Colon cleansing composition with enhanced cleansing efficiency and ease of administration

Abstract

The present invention relates to a colon cleansing composition with improved ease of administration. The composition minimizes side effects caused by excessive ingredient content in conventional colonic laxatives while providing equivalent or superior intestinal cleansing efficacy, thereby remarkably improving patient compliance and ingestion convenience. In addition, as an uncoated tablet requiring no separate coating processes, a preparation that maintains the quality of tablets such as rapid disintegration and does not have a bitter taste can be provided. The present invention provides a pharmaceutical formulation comprising the colon cleansing composition with improved ease of administration and a method for colon cleansing using the formulation, thereby realizing a patient-centered colon cleansing process and ultimately greatly contributing to the improvement of colonoscopy quality.

Description

Colon cleansing composition with enhanced colon cleansing power and ease of administration

[0001] The present invention relates to a composition for colon cleansing that has improved colon cleansing power and ease of administration.

[0002] Colonoscopy is a widely performed procedure essential for the diagnosis, screening, and treatment of colon diseases. Achieving a clear view of the colon is crucial for a successful colonoscopy, and bowel preparation prior to the examination is essential. Insufficient bowel preparation can lead to various problems, including a reduced detection rate, delayed examination time, and increased need for repeat examinations.

[0003] Existing colon cleansing medications primarily utilize osmotic or stimulant laxatives, either alone or in combination, to achieve bowel cleansing effects. Representative colon cleansing medications include single sulfate preparations and combinations of magnesium and citrate.

[0004] Among existing sulphate-based laxatives, sulfate-based formulations exhibit a high osmotic pressure per unit weight, which has the advantage of inhibiting intestinal water absorption and enhancing bowel cleansing. However, excessive sulfate intake has been reported to cause gastrointestinal irritation and subsequent adverse effects. For example, a sulphate-containing laxative composition is disclosed as a liquid bowel cleansing composition comprising anhydrous sodium sulfate, anhydrous magnesium sulfate, and potassium sulfate. While this composition utilizes the osmotic action of sulfate ions, its high dosage and characteristic bitterness lead to poor patient compliance.

[0005] Magnesium and citrate complex preparations are known to enhance intestinal cleansing by providing a complex intestinal motility-promoting effect via CCK (cholecystokinin) in addition to their osmotic effect. However, concerns have been raised about the potential side effects of hypermagnesemia due to magnesium and blood acidification due to citrate.

[0006] These existing laxative products have limitations, such as low patient compliance due to the need for large doses of medication or liquids for effective bowel cleansing. Furthermore, excessive use of certain ingredients can lead to side effects such as gastrointestinal upset, electrolyte imbalances, and blood acidification. For example, sulfate-containing laxative compositions have been reported to cause side effects such as nausea and vomiting. Furthermore, polyethylene glycol (PEG)-based colon cleansers require large amounts of water, leading to low compliance and potentially insufficient bowel cleansing.

[0007] Therefore, there is a pressing need to develop a new colon cleansing composition that minimizes the side effects of existing laxatives due to excessive ingredient content, while maintaining excellent bowel cleansing properties and dramatically increasing patient convenience. In particular, there is a growing need for a colon cleansing composition that reduces dosage, improves patient compliance, and reduces residual volume.

[0008] Additionally, commercialized laxative tablets are coated with an organic solvent to prevent disintegration delays due to salt accumulation and to mask the bitter taste. This coating process complicates the manufacturing process and increases manufacturing costs. Furthermore, due to the nature of the main ingredient, aqueous coating is not feasible, leading to the use of organic solvent coating. This is an environmentally undesirable manufacturing process.

[0009] There is a need to develop a colon cleansing composition that can solve these problems.

[0010] [Prior Art Literature]

[0011] [Patent Document]

[0012] KR 10-2111094 B1

[0013] The purpose of the present invention is to provide a composition for colon cleansing with improved convenience of administration.

[0014] Another object of the present invention is to provide a novel colon cleansing composition that minimizes side effects caused by excessive ingredient content of existing colon cleansing agents while providing equivalent or superior intestinal cleansing power and dramatically increasing patient convenience and compliance.

