CN116801888A

CN116801888A - Oral solid preparation for colon cleaning

Info

Publication number: CN116801888A
Application number: CN202180088680.5A
Authority: CN
Inventors: 李俊晔; 丘完; 张优荣; 金荣云; 金容峻
Original assignee: Taejoon Pharm Co Ltd
Current assignee: Taejoon Pharm Co Ltd
Priority date: 2020-12-31
Filing date: 2021-12-30
Publication date: 2023-09-22

Abstract

The present invention relates to an oral solid preparation for colon cleansing, wherein the oral solid preparation minimizes side effects, has excellent administration convenience and administration compliance, can rapidly exhibit drug efficacy, and has excellent colon cleansing ability.

Description

Oral solid preparation for colon cleaning

Technical Field

The present invention relates to oral solid formulations for colon cleansing.

Background

Colon cancer is one of the most common cancers worldwide, with its incidence increasing gradually. Colon cancer does not exhibit any special symptoms and is therefore difficult to detect early, whereas colonoscopy is critical for early detection and diagnosis of colon cancer.

For accurate examination and disease diagnosis in colonoscopy, whether the colon is washed and the degree of colon cleaning are very important, and if the colon is not washed cleanly, there may be a problem that diagnosis is impossible or the examination accuracy is lowered. In some cases, the colon cleansing agent may be taken again for re-examination.

In particular, for successful colonoscopy and diagnosis of disease, it is important to administer all drug solutions according to the intended use and dosage of the colon cleansing agent. Colon cleansers are typically prescribed without face-to-face contact between the physician and the patient, and thus the patient often administers the colon cleanser himself.

Representative colon cleansers having sulfate as the active ingredient include Suprep solutions consisting of 35g anhydrous sodium sulfate, 6.26g potassium sulfate, and 3.2g anhydrous magnesium sulfate.

However, in the case of a liquid for colon cleansing, the amount of the liquid medicine to be administered is too large or has a bitter taste, and thus patients often cannot take all the liquid medicine. In addition, there is a problem in that patients complain about side effects such as nausea, vomiting, etc. after taking the medicine. To solve this problem, tablet-type colon cleansers have been developed, but for colon cleansing, about at least 28 tablets weighing about 1.6g to 1.7g need to be taken. Thus, patients still have difficulty taking tablets because they must swallow bulky tablets, and there still remain problems with patients complaining of gastrointestinal disorders such as nausea, vomiting and abdominal pain after taking tablets. In addition, the bulky tablet may not be completely dissolved in the gastrointestinal tract, and its residue may remain in the gastrointestinal tract, thus causing gastrointestinal diseases such as redness (rubefaction). Residues can reduce the accuracy of endoscopy by obstructing the field of view during gastroscopy and colonoscopy, and make it difficult to detect lesions during endoscopy due to insufficient colon cleaning capability.

Thus, there is a need for colon cleansing formulations that exhibit improved ease of administration and drug compliance while exhibiting excellent cleansing capabilities.

Disclosure of Invention

Technical problem

It is an object of the present invention to provide oral solid formulations for colon cleansing.

Technical proposal

Embodiments of the present invention are described below, but these embodiments are provided for the purpose of illustrating the present invention only, and the present invention is not limited thereto. Each of the descriptions and embodiments disclosed in the present invention below may be applied to each of the other descriptions and embodiments. In other words, all combinations of the various elements disclosed in the invention are within the scope of the invention.

Furthermore, unless the context of the present specification specifically defines, singular forms may include plural forms and vice versa.

The present invention can provide an oral solid preparation comprising a cathartic component as an active ingredient.

The oral solid preparation of the invention can be used for colon cleaning. In other words, the oral solid preparation of the present invention may be a colon cleansing agent.

The oral solid preparation may include a unit solid preparation, and the weight of the unit solid preparation of the oral solid preparation is about 0.5g or less. In addition, the weight of the unit solid preparation of the oral solid preparation may be about 0.05g or more.

In the present invention, the term "unit solid preparation" may refer to one (single) solid preparation constituting a solid preparation, and the term "solid preparation" may refer to a group comprising a plurality of unit solid preparations.

In the present invention, the weight per unit solid preparation may refer to the weight per unit solid preparation (unit). In other words, the solid formulation of the present invention may comprise a unit solid formulation having a weight per unit solid formulation (unit) of about 0.5g or less. Further, the weight per unit solid formulation (unit) may be about 0.05g or more.

The solid formulation may comprise a plurality of unit solid formulations. In embodiments of the present invention, the solid formulation may comprise from about 70 to about 2000 units of the solid formulation. In particular, the solid formulation may comprise about 70 or more, about 71 or more, about 72 or more, about 80 or more, about 86 or more, about 89 or more, about 90 or more, about 100 or more, about 107 or more, about 110 or more, about 120 or more, about 125 or more, about 129 or more, about 130 or more, about 134 or more, about 140 or more, about 143 or more, about 150 or more, about 160 or more, about 161 or more, about 170 or more, about 172 or more, about 180 or more, about 188 or more, about 190 or more, about 200 or more, about 210 or more, about 215 or more, about 220 or more, about 230 or more, about 240 or more, about 250 or more, about 260 or more, about 270 or more, about 280 or more, about 290 or more, about 300 or more, about 172 or more, about 180 or more, about 188 or more, about 190 or more, about 200 or more, about 210 or more, about 215 or more, about 220 or more, about 230 or more, and may comprise about 2000 or less, about 1500 or less, about 1434 or less, about 1200 or less, about 1100 or less, about 1075 or less, about 1000 or less, about 968 or less, about 900 or less, about 860 or less, about 800 or less, about 753 or less, about 700 or less, about 645 or less, about 600 or less, about 592, about 500 or less, or about 400 or less units of solid formulation.

In embodiments of the present invention, a unit solid formulation may have a weight of about 0.05g or greater, about 0.1g or greater, about 0.15g or greater, about 0.2g or greater, about 0.25g or greater, and may have a weight of about 0.5g or less, less than about 0.5g, about 0.4g or less, about 0.3g or less, about 0.25g or less, about 0.2g or less.

In embodiments of the present invention, the weight per solid formulation may be from about 0.05g to about 0.5g, from about 0.1g or more and less than about 0.5g, from about 0.1g to about 0.4g, from about 0.05g to about 0.3g, from about 0.1g to about 0.3g, and more specifically, from about 0.1g to about 0.2g, or from about 0.15g to about 0.2g.

The solid preparation comprising the cathartic component of the present invention may comprise a unit solid preparation having a weight of about 0.5g or less, specifically less than about 0.5g, about 0.4g or less, and more specifically about 0.3g or less, thereby minimizing side effects, improving convenience of administration, enabling rapid manifestation of drug effects, and exhibiting excellent colon cleansing ability. In the case of a solid preparation comprising a cathartic component, if the weight per unit solid preparation is higher than the above weight, dysphagia (dysphagia), gastrointestinal diseases such as nausea, vomiting or feeling of vomiting, and/or side effects such as congestion, bleeding, erosion, edema, etc. of the stomach or large intestine may be significantly increased when the solid preparation is taken, and thus the convenience of administration and drug compliance may be greatly reduced. In addition, the disintegration rate may be greatly reduced, the colon cleaning ability may be reduced, and the formulation residues may remain in the body, thereby causing blurring of the visual field. In other words, there may be a significant difference in effect in terms of safety (side effects), convenience of administration, drug compliance, colon cleansing ability, disintegrability, appearance of formulation residues, etc., between the inside and outside of the weight range of the unit solid preparation of the above-described solid preparation containing the cathartic component.

