may be about 400 mL.

[0137] In a more specific example, the composition, packaging method, and administration method of the first part of the intestinal cleansing composition according to the present invention can be as follows.

[0138]

Table 11

[0139] 1) Take 800 mL of the preparation solution on the night before the colonoscopy and drink 200 mL of water. 2) Take 200 mL of the preparation solution on the morning of the day of colonoscopy and drink 200 mL of water (total 400 mL).

[0140] In one embodiment, the present invention is based on the overall composition, sodium picosulfate or its hydrate from about 0.001 g / L to about 0.1 g / L, preferably from about 0.005 g / L to about 0.05 g / L; magnesium oxide from about 0.5 g / L to about 50 g / L, preferably from 1 g / L to about 10 g / L; citric acid from about 1 g / L to about 50 g / L, preferably from 5 g / L to about 30 g / L; and water-soluble solvent from about 1.0 L to about 3.0 L to provide an intestinal cleansing composition.

[0141] In one specific example, the intestinal cleansing composition sodium picosulfate hydrate about 0.03 g; magnesium oxide about 10.5 g; citric acid about 36 g; and water from about 1.0 L to about 3.0 L can include. The content (g) of each of the above components can be the content of the first part described above, that is, the content of the active ingredient. At this time, the water can be administered in the form of a solution in which the above components are dissolved or can be administered alone.

[0142] In a more specific example, the composition can include about 3.0 L of water, or the total dosage taken on the day of the examination and the day before for the examination can be about 3.0 L, and the total dosage taken on the day of the examination can be about 600 mL.

[0143] In a more specific example, the composition, packaging method, and administration method of the first part of the intestinal cleansing composition according to the present invention can be as follows.

[0144]

Table 12

[0145] 1) Take 240 mL of the preparation solution on the night before the colonoscopy and drink 2,160 mL of water. 2) Take 60 mL of the preparation solution in the morning on the day of the colonoscopy and drink 540 mL (total 600 mL) of water.

[0146] In one embodiment, based on the overall composition, the present invention provides polyethylene glycol from about 10 g / L to about 500 g / L, preferably from about 30 g / L to about 300 g / L, more preferably from about 50 g / L to about 100 g / L; sorbitol from about 1 g / L to about 300 g / L, preferably from about 10 g / L to about 100 g / L, more preferably from about 20 g / L to about 50 g / L; sodium picosulfate or its hydrate from 0.001 g / L to 1 g / L, preferably from about 0.002 g / L to about 0.007 g / L; and a water-soluble solvent from about 1.0 L to about 3.0 L and provides a composition for intestinal lavage.

[0147] In one specific example, the composition for intestinal lavage contains polyethylene glycol about 75 g / L; sorbitol about 27.3 g / L; sodium picosulfate or its hydrate about 0.005 g / L; and water from about 1.0 L to about 3.0 L and can include. The content (g) of each component described above can be the content of the first part described above, that is, the content of the active ingredient. At this time, the water can be administered in the form of a solution in which the components are dissolved or can be administered alone.

[0148] In a more specific example, the composition can contain about 2.0 L of water, or the total dosage taken on the day of the examination and the day before for the examination can be about 2.0 L at that time, and the total dosage taken on the day of the examination can be about 400 mL.

[0149] More specifically, the composition, packaging method, and administration method of the first part of the intestinal lavage composition according to the present invention can be as follows.

[0150] [Table 13]

[0151] 1) Take 800 mL of the preparation solution on the night before the colonoscopy and drink 200 mL of water. 2) Take 200 mL of the preparation solution in the morning on the day of the colonoscopy and drink 200 mL of water (total 400 mL).

[0152] In one embodiment, based on the total composition, the present invention provides Sodium sulfate: about 5 g / L to about 300 g / L, preferably about 7 g / L to about 50 g / L, more preferably about 10 g / L to about 30 g / L; Potassium sulfate: about 0.1 g / L to about 50 g / L, preferably about 0.5 g / L to about 10 g / L, more preferably about 0.7 g / L to about 5 g / L; Magnesium sulfate: about 0.1 g / L to about 50 g / L, preferably about 0.5 g / L to about 10 g / L, more preferably about 0.7 g / L to about 5 g / L; and Water-soluble solvent: about 1.0 L to about 3.0 L and provides an intestinal lavage composition.

[0153] In one specific example, the intestinal lavage composition can contain anhydrous sodium sulfate: about 12.333 g / L; potassium sulfate: about 2.206 g / L; magnesium sulfate: about 1.128 g / L; and water: about 1.0 L to about 3.0 L. The content (g) of each component can be the content of the first part described above, that is, the content of the active ingredient. At this time, the water can be administered in the form of a solution in which the components are dissolved or can be administered alone.

[0154] In more specific examples, the composition may contain about 2.838 L of water, or the total dosage taken on the day of the examination and the day before for examination purposes may be about 2.838 L, and the total dosage taken on the day of the examination may be about 568 mL.

[0155] In more specific examples, the composition, packaging method, and administration method of the first part of the colon cleansing composition according to the present invention may be as follows.

[0156]

Table 14

[0157] 1) Take 757 mL of the preparation solution on the night before the colonoscopy and drink 1,514 mL of water. 2) Take 189 mL of the preparation solution in the morning on the day of the colonoscopy and drink 378 mL (total 568 mL) of water.

Advantages of the Invention

[0158] Most existing colon cleansing agents have the same dosage for the first administration on the day before and the second administration on the day of the examination, and the total dosage of the preparation solution or medicine and water on the day of the examination exceeds at least 1 liter. The end time of taking the colon cleansing agent is also 1 to 2 hours immediately before the examination, which is contrary to the principle of taking it 2 to 3 hours before the examination recommended in existing literature or at least 3 hours before performing a sleep endoscopy examination. Eventually, there is a problem that the safety and convenience of taking the existing colon cleansing agent for the subject are reduced.

[0159] Among some colon cleansing agents, there are those that make the dosages on the night before and the day of the examination different, and take a smaller amount of the preparation solution and water on the day of the examination than on the day before. However, it also requires taking about 1 liter or more of the medicine and water not only on the day before but also on the day of the examination, and it is impossible to eliminate the potential risks that may occur when parallel to the safety of the aforementioned colonoscopy and gastroscopy.

[0160] Thus, the method of drinking a large amount of water until 1 to 2 hours before the test cannot completely eliminate the safety issues related to the risk of aspiration when performing a gastroscopy or a sleep endoscopy.

[0161] In contrast, the composition for bowel cleansing of the present invention has a dosage on the day of the test of 700 mL or less in total, for example, 200 to 700 mL, preferably 600 mL or less, more preferably 500 mL or less. Despite being a very small amount compared to the existing dosage, it shows a bowel cleansing or cleansing effect sufficient to ensure the effectiveness of a colonoscopy and can more effectively improve the safety of the subject. Furthermore, the shorter dosage results in a correspondingly shorter administration time, and the interval with the test time can be further ensured. By minimizing the amount of the preparation liquid and water remaining in the stomach and large intestine, the safety of the test can be improved.

Mode for Carrying Out the Invention

[0162] Best Mode for Carrying Out the Invention

[0163] Hereinafter, the present invention will be described in more detail through examples. However, the present invention is not limited to the following examples.

[0164] For randomly and arbitrarily selected patients, the compositions of the following respective compositions were administered according to the administration methods described in each of the examples and comparative examples, and the degree of bowel cleansing, endoscopy time, intestinal residue amount, ease of administration, side effects (abnormal cases - nausea, vomiting, dizziness, etc.), willingness to take again, etc. were evaluated.

[0165] Example 1

[0166] In this example, a composition with the components and contents shown in the following table was used.

[0167]

Table 15

[0168] Dosage method

[0169] After mixing well the active ingredients in the said table according to their contents, an appropriate amount of water was added and dissolved, then water was added again so that the total volume became 2 L in total, and then they were mixed well to produce a preparation solution. It is necessary to take a total of 1 L of water with respect to 2 L of the total preparation solution.

[0170] In each of the comparative examples and examples, the total preparation solution was divided according to the said ratio (%) on the previous day or the same day and taken together with water, or the active ingredients in the said table were divided according to the content corresponding to the said ratio (%) and then a preparation solution for the previous day or the same day was separately produced, and then they were guided to take it together with water. The administration methods (ratio % of the preparation solution) of each of the comparative examples and examples are as follows.