[0015] Another object of the present invention is to provide a preparation that maintains the quality of tablets such as tablets without undergoing a separate coating process and does not have a bitter taste.

[0016] Another object of the present invention is to provide a pharmaceutical formulation comprising the colon cleansing composition having improved convenience of administration and a colon cleansing method using the formulation.

[0017] To achieve the above-described purpose, the present invention relates to a colon cleansing composition for oral administration comprising sodium picosulfate hydrate; anhydrous sodium sulfate; and magnesium hydroxide or magnesium oxide.

[0018] Additionally, the composition may contain sodium picosulfate hydrate in an amount of 0.5 mg to 2.0 mg per tablet.

[0019] Additionally, the composition may contain 1,000 mg to 1,500 mg of anhydrous sodium sulfate per tablet.

[0020] Additionally, the composition may contain simethicone in an amount of 10 mg to 20 mg per tablet.

[0021] Additionally, the composition may further comprise one or more additives selected from the group consisting of povidone, crospovidone, hydroxypropylcellulose, and mixtures thereof.

[0022] Additionally, the composition may further comprise simethicone.

[0023] Another invention for achieving the above-described purpose may be a colon cleansing tablet prepared by mixing the composition with purified water in an amount of 0.2 to 1 part by weight relative to the total weight of one tablet.

[0024] Additionally, the composition may contain 1,600 mg to 1,700 mg.

[0025] Additionally, the above tablets can be administered in divided doses on the day before and on the day of colonoscopy.

[0026] Additionally, the above tablets can be divided into 10 tablets the day before the colonoscopy and 10 tablets on the day of the examination.

[0027] Another invention for achieving the above-described purpose may be a capsule formulation for colon cleansing, which is prepared by mixing the composition with purified water in an amount of 0.2 to 1 part by weight relative to the total weight of one tablet and filling or filling and compressing the composition.

[0028] Another invention for achieving the above-described purpose may be a bowel cleansing kit for colonoscopy comprising the composition.

[0029] Another invention for achieving the above-described purpose may be a colon cleansing method characterized by administering the colon cleansing kit to a subject in need of colon cleansing.

[0030] The present invention minimizes the side effects caused by the excessive ingredient content of existing laxatives, while providing equivalent or superior intestinal cleansing properties and dramatically increasing patient convenience and compliance. Furthermore, the formulation, which does not require a separate coating process, maintains tablet quality, such as disintegration, and provides a formulation that does not have a bitter taste.

[0031] The present invention can realize a patient-centered colon cleansing process, which can ultimately contribute to improving the quality of colonoscopy.

[0032] Figure 1 shows the results of evaluating the colon cleansing power after administering a colon cleansing composition according to one embodiment of the present invention to rats.

[0033] Figure 2 shows the results of evaluating the colon cleansing ability after administering a colon cleansing composition according to one embodiment of the present invention to rats.

[0034] Figure 3 shows the results of evaluating the colon cleansing ability after administering a colon cleansing composition according to one embodiment of the present invention to rats.

[0035] Figure 4 shows the results of evaluating the colon cleansing ability after administering a colon cleansing composition according to one embodiment of the present invention to rats.

[0036] The present invention relates to a colon cleansing composition for oral administration comprising sodium picosulfate hydrate; anhydrous sodium sulfate; and magnesium hydroxide or magnesium oxide.

[0037] Hereinafter, embodiments of the present invention will be described in detail so that those skilled in the art can easily implement them. However, the present invention may be implemented in various different forms and is not limited to the embodiments described herein.

[0038] In the present invention, a tablet is a solid preparation for oral administration, which means a compressed molded form including a main ingredient and various additives as needed.

[0039] In the present invention, the composition for bowel cleansing refers to a pharmaceutical preparation used to cleanly empty the intestines before colonoscopy or other colon-related procedures.

[0040] In the present invention, a capsule is a solid preparation for oral administration, which means a tablet formed by filling a granule containing a main ingredient and various additives as needed, or a tablet formed by compressing the granule into a mini tablet and filling the tablet into a capsule.

[0041] In the present invention, milligrams (mg) means the content per tablet unless otherwise specified.

[0042] The present invention provides an oral colon cleansing composition that minimizes the side effects of existing colonic laxatives, improves patient compliance, and provides excellent bowel cleansing properties, and is used for colon cleansing for colonoscopy, colon surgery, or other colon-related medical procedures.

[0043] Specifically, by reducing the total sulfate dosage by approximately 60% compared to existing sulfate-only products, and reducing the total magnesium dosage by approximately 50% compared to magnesium and citrate combination products, and eliminating citrate, the risk of side effects such as gastrointestinal irritation, electrolyte imbalance, hypermagnesemia, and blood acidification can be significantly reduced.

[0044] In addition, the present invention can provide an intestinal cleansing effect equivalent to or superior to that of existing formulations through an optimized complex composition of an osmotic pressure-inducing and intestinal peristalsis-promoting component and a stimulant laxative, sodium picosulfate hydrate, and can also resolve the inconvenience of existing formulations requiring the intake of a large amount of liquid by formulating it in the form of oral tablets. The total dosage of Orapang tablets, which are commercially available in the form of oral tablets, is 28 tablets, but the present invention can dramatically improve patient compliance with medication with 20 tablets.

[0045] Specifically, the present invention relates to an oral colon cleansing composition comprising sodium picosulfate hydrate; anhydrous sodium sulfate; and magnesium hydroxide or magnesium oxide. The composition may further comprise simethicone.

[0046] As described above, sodium picosulfate hydrate acts as a stimulant laxative, and due to the osmotic pressure and CCK (cholecystokinin) effect of the sulfate, which is anhydrous sodium sulfate, and the magnesium hydroxide or magnesium oxide, it further promotes the intestinal motility promoting effect, thereby providing an intestinal cleansing effect equivalent to or superior to that of existing commercially available preparations.

[0047] The above-mentioned sodium picosulfate hydrate is a stimulant laxative, primarily used for colonic emptying and constipation treatment. When administered orally, sodium picosulfate hydrate can be converted into active metabolites by colonic microorganisms. These active metabolites directly stimulate the colonic mucosa, strongly promoting intestinal peristalsis. Simultaneously, they inhibit the absorption of water and electrolytes in the colon, increasing the moisture content of intestinal contents and softening stool. Through this dual mechanism of action, sodium picosulfate hydrate rapidly promotes intestinal emptying, leading to effective bowel cleansing.

[0048] The above anhydrous sodium sulfate has the characteristic of being hardly absorbed in the digestive tract, especially in the small and large intestine, when administered orally. ... creates a high concentration of sodium ions (Na) in the intestinal lumen. + ) and sulfate ion (SO4 2- ), which causes the osmotic pressure of the intestinal lumen to be significantly higher than that of the surrounding tissues (blood, cells). The high osmotic pressure of the intestinal lumen draws a large amount of water from the blood and tissues of the body into the intestinal lumen to maintain osmotic balance. This significantly increases the water content of the intestinal contents, and the volume of the stool expands. The stool, with its high water content and increased volume, increases the physical pressure applied to the intestinal wall, reflexively stimulating peristalsis. The softening of the stool also facilitates its movement through the intestines, inducing rapid defecation.

[0049] The above magnesium hydroxide and magnesium oxide commonly contain magnesium ions (Mg 2+ ) as compounds that provide osmotic laxatives, which mainly act as osmotic laxatives and promote intestinal movement. The magnesium hydroxide or magnesium oxide is dissolved by gastric acid when administered orally and forms magnesium ions (Mg 2+) exists in the form of magnesium ions. The absorption rate of the magnesium ions is very low in the digestive tract. Unabsorbed magnesium ions remain in the intestinal lumen, forming a high osmotic pressure gradient, which attracts a large amount of water from the surrounding tissues into the intestinal lumen. The water accumulated in the intestines in this way softens the stool and increases its volume, facilitating defecation. The magnesium ions affect intestinal motility beyond the simple osmotic pressure effect. The magnesium ions can indirectly induce intestinal peristalsis by stimulating sensory receptors in the intestinal wall. In addition, magnesium is involved in the process of muscle contraction and relaxation, and contributes to the overall regulation of intestinal motility by supporting the proper function of the enteric nervous system along with its relaxing effect on intestinal smooth muscles. According to some studies, magnesium ions can also stimulate the secretion of gastrointestinal hormones such as cholecystokinin (CCK), which is associated with the promotion of intestinal motility.

[0050] The above-mentioned anhydrous sodium sulfate, magnesium hydroxide, and magnesium oxide primarily exert a common osmotic laxative effect, increasing intestinal osmotic pressure and attracting water, thereby increasing stool volume and softening it. In the case of the above-mentioned magnesium compounds, the combined effects of magnesium ions regulating the enteric nervous system and indirectly stimulating peristalsis activate intestinal motility and promote defecation.

[0051] Simethicone is a surfactant used to remove gas from the gastrointestinal tract. Simethicone alters the physical properties of gas bubbles (bubbles) accumulated in the digestive tract, helping them to be easily expelled from the body. More specifically, simethicone effectively reduces the surface tension of gas bubbles (bubbles) present in the gastrointestinal tract by adsorbing them to the surface. Normally, gas generated in the intestines tends to clump together to form large bubbles, which causes abdominal bloating and discomfort. Therefore, when surface tension is reduced, large gas bubbles become unstable and can easily break apart. The broken large bubbles disperse into smaller, more finely divided gas bubbles, and simethicone prevents the small gas bubbles from clumping together to form larger bubbles. Small, separated gas bubbles are more easily absorbed by the intestinal wall or are more easily expelled from the body through belching or flatus.

[0052] The composition may contain 0.5 mg to 2.0 mg of sodium picosulfate per tablet, 0.7 mg to 1.5 mg, or 1 mg.

[0053] The composition may contain 1,000 mg to 1,500 mg of anhydrous sodium sulfate per tablet, 1,100 mg to 1,400 mg, 1,200 mg to 1,300 mg, or 1,250 mg.

[0054] The composition may contain simethicone in an amount of 10 mg to 20 mg per tablet, 12 mg to 18 mg, or 16.00 mg per tablet.

[0055] The composition may contain 100 mg to 400 mg of magnesium hydroxide or magnesium oxide per tablet, 150 mg to 300 mg, or 250 mg.

[0056] The above composition may contain magnesium hydroxide or magnesium oxide, but preferably, magnesium hydroxide is used instead of magnesium oxide to solve the conversion problem during wet granulation or the weight increase and strength decrease problem during stability testing, thereby ensuring the stability of the formulation.

[0057] Within the above range, by being included in a colon cleansing composition for oral administration, it can provide excellent colon cleansing power and dramatically increase patient convenience and compliance.

[0058] The composition may further comprise one or more additives selected from the group consisting of povidone, crospovidone, hydroxypropylcellulose, and mixtures thereof. Specifically, the povidone may be contained in an amount of 30.00 mg per tablet, the crospovidone in an amount of 40.00 mg per tablet, and the hydroxypropylcellulose in an amount of 35.00 mg per tablet.

[0059] Accordingly, the colon cleansing composition of the present invention may include sodium picosulfate hydrate, anhydrous sodium sulfate, simethicone, magnesium hydroxide or magnesium oxide, povidone, crospovidone, and hydroxypropylcellulose, and may be included in an amount of 1,600 mg to 1,700 mg per tablet. The colon cleansing composition of the present invention may be provided in a tablet form or a capsule form as described below, and at this time, may include 1,600 mg to 1,700 mg of the composition per tablet. In order to be provided in a tablet form or a capsule form, after preparing a mixture containing all of the above-described compositions, purified water may be mixed in an amount of 0.2 part by weight to 1 part by weight based on the total weight of one tablet.

[0060] According to another embodiment of the present invention, a colon cleansing tablet is characterized by comprising the colon cleansing composition described above.

[0061] The method for manufacturing the above colon cleansing tablets may be based on a conventional tablet manufacturing method. Without being limited to the examples described below, any method for manufacturing tablets for oral administration can be applied without limitation.

[0062] Specifically, the method for manufacturing a colon cleansing tablet of the present invention comprises the steps of: weighing raw materials by quantitatively measuring anhydrous sodium sulfate, sodium picosulfate hydrate, magnesium hydroxide, simethicone, hydroxypropyl cellulose, crospovidone, and povidone respectively; dissolving the sodium picosulfate hydrate, simethicone, and povidone using purified water and ethanol to prepare a binding solution; uniformly mixing the weighed anhydrous sodium sulfate and magnesium hydroxide to prepare a mixture; slowly adding the prepared binding solution to the mixture and kneading it to prepare a kneaded product; granulating the kneaded product into granules of an appropriate size; drying the granulated product under appropriate conditions; sieving the dried product to adjust the particle size to prepare a sieved product; sieving hydroxypropyl cellulose and crospovidone to prepare a sieved product; adding the sieved product to the sieved product and further mixing it; A step of adding purified water (KP) to the above mixture, mixing the mixture, and finally forming the final mixture to manufacture a semi-finished product; and a step of compressing and molding the semi-finished product into a tablet form using a tablet press may be included.

[0063] The above capsule formulation can be prepared by directly filling the final mixture into capsules or by pressing tablets with a round punch of 8 mm or less and then filling the capsules.

[0064] The colon cleansing tablet or colon cleansing capsule of the present invention may be administered in divided doses on the day before and the day of a colonoscopy. More specifically, the tablet may be administered in divided doses of 10 tablets on the day before and 10 tablets on the day of a colonoscopy. The colon cleansing tablet or capsule administered by the above-described administration method can not only significantly improve the convenience of taking the tablet, but can also exhibit a colon cleansing effect equivalent to or superior to that of conventional oral colon cleansing tablets.

[0065]

[0066] Manufacturing example

[0067] The examples below are manufactured according to the manufacturing method set forth in the General Prescriptions of the Korean Pharmacopoeia. The manufacturing process is as follows:

[0068] Weighing of raw materials (Step 1): Anhydrous sodium sulfate, sodium picosulfate hydrate, magnesium hydroxide, hydroxypropyl cellulose, crospovidone, and povidone were each weighed and prepared.

[0069] Preparation of binding solution (Process 2): A binding solution was prepared by dissolving sodium picosulfate hydrate and povidone in purified water (KP) (10.0 mg / tablet) and ethanol (95) (KP) (50.0 mg / tablet).

[0070] Mixing 1 (Process 3): The weighed anhydrous sodium sulfate and magnesium hydroxide were mixed evenly.

[0071] Union (Process 4): The binding solution prepared in Process 2 was slowly added to the mixture prepared in Process 3 and combined.

[0072] Granulation (Process 5): The mixture of Process 4 was granulated into granules of appropriate size.

[0073] Drying (Step 6): The granules from Step 5 were dried under appropriate conditions.

[0074] Formulation 1 (Process 7): The dried material from Process 6 was formed to control the particle size.

[0075] Sieving (Process 8): Uniformity was ensured by sieving hydroxypropyl cellulose and crospovidone.

[0076] Mixing 2 (Process 9): The sieved material of Process 8 was added to the established material of Process 7 and further mixed.

[0077] Final mixing (Step 10): 0.5 to 1 part by weight of purified water (KP) was added to the mixture of Step 9, and final mixing was performed.

[0078] Establishment 2 (Step 11): The final mixture of Step 10 was finally established.

[0079] Compression (Process 12): The semi-finished product of Process 11 was compressed into tablet form using a compression press.

[0080] Selection (Process 13): Defective tablets were selected from the pressed tablets.

[0081] Packaging (Step 14): The selected tablets were packaged in appropriate containers and packaging materials such as HDPE bottles and PP caps.

[0082] The contents of the components for manufacturing the above tablets are as shown in Table 1 below:

[0083] Raw material name Placebo Control group Example 1 (mg) Example 2 (mg) Control group (Orapang tablet) (mg) Sodium picosulfate monohydrate-11-Anhydrous sodium sulfate-1,2501,2501125.00Magnesium hydroxide-125250-Simethicone-161611.43Potassium sulfate---201.07Anhydrous magnesium sulfate---102.86Povidone 3030-Crospovidone 4040-Hydroxypropylcellulose 3535-Total (per tablet)-1,4971,622Total number of tablets taken-20 tablets20 tablets28 tablets

[0084] The placebo control group is a vehicle that does not contain the active ingredient. Examples 1 and 2 were designed to be taken 10 tablets the day before the test and 10 tablets on the day of the test, with a total magnesium hydroxide dosage of 2.5 g.

[0085] Experimental example

[0086] Colon Cleansing Test_1

[0087] The intestinal cleansing power and side effects according to the composition ratio were confirmed through comparison with the existing commercially available laxative, 'Orapang', Examples 1 and 2.

[0088] Test substance

[0089] Orapan (control): 1,125 mg of anhydrous sodium sulfate, 201.07 mg of potassium sulfate, 102.86 mg of anhydrous magnesium sulfate, and 11.43 mg of simethicone (28 tablets in total)

[0090] Placebo control group: vehicle (sterile water) without active ingredient

[0091] Example 1: 1,250 mg of anhydrous sodium sulfate, 1 mg of sodium picosulfate monohydrate, 125 mg of magnesium hydroxide, and 16 mg of simethicone (20 tablets in total)

[0092] Example 2: 1,250 mg of anhydrous sodium sulfate, 1 mg of sodium picosulfate monohydrate, 250 mg of magnesium hydroxide, and 16 mg of simethicone (total 20 tablets)

[0093]

[0094] test animals

[0095] rats (SD strain)

[0096] Test method

[0097] The animals were fasted for 24 hours prior to the test, and the cage floors were replaced with wire mesh to prevent fecal ingestion during the fasting period. The control drug, Examples 1 and 2 (two doses) were administered orally. The volume per dose was 4.8 mL, and the dosing interval was 1 hour. The dose was set at 2.64% of the human dose.

[0098] After drug administration, the animals were observed for general symptoms and abnormalities (e.g., gastric / cecal hypertrophy) for a certain period of time. To assess intestinal cleansing, the animals were euthanized after drug administration. The presence and condition of the large intestine (cecum-colon-rectum) were visually assessed (cleanliness scoring). In particular, changes in the clamping position and cross-sectional cutting were used to enhance the clarity of colon cleansing observations.

[0099] Evaluation criteria

[0100] 5: Only clear or transparent liquids are present

[0101] 4: A small amount of brown liquid is present and there is almost no semi-solid stool.

[0102] 3: Presence of brown liquid, semi-solid stool that is completely removable

[0103] 2: Presence of partially removable semi-solid stool

[0104] 1: Presence of hard, inextricable stool

[0105]

[0106] The test results are shown in Table 2 and Figures 1 to 4 below:

[0107] Raw material name Placebo Control group Example 1 Example 2 Control group (Orapang tablet) Purity evaluation 244423532444 Total 23.74.33.7

[0108] As a result of the evaluation of the intestinal cleansing power, the control group (Orapang) and Examples 1 and 2 all showed excellent intestinal cleansing power with scores of 3 to 5 points. Example 1 and the control group had an average score of 3.7 points, and Example 2 had an average score of 4.3 points, showing that Example 2 showed better intestinal cleansing power than Example 1 and the control group. Based on the above experimental results, it was confirmed that Example 3, which is the composition for colon cleansing of the present invention, showed a better intestinal cleansing effect than Example 1 and the control group. This can be said to mean that the optimized ingredient combination of the composition of the present invention can induce efficient intestinal cleansing. The composition of the present invention can contribute to improving the colon cleansing process by providing excellent intestinal cleansing power while reducing the dosage to increase patient compliance and minimize side effects.

[0109]

[0110] Measurement of osmotic pressure changes by composition

[0111] This study was conducted to measure the content of major ingredients and the resulting osmotic pressure changes in colon cleansing compositions, and to compare and analyze their intestinal cleansing power and safety based on these results. In particular, the study aimed to confirm the difference in osmotic pressure according to the amount of magnesium oxide (or magnesium hydroxide) and demonstrate the advantages of the composition of the present invention over a control drug.

[0112] Osmotic pressure test method

[0113] As shown in Table 3 below, a formulation containing the components was crushed, an amount corresponding to 10% of a single dose was precisely weighed, placed in a 200 mL beaker, 127.5 mL of purified water was added, and the solution was dissolved by stirring for 30 minutes to prepare the test solution. Each sample was dispensed in 50 uL units, and the osmolality was measured using an osmotic pressure meter (Osmomat3000).

[0114] Raw material nameExample 1 (mg)Example 2 (mg)Example 3 (mg)Example 4 (mg)Control (Orapang tablet) (mg)Sodium picosulfate hydrate 1111-Anhydrous sodium sulfate 1,250 1,250 1,250 1,250 1,250 1125.00Magnesium hydroxide 125 (52 as magnesium) 250 (104 as magnesium) 375 (156 as magnesium) -Magnesium oxide---173 (104 as magnesium) Simethicone 16 16 16 16 11.43Potassium sulfate 20 1.07Anhydrous magnesium sulfate 102.86Osmolarity (mOsmol / kg) 20 42 48 289 250 341Total number of tablets taken 20 tablets 20 tablets 20 tablets 20 tablets 28 tablets

[0115] Through a comparison of Examples 1, 2, and 3, it was confirmed that there was a difference in osmotic pressure depending on the amount of salt used. In addition, the reason why Example 2 showed excellent detergency in the rat detergency test despite having a lower osmotic pressure than the control drug is the combined effect of sodium picosulfate hydrate, and this can be the basis for showing excellent detergency without using excessive salt. In addition, Example 4 was manufactured into tablets with the same components as Example 3, except that magnesium hydroxide was changed to magnesium oxide. Through the above Example 5, the prescriptions in which magnesium hydroxide was converted to magnesium oxide were compared, and it was confirmed that the same osmotic pressure was shown when the amount of magnesium used, which shows osmotic pressure, was the same even if the form of the raw material was different.

[0116] The above experimental results demonstrate that superior bowel cleansing is not solely dependent on osmotic action, but rather on the synergistic effect of a small amount of the stimulant laxative sodium picosulfate monohydrate, combined with an appropriate combination of osmotic pressure-inducing salts, anhydrous sodium sulfate and magnesium hydroxide. This allows for a reduced total dosage while still ensuring sufficient efficacy, while also minimizing the risk of side effects such as gastrointestinal irritation and electrolyte imbalance.

[0117]

[0118] Although the preferred embodiments of the present invention have been described in detail above, the scope of the present invention is not limited thereto, and various modifications and improvements made by those skilled in the art using the basic concept of the present invention defined in the following claims also fall within the scope of the present invention.

[0119] The present invention relates to a composition for colon cleansing that has improved colon cleansing power and ease of administration.

Claims

1. Sodium picosulfate hydrate; anhydrous sodium sulfate; and Containing magnesium hydroxide or magnesium oxide Colon cleansing composition for oral administration.

2. In paragraph 1, The composition comprises 0.5 mg to 2.0 mg of sodium picosulfate per tablet. Colon cleansing composition for oral administration.

3. In paragraph 1, The composition contains 1,000 mg to 1,500 mg of anhydrous sodium sulfate per tablet. Colon cleansing composition for oral administration.

4. In paragraph 1, The composition further comprises at least one additive selected from the group consisting of povidone, crospovidone, hydroxypropyl cellulose and mixtures thereof. Colon cleansing composition for oral administration.

5. In paragraph 1, The above composition further comprises simethicone. Colon cleansing composition for oral administration.

6. In paragraph 5, The above simethicone is contained in 10 mg to 20 mg per tablet. Colon cleansing composition for oral administration.

7. Mix the composition according to any one of the clauses 1 to 8 with purified water in an amount of 0.2 to 1 part by weight based on the total weight of one tablet and compress it. Colon cleansing tablets.

8. In paragraph 7, Containing 1,600 mg to 1,700 mg of the above composition Colon cleansing tablets.

9. In paragraph 7, The above tablets are administered in divided doses on the day before and on the day of colonoscopy. Colon cleansing tablets.

10. In paragraph 7, The above tablets are divided into 10 tablets the day before the colonoscopy and 10 tablets on the day of the examination. Colon cleansing tablets.

11. Mix the composition according to any one of the clauses 1 to 8 with purified water in an amount of 0.2 to 1 part by weight based on the total weight of one tablet and fill or compress and fill. Capsule formulation for colon cleansing.

12. A composition comprising any one of the following items: 1 to 8. Bowel cleansing kit for colonoscopy.

13. Characterized in that it is administered to a subject requiring colon cleansing using the colon cleansing kit according to Article 12. Colon cleansing method.

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