The laxative component may refer to a component for the purpose of excreting intestinal contents, and the laxative component may include at least one selected from the group consisting of: polyethylene glycol, ascorbic acid, salts of ascorbic acid, sorbitol, mannitol, citric acid, salts of citric acid, magnesium salts, carboxymethyl cellulose, salts of carboxymethyl cellulose, lactulose and sulfates.

The salt may be used without limitation as long as the salt is any pharmaceutically acceptable salt, but may be, for example, sodium, potassium, magnesium, and the like. Specifically, the salt of ascorbic acid may be sodium ascorbate, potassium ascorbate, magnesium ascorbate, or the like. Further, the salt of citric acid may be sodium citrate, potassium citrate, magnesium citrate, or the like. Further, the salt of carboxymethyl cellulose may be sodium carboxymethyl cellulose.

In an embodiment of the invention, the magnesium salt may comprise at least one selected from the group consisting of: magnesium oxide, heavy magnesium oxide, magnesium hydroxide, magnesium carbonate, heavy magnesium carbonate and magnesium sulfate.

In an embodiment of the present invention, the sulfate may include at least one selected from sodium sulfate, potassium sulfate, and magnesium sulfate. In embodiments of the present invention, the sulfate may be sodium sulfate and potassium sulfate. In other embodiments, the sulfate may be sodium sulfate and magnesium sulfate. In still other embodiments, the sulfate may be a mixture of sodium sulfate, potassium sulfate, and magnesium sulfate. Furthermore, the sulfate may be an anhydride or a hydrate, preferably sodium sulfate or magnesium sulfate may be an anhydride.

The solid formulation may contain the cathartic component in an amount of about 20g or more. In particular, the solid formulation may contain the cathartic component in an amount of about 25g or more, about 30g or more, about 35g or more, but is not necessarily limited thereto. The solid formulation may contain the cathartic component in an amount of about 500g or less. Specifically, the solid formulation may comprise the cathartic component in an amount of about 465g or less, about 420g or less, about 372g or less, about 300g or less, about 279g or less, about 270g or less, about 260g or less, about 240g or less, about 230g or less, about 200g or less, about 186g or less. More specifically, the solid formulation may contain the cathartic component in an amount of about 150g or less, about 140g or less, about 130g or less, about 120g or less, about 110g or less, about 100g or less, about 93g or less, about 90g or less, about 80g or less, about 70g or less, about 60g or less, about 55g or less, but is not necessarily limited thereto.

In embodiments of the present invention, the solid formulation may comprise a total amount of the laxative component of about 20g to about 500 g. In particular, the solid formulation may comprise a total amount of the laxative component of about 20g to about 420g, about 20g to about 300g, about 20g to about 200g, or about 20g to about 150 g. More specifically, the solid formulation may contain the laxative component in an amount of about 20g to about 100g, about 20g to about 90g, about 20g to about 80g, about 25g to about 100g, about 25g to about 90g, about 25g to about 80g, about 25g to about 70g, about 25g to about 60g, or about 25g to about 55g, but is not limited thereto.

In the embodiment of the present invention, the solid formulation may contain sulfate in a total amount of about 0.1g or more, about 5g or more, about 10g or more, and may contain sulfate in a total amount of about 60g or less, about 50g or less, about 45g or less, about 40g or less, but is not limited thereto. In embodiments of the present invention, the solid formulation may comprise a total amount of sulfate from about 0.1 to about 60 g. In particular, the solid formulation may comprise a total amount of sulfate from about 5 to about 50 g. More specifically, the solid formulation may contain sulfate in an amount of about 5g to about 45g, or about 10g to about 40g, but is not necessarily limited thereto.

In embodiments of the present invention, the solid formulation may include polyethylene glycol in a total amount of about 0.1g or more, about 5g or more, about 10g or more, and may include polyethylene glycol in a total amount of about 450g or less, about 300g or less, about 250g or less, about 200g or less, about 100g or less, about 80g or less, about 50g or less, about 40g or less, but is not necessarily limited thereto. In embodiments of the present invention, the solid formulation may comprise polyethylene glycol in a total amount of about 0.1 to about 450 g. Specifically, the solid formulation may comprise polyethylene glycol in a total amount of about 0.1g to about 300g, or about 5g to about 250 g. More specifically, the solid formulation may contain polyethylene glycol in a total amount of about 10g to about 200g, about 10g to about 100g, about 10g to about 80g, about 10g to about 50g, about 10g to about 40g, but is not necessarily limited thereto.

In the embodiment of the present invention, the solid formulation may contain ascorbic acid and/or its salt in a total amount of about 0.1g or more, about 5g or more, about 10g or more, and may contain ascorbic acid and/or its salt in a total amount of about 150g or less, about 100g or less, about 50g or less, about 30g or less, but is not limited thereto. In embodiments of the present invention, the solid formulation may comprise a total amount of about 0.1g to about 150g, specifically about 5 to about 100g, and more specifically about 5g to about 50g, about 10g to about 30g of ascorbic acid and/or a salt thereof, but is not necessarily limited thereto.

In embodiments of the present invention, the solid formulation may include sorbitol and/or mannitol in a total amount of about 0.1g or more, about 5g or more, about 10g or more, and may include sorbitol and/or mannitol in a total amount of about 150g or less, about 100g or less, about 50g or less, but is not necessarily limited thereto. In embodiments of the present invention, the solid formulation may comprise sorbitol and/or mannitol in a total amount of about 0.1g to about 150g, specifically about 5g to about 100g, and more specifically about 5g to about 50g, but is not necessarily limited thereto.

In embodiments of the present invention, the solid formulation may include citric acid and/or salts thereof in a total amount of about 0.1g or more, about 1g or more, about 10g or more, and may include citric acid and/or salts thereof in a total amount of about 100g or less, about 50g or less, about 30g or less, but is not limited thereto. In an embodiment of the present invention, the solid formulation may contain citric acid and/or a salt thereof in a total amount of about 0.1g to about 100g, specifically about 1g to about 50g, and more specifically about 10g to about 30g, but is not limited thereto.

In embodiments of the present invention, the solid formulation may include a total amount of magnesium salt of about 0.1g or more, about 1g or more, and may include a total amount of magnesium salt of about 30g or less, about 10g or less, but is not limited thereto. In embodiments of the present invention, the solid formulation may comprise a magnesium salt in a total amount of about 0.1g to about 30g, specifically about 1g to about 30g, and more specifically about 1g to about 10g, but is not limited thereto.

In the embodiment of the present invention, the solid formulation may contain carboxymethyl cellulose and/or its salt in a total amount of about 0.1g or more, about 0.2g or more, and may contain carboxymethyl cellulose and/or its salt in a total amount of about 20g or less, about 12g or less, about 8g or less, about 6g or less, but is not limited thereto. In an embodiment of the present invention, the solid formulation may contain carboxymethyl cellulose and/or its salts in a total amount of about 0.1 to about 20g, specifically about 0.2 to about 6g, but is not limited thereto.

In the embodiment of the present invention, the solid preparation may contain lactulose in a total amount of about 1g or more, about 2g or more, about 5g or more, and may contain lactulose in a total amount of about 100g or less, about 50g or less, about 40g or less, but is not limited thereto. In embodiments of the present invention, the solid formulation may comprise lactulose in a total amount of about 1 to about 100g, specifically about 2g to about 50g, and more specifically about 5g to about 40g, but is not limited thereto.

In the solid preparation, the content of the cathartic component may mean the total content of the cathartic component contained in a plurality of unit solid preparations contained in the solid preparation. The solid preparation comprising the cathartic component may comprise the content of the cathartic component as above and thus exhibit excellent colon cleaning ability while minimizing side effects.

In embodiments of the present invention, the unit solid formulation of the present invention may contain a total amount of about 20mg or more, about 25mg or more, about 30mg or more, about 35mg or more, about 40mg or more, about 45mg or more of the laxative component, and may contain a total amount of about 500mg or less, less than about 500mg, about 450mg or less, about 400mg or less, about 350mg or less, specifically about 300mg or less, about 295mg or less, about 290mg or less, about 285mg or less, about 280mg or less, about 275mg or less, about 270mg or less of the laxative component, but is not limited thereto.

In embodiments of the present invention, a unit solid formulation may comprise a cathartic component in an amount of about 20mg to about 500 mg. In embodiments of the present invention, a unit solid formulation may comprise a cathartic component in an amount of about 20mg or more and less than 500 mg. Specifically, the unit solid preparation may contain the cathartic component in a total amount of about 20mg to about 300mg, about 25mg to about 295mg, and more specifically the unit solid preparation may contain the cathartic component in an amount of about 29mg to about 290mg, about 40mg to about 290mg, about 45mg to about 290mg, about 40mg to about 295mg, about 45mg to about 295mg, about 40mg to about 285mg, or about 45mg to about 285mg, but is not limited thereto.

The unit solid preparation of the present invention may contain the cathartic component in an amount of about 40% or more, about 50% or more, about 60% or more, about 70% or more, about 80% or more, about 90% or more, about 95% or more, about 96% or more, about 97% or more, about 98% or more, about 99% or more, about 100% or less, by weight of the unit solid preparation, but is not limited thereto.

The unit solid preparation comprising the cathartic component may comprise the same content of the cathartic component as described above, thereby exhibiting excellent colon cleaning ability while minimizing side effects, and thus the unit solid preparation may have excellent physical properties at the time of preparation.

The solid formulation may further comprise simethicone. The simethicone may be contained as an active ingredient in a solid formulation.

In embodiments of the present invention, the solid formulation may comprise a total amount of dimethicone from about 0.01g to about 1.2 g. Specifically, the solid formulation may contain simethicone in a total amount of about 0.01g or more, about 0.04g or more, about 0.1g or more, about 0.2g or more, about 0.3g or more, or about 0.4g, and may contain simethicone in an amount of about 1.2g or less, about 1g or less, about 0.8g or less, about 0.6g or less, about 0.5g or less.

In embodiments of the present invention, a unit solid formulation may comprise simethicone in an amount of from about 0.005mg to about 17.14 mg. Specifically, the unit solid preparation may contain simethicone in an amount of about 0.04mg to about 17.14mg, about 0.04mg to about 14.3 mg. Specifically, a unit solid formulation may contain simethicone in an amount of about 1 to about 2 mg.

The solid formulation may further comprise additional active ingredients. For example, the solid formulation may further comprise a stimulant laxative. For example, the solid formulation may further comprise at least one of the components such as: bisacodyl, castor oil, senna, bisphenol Sha Ting (bisoxatin), docusate (docusate), picosulfate (picosulfate), linaclotide (linaclotide), lubiprostone (lubiprostone), dietary fiber, a bulk laxative (plantago seed), polycarbophil (calcium polycarbophil), methylcellulose, wheat bran, etc.), anthraquinone, diphenylmethane, probiotics, etc.

Furthermore, the present invention can provide an oral solid preparation containing a sulfate as an active ingredient.

The oral solid preparation may comprise a unit solid preparation, and the weight of the unit solid preparation of the oral solid preparation is about 0.3g or less. In addition, the weight of the unit solid preparation of the oral solid preparation may be about 0.05g or more.

In the present invention, the weight per unit solid preparation may refer to the weight per unit solid preparation (unit). In other words, a solid preparation containing sulfate as an active ingredient of the present invention may contain unit solid preparations (units) of the solid preparation each having a weight of about 0.3g or less. Further, the weight of each unit solid preparation (unit) of the solid preparation containing the sulfate as an active ingredient may be about 0.05g or more.

The solid preparation containing a sulfate as an active ingredient may contain a plurality of unit solid preparations containing a sulfate as an active ingredient. In an embodiment of the present invention, the solid preparation comprising sulfate as an active ingredient may comprise about 80 to about 1200 unit solid preparations comprising sulfate as an active ingredient. Specifically, the solid formulation may comprise about 80 or more, about 90 or more, about 100 or more, about 110 or more, about 120 or more, about 130 or more, about 140 or more, about 150 or more, about 160 or more, about 170 or more, about 180 or more, about 190 or more, about 200 or more, about 210 or more, about 220 or more, about 230 or more, about 240 or more, about 250 or more, about 260 or more, about 270 or more, about 280 or more, about 290 or more, about 300 or more, about 320 or more, or about 350 or more unit solid formulations, and may comprise about 1200 or less, about 1100 or less, about 1000 or less, about 900 or less, about 800 or less, about 700 or less, about 600 or less, or about 500 or less unit solid formulations.

In an embodiment of the present invention, a unit solid preparation containing sulfate as an active ingredient may have a weight of about 0.05g or more, about 0.1g or more, about 0.15g or more, about 0.2g or more, about 0.25g or more, and may have a weight of about 0.3g or less, about 0.25g or less, about 0.2g or less.

In the embodiment of the present invention, the weight of the unit solid preparation including sulfate as an active ingredient may be about 0.05g to about 0.3g, about 0.1g to about 0.3g, more specifically about 0.1g to about 0.2g, or about 0.15g to about 0.2g, but is not limited thereto.

The solid preparation comprising sulfate as an active ingredient of the present invention may have a unit solid preparation having a weight of about 0.3g or less, thereby minimizing dysphagia (dysphagia), gastrointestinal diseases such as nausea, vomiting, emesis, or feeling of vomiting, or side effects such as congestion, bleeding, erosion, edema, etc. of the stomach or large intestine when the solid preparation is taken, improving administration convenience, enabling a rapid manifestation of a drug effect, and exhibiting excellent colon cleansing ability. Furthermore, there may be no residual formulation in the gastrointestinal tract and a clear field of view may be ensured during colonoscopy. However, in the case of a solid preparation containing sulfate as an active ingredient, when the weight per unit solid preparation is more than about 0.3g, there may be a significant difference in gastrointestinal diseases and/or side effects and the like, and the convenience of administration and drug compliance may be greatly reduced. In addition, the disintegration rate may be greatly reduced, the colon cleaning ability may be reduced, and the formulation residues may remain in the body, thereby causing blurring of the visual field. In other words, there may be a significant difference in effects in terms of safety (side effects), convenience of administration, drug compliance, colon cleansing ability, disintegrability, appearance of formulation residues, and the like between the inside and outside of the weight range of the unit solid formulation of the above-described solid formulation containing sulfate.