[0171]

Table 16

[0172]

Table 17

[0173] Example 2

[0174] In this example, a composition with the components and contents in the following table was used.

[0175]

Table 18

[0176] After mixing well the active ingredients of the composition in the said table according to their contents, an appropriate amount of water was added and dissolved, then water was added again so that the total amount became 1 L in total, and then they were mixed well to produce a preparation solution. It is necessary to take a total of 1 L of water with respect to 1 L of the total preparation solution.

[0177] In each of the comparative examples and examples, the total preparation solution was divided at the ratio (%) of the previous day or the same day and taken together with water, or the active ingredients in the above table were divided at a content corresponding to the ratio (%) and separately prepared the preparation solution of the previous day or the same day, and then were guided to take it together with water. The administration methods (ratio % of the preparation solution) of each example are as follows.

[0178]

Table 19

[0179]

Table 20

[0180] Example 3

[0181] In this example, a composition with the components and contents in the following table was used. The composition was manufactured by mixing each active ingredient.

[0182]

Table 21

[0183] Dosage method

[0184] After mixing the active ingredients in the above table well according to the content, an appropriate amount of water was added and dissolved, and then water was added again so that the total amount became 960 mL in total, and then they were mixed well to prepare a preparation solution. A total of 480 mL of water must be taken for the total 960 mL of the preparation solution.

[0185] In each of the comparative examples and examples, the total preparation solution was divided at the ratio (%) of the previous day or the same day and taken together with water, or the active ingredients in the above table were divided at a content corresponding to the ratio (%) and separately prepared the preparation solution of the previous day or the same day, and then were guided to take it together with water. The administration methods (ratio % of the preparation solution) of each example are as follows.

[0186]

Table 22

[0187]

Table 23

[0188] Example 4

[0189] In this example, a composition with the components and contents shown in the following table was used.

[0190]

Table 24

[0191] Dosage method

[0192] After thoroughly mixing the active ingredients in the table according to the content, an appropriate amount of water was added and dissolved, and then water was added again so that the total volume became 300 mL in total. After thoroughly mixing them with each other, a preparation solution was produced. A total of 2700 mL of water must be taken for every 300 mL of the total preparation solution.

[0193] In each comparative example and example, the total preparation solution was divided and taken at the ratio (%) of the previous day or the current day, or the active ingredients in the table were divided according to the content corresponding to the ratio (%), and then a preparation solution for the previous day or the current day was separately produced and taken.

[0194] The administration methods (ratio % of the preparation solution) of each example are as follows.

[0195]

Table 25

[0196]

Table 26

[0197] Example 5

[0198] In this example, a composition with the components and contents shown in the following table was used.

[0199]

Table 27

[0200] Dosage method

[0201] After thoroughly mixing the active ingredients in the table according to their contents, an appropriate amount of water was added and dissolved, and then water was added again so that the total volume became 946 mL. After thoroughly mixing them, a preparation solution was produced. A total of 1892 mL of water must be taken for 946 mL of the total preparation solution.

[0202] In each comparative example and example, the total preparation solution was divided and taken according to the ratio (%) of the previous day or the current day, or the active ingredients in the table were divided according to the content corresponding to the ratio (%) and the preparation solution of the previous day or the current day was separately produced and then taken.

[0203] The method of taking the preparation solution (ratio % of the preparation solution) in each example is as follows.

[0204]

Table 28

[0205]

Table 29

[0206] Results of Examples 1 to 5

[0207] To randomly selected patients, the compositions of the following respective formulations were administered according to the administration methods described in each of the examples and comparative examples, and the degree of bowel cleansing, examination time required, gastric / gastrointestinal residual amount, administration time required, morning bowel movement frequency, administration completion rate, side effects (abnormal cases - nausea, vomiting, urgent bowel movement), willingness to re-administer, etc. were evaluated. The above-mentioned patients were healthy adults who had planned a regular outpatient colonoscopy and had never had a specific reaction to other commercially available bowel cleansing agents before, and patients with serious medical problems, heart diseases, diabetes, or any potentially serious symptoms were excluded.

[0208] Among the evaluation items, the degree of bowel cleansing, residual amount, and examination time required (in minutes) were evaluated by the clinician performing the endoscopy.

[0209] Degree of success of bowel cleansing

[0210] The degree of bowel cleansing was confirmed through colonoscopy. For the objective evaluation of the bowel cleansing effect, the grade of the bowel cleansing effect was evaluated based on the Harefield Cleansing Scale, and the degree of bowel cleansing of each subject was evaluated by dividing it into a total of five levels.

[0211]

Table 30

[0212] The above five scores were classified into grades from A to D as follows to evaluate the degree of bowel cleansing. Specifically, based on the Harefield cleansing scale, grades A and B were evaluated as successful bowel cleansing, and grades C and D were evaluated as failed bowel cleansing.

[0213] <Evaluation of overall colon cleansing degree> Grade A: All segments scored 1 or 2 (All segments scored 1 or 2) Grade B: 1 segment scored 3 (1 segments scored 3) Grade C: 1 segment scored 4 Grade D: 1 segment scored 5

[0214] Residual amount

[0215] Gastric residue volume and intestinal residue volume were measured by aspirating the water remaining in the gastrointestinal tract through the suction channel within the scope during endoscopy.

[0216] Inspection time required

[0217] The time from the start to the completion of colonoscopy was recorded.

[0218] Among the evaluation items, the time required for administration (minutes), the number of morning bowel movements (times), the completion rate of administration (%), the number of abnormal cases (%), and the intention to take the drug again (%) were evaluated through questionnaires from the subjects (patients). Among them, the completion rate of administration, the number of abnormal cases, and the intention to take the drug again were calculated as the ratio of the number of subjects corresponding to the item to the total number of subjects.

[0219] The results are shown in Table 31.

[0220]

Table 31

[0221] In Examples 1 to 5, the total dosage of the preparation solution and water taken on the same day was all 700 mL or less. However, in terms of the success degree of bowel cleansing, these showed excellent or equivalent effects compared with the comparative examples. In terms of the gastric residue amount / intestinal residue amount as an index of safety, the residue amount was significantly reduced compared with each comparative example. In particular, the gastric residue amount was reduced to less than half compared with the comparative examples. A considerable number of patients undergoing colonoscopy also undergo gastroscopy at the same time. Since fasting for at least 8 hours or more including water is recommended during gastroscopy, there is a problem of direct opposition to the method of taking the bowel cleansing agent for colonoscopy. From the aspect of improving the safety of the subjects, the gastric residue amount is also an important evaluation criterion. When taking the composition of the example of the present invention, the gastric residue amount was remarkably improved, and the safety of the subjects was very effectively improved.

[0222] In addition, the time required for the endoscopy examination was reduced compared with the comparative examples. This is because the intestinal environment was in a state suitable for colonoscopy, so the reaching time and recovery time to the cecum during endoscopy were shortened. The ease of examination also increased, and the visualization for endoscopy implementation and polyp confirmation became easier due to the improvement of the cleansing degree in the intestine and the reduction of the residual fluid.

[0223] The time required for the patients to take the medicine was significantly reduced to less than half compared with the comparative examples. The number of morning bowel movements also decreased, the convenience of taking the medicine for the patients increased, and the completion rate of taking the medicine also increased.

[0224] Abnormal cases such as nausea, vomiting, and sudden urge to defecate were very significantly reduced compared with the comparative examples.

[0225] The willingness of the patients to take the medicine again also increased significantly. In particular, in the case of Example 3, 100% willingness to take the medicine again was shown.

[0226] Examples 6 to 16

[0227] Similar to Examples 1 to 5, the composition of each active ingredient in the following table was divided and taken at a ratio of 80:20 to 75:25 for the previous day: the current day (however, the total dosage of the preparation solution and water on the current day was 700 mL, 600 mL, or 500 mL or less). Examples 6 to 16 are the compositions of products that have already been approved as intestinal cleansers by the Korean Food and Drug Administration. The packages of these products were used as they were. Similar to Examples 1 to 5, the total preparation solution was divided at the ratio (%) of the previous day or the current day and taken, or each active ingredient was divided according to the content corresponding to the ratio (%) and the preparation solution of the previous day or the current day was separately manufactured and then taken. The method of taking for each example (ratio % of the preparation solution) is as follows.

