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Mucoadhesive pharmaceutical composition and preparation method therefor

Inactive Publication Date: 2019-01-24
SAMYANG HLDG CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patent describes a pharmaceutical composition that has the ability to stick to mucous membranes in the body, making it suitable for a variety of applications including oral, buccal, ophthalmic, vaginal, and nasal formulations, among others. When taken as an oral formulation, it can remain in the gastro-intestinal tract for a longer period of time, increasing the effectiveness of limited absorption active ingredients. The composition is made up of a mixture of chitosan and polyacrylic acid that forms a complex in the body, allowing for controlled release of the active ingredient. This results in a more consistent and effective delivery of the medication, improving its efficacy and reducing the need for frequent dosing.

Problems solved by technology

However, the poly-ionic complex has too low molecular weight as a drug carrier.
In addition, because it was not easy to find a solvent which can solubilize the formed poly-ionic complex, it has only a limited application, e.g. as a membrane formed through simple drying or freeze drying, etc. or as a hydrogel.
In particular, studies on application as an oral drug carrier could hardly be progressed.
In some cases, conventional facilities for manufacturing solid formulations were inapplicable for its production, but special facilities were required or only lab-scale production was available.
Furthermore, no study has been carried out on drying followed by milling for micronization of the formed poly-ionic complex.
Also, there were problems that active ingredient release is not readily controllable and active ingredient dissolution pattern depends on a pH due to properties of poly-ionic complex.

Method used

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  • Mucoadhesive pharmaceutical composition and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

reference example 1

[0128]Dissolution test of an active ingredient from the formulation was conducted according to Method 2 Paddle Method of “36. Dissolution Test Method” in Korean Pharmacopoeia 8th edition (KP VIII). The eluent was selected from a buffer of pH 1.2, a buffer of pH 4.0, a buffer of pH 6.8, water and 0.1N HCl, and used in an amount of 900 ml. The test was conducted at 37° C. with 100 rotations per minute.

[0129]After dissolution, analysis of drug was conducted by using high performance liquid chromatography (HPLC). Analysis of drug was performed under conventionally known conditions.

[0130]For example, when the active ingredient was paliperidone, the following conditions were used for the analysis:

[0131]Mobile phase: A mixed solution of a solution prepared by dissolving 21.76 g of potassium phosphate monobasic in 4 L of water and adjusting the pH to 2.0 with phosphoric acid, and 1 L of acetonitrile

[0132]Column: XBridge phenyl. 150×4.6 mm, 3.5 μm

[0133]Flow rate: 1.0 ml / min

[0134]Column Tempe...

reference example 2

[0144]In order to test the mucoadhesiveness of the matrix-forming agent, the sample was prepared in disc form using a die to make disc for measuring IR (Infrared) spectrum. 100 mg of the sample was put into a die for preparing KBr disc and 5 to 10 tons of pressure was maintained for 3 minutes, and then a compressed disc with diameter of about 12 mm and thickness of about 0.75 mm was obtained.

reference example 3

veness Test

[0145]The in vitro test for mucoadhesiveness was conducted by utilizing a texture analyzer. A probe with diameter of 5 mm was used. The sample was fixed to the probe with double-sided tape, and cellulose acetate membrane filter was fixed at the lower part with double-sided tape and wetted with 100 μl of 3% mucin solution to simulate the environment of gastro-intestinal tract. Mucin was dissolved in a buffer of pH 1.2 or distilled water to make 3% solution for use. The measurement was made 1 minute after the wetting of the membrane. The descending speed of the probe was 0.5 mm / s, the pressing force of 1 N was maintained for 30 seconds, and then, the ascending speed was 0.5 mm / s, to measure mucoadhesiveness. The result is shown as adhesion force (N).[0146](Reference: Int J Pharm Sci Drug Res, 2011, 3, 84˜88, Eur J Pharm Biopharm. 2009. 71, 325-331)

[0147]The disc prepared according the method disclosed in Reference Example 2 was cut into a size of 2.5 mm×2.5 mm and attached ...

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Abstract

Disclosed is a mucoadhesive pharmaceutical composition comprising a poly-ionic complex of chitosan and a polyacrylic acid polymer. As an oral formulation, the composition has the extended retention time in the gastrointestinal tract by its mucoadhesive and swelling properties, which is useful as sustained release formulations, retentive formulations of active ingredients with limited absorption regions, and active ingredients with pH dependent solubility.

Description

TECHNICAL FIELD[0001]The present disclosure relates to a mucoadhesive pharmaceutical composition, and more specifically, a mucoadhesive pharmaceutical composition or formulation which is applicable as a gastro-intestinal retentive formulation, a sustained release oral formulation, etc. for an active ingredient having limited absorption region, by increasing the retention time in gastro-intestinal tract due to mucoadhesiveness particularly in gastro-intestinal tract and swelling property.BACKGROUND ART[0002]Chitin, a natural polymer occurring in the second largest quantity next to cellulose among natural polymers in the natural system, is a natural polysaccharide having a molecular weight of about 1,000,000 or higher wherein N-acetyl-D-glucosamine is linked by β-1,4-linkage. It is contained in a large amount mainly in shells of crustaceans such as crab, shrimp, etc. Chitosan is a natural cationic polysaccharide obtained by deacetylation of N-acetyl group in chitin followed by substit...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/16A61K47/36A61K47/32A61K47/10A61K47/42
CPCA61K9/006A61K9/1635A61K9/1652A61K9/0065A61K47/36A61K47/32A61K47/10A61K47/42B82Y5/00A61K9/2059
Inventor PARK, SANG YEOBYOON, JONG WON
Owner SAMYANG HLDG CORP
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