Enteric coating composition, solid preparation and method for producing solid preparation

A technology of enteric coating and composition, which is applied in the field of aqueous dispersion, and can solve problems such as difficulty in exerting the effect of drug administration

Pending Publication Date: 2020-10-20
SHIN ETSU CHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is difficult to exert the effect of administration

Method used

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  • Enteric coating composition, solid preparation and method for producing solid preparation
  • Enteric coating composition, solid preparation and method for producing solid preparation
  • Enteric coating composition, solid preparation and method for producing solid preparation

Examples

Experimental program
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Effect test

preparation example Construction

[0019] From the viewpoint of the production rate of the HPMCAS, the molar substitution (MS) of hydroxypropoxy in the HPMCAS is preferably 1.00 or less, more preferably 0.90 or less, further preferably 0.85 or less, particularly preferably 0.80 or less.

[0020] More specifically, the molar substitution (MS) of hydroxypropoxy in the HPMCAS is preferably 0.40 to 1.00, more preferably 0.42 to 0.90, even more preferably 0.50 to 0.85, even more preferably 0.55 to 0.85, particularly preferably 0.60 ~0.80.

[0021] The degree of substitution (DS) of the methoxy group in this HPMCAS is not particularly limited. From the viewpoint of the production rate of the HPMCAS and the film strength, it is preferably 0.70 to 2.50, more preferably 1.00 to 2.20, and still more preferably 1.40 to 1.95.

[0022] The degree of substitution (DS) of the acetyl group in this HPMCAS is not particularly limited. From the viewpoint of acid resistance and enteric properties, it is preferably 0.10 to 2.50, ...

Embodiment 1～5 and comparative example 1

[0138] Pure water (1325.6 parts by mass) was added to a 200-ml beaker and stirred at 200 rpm using a propeller stirrer (NZ-1100, a product of Tokyo Rikakikai Co., Ltd.) while stirring on ice Cool in the bath to about 10°C. Next, while cooling to about 10° C., sodium lauryl sulfate (SLS) (3 parts by mass) as a surfactant was added thereto and mixed, and then HPMCAS-2 to 4 and 6 to 8 were added. HPMCAS (100 parts by mass), followed by stirring at 200 rpm for 30 minutes while cooling to about 10° C., to prepare an enteric coating composition, which is an aqueous dispersion of HPMCAS.

[0139] In order to evaluate the coating performance (film-forming performance) of each prepared enteric coating composition, the film-forming property on a glass plate was tested. A 100 μl aliquot of the enteric coating composition was poured onto five glass plates and dried in an oven for 2 hours at each temperature (25, 30, 40, 50 or 60° C.) to visually inspect the film Formation. The lowest d...

Embodiment 6～8 and comparative example 2

[0141] Pure water (1323.0 parts by mass) was added to a 200 mL beaker at room temperature, and sodium lauryl sulfate (SLS) (3 parts by mass) was added thereto as a surfactant, and while using a propeller stirrer (NZ-1100, Tokyo Rikaki Co., Ltd.) was mixed while stirring at 200 rpm. Next, HPMCAS-1, 3, 5, or 8 (100 parts by mass) was added thereto, and stirred at 200 rpm at room temperature to prepare an aqueous dispersion. Then, 10% by mass of ammonia solution (2.60 parts by mass in terms of ammonia) was added thereto, and stirred at room temperature at 200 rpm for 30 minutes to prepare an enteric coating composition, which was an aqueous dispersion of partially neutralized HPMCAS .

[0142] In order to evaluate the coating performance (film-forming property) of each prepared enteric coating composition, film formation on a glass plate was tested in the same manner as in Examples 1 