[0228]

Table 32

[0229] Example 17

[0230] A composition was manufactured according to the components and contents in the following table (see Example 3).

[0231]

Table 33

[0232] (1) Example 17-1

[0233] Dosage method

[0234] After mixing the active ingredients in the table well according to the content, an appropriate amount of water was added and dissolved, then water was added again so that the total volume became 960 mL in total, and then they were mixed well to produce a preparation solution. For the total 960 mL of the preparation solution, a total of 390 mL of water must be taken.

[0235] In each of the comparative examples and the examples, the active ingredients in the said table were divided into contents corresponding to the said ratio (%), and after separately preparing the preparation liquid of the previous day or the same day, the subjects were guided to take it.

[0236] In the comparative examples, the said composition was divided into two packages respectively, and one package was taken each on the previous day and the same day. In the examples, it was divided into a total of three packaging units. Two packages were provided on the previous day and one package was provided in the morning of the same day. That is, each packaging unit in the examples contained 36.67 g of D-sorbitol, 5 g of ascorbic acid, 0.7 g of sodium hydrogen carbonate, 0.3 g of potassium hydrogen carbonate, and 0.8 g of flavor powder. In contrast, the subjects were recommended to take it as follows: the packaging unit to be taken on the previous night was labeled as Agent A, and the packaging unit to be taken on the day of the test was labeled as Agent B.

[0237] (1) At 8:00 p.m. on the night before the test, take the solution obtained by sufficiently diluting one package of Agent A in 320 mL of water over 10 minutes, and then drink an additional 130 mL of water. Subsequently, dilute another package in the same way (320 mL of water) and take it over 10 minutes, and then drink an additional 130 mL of water.

[0238] (2) At dawn or in the morning on the day of the test, dilute each one package of Agent B in 320 mL of water and take it over 10 minutes. Then, drink an additional 130 mL of water. For safety during the test, it is recommended to complete the intake by 2 hours before the start of the test.

[0239] For taking the comparative example, it was prepared in four packaging units respectively. That is, each packaging unit contained 27.5 g of D-sorbitol, 3.75 g of ascorbic acid, 0.525 g of sodium hydrogen carbonate, 0.225 g of potassium hydrogen carbonate, and 0.6 g of flavor powder. In contrast, the subjects were recommended to take it as follows: the packaging unit to be taken on the previous night was labeled as Agent A, and the packaging unit to be taken on the day of the test was labeled as Agent B.

[0240] (1) In the comparative example, at 8:00 p.m. the night before the test, a solution prepared by sufficiently diluting one packet of Agent A in 240 mL of water was taken over 10 minutes, and an additional 97.5 mL of water was drunk. Subsequently, one packet was diluted again in the same manner (240 mL of water), taken over 10 minutes, and then an additional 97.5 mL of water was drunk.

[0241] (2) At dawn or in the morning on the day of the test, a solution prepared by sufficiently diluting one packet of Agent B in 240 mL of water was taken over 10 minutes, and an additional 97.5 mL of water was drunk. Subsequently, one packet was diluted again in the same manner (240 mL of water), taken over 10 minutes, and then an additional 97.5 mL of water was drunk. For safety during the test, it is recommended to complete the intake by 2 hours before the start of the test.

[0242] The intake methods for each comparative example and example are as follows.

[0243]

Table 34

[0244]

Table 35

[0245] (2) Example 17-2

[0246] Dosage method

[0247] After thoroughly mixing the active ingredients in the table according to the content, adding an appropriate amount of water to dissolve them, adding water again so that the total volume becomes 960 mL in total, and then thoroughly mixing them together, a preparation solution was produced. For a total of 960 mL of the preparation solution, a total of 320 mL of water must be taken.

[0248] In each comparative example and example, the active ingredients in the table were divided according to the corresponding ratio (%) content, and a preparation solution for the day before or the day of was separately produced, and then guided to be taken together with water.

[0249] The administration methods of each comparative example and example are as follows.

[0250]

Table 36

[0251]

Table 37

[0252] Example 18

[0253] In this example, a composition with the components and contents shown in the following table was used.

[0254]

Table 38

[0255] Dosage method

[0256] After mixing the active ingredients well according to the content, an appropriate amount of water was added and dissolved, then water was added again so that the total volume became 1 L in total, and then they were mixed well to produce a preparation solution. 1 L of water must be taken for every 1 L of the total preparation solution.

[0257] In each comparative example and example, the total preparation solution was divided into the corresponding ratio (%) on the previous day or the same day and taken together with water, or the active ingredients in the above table were divided according to the content corresponding to the ratio (%), and after separately preparing the preparation solution on the previous day or the same day, it was guided to take it together with water.

[0258] The administration methods (ratio % of the preparation solution) of each example are as follows.

[0259]

Table 39

[0260]

Table 40

[0261] Example 19

[0262] A composition was produced according to the components and contents in the following table.

[0263]

Table 41

[0264] Dosage method

[0265] After thoroughly mixing the active ingredients according to their contents, an appropriate amount of water was added and dissolved, then water was added again so that the total volume became 1 L in total, and then they were thoroughly mixed to produce a preparation solution. A total of 1 L of water must be taken for every 1 L of the total preparation solution.

[0266] In each comparative example and example, it was guided to take the total preparation solution divided into the corresponding ratio (%) on the previous day or the same day together with water, or to divide the active ingredients in the above table according to the content corresponding to the ratio (%), and after separately producing the preparation solution on the previous day or the same day, take it together with water.

[0267] The administration methods (ratio % of the preparation solution) of each example are as follows.

[0268]

Table 42

[0269]

Table 43

[0270] Example 20

[0271] A composition was produced according to the components and contents in the following table.

[0272]

Table 44

[0273] Dosage method

[0274] After mixing the active ingredients well according to their contents, an appropriate amount of water was added and dissolved, and then water was added again so that the total volume became 1 L in total. After that, they were mixed well to produce a preparation liquid. 1 L of water in total must be taken with respect to 1 L of the total preparation liquid.

[0275] In each comparative example and example, the total preparation liquid was divided into the corresponding ratio (%) on the previous day or the same day and taken together with water, or the active ingredients in the above table were divided according to the content corresponding to the ratio (%), and after separately producing the preparation liquid on the previous day or the same day, they were guided to take it together with water. The taking methods (ratio % of the preparation liquid) of each example are as follows.

[0276]

Table 45

[0277]

Table 46

[0278] Results of Examples 17 to 20

[0279] The compositions of the following respective formulations were administered to randomly selected patients according to the administration methods described in each of the examples and comparative examples, and the degree of bowel cleansing, endoscopy time, residual amount in the intestine, ease of administration, side effects (abnormal cases - nausea, vomiting, dizziness), willingness to take again, etc. were evaluated. The said patients were healthy adults who had planned a regular outpatient colonoscopy and had not previously had a specific reaction to other commercially available bowel cleansing agents, and patients with serious medical problems, heart disease, diabetes, or any potentially serious symptoms were excluded.

[0280] Among the items to be evaluated, the degree of bowel cleansing, ease of examination, residual amount, and examination time (minutes) were evaluated by the clinician performing the endoscopy.

[0281] Degree of success of bowel cleansing

[0282] The degree of bowel cleansing was confirmed through colonoscopy. For the objective evaluation of the bowel cleansing effect, the bowel cleansing effect grade was evaluated based on the Harefield Cleansing Scale, and the degree of bowel cleansing of each subject was evaluated in five levels.

[0283] Specifically, according to the Harefield cleansing scale, it was evaluated that the bowel cleansing was successful from 1 point to 3 points, and 4 points and 5 points were evaluated as the failure of bowel cleansing.

[0284]

Table 47

[0285] Endoscopy time

[0286] The time from the start to the completion of the colonoscopy was recorded.

[0287] Residual amount

[0288] The amount of water remaining in the intestine was measured by sucking the water remaining in the gastrointestinal tract through the suction channel in the scope during endoscopy and observing the results.

[0289] Ease of inspection

[0290] The ease of endoscopy and polyp confirmation was evaluated based on the degree of intestinal cleansing and the reduction of the residual fluid.

[0291] Among the evaluation items, ease of administration, abnormal cases, and willingness to re-administer were evaluated through questionnaires from the subjects (patients) and classified as follows.

[0292] - Evaluation criteria for ease of administration: not difficult (1 point), slightly difficult (2 points), very difficult (3 points)

[0293] - Evaluation criteria for abnormal cases: did not occur (1 point), occurred slightly (2 points), occurred frequently (3 points)

[0294] - Evaluation criteria for willingness to re-administer: willing to re-administer (1 point), not willing (2 points)

[0295] The results are shown in Table 48.

[0296]

Table 48

[0297] In Examples 17 to 20, the total dosage of the preparation solution and water taken on the same day was all 500 mL or less. However, in almost all items (i.e., cleanliness, ease of taking, willingness to take again, time required for colonoscopy, residual amount, etc.), they showed significantly better effects compared to the comparative examples. In particular, a considerable number of colonoscopy patients are undergoing gastroscopy simultaneously. Since fasting for at least 8 hours or more, including water, is recommended during gastroscopy, there is a problem of direct opposition to the method of taking the intestinal lavage agent for colonoscopy. From the aspect of improving the safety of the subjects, the residual amount also becomes an important evaluation criterion. When taking the composition of the example of the present invention, the residual amount was improved epoch-makingly, and the safety of the subjects was very effectively improved.

[0298] Through the above examples, the following effects were confirmed.

[0299] In all examples, although the dosage taken in the morning on the day of the examination was reduced to 700 mL or less, particularly 600 mL or less, and further 500 mL or less, not only was the intestinal lavage degree better, but also the mucosal lavage degree was shown. Since the intestinal environment was in a state suitable for colonoscopy, the time to reach the cecum and the recovery time during endoscopy were shortened, and the time required for the examination was reduced epoch-makingly. Also, due to the reduction of the intestinal lavage degree and the residual fluid, ensuring the visual field for the implementation of endoscopy and polyp confirmation etc. proceeded easily, and the ease of examination for clinicians also increased.

[0300] Furthermore, the ease of implementing endoscopy evaluated by the subjects etc. was excellent, the completion rate of taking the medicine increased, and abnormal cases decreased. Therefore, the ease of taking the medicine was improved epoch-makingly, and a high willingness to take it again was confirmed.

[0301] Considering that most of the compositions used in the examples are drugs that have already been proven effective and safe clinically etc. through the existing method of taking (comparative examples) and are commercially available with approval in the country, the new method of taking based on the present invention was confirmed to be more effective and safe compared to the existing approved methods of taking for the drugs currently on the market.

[0302] Thus, not only abnormal cases experienced during the process of taking the medicine by the patient, but also during the actual colonoscopy, the reduction of the water content in the intestine facilitates the implementation of colonoscopy, and the risk associated with colonoscopy can be reduced by shortening the examination time. Therefore, an epoch-making improvement effect has been confirmed from the aspect of safety. In particular, many colonoscopy patients also undergo gastroscopy at the same time. During gastroscopy, fasting for at least 8 hours including water is recommended, and there is a problem of direct opposition to the method of taking the intestinal cleansing agent for colonoscopy. The gastric residual volume is also an important evaluation criterion from the aspect of improving the safety of the subject. However, when taking the composition of the embodiment of the present invention, it was confirmed that the gastric residual volume was improved epoch-makingly, and the safety of the subject was very effectively improved.

Claims

1. An intestinal lavage composition to be taken before an examination requiring intestinal lavage, wherein the composition is taken separately on the day before and on the day of the examination, and the total dosage taken on the day of the examination is 700 mL or less.

2. The intestinal lavage composition according to claim 1, wherein the total dosage taken on the day of the examination is 500 mL or less.

3. The intestinal lavage composition according to claim 1, wherein the total dosage taken on the day before and on the day of the examination is 1.0 L to 4.0 L.

4. The intestinal lavage composition is a preparation solution obtained by dissolving a composition in the form of a powder, granule, liquid preparation, tablet or capsule containing an active ingredient in a water-soluble solvent; and separately contains a water-soluble solvent. The intestinal lavage composition is administered by a method of taking the water-soluble solvent separately after taking the preparation solution, and the method is repeated a total of 2 to 4 times on the day before and on the day of the examination.

5. The intestinal lavage composition according to claim 1, which is in any form of a solution, suspension or emulsion.

6. An intestinal lavage composition containing, as a first active ingredient, one or more sugar alcohols selected from xylitol, sorbitol, glycerol, erythritol, threitol, arabitol, ribitol, mannitol, galactitol, fucitol, iditol, inositol, volemitol, isomalt, maltitol, lactitol, maltotriitol, maltotetraitol and polyglycitol; as a second active ingredient, ascorbic acid or a mixture of ascorbic acid and ascorbate; and a water-soluble solvent, wherein the content of the first active ingredient is 10 g / L to 500 g / L based on the total composition, the content of the second active ingredient is 1 g / L to 300 g / L based on the total composition, and the content of the water-soluble solvent is 1.0 L to 3.0 L.

7. The intestinal lavage composition according to claim 6, further containing sodium bicarbonate and / or potassium bicarbonate as a third active ingredient, and the content of the third active ingredient is 0.5 g / L to 5 g / L based on the total composition.

8. 110 g of D-sorbitol; 15 g of ascorbic acid; 2.1 g of sodium hydrogen carbonate; 0.9 g of potassium hydrogen carbonate; and 1.0 L to 3.0 L of water, wherein the water is administered in the form of a solution in which the components are dissolved or is administered alone, the composition for intestinal lavage according to claim 6.

9. A composition for intestinal lavage comprising polyethylene glycol as a first active ingredient; ascorbic acid or a mixture of ascorbic acid and ascorbate as a second active ingredient; and a water-soluble solvent, wherein the content of the first active ingredient is 10 g / L to 500 g / L based on the total composition, the content of the second active ingredient is 1 g / L to 300 g / L based on the total composition, and the content of the water-soluble solvent is 1.0 L to 3.0 L, the composition for intestinal lavage according to any one of claims 1 to 5.

10. 200 g of polyethylene glycol 3350; 9.4 g of ascorbic acid; 11.8 g of sodium ascorbate; 15 g of anhydrous sodium sulfate; 5.382 g of sodium chloride; 2.030 g of potassium chloride; and 1.0 L to 3.0 L of water, wherein the water is administered in the form of a solution in which the components are dissolved or is administered alone, the composition for intestinal lavage according to claim 9.

11. 140 g of polyethylene glycol 3350; 7.54 g of ascorbic acid; 48.11 g of sodium ascorbate; 9 g of anhydrous sodium sulfate; 5.2 g of sodium chloride; 2.2 g of potassium chloride; and 1.0 L to 3.0 L of water, wherein the water is administered in the form of a solution in which the components are dissolved or is administered alone, the composition for intestinal lavage according to claim 9.

12. 160 g of polyethylene glycol 3350; 40.6 g of ascorbic acid; 9.4 g of sodium ascorbate; 18 g of anhydrous sodium sulfate; 2.7 g of sodium chloride; 1 g of potassium chloride; and 1.0 L to 3.0 L of water, wherein the water is administered in the form of a solution in which the components are dissolved or is administered alone, the composition for intestinal lavage according to claim 9.

13. The composition for intestinal lavage according to any one of claims 1 to 5, comprising, based on the total composition, 0.001 g / L to 0.1 g / L of sodium picosulfate or its hydrate; 0.5 g / L to 50 g / L of magnesium oxide; 1 g / L to 50 g / L of citric acid; and 1.0 L to 3.0 L of a water-soluble solvent.

14. The composition for intestinal lavage according to any one of claims 1 to 5, comprising, based on the total composition, 10 g / L to 500 g / L of polyethylene glycol; 1 g / L to 300 g / L of sorbitol; 0.001 g / L to 1 g / L of sodium picosulfate or its hydrate; and 1.0 L to 3.0 L of a water-soluble solvent.

15. The composition for intestinal lavage according to any one of claims 1 to 5, comprising, based on the total composition, 5 g / L to 300 g / L of sodium sulfate; 0.1 g / L to 50 g / L of potassium sulfate; 0.1 g / L to 50 g / L of magnesium sulfate; and 1.0 L to 3.0 L of a water-soluble solvent.

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