CN111836629A - Pharmaceutical composition - Google Patents
Pharmaceutical composition Download PDFInfo
- Publication number
- CN111836629A CN111836629A CN201980018249.6A CN201980018249A CN111836629A CN 111836629 A CN111836629 A CN 111836629A CN 201980018249 A CN201980018249 A CN 201980018249A CN 111836629 A CN111836629 A CN 111836629A
- Authority
- CN
- China
- Prior art keywords
- pharmaceutical composition
- present
- chlorhexidine
- composition
- simethicone
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/695—Silicon compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/74—Synthetic polymeric materials
- A61K31/80—Polymers containing hetero atoms not provided for in groups A61K31/755 - A61K31/795
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
- A61K33/08—Oxides; Hydroxides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/42—Phosphorus; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
Abstract
The present invention relates to a pharmaceutical composition comprising aluminium phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride and chlorhexidine salt. The pharmaceutical composition of the present invention can be effectively used as a pharmaceutical composition by having excellent preservative ability.
Description
Technical Field
The invention relates to a pharmaceutical composition which comprises aluminum phosphate gel, magnesium hydroxide and simethicone
DL-carnitine hydrochloride and chlorhexidine salts
Background
The stomach is an organ that finely breaks down food passing through the esophagus so as to be easily stored and digested, and controls the transfer of food into the duodenum to coordinate with the secretion of pancreatic enzymes, thereby contributing to the efficient digestion and absorption of food. After food enters, the stomach secretes strong acids (i.e., stomach acid) to digest the food. When they do, the protective layer of the gastric mucosa protects the gastric mucosa from such gastric acid.
However, the protective layer of the gastric mucosa is vulnerable to damage caused by attacks from various factors. As representative invasive factors, there are gastric acid, alcohol, smoking, steroids, nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin, bacteria such as Helicobacter pylori (Helicobacter pylori), irritant food, nutritional deficiencies, stress, and the like. When the gastric mucosa is damaged by such factors, inflammation with erosion, redness, bleeding or edema can occur. In severe cases, gastric ulcers appear if the injury progresses to form a hole in the gastric mucosa and even damages the bottom and muscle layers of the mucosa.
In order to prevent and treat the above gastric injury, a drug in which gastric acid is neutralized, absorbed or inhibited or which is applied to the gastric mucosa to form a protective layer may be used. Products using aluminum phosphate gel, aluminum magnesium oxide, alginic acid, etc. as main components are sold in the market. However, according to the diversification of the tastes of patients, there is a demand for products having a milder and fresher feeling of ingestion while maintaining the stomach-protecting effect.
[ Prior art reference ]
[ patent document ]
(patent document 1) korean patent registration No. 10-0903743.
Disclosure of Invention
Technical problem
The object of the present invention is to provide a pharmaceutical composition having excellent preservative efficacy comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride and chlorhexidine salt.
Further, it is an object of the present invention to provide a pharmaceutical composition for preventing or treating gastrointestinal dysfunction, which has excellent preservative efficacy, comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride, and chlorhexidine salt, and a method for preparing the same.
It is another object of the present invention to provide a method for preventing or treating gastrointestinal dysfunction, comprising the step of administering to a subject a pharmaceutical composition comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride, and chlorhexidine salt.
Further, another object of the present invention is to provide a use of a composition comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride and chlorhexidine salt for preventing or treating gastrointestinal dysfunction.
Further, another object of the present invention is to provide a use of a composition comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride and chlorhexidine salt for the preparation of a medicament for preventing or treating gastrointestinal dysfunction.
Technical scheme
To achieve the above objects, the present inventors have continued to research and thus identified that the antibacterial level of a pharmaceutical composition comprising aluminum phosphate gel, magnesium hydroxide, simethicone and DL-carnitine hydrochloride can be improved by including chlorhexidine salt, thereby completing the present invention.
The present invention provides a pharmaceutical composition comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride and chlorhexidine salt.
The pharmaceutical composition of the present invention shows excellent activity for improving gastrointestinal dysfunction, and achieves excellent preservative efficacy of the composition, good patient's liking and fresh feeling of the drug.