In this case, in the embodiment of the present invention, the solid preparation containing sulfate as an active ingredient and the unit solid preparation thereof may be a solid preparation in which the active ingredient contains sulfate (consists of sulfate). Alternatively, the solid preparation may be a solid preparation in which the active ingredient contains (consists of) sulfate and simethicone.

In the solid preparation, the sulfate may include at least one selected from sodium sulfate, potassium sulfate, and magnesium sulfate. In embodiments of the invention, the sulfate may comprise sodium sulfate. In other embodiments, the sulfate may include potassium sulfate. In still other embodiments, the sulfate may include magnesium sulfate. In embodiments of the present invention, the sulfate may be sodium sulfate and potassium sulfate. In other embodiments, the sulfate may be sodium sulfate and magnesium sulfate. In still other embodiments, the sulfate may be a mixture of sodium sulfate, potassium sulfate, and magnesium sulfate. Furthermore, the sulfate may be an anhydride or a hydrate, preferably sodium sulfate or magnesium sulfate may be an anhydride.

In embodiments of the present invention, the solid formulation comprising sulfate as an active ingredient may comprise a total amount of sulfate of about 25g or more. In particular, the solid preparation may contain sulfate in a total amount of about 30g or more, about 35g or more, about 40g or more, about 45g or more, but is not necessarily limited thereto. The solid preparation comprising sulfate as an active ingredient may comprise a total amount of sulfate of about 60g or less. In particular, the solid preparation may contain sulfate in a total amount of about 55g or less, about 50g or less, about 45g or less, about 40g or less, but is not necessarily limited thereto. For example, the solid formulation may comprise a total amount of sulfate of about 44.46 g.

In embodiments of the present invention, the solid formulation comprising sulfate as an active ingredient may comprise a total amount of sulfate from about 25g to about 60 g. In particular, the solid formulation may comprise a total amount of sulfate from about 25g to about 55g, from about 30g to about 60g, from about 30g to about 55g, or from about 30g to about 50 g. More specifically, the solid preparation may contain a total amount of sulfate from about 40g to about 55g, from about 40g to about 50g, from about 35g to about 45g, from about 30g to about 45g, or from about 30g to about 40g, but is not limited thereto.

In an embodiment of the present invention, when the sulfate salt includes sodium sulfate, the solid preparation containing the sulfate salt as an active ingredient may contain sodium sulfate in a total amount of about 10g to about 60 g. Specifically, the solid formulation may contain sodium sulfate in a total amount of about 10g or more, about 15g or more, about 20g or more, about 25g or more, about 30g or more, about 33g or more, or about 35g or more, and may contain sodium sulfate in a total amount of about 60g or less, about 55g or less, about 52g or less, about 50g or less, about 45g or less, about 42g or less, about 40g or less, or about 36g or less.

In an embodiment of the present invention, when the sulfate salt includes potassium sulfate, the solid formulation including the sulfate salt as an active ingredient may include potassium sulfate in a total amount of about 0.1g to about 15 g. Specifically, the solid formulation may contain potassium sulfate in a total amount of about 0.1g or more, about 0.5g or more, about 1g or more, about 2g or more, about 3g or more, about 4g or more, or about 5g or more, or about 6g or more, and may contain potassium sulfate in a total amount of about 15g or less, about 12g or less, about 10g or less, about 9g or less, about 8g or less, or about 7g or less.

In an embodiment of the present invention, when the sulfate salt includes magnesium sulfate, the solid formulation including the sulfate salt as an active ingredient may include magnesium sulfate in a total amount of about 0.1g to about 8 g. Specifically, the solid formulation may contain magnesium sulfate in a total amount of about 0.1g or more, about 0.5g or more, about 1g or more, about 2g or more, about 3g or more, or about 4g or more, and may contain magnesium sulfate in a total amount of about 8g or less, about 7g or less, or about 6g or less.

The total content of sulfate in the solid preparation containing sulfate as an active ingredient may refer to the total content of sulfate contained in a unit solid preparation contained in the solid preparation containing sulfate as an active ingredient. The solid preparation comprising sulfate as an active ingredient may contain the content of sulfate as above and thus exhibit excellent colon cleaning ability while minimizing side effects.

The unit solid preparation of the solid preparation comprising a sulfate salt as an active ingredient of the present invention may comprise a sulfate salt in an amount of about 20mg to about 300 mg. Specifically, the unit solid preparation may contain sulfate in a total amount of about 20mg or more, about 25mg or more, about 30mg or more, about 35mg or more, about 40mg or more, about 45mg or more, and may contain sulfate in a total amount of about 300mg or less, about 295mg or less, about 290mg or less, about 285mg or less, about 280mg or less, about 275mg or less, about 270mg or less, but is not limited thereto.

In the embodiment of the present invention, a unit solid preparation comprising a solid preparation of sulfate as an active ingredient may comprise a total amount of sulfate from about 25mg to about 295 mg. More specifically, the unit solid preparation may contain sulfate in an amount of about 29mg to about 290mg, about 40mg to about 290mg, about 45mg to about 290mg, about 40mg to about 295mg, about 45mg to about 295mg, about 40mg to about 285mg, or about 45mg to about 285mg, but is not necessarily limited thereto.

The unit solid preparation comprising the sulfate salt as an active ingredient of the present invention may comprise the sulfate salt in an amount of about 6.7% or more, about 9% or more, about 10% or more, about 20% or more, about 30% or more, and more specifically 40% or more, about 50% or more, about 60% or more, about 70% or more, about 80% or more, about 90% or more, about 95% or more, about 96% or more, about 97% or more, about 98% or more, about 99% or more, about 100% or less by weight based on the weight of the unit solid preparation, but is not limited thereto.

In embodiments of the present invention, when the sulfate salt comprises sodium sulfate, the unit solid formulation may comprise sodium sulfate in an amount of about 8mg to about 300 mg. Specifically, the unit solid preparation may contain sodium sulfate in an amount of about 8mg or more, about 12mg or more, about 15mg or more, about 16mg or more, about 20mg or more, about 25mg or more, about 27mg or more, about 29mg or more, about 30mg or more, and may contain sodium sulfate in a total amount of about 300mg or less, about 295mg or less, about 290mg or less, about 285mg or less, about 280mg or less, about 275mg or less, about 270mg or less, but is not limited thereto.

In an embodiment of the present invention, the unit solid preparation may contain sodium sulfate in an amount of about 8mg to about 300mg, about 12mg to about 300mg, or about 15mg to about 300mg, and more particularly, the unit solid preparation may contain sodium sulfate in an amount of about 30 to about 270mg, about 30 to about 250mg, or about 50 to about 220mg, and more particularly, the unit solid preparation may contain sodium sulfate in an amount of about 80mg to about 170mg, but is not limited thereto.

In an embodiment of the present invention, when the sulfate salt includes sodium sulfate, the unit solid preparation may contain sodium sulfate in an amount of about 2.67% or more, about 5% or more, about 10% or more, specifically about 12% or more, about 16% or more, about 20% or more, about 30% or more, about 40% or more, about 60% or more, about 75% or more, about 80% or more, about 85% or more, about 90% or more, about 95% or more, about 100% or less, based on the weight of the unit solid preparation, but is not limited thereto.

In embodiments of the present invention, when the sulfate salt comprises potassium sulfate, the unit solid formulation may comprise potassium sulfate in an amount of about 0.08mg to about 187.5 mg. Specifically, the unit solid preparation may contain potassium sulfate in an amount of about 0.08mg or more, about 0.4mg or more, about 0.8mg or more, about 1mg or more, about 2mg or more, about 3mg or more, about 4mg or more, about 5mg or more, about 9mg or more, about 12mg or more, and the unit solid preparation may contain potassium sulfate in an amount of about 187.5mg or less, about 180mg or less, about 170mg or less, about 150mg or less, about 130mg or less, about 120mg or less, about 100mg or less, about 90mg or less, about 80mg or less, about 50mg or less, about 40mg or less, about 30mg or less, but is not limited thereto.

In an embodiment of the present invention, the unit solid preparation may contain potassium sulfate in an amount of about 2mg to about 50mg, and in particular, the unit solid preparation may contain potassium sulfate in an amount of about 5mg to about 38mg, about 9mg to about 32mg, or about 12mg to about 26mg, but is not limited thereto.

In embodiments of the present invention, when the sulfate salt includes potassium sulfate, the unit solid formulation may include potassium sulfate in an amount of about 0.01% or more, about 0.02% or more, about 0.03% or more, about 0.05% or more, about 0.067% or more, about 0.08% or more, about 0.1% or more, about 0.3% or more, about 0.4% or more, about 0.5% or more, about 1% or more, about 1.5% or more, about 2% or more, about 3% or more, about 4% or more, about 5% or more, about 6% or more, about 8% or more, about 10% or more, about 20% or more, about 30% or more, about 50% or more, about 60% or less, by weight based on the weight of the unit solid formulation, but is not limited thereto.

In embodiments of the present invention, when the sulfate salt comprises magnesium sulfate, the unit solid formulation may comprise magnesium sulfate in an amount of about 0.08mg to about 100 mg. Specifically, the unit solid preparation may contain magnesium sulfate in an amount of about 0.08mg or more, about 0.4mg or more, about 0.8mg or more, about 1mg or more, about 2mg or more, about 3mg or more, about 4mg or more, about 6mg or more, about 8mg or more, about 10mg or more, about 12mg or more, and the unit solid preparation may contain magnesium sulfate in an amount of about 100mg or less, about 90mg or less, about 80mg or less, about 70mg or less, about 60mg or less, about 50mg or less, about 40mg or less, about 30mg or less, about 20mg or less, about 10mg or less, but is not limited thereto.

In embodiments of the present invention, a unit solid formulation may comprise magnesium sulfate in an amount of about 1mg to about 25 mg. Specifically, the unit solid preparation may contain magnesium sulfate in an amount of about 1mg to about 13mg, about 1mg to about 12mg, or about 1mg to about 10mg, but is not limited thereto.

In embodiments of the present invention, when the sulfate salt includes magnesium sulfate, the unit solid formulation may include magnesium sulfate in an amount of about 0.01% or more, about 0.02% or more, about 0.03% or more, about 0.05% or more, about 0.067% or more, about 0.08% or more, about 0.1% or more, about 0.3% or more, about 0.4% or more, about 0.5% or more, about 0.8% or more, about 1% or more, about 1.5% or more, about 2% or more, about 3% or more, about 4% or more, about 5% or more, about 10% or more, about 20% or more, about 30% or more, about 32% or less, by weight based on the weight of the unit solid formulation, but is not limited thereto.

The unit solid preparation containing sulfate as an active ingredient may contain the same amount of sulfate as described above, thereby exhibiting excellent colon cleaning ability while minimizing side effects, and thus the unit solid preparation may have excellent physical properties at the time of preparation.

The solid preparation containing a sulfate as an active ingredient may further contain simethicone. The simethicone may be contained as an active ingredient in a solid formulation.

In the embodiment of the present invention, the solid preparation including sulfate as an active ingredient may include simethicone in a total amount of about 0.01g to about 1.2g, specifically, the solid preparation may include simethicone in a total amount of about 0.01g or more, about 0.04g or more, about 0.1g or more, about 0.2g or more, about 0.3g or more, or about 0.4g or more, and may include simethicone in an amount of about 1.2g or less, about 1g or less, about 0.8g or less, about 0.6g or less, about 0.5g or less.

In an embodiment of the present invention, a unit solid preparation comprising a solid preparation of sulfate as an active ingredient may comprise simethicone in an amount of about 0.008mg to about 15 mg. Specifically, the unit solid preparation may contain simethicone in an amount of about 0.008mg or more, about 0.01mg or more, about 0.05mg or more, about 0.1mg or more, about 0.5mg or more, about 1mg or more, and may contain simethicone in an amount of about 15mg or less, about 12.5mg or less, about 10mg or less, about 8mg or less, about 6mg or less, but is not limited thereto.

In the embodiment of the present invention, the unit solid preparation may contain simethicone in an amount of about 0.04mg to about 15mg, and more particularly, the unit solid preparation may contain simethicone in an amount of about 1mg to about 2mg, but is not limited thereto.

In the embodiment of the present invention, the solid preparation and unit solid preparation of the present invention containing a sulfate as an active ingredient may mean a solid preparation and unit solid preparation containing a sulfate or a sulfate as an active ingredient and simethicone (composed of a sulfate or a sulfate as an active ingredient). In a solid preparation in which the active ingredient contains a sulfate or a sulfate and a simethicone (composed of a sulfate or a sulfate and a simethicone), in a unit solid preparation having a weight of about 0.3g or less, side effects can be minimized, convenience of administration can be improved, and excellent colon cleaning ability can be exhibited. However, when the weight per unit solid preparation is more than about 0.3g, side effects may be significantly increased, and there may be significant differences in safety (side effects), administration convenience, drug compliance, colon cleansing ability, disintegrability, appearance of preparation residues, and the like.

In the present invention, the term "active ingredient" may have the same meaning as the active ingredient, and the active ingredient may also be referred to as an active ingredient.

In the present invention, the term "oral solid preparation" may have the same meaning as a solid preparation for oral administration, and may also be referred to as a solid preparation for oral administration.

The solid preparation of the present invention may further comprise pharmaceutically acceptable additives.

In the present specification, a pharmaceutically acceptable additive may refer to a component that does not impair the effect of the active ingredient. Additives used herein may include, for example, fillers, disintegrants, binders, plasticizers, glidants, coating agents, pH adjusters, diluents, lubricants, preservatives, buffers, sweeteners, wetting agents, suspending agents, colorants, flavors, excipients, and the like, and any pharmaceutically acceptable additive conventionally used in respective dosage forms may also be used.

The additive may be a known additive.

For example, disintegrants used herein may include crospovidone, guar gum, xanthan gum, sodium starch glycolate, low-substituted hydroxypropyl cellulose, croscarmellose sodium, microcrystalline cellulose, dextran, mannitol, mixtures thereof, and the like, but are not limited thereto.

For example, the binder used herein may include alginic acid, sodium alginate, carbomer, copovidone, starch, polyethylene glycol, polyvinylpyrrolidone, polyethylene derivatives, microcrystalline cellulose, methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, low substituted hydroxypropylcellulose, hydroxypropylmethyl cellulose, mixtures thereof, and the like, but is not limited thereto.

For example, glidants used herein may include stearic acid, stearates, stearyl fumarate, lauryl sulfate, stearyl sulfate, vegetable oils, polyethylene glycol, poloxamers (poloxamers), octoates, mixtures thereof, and the like, but are not limited thereto.

For example, the coating agent used herein may include polyvinyl alcohol-polyethylene glycol copolymer, amino methacrylate copolymer, methyl methacrylate copolymer, sucrose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, hydroxyethyl methylcellulose, carboxymethyl cellulose, hydroxypropyl cellulose, polyethylene glycol, ethyl cellulose, mixtures thereof, and the like, but is not limited thereto.

The unit solid preparation of the present invention may have a circular or oval shape, but is not necessarily limited thereto.

In the embodiment of the present invention, when the unit solid preparation has a circular or oval shape, the diameter or length of the unit solid preparation may be about 1mm to about 20mm, about 1mm to about 15mm, specifically about 1 to about 12mm, about 1 to about 10mm, but is not necessarily limited thereto.

In the embodiment of the present invention, when the unit solid preparation has a circular or oval shape, the thickness or height of the unit solid preparation may be about 1mm to about 10mm, specifically about 1 to about 5mm, but is not necessarily limited thereto.

In the solid formulation of the present invention, the unit solid formulation may have a form of a tablet, pellet, capsule or pill (pill), and the solid formulation may include the unit solid formulation in the form of a tablet, pellet, capsule or pill, or any combination thereof. In an embodiment of the present invention, the unit solid preparation may be a tablet, and the solid preparation may comprise the unit solid preparation in the form of a tablet. Furthermore, the tablets may be bare tablets or coated tablets.

The oral solid preparation of the present invention can be prepared by an appropriate method according to its specific dosage form. In embodiments of the present invention, when the solid formulation is prepared in the form of a tablet, the solid formulation may be prepared using a granulation process, a mixing process, and/or a tabletting process. The granulation process may be suitably selected from the group consisting of a dry granulation process, a wet granulation process and a coating process.

The unit solid preparation of the present invention can be prepared to have a weight of about 0.05g or more, more specifically about 0.1g or more, thereby improving production efficiency.

The unit solid preparation of the present invention can be easily prepared and has excellent physical properties as a solid preparation. In addition, the unit solid preparation of the present invention may have a weight as described above, and thus may not be stuck in the esophagus when taken, or may not cause any irritation caused by foreign substances, and may minimize side effects of gastrointestinal diseases such as dysphagia (dysphagia), like nausea, vomiting or vomiting feeling. In addition, side effects such as congestion, bleeding, erosion, edema, etc. in the stomach or large intestine can be minimized when taken. Thus, the solid formulation of the present invention can have very excellent administration convenience and drug compliance, thereby contributing to successful completion of administration, exhibiting excellent colon cleansing effect, and minimizing side effects from administration. In addition, the solid preparation can be rapidly disintegrated and dissolved in the stomach after administration, can reduce side effects such as congestion, bleeding, erosion, edema, etc. in the stomach after administration, and can enable the pharmaceutical effect to be rapidly exhibited, thereby reducing the time to start and end the excretion of feces. Thus, pain of the user caused by defecation can be minimized. Furthermore, the solid formulation may have no formulation residues remaining in the gastrointestinal tract and may have a clear view ensured during colonoscopy.

The oral solid preparation of the present invention may be taken in such a manner that the total dose thereof is taken entirely at one time point (referred to as non-divided administration or divided administration of the same day) or at several time points by splitting the total dose of the composition (referred to as divided administration or divided administration of two days).

As an example of non-divided administration (divided dose administration on the same day), the oral solid preparation of the present invention may be taken in the evening on the day before examination or in the morning on the same day of examination for several hours. In particular, a portion of the total dose may be taken and then the remainder thereof may be taken after a period of time, for example, after about 0.5 to 3 hours.

As an example of divided dose administration (or two-day divided dose administration), the oral solid preparation of the present invention may be taken in such a manner that a part thereof is taken at night the day before examination and then the rest thereof is taken in the morning of the day of examination.

When taking oral solid preparations, each dose may be taken within a certain period of time. Specifically, each dose may be taken within about two hours, about one hour, or about 30 minutes.

The oral solid preparation of the present invention may be taken together with about 1L or more of water. Specifically, the oral solid preparation may be taken together with about 2L or more of water. The oral solid preparation of the present invention may be taken together with about 1L to 4L, about 2L to 3L of water.

In an embodiment of the present invention, there may be provided (1) an oral solid preparation, wherein the oral solid preparation of the present invention contains a sulfate as an active ingredient, and the weight per unit solid preparation is about 0.3g or less.

(2) In the above (1), an oral solid preparation may be provided, wherein the solid preparation comprises unit solid preparations each having a weight of about 0.05g or more.

(3) In any one of the above (1) and (2), an oral solid preparation may be provided, wherein the solid preparation comprises sulfate in an amount of about 25 to about 60 g.

(4) In any one of the above (1) to (3), an oral solid preparation may be provided, wherein the sulfate salt includes at least one selected from sodium sulfate, potassium sulfate and magnesium sulfate.

(5) In any one of the above (1) to (4), an oral solid preparation may be provided, wherein the sulfate salt includes sodium sulfate and potassium sulfate.

(6) In any one of the above (1) to (5), an oral solid preparation may be provided, wherein the sulfate salt includes sodium sulfate, magnesium sulfate and potassium sulfate.

(7) In any one of the above (1) to (6), an oral solid preparation may be provided, which further comprises simethicone.

(8) In any one of the above (1) to (7), an oral solid preparation may be provided, which further comprises a pharmaceutically acceptable additive.

(9) In any one of the above (1) to (8), an oral solid preparation may be provided, wherein the solid preparation comprises about 80 to about 1200 units of the solid preparation.

(10) In any one of the above (1) to (9), an oral solid preparation may be provided, wherein the unit solid preparation is in the form of a tablet, a pellet, a capsule or a pill.

(11) In any one of the above (1) to (10), an oral solid preparation can be provided, wherein the solid preparation is used for colon cleaning.

(12) In any one of the above (1) to (11), an oral solid preparation may be provided, wherein the unit solid preparation contains sulfate in an amount of about 20mg to about 300 mg.

(13) In any one of the above (1) to (12), an oral solid preparation may be provided, wherein the solid preparation contains simethicone in a total amount of about 0.01g to about 1.2 g.

(14) In any one of the above (1) and (13), an oral solid preparation may be provided, wherein the unit solid preparation comprises simethicone in an amount of about 0.008mg to about 15 mg.

In other embodiments of the present invention, there may be provided (i) an oral solid preparation, wherein the oral solid preparation of the present invention comprises a cathartic component as an active ingredient, and the weight per unit solid preparation is about 0.5g or less.

(ii) In the above (i), an oral solid preparation may be provided, wherein the oral solid preparation comprises unit solid preparations each having a weight of about 0.05g or more.

(iii) In any one of the above (i) and (ii), there may be provided an oral solid preparation, wherein the oral solid preparation comprises at least one selected from the group consisting of: polyethylene glycol, ascorbic acid, salts of ascorbic acid, sorbitol, mannitol, citric acid, salts of citric acid, magnesium salts, carboxymethyl cellulose, salts of carboxymethyl cellulose, lactulose and sulfates.

(iv) In any one of the above (i) to (iii), an oral solid formulation may be provided wherein the magnesium salt comprises at least one selected from the group consisting of: magnesium oxide, heavy magnesium oxide, magnesium hydroxide, magnesium carbonate, heavy magnesium carbonate and magnesium sulfate.

(v) In any one of the above (i) to (iv), an oral solid preparation may be provided, wherein the sulfate salt includes at least one selected from sodium sulfate, potassium sulfate and magnesium sulfate.

(vi) In any one of the above (i) to (v), an oral solid preparation may be provided, wherein the unit solid preparation is in the form of a tablet, a pellet, a capsule or a pill.

(vii) In any one of the above (i) to (vi), an oral solid preparation may be provided, which further comprises a pharmaceutically acceptable additive.

(viii) In any one of the above (i) to (vii), an oral solid formulation may be provided, wherein the solid formulation comprises from about 70 to about 2000 units of the solid formulation.

(ix) In any one of the above (i) to (viii), an oral solid preparation may be provided, wherein the solid preparation is for colon cleaning.

(x) In any one of the above (i) to (ix), an oral solid formulation may be provided, wherein the solid formulation comprises a total amount of the laxative component of about 20g to about 500 g.

(xi) In any one of the above (i) to (x), an oral solid preparation may be provided, wherein the unit solid preparation comprises the cathartic component in an amount of about 20mg to about 500 mg.

In the above, the solid formulation according to the embodiment of the present invention is exemplarily described, but the present invention is not limited thereto, and all combinations of the various elements for the solid formulation according to the present invention described in the solid formulation of the present invention fall within the scope of the present invention.

The present invention may also provide a method of colon cleansing comprising administering an oral solid formulation of the invention (in an effective amount).

The present invention may also provide the use of the oral solid preparation of the present invention for colon cleansing.

In the above-described method and use, the oral solid preparation of the present invention may be the same as described in the oral solid preparation of the present invention.

Advantageous effects

The oral solid preparation of the present invention can minimize side effects such as dysphagia (dysphagia), gastrointestinal diseases like nausea or vomiting when taken, and has excellent administration convenience and drug compliance. In addition, the solid preparation of the present invention can be rapidly disintegrated and dissolved, can reduce side effects such as congestion, bleeding, erosion, edema, etc. in the stomach, and can rapidly exert a pharmaceutical effect, thereby reducing the time to start and end the excretion of feces after taking the solid preparation. In addition, residues in the gastrointestinal tract can be minimized and excellent colon cleansing effect can be exhibited.

Drawings

Fig. 1 is a graph showing the results of evaluating the side effects of experimental example 4.

Fig. 2 is a graph showing the results of evaluating the colon cleansing ability of experimental example 7.

Detailed Description

Hereinafter, the present invention will be described in detail by way of preferred examples for better understanding of the present invention. However, the following examples are provided for the purpose of illustrating the present invention only, and thus the present invention is not limited thereto.

Experimental example 1: determination of disintegration time

Tablets were prepared according to the components and amounts shown in table 1 below. Specifically, 109.375g of anhydrous sodium sulfate, 19.563g of potassium sulfate, 10g of anhydrous magnesium sulfate, and 4.663g of copovidone were mixed, then 1mL of purified water was slowly added and mixed, then the mixture was passed through a 20-mesh net, 1.4g of stearic acid was added, mixed, and then tableted with a tablet tableting machine.

[ Table 1 ]

The disintegration time of the tablets of example 1 and comparative example 1 prepared above was measured in water according to the disintegration test of korean pharmacopoeia, general test (Disintegration Test of Korean Pharmacopeia, general Tests).

The disintegration times of the tablets of example 1 and comparative example 1 were 7 minutes 20 seconds and 17 minutes 30 seconds, respectively, confirming that the tablets of example 1 disintegrated much faster. The tablet of example 1, which disintegrates rapidly, was confirmed to be more suitable as a solid colon cleaner.

Experimental example 2: determination of dissolution time

Tablets were prepared according to the components and amounts shown in table 2 below. Specifically, 109.375g of anhydrous sodium sulfate, 19.563g of potassium sulfate, 10g of anhydrous magnesium sulfate, and 5.062g of copovidone were mixed, then 3mL of purified water was slowly added and mixed, then the mixture was passed through a 20 mesh net, 1.5g of stearic acid was added, mixed, and tableted with a tablet press. Next, the polyethylene glycol-polyvinyl alcohol copolymer was dissolved in purified water at a concentration of 5%, and then film-coated with a coating machine.

[ Table 2 ]

The dissolution time of the 30 tablets of example 2 and the three tablets of comparative example 2 prepared were measured by the paddle method at about 37 ℃, 50rpm and 900ml of pH 1.2 dissolution medium (dissolution tester, pharmatest). The tablets of example 2 and comparative example 2 were evaluated by placing ten tablets and one tablet, respectively, into one container of a dissolution tester. The dissolution rate was analyzed by liquid chromatography (HPLC).

It was confirmed that all the tablets of example 2 dissolved within 15 minutes, while all the tablets of comparative example 2 eluted at about 30 minutes. It can be seen that the tablet of example 2 is more preferred as a solid colon cleaner than the tablet of comparative example 2.

Experimental example 3: preparation and disintegration time of solid formulations

Tablets of example 3 and comparative example 3 were prepared according to the components and contents of table 3 below. Specifically, 123.15g of polyethylene glycol 3350, 5.79g of ascorbic acid, 7.27g of sodium ascorbate, 9.24g of anhydrous sodium sulfate, 3.31g of sodium chloride and 1.24g of potassium chloride were passed through a 20-mesh net, mixed, and then compressed with a tablet compression machine to prepare tablets.

[ Table 3 ]

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The disintegration time of the tablets of example 3 and comparative example 3 prepared above was measured in water according to the disintegration test method of korean pharmacopoeia, general test (Disintegration Test method of the Korean Pharmacopeia, general Tests).

The disintegration times of the tablets of example 3 and comparative example 3 were 5 minutes 45 seconds and 15 minutes 50 seconds, respectively, confirming that the tablets of example 3 disintegrated much faster. The tablet of example 3, which disintegrates rapidly, was confirmed to be more suitable as a solid colon cleaner.

Experimental example 4: side effect evaluation (1)

To confirm the improvement of the side effects of the solid formulation of the present invention, tablets were prepared according to the components and contents of table 4 below. Specifically, 109.375g of anhydrous sodium sulfate, 19.563g of potassium sulfate, 10g of anhydrous magnesium sulfate, and 5.062g of copovidone were mixed, then 3mL of purified water was slowly added and mixed, then the mixture was passed through a 20 mesh net, 1.5g of stearic acid was added, mixed, and tableted with a tablet press. The polyethylene glycol-polyvinyl alcohol copolymer was then dissolved in a 50% ethanol solution at a concentration of 10%, and then film-coated with a coating machine.

[ Table 4 ]

Side effects occurring in the gastrointestinal tract were observed by administering the prepared tablets 1 to 3 to beagle dogs (about 10 kg). 80 tablets 1, 40 tablets 2, and 8 tablets 3 were orally administered so that the same amount of sulfate could be administered and observed under anesthesia to prevent vomiting. Each of the tablets 1 to 3 was administered to three beagle dogs together with water, and then euthanized at three hours to collect and cut the stomach, and the degree of damage of the gastric mucosa was estimated with naked eyes at 0 to 16 according to the occurrence area and intensity of congestion, bleeding, erosion, and edema. Specifically, the degree of damage was evaluated as 0 to 4 points according to the area where the side effect occurred, as 0 to 4 points according to the intensity of the side effect, and the two values were multiplied. The higher the score, the greater the side effects.

As a result of the side effect evaluation, it was found that the side effects in tablets 1 and 2 were much smaller than those in tablet 3 (fig. 1). The unexpected result is that tablets 1 and 2 have fewer side effects than tablet 3, albeit with a greater number of tablets and a wider surface area in contact with the stomach.

Thus, it was confirmed that the tablets 1 and 2 according to the present invention can improve side effects.

Experimental example 5: side effect evaluation (2)

Tablets 1 to 3 of table 4 above were administered to assess the occurrence of side effects (oedema) in the gastrointestinal tract by tissue testing. Tablets 1 to 3 were prepared and applied to three beagle dogs, respectively, and a series of gastric cutting processes were performed in the same manner as in experimental example 4. Tissue was removed from the dissected stomach to prepare specimens for tissue testing, and then stained with hematoxin & Eosin (H & E) to observe the occurrence of edema by optical microscopy.

As a result, it was found that no edema occurred in all of the individuals taking tablets 1 and 2, while the individuals taking tablet 3 had edema (Table 5). The unexpected result was that, although there was a greater number of tablets and a wider surface area in contact with the stomach, no edema occurred for tablets 1 and 2 compared to tablet 3.

[ Table 5 ]

	Tablet 1	Tablet 2	Tablet 3
				Ratio of edema patients (%)	0	0	100

Experimental example 6: assessment of ease of administration

Tablets 1 and 3 of table 4 above were administered to beagle dogs to compare ease of administration. 80 tablets 1 and 8 tablets 3 were administered to beagle dogs (about 10 kg) without anesthesia to see if administration was performed without problems such as swallowing disorder, etc.

Tablet 3 is not easy to swallow and therefore can only be administered when a researcher forces it into the throat area by hand, whereas in the case of tablet 1 it is observed that beagle itself can easily swallow several tablets at a time, even ten times the number of administrations of tablet 3. Thus, it can be seen that the tablet 1 of the present invention is much easier to take than the tablet 3 having a weight similar to that of the commercial product, although the number of tablets to be taken is ten times that of the tablet 3.

Experimental example 7: assessment of colon cleaning ability

60 tablets 1 prepared by the method of experimental example 4 were administered to beagle dogs (about 10 kg) without anesthesia and euthanized after three hours, and then the large intestine was collected and resected to confirm the colon cleaning ability.

As a result, as shown in fig. 2, it can be seen that the large intestine is cleanly washed. Thus, it can be seen that the solid formulation of the present invention has excellent colon cleaning ability.

Preparation example 1 preparation of solid preparation

Tablets were prepared according to the components and amounts shown in table 6 below. Specifically, in the case of tablet 4, 138.938g of anhydrous sodium sulfate, 4.663g of copovidone and 2.4g D-mannitol were mixed, then 0.7mL of purified water was slowly added and mixed, then the mixture was passed through a 20 mesh net, 1.0g of stearic acid was added, mixed, and tableted with a tablet tableting machine. The polyethylene glycol-polyvinyl alcohol copolymer was then dissolved in a 50% ethanol solution at a concentration of 10%, and then film-coated with a coating machine. In the case of tablet 5, 113.938g of anhydrous sodium sulfate, 25.0g of anhydrous magnesium sulfate and 4.663g of copovidone were mixed, then 1.0mL of purified water was slowly added and mixed, then the mixture was passed through a 20 mesh net, 1.4g of stearic acid was added, mixed, and tableted with a tablet tableting machine. The polyethylene glycol-polyvinyl alcohol copolymer was then dissolved in a 50% ethanol solution at a concentration of 10%, and then film-coated with a coating machine. In the case of tablet 6, 113.938g of anhydrous sodium sulfate, 25.0g of potassium sulfate, 4.663g of copovidone and 2.4g D-mannitol were mixed, then 0.7mL of purified water was slowly added and mixed, then the mixture was passed through a 20 mesh net, 1.0g of stearic acid was added, mixed, and tableted with a tablet tableting machine. The polyethylene glycol-polyvinyl alcohol copolymer was then dissolved in a 50% ethanol solution at a concentration of 10%, and then film-coated with a coating machine.

[ Table 6 ]

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Claims

1. An oral solid preparation comprising sulfate, wherein the weight of each of the unit solid preparations of the oral solid preparation is about 0.3g or less.

2. The oral solid formulation of claim 1, wherein the sulfate is present in an amount of about 25g to about 60g.

3. The oral solid preparation of claim 1, wherein the sulfate comprises at least one selected from sodium sulfate, potassium sulfate, and magnesium sulfate.

4. The oral solid formulation of claim 3, wherein the sulfate salt comprises sodium sulfate and potassium sulfate.

5. The oral solid formulation of claim 3, wherein the sulfate salt comprises sodium sulfate, magnesium sulfate, and potassium sulfate.

6. The oral solid formulation of claim 1, further comprising simethicone.

7. The oral solid formulation of claim 1, wherein the solid formulation comprises from about 80 to about 1200 units of solid formulation.

8. An oral solid formulation comprising a cathartic component, wherein the weight of each of the unit solid formulation of the oral solid formulation is about 0.5g or less.

9. The oral solid formulation of claim 8, wherein the cathartic component comprises at least one selected from the group consisting of: polyethylene glycol, ascorbic acid, salts of ascorbic acid, sorbitol, mannitol, citric acid, salts of citric acid, magnesium salts, carboxymethyl cellulose, salts of carboxymethyl cellulose, lactulose and sulfates.

10. The oral solid formulation of claim 9, wherein the magnesium salt comprises at least one selected from the group consisting of: magnesium oxide, heavy magnesium oxide, magnesium hydroxide, magnesium carbonate, heavy magnesium carbonate and magnesium sulfate.

11. The oral solid preparation of claim 9, wherein the sulfate comprises at least one selected from sodium sulfate, potassium sulfate, and magnesium sulfate.

12. The oral solid formulation of claim 8, wherein the solid formulation comprises about 70 to about 2000 units of solid formulation.

13. The oral solid formulation of claim 1 or 8, wherein the weight per unit solid formulation is about 0.05g or greater.

14. The oral solid formulation of claim 1 or 8, further comprising a pharmaceutically acceptable additive.

15. The oral solid formulation of claim 1 or 8, wherein the unit solid formulation is in the form of a tablet, pellet, capsule, or pill.

16. The oral solid formulation of claim 1 or 8, wherein the solid formulation is for colon cleansing.