The pharmaceutical composition of the present invention maintains antibacterial quality even at high pH, thereby allowing the proliferation of microorganisms to be greatly inhibited. In particular, the composition of the present invention can rapidly kill microorganisms even after such microorganisms have infiltrated, so that the composition can be stably stored for a long time without being damaged by the microorganisms. For example, the composition of the present invention can exhibit excellent antibacterial activity against staphylococcus aureus (s. aureus), pseudomonas aeruginosa (p. aeruginosa), escherichia coli (e. coli), candida albicans (c. albicans), aspergillus brasiliensis (a. brasiliensis), Bacillus circulans (Bacillus circulans), and the like for a long period of time.
Furthermore, the pharmaceutical compositions of the present invention can maintain the level of microorganisms present therein low, even if such compositions are exposed to the outside for a long time during the preparation process. As a result, it is possible to dispense with a great investment for management aiming at preventing the infiltration of microorganisms during the preparation process, thereby making the composition advantageous for mass production and industrial use and economically effective.
In addition, the pharmaceutical composition of the present invention can maintain preservative efficacy for a long time regardless of the type of external container used to contain the composition, and also does not cause problems of absorption onto the outer wall of the container.
In the present invention, the composition may comprise 5 to 30 w/w% of aluminum phosphate gel, 0.5 to 10 w/w% of magnesium hydroxide, 0.001 to 1 w/w% of simethicone, 0.1 to 1.5 w/w% of DL-carnitine hydrochloride, and 0.001 to 0.05 w/w% of chlorhexidine salt, based on the total weight of the composition. In particular, the composition of the present invention may comprise 10 to 15 w/w% of aluminum phosphate gel, 1 to 5 w/w% of magnesium hydroxide, 0.01 to 0.5 w/w% of simethicone, 0.4 to 1 w/w% of DL-carnitine hydrochloride, and 0.001 to 0.03 w/w% of chlorhexidine salt, based on the total weight of the composition.
In the present invention, the content of the aluminum phosphate gel may be 5 to 30 w/w%, preferably 10 to 15 w/w%, based on the total weight of the composition. The aluminum phosphate gel of the present invention may be one that meets the requirements of the united states pharmacopeia. The aluminum phosphate gel of the present invention can give a fresh feeling of ingestion while exhibiting gastric mucosal protection by deacidification and neutralization of gastric acid in the content range. In addition, the aluminum phosphate gel plays a role in preventing diarrhea that may be caused by magnesium hydroxide.
In the present invention, the content of magnesium hydroxide may be 0.5 to 10 w/w%, preferably 1 to 5 w/w%, based on the total weight of the composition. The magnesium hydroxide may act as an antacid and act in neutralizing stomach acid in the stomach and intestine. In addition, the magnesium hydroxide plays a role in preventing constipation that may be caused by aluminum phosphate gel.
The pharmaceutical composition of the present invention shows a buffering effect of neutralizing gastric acid in the gastrointestinal tract and maintaining high pH in the stomach by means of aluminum phosphate gel and magnesium hydroxide, and does not cause secondary acid rebound. Furthermore, the pharmaceutical compositions of the present invention reduce the occurrence of gastrointestinal side effects in a manner such that the aluminum and magnesium salts function in a complementary manner.
In addition to the aluminum phosphate gel and the magnesium hydroxide, the pharmaceutical composition of the present invention may further comprise an antacid. The additional antacid may be, for example, an aluminum salt, a magnesium salt, a calcium salt and a sodium salt, particularly, but not limited to, aluminum hydroxide, aluminum silicate, magnesium carbonate, magnesium oxide, calcium carbonate and sodium bicarbonate.
The pharmaceutical composition of the present invention may further comprise a gastric acid inhibitor. The gastric acid inhibitor may for example be H2Receptor antagonists and proton pump inhibitors, especially cimetidine
Ranitidine
Famotidine
Nizatidine
Omeprazole
Esomeprazole
Lansoprazole
Pantoprazole
And rabeprazole
But is not limited thereto.
In the present invention, the simethicone may be present in an amount of 0.001 w/w% to 1 w/w%, preferably 0.01 w/w% to 0.5 w/w%, based on the total weight of the composition. The simethicone eliminates abdominal distension and discomfort by removing gas from the stomach.
In the present invention, the content of DL-carnitine hydrochloride may be 0.1 to 1.5 w/w%, preferably 0.4 to 1.0 w/w%, based on the total weight of the composition. The DL-carnitine hydrochloride can stimulate secretion of gastric juice and promote gastrointestinal motility.
In the present invention, the chlorhexidine salt may be selected from chlorhexidine acetate, chlorhexidine gluconate, chlorhexidine hydrochloride, or a combination thereof, and preferably may be chlorhexidine acetate (chlorhexidine diacetate), but is not limited thereto. In the present invention, the content of the chlorhexidine salt may be 0.001 w/w% to 0.05 w/w%, preferably 0.001 w/w% to 0.03 w/w%, based on the total weight of the composition. The chlorhexidine salt may act as a preservative. The pharmaceutical composition of the present invention can exhibit antibacterial effects against various environmental bacteria by including the chlorhexidine salt, thereby making the pharmaceutical composition of the present invention excellent in preservative efficacy. The pharmaceutical composition of the present invention is excellent in preservative efficacy even at a low concentration of chlorhexidine salt. In addition, the pharmaceutical composition of the present invention can maintain excellent antibacterial activity at high pH (e.g., even at pH 7 to 9) by including the chlorhexidine salt. In addition, the pharmaceutical composition of the present invention can rapidly kill microorganisms even after such microorganisms have infiltrated, thereby allowing the composition to be stably preserved for a long time without being damaged by the microorganisms. Furthermore, the pharmaceutical compositions of the present invention can maintain the level of microorganisms present therein low, even if such compositions are exposed to the outside for a long time during the preparation process. As a result, it is possible to dispense with a great investment for management aiming at preventing the infiltration of microorganisms during the preparation process, thereby making the composition advantageous for mass production and industrial use and economically effective.
In addition to the chlorhexidine salt, the pharmaceutical composition of the present invention may further comprise a preservative. The additional preservative may be, for example, aminobenzoic acid, lanolin with water, dried sodium sulfite, sodium dehydroacetate, dibutylhydroxytoluene, dichlorobenzyl alcohol, benzoic acid, sodium benzoate, benzyl alcohol, butylhydroxyanisole, butylhydroxytoluene, potassium sorbate, sorbic acid, methyl paraben, sodium methyl paraben, ethyl paraben, propyl paraben, sodium propyl paraben, butyl paraben, and phenoxyethanol, but is not limited thereto.
The pharmaceutical composition of the present invention may further comprise a viscosity controlling agent. The viscosity control agent may be, for example, agar, pectin, calcium sulfate, xanthan gum, polyvinylpyrrolidone, ethylcellulose, sodium carboxymethylcellulose, surimi gum, alginic acid, alginates, aluminum monostearate, bentonite, carbomer copolymer, carrageenan, dextrin, gelatin, guar gum, and silica, but is not limited thereto, and may be preferably selected from agar, pectin, calcium sulfate, xanthan gum, or a combination thereof. In a preferred embodiment of the invention, the pharmaceutical composition of the invention comprises agar, pectin, calcium sulfate and xanthan gum. The agar and pectin may enhance coverage of the gastric mucosa by interacting with an aluminium phosphate gel. The xanthan gum is effective in controlling the viscosity of the pharmaceutical composition. In the present invention, the xanthan gum may be present in an amount of 0.1 to 1 w/w%, preferably 0.1 to 0.7 w/w%, based on the total weight of the composition. The pharmaceutical composition of the present invention has an appropriate viscosity so that the amount of residues in the oral cavity after it is ingested is reduced, and the pharmaceutical composition is easily swallowed via the throat, so that patient compliance with the drug can be enhanced.
The pharmaceutical composition of the present invention may further comprise a sweetener. The sweetener may be selected from, for example, sucralose, white sugar, enzyme-modified stevia, xylitol, saccharin salts, stevioside, sorbitol, dextrose, glycyrrhizic acid, or combinations thereof, but is not limited thereto, and may preferably be selected from sucralose, white sugar, enzyme-modified stevia, or combinations thereof. The amount of the sweetener can be appropriately selected by those skilled in the art. In a preferred embodiment of the present invention, the pharmaceutical composition of the present invention comprises white sugar and sucralose as sweeteners. White sugar has an extremely pure taste compared to other sweeteners, so that it contributes to the fresh sensation of ingestion of the pharmaceutical composition of the invention. In the present invention, the content of white sugar may be 5 to 20 w/w%, preferably 5 to 15 w/w%, based on the total weight of the pharmaceutical composition. In a preferred exemplary embodiment of the present invention, sucralose has an excellent effect of covering the unpleasant bitter taste of chlorhexidine, thereby making it possible to enhance the sensation of ingestion of the pharmaceutical composition of the present invention. The sucralose may be present in an amount of 0.001 w/w% to 0.1 w/w%, preferably 0.005 w/w% to 0.03 w/w%, based on the total weight of the pharmaceutical composition.
The pharmaceutical composition of the present invention may further comprise a flavoring agent. The flavoring agent can be, for example, synthetic flavor oil, natural oil, plant extract, etc., especially banana flavor, apple flavor, orange flavor, banana mixed flavor, grapefruit flavor, mixed berry flavor, lime flavor, etc
Lavender flavor, lemon flavor, mint flavor, peppermint flavor, and strawberry flavor, but are not limited thereto. The amount of the flavoring agent can be appropriately selected by those skilled in the art. In a preferred embodiment of the present invention, the pharmaceutical composition of the present invention comprises banana mixed aroma as a flavoring agent. In particular, the banana blendstock may be a combination of banana flavor and strawberry flavor, and may be, for example, commercially pervasive banana blendstock B-17026.
In particular, the dosage form of the pharmaceutical composition of the invention may be an oral liquid composition, preferably a suspension. The suspension may comprise water, preferably purified water, as an excipient. The viscosity of the suspension may be from 200cps to 2200cps, preferably from 700cps to 1900cps, more preferably from 900cps to 1800cps at 20 ℃. Patient preferences may vary depending on the control of the viscosity of the pharmaceutical composition. The pharmaceutical composition of the present invention exhibits an appropriate viscosity so that the amount of residues in the oral cavity is reduced after it is ingested, and it is easily swallowed via the throat. Thus, the pharmaceutical composition of the present invention can enhance patient compliance with the drug and improve adherence to the drug.
The amounts of aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride and chlorhexidine salt per unit dosage form of the pharmaceutical composition of the present invention can be determined by one skilled in the art.
The amount of aluminium phosphate gel per unit dosage form of the pharmaceutical composition of the invention may preferably be from 5g to 30g, more preferably from 10g to 15g, most preferably about 12.5g per 100g of unit dosage form of the pharmaceutical composition; the amount of magnesium hydroxide may be from 0.5g to 10g, more preferably from 1g to 5g, most preferably about 2g per 100g of pharmaceutical composition unit dosage form; simethicone may be present in an amount of from 0.001g to 1g, more preferably from 0.01g to 0.5g, most preferably about 0.225g per 100g of pharmaceutical composition in unit dosage form; the amount of DL-carnitine hydrochloride can be from 0.1g to 1.5g, more preferably from 0.4g to 1.0g, most preferably about 0.75g per 100g of unit dosage form of the pharmaceutical composition; and the amount of chlorhexidine salt may be from 0.001g to 0.05g, preferably from 0.001g to 0.03g, most preferably about 0.015g per 100g of pharmaceutical composition unit dosage form.
The pharmaceutical composition of the present invention comprises the ranges of aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride and chlorhexidine salt per unit dosage form, thereby exhibiting excellent deacidification, degassing and gastrointestinal motivating effects, and also exhibiting remarkably high antibacterial activity, thereby exhibiting remarkably excellent preservative efficacy.
The pharmaceutical composition of the present invention may further comprise pharmaceutically acceptable additives within a range that does not impair the effects of the present invention. The additives may be, for example, dissolution aids, stabilizers, suspending agents, surfactants, antioxidants, and pH adjusters, but are not limited thereto.
The pharmaceutical composition of the present invention can be used for preventing and treating gastrointestinal dysfunction. In particular, the pharmaceutical composition of the present invention can prevent and treat gastrointestinal dysfunction by absorbing and neutralizing intestinal gas, bacteria, toxins, viruses, and the like. In particular, the pharmaceutical composition of the present invention can also be used for preventing and treating hyperacidity, heartburn, belching with a sour vomit, gastric distress or hyperphagia by neutralizing gastric acid. In particular, the pharmaceutical composition of the present invention can also relieve a feeling of bloating or stomach discomfort by removing gas from the stomach and intestine. In particular, the pharmaceutical composition of the present invention also stimulates secretion of gastric juice and promotes gastrointestinal motility, so that the composition can enhance digestive ability of the stomach and can be used for preventing and treating anorexia and anorexia. In particular, the pharmaceutical composition of the present invention is also applied to the gastric mucosa, deposited thereon and forms a protective layer on the ulcer surface, thereby making the composition useful for the prevention and treatment of nausea, vomiting or stomachache.
Thus, the pharmaceutical composition of the invention may be intended for the prevention or treatment of gastrointestinal disorders selected from, for example: gastric hyperacidity, heartburn, stomach upset, stomach discomfort, nausea, vomiting, stomach pain, belching with a sour vomit, loss of appetite, anorexia, dyspepsia, hyperphagia, or a combination thereof.
The pharmaceutical composition of the present invention can significantly reduce the level of environmental bacteria by including the chlorhexidine salt. Therefore, the pharmaceutical composition of the present invention is excellent in preservative efficacy.
The pharmaceutical composition of the present invention has good taste and appropriate viscosity. Therefore, the pharmaceutical composition of the present invention can enhance patient's liking and improve patient's compliance and adherence to the drug by virtue of a light and fresh feeling of ingestion.
The present invention provides a method for preparing a pharmaceutical composition for preventing or treating gastrointestinal dysfunction, comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride, and chlorhexidine salt.
The process for preparing the pharmaceutical composition according to the invention may comprise: a first mixing step of mixing magnesium hydroxide and simethicone with purified water; a step of heating the resulting mixed solution obtained from the first mixing step to thereby dissolve it; a second mixing step of adding an aluminum phosphate gel to the solution to thereby mix them; a step of cooling the mixture; a third mixing step of mixing the cooled mixture with a chlorhexidine salt; a step of cooling the mixture obtained from the third mixing step; and a fourth mixing step of mixing the cooled mixture with DL-carnitine hydrochloride.
The present invention provides a method for preventing or treating gastrointestinal dysfunction, comprising the step of administering a pharmaceutical composition comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride, and chlorhexidine salt to a subject in need thereof.
The gastrointestinal dysfunction means symptoms such as hyperacidity, heartburn, stomach discomfort, stomach distention, stomach discomfort, nausea, vomiting, stomach pain, belching of a sour vomit, loss of appetite, anorexia, dyspepsia, hyperphagia, etc.
By prevention is meant a prevention that reduces gastrointestinal dysfunction or the pathological appearance of symptoms caused by gastrointestinal dysfunction. By treatment is meant a treatment that ameliorates at least one symptom of gastrointestinal dysfunction or halts its development, which may encompass the meaning of commonly employed treatments.
The administration may be oral administration. Where the pharmaceutical composition is administered to a subject, such composition may be administered in an effective amount necessary to prevent or treat gastrointestinal dysfunction.
The present invention provides the use of a composition comprising aluminium phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride and chlorhexidine salt in the prevention or treatment of gastrointestinal dysfunction.
The invention provides the use of a composition comprising aluminium phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride and a chlorhexidine salt in the manufacture of a medicament for the prevention or treatment of gastrointestinal dysfunction. The composition for the preparation of a medicament according to the present invention may be mixed with an acceptable carrier or the like, and further comprise other agents.
The substances mentioned in the compositions, methods of treatment and uses of the invention are equally applicable, if not contradictory.
Advantageous effects
The pharmaceutical composition of the present invention maintains antibacterial qualities even at high pH, so that the proliferation of microorganisms is greatly inhibited. Even after the penetration of microorganisms, the composition can rapidly kill such microorganisms, so that the composition can be stably stored for a long time without being damaged by the microorganisms. Therefore, the pharmaceutical composition of the present invention is remarkably excellent in preservative efficacy.
In addition, the pharmaceutical composition of the present invention can maintain preservative efficacy for a long time regardless of the type of external container used to contain the composition, and also does not cause problems of absorption onto the outer wall of the container.
Furthermore, the pharmaceutical compositions of the present invention can maintain the level of microorganisms present therein low, even if such compositions are exposed to the outside for a long time during the preparation process. As a result, it is possible to dispense with a great investment for management aiming at preventing the infiltration of microorganisms during the preparation process, thereby making the composition advantageous for mass production and industrial use and economically effective.
Further, the pharmaceutical composition of the present invention has a less bitter taste, and also has an appropriate viscosity, so that the amount of residues in the oral cavity after it is ingested is reduced, and the pharmaceutical composition is easily swallowed via the throat, so that high liking of patients is achieved and compliance with and adherence to drugs are significantly enhanced.
In addition, the pharmaceutical composition of the present invention shows excellent activity for improving gastrointestinal dysfunction.
Therefore, the pharmaceutical composition of the present invention can be effectively used as a pharmaceutical composition because it is excellent in preservative efficacy; the preparation method thereof is advantageous for mass production and economically efficient; enhancing compliance with and adherence to medications; and also excellent in the activity of improving gastrointestinal dysfunction.
Detailed Description
Hereinafter, the present invention will be described in more detail via specific exemplary embodiments. However, the following exemplary embodiments are provided only for the purpose of illustrating the present invention, and thus the present invention is not limited thereto.
Example 1
Magnesium hydroxide, simethicone, agar, pectin, xanthan gum, calcium sulfate and white sugar were mixed in purified water at 25 ℃ in the amounts indicated in table 1 below. The resulting mixed solution was heated up to 70 ℃ so that the mixture was dissolved for 10 to 20 minutes. Aluminum phosphate gel was added and mixed thereto in the amount as indicated in table 1, and the mixture was cooled to 50 to 60 ℃. Chlorhexidine acetate was added and mixed in the cooled mixture in the amounts as indicated in table 1. Chlorhexidine acetate (chlorhexidine diacetate) was mixed therein and cooled to 30 ℃ or less, after which DL-carnitine hydrochloride was added thereto in an amount as indicated in table 1 below, followed by further addition of an appropriate amount of sucralose (0.005g to 0.03g), mixing, and cooling at room temperature. Finally, banana blendstocks were added thereto in the amounts as indicated in table 1, after which the resulting mixture was mixed, ground and filled to prepare a total of 100g of suspension.
[ Table 1]
Example 2 and example 3
Suspensions were prepared by the same method as shown in example 1, except that the content of chlorhexidine acetate used was 0.02g and 0.03g, respectively.
Example 4 and example 5
A suspension was prepared by the same method as shown in example 1 except that xanthan gum was further added to the purified water in the amount as indicated in table 2 below.
[ Table 2]
| Example 4 | Example 5 | |
| Xanthan gum (g) | 0.3 | 0.5 |
Experimental example 1 identification of preservative efficacy
The preservative efficacy of the compositions according to examples 1 to 3 was identified by means of the "preservative efficacy test method" of the general test method of the korean pharmacopoeia. To confirm that the preservative efficacy is sufficient, when inoculated with bacteria, the number of bacteria should be reduced from the number of inoculated bacteria to 10% or less at 14 days after inoculation, and the number of bacteria should also be maintained or reduced to a level at 28 days thereafter which is equal to or lower than the above-described level of bacteria measured at 14 days thereafter. In the case of fungi, it was confirmed that preservative efficacy was exhibited if the number of fungi was equal to or lower than the number of inoculated fungi at 14 days after inoculation with fungi, and if the number of fungi was also equal to or lower than the number of inoculated fungi at 28 days thereafter. In other words, the reduction (%) was measured according to the following formula, namely: (number of inoculated bacteria-number of viable bacteria)/number of inoculated bacteria × 100. If the reduction rate is 90% or more, the preservative efficacy of the preservative is judged to be present. If preservative efficacy is present in all tested bacteria, it is judged that preservative efficacy is appropriate.
The following were used as test strains: standard bacteria, i.e., staphylococcus aureus (staphylococcus aureus), Pseudomonas aeruginosa (Pseudomonas aeruginosa) and Escherichia coli (Escherichia coli); standard fungi, i.e., Candida albicans (Candida albicans) and Aspergillus brasiliensis (Aspergillus brasiliensis); and environmental bacteria, i.e., Bacillus circulans. Bacteria were cultured in Tryptic Soyagar (Tryptic Soyagar) medium and fungi were cultured in Sabouraud Dextrose Agar (Sabouraud Dextrose Agar) medium.
As a result of the test for preservation efficacy, the composition according to example 1 of the present invention not only satisfied the standard for preservation efficacy for all the strains, but also showed significantly excellent antibacterial activity with a reduction rate of 99% or more.
Claims (16)
1. A pharmaceutical composition comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride, and chlorhexidine salt.
2. The pharmaceutical composition of claim 1, wherein the chlorhexidine salt is chlorhexidine acetate, chlorhexidine gluconate, chlorhexidine hydrochloride, or a combination thereof.
3. The pharmaceutical composition of claim 1, wherein the chlorhexidine salt is chlorhexidine acetate.
4. The pharmaceutical composition of claim 1, wherein a sweetener is further comprised in the pharmaceutical composition.
5. The pharmaceutical composition of claim 4, wherein the sweetener is selected from the group consisting of enzymatically modified stevia, xylitol, saccharin salts, stevioside, sorbitol, dextrose, glycyrrhizic acid, white sugar, sucralose, or combinations thereof.
6. The pharmaceutical composition of claim 4, wherein the sweeteners are white sugar and sucralose.
7. The pharmaceutical composition of claim 6, wherein white sugar is present in an amount of 5 w/w% to 20 w/w% based on the total weight of the pharmaceutical composition, and sucralose is present in an amount of 0.001 w/w% to 0.1 w/w% based on the total weight of the pharmaceutical composition.
8. The pharmaceutical composition of claim 1, wherein a viscosity control agent selected from agar, pectin, calcium sulfate, xanthan gum or a combination thereof is further comprised in the pharmaceutical composition.
9. The pharmaceutical composition of claim 1, wherein a flavoring agent is further included in the pharmaceutical composition.
10. The pharmaceutical composition of claim 1, wherein the dosage form is a suspension.
11. The pharmaceutical composition of claim 10, wherein the viscosity of the suspension is 700cps to 1500cps at 20 ℃.
12. The pharmaceutical composition of claim 1, wherein the composition comprises 10 to 15 w/w% of the aluminum phosphate gel, 1 to 5 w/w% of the magnesium hydroxide, 0.01 to 0.5 w/w% of simethicone, 0.4 to 1.0 w/w% of DL-carnitine hydrochloride, and 0.001 to 0.03 w/w% of chlorhexidine salt, based on the total weight of the composition.
13. The pharmaceutical composition of claim 12, wherein the chlorhexidine salt is chlorhexidine acetate.
14. The pharmaceutical composition according to claim 1, wherein the composition is intended for the prevention or treatment of gastrointestinal disorders selected from the group consisting of: gastric hyperacidity, heartburn, stomach upset, stomach discomfort, nausea, vomiting, stomach pain, belching with a sour vomit, loss of appetite, anorexia, dyspepsia, hyperphagia, or a combination thereof.
15. The pharmaceutical composition according to claim 1, wherein the composition is intended for an oral composition.
16. A method for preventing or treating gastrointestinal dysfunction, comprising the step of administering to a subject a pharmaceutical composition comprising aluminum phosphate gel, magnesium hydroxide, simethicone, DL-carnitine hydrochloride, and chlorhexidine salt.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR10-2018-0043360 | 2018-04-13 | ||
| KR1020180043360A KR101926853B1 (en) | 2018-04-13 | 2018-04-13 | Pharmaceutical composition |
| PCT/KR2019/004415 WO2019199100A1 (en) | 2018-04-13 | 2019-04-12 | Pharmaceutical composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN111836629A true CN111836629A (en) | 2020-10-27 |
Family
ID=64669671
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980018249.6A Pending CN111836629A (en) | 2018-04-13 | 2019-04-12 | Pharmaceutical composition |
Country Status (4)
| Country | Link |
|---|---|
| KR (1) | KR101926853B1 (en) |
| CN (1) | CN111836629A (en) |
| TW (1) | TWI698258B (en) |
| WO (1) | WO2019199100A1 (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101926853B1 (en) * | 2018-04-13 | 2018-12-07 | 보령제약 주식회사 | Pharmaceutical composition |
| US11396139B2 (en) | 2019-05-22 | 2022-07-26 | The Regents Of The University Of Michigan | High-speed polymer-to-metal direct joining system and method |
| US11890788B2 (en) | 2020-05-20 | 2024-02-06 | The Regents Of The University Of Michigan | Methods and process for producing polymer-metal hybrid components bonded by C—O-M bonds |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1203079A (en) * | 1997-04-16 | 1998-12-30 | 麦克尼尔-Ppc公司 | Liquid antiacid compositions |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR0130427B1 (en) * | 1994-08-01 | 1998-04-09 | 김승호 | Complexed antiulcer compositions |
| JPH08259445A (en) * | 1995-01-27 | 1996-10-08 | Takeda Chem Ind Ltd | Medicinal composition for improving gastric emptying performance |
| KR0174648B1 (en) * | 1996-11-04 | 1999-10-01 | 김승호 | Composite antacid composition |
| KR20110065417A (en) * | 2008-01-03 | 2011-06-15 | 욱크하르트 리미티드 | Oral pharmaceutical suspension comprising paracetamol and ibuprofen |
| KR101926853B1 (en) * | 2018-04-13 | 2018-12-07 | 보령제약 주식회사 | Pharmaceutical composition |
-
2018
- 2018-04-13 KR KR1020180043360A patent/KR101926853B1/en active IP Right Grant
-
2019
- 2019-04-12 CN CN201980018249.6A patent/CN111836629A/en active Pending
- 2019-04-12 WO PCT/KR2019/004415 patent/WO2019199100A1/en active Application Filing
- 2019-04-12 TW TW108112937A patent/TWI698258B/en active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1203079A (en) * | 1997-04-16 | 1998-12-30 | 麦克尼尔-Ppc公司 | Liquid antiacid compositions |
Non-Patent Citations (2)
| Title |
|---|
| 宋修军: "《临床骨科药物学》", 31 May 2010 * |
| 李平等: "《部队消毒工作手册》", 31 December 2012 * |
Also Published As
| Publication number | Publication date |
|---|---|
| TW201946612A (en) | 2019-12-16 |
| WO2019199100A1 (en) | 2019-10-17 |
| TWI698258B (en) | 2020-07-11 |
| KR101926853B1 (en) | 2018-12-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN111836629A (en) | Pharmaceutical composition | |
| US7776831B2 (en) | Use of antifungal compositions to treat upper gastrointestinal conditions | |
| US20080213241A1 (en) | Protease composition and method for treating a digestive disorder | |
| EP3703657B1 (en) | Suckable and/or melt-in-mouth tablet based on hyaluronic acid and chondroitin sulphate and salts thereof for use in the treatment of a subpopulation of gerd patients | |
| US20200337996A1 (en) | Suckable and/or melt-in-mouth tablet based on hyaluronic acid and chondroitin sulphate and salts thereof | |
| US11110118B2 (en) | Formulations for treating acid reflux comprising sodium alginate | |
| EP3773615B1 (en) | Liquid composition for use in the treatment of the mucosa of the oro-pharyngo-laryngo-esophageal tract | |
| US20230000899A1 (en) | Alginate, polylysine, and seed preservative nutritional product and digestive aid | |
| KR101488921B1 (en) | Mint liquid for improving digestive functions and manufacturing method thereof | |
| US20120121655A2 (en) | Chewable Formulation Comprising Alginate, Bicarbonate And Carbonate | |
| KR101088779B1 (en) | Sulglycotide-containing liquidic formulation for oral administration | |
| WO2010108494A1 (en) | Dayspepsia treatment with alginate | |
| US11723939B2 (en) | Composition for gastric and oesophageal diseases | |
| JP2002509539A (en) | Combination of antacid and papain | |
| KR101088781B1 (en) | Sulglycotide-containing liquidic formulation for oral administration | |
| EP2537528B1 (en) | Pharmaceutical compositions containing beta- and alpha-galactosidase and their use in the treatment of gastroesophageal reflux disease | |
| WO2023026231A1 (en) | Composition for the prevention and/or treatment of gastric and esophageal diseases | |
| ES2274550T3 (en) | PROCEDURES AND COMPOSITIONS TO PREVENT AND TREAT BURNING OF STOMACH. | |
| KR0174648B1 (en) | Composite antacid composition | |
| KR20150082906A (en) | Aqueous flowable liquid composition and preparing methode thereof | |
| IT202100021995A1 (en) | Composition for the prevention and/or treatment of gastric and oesophageal pathologies | |
| CN114468301A (en) | Composition for resisting helicobacter pylori and preparation thereof | |
| PT1019066E (en) | Methods and compositions for preventing and treating heartburn | |
| KR20060122389A (en) | Antacid complex compound comprising diomagnite |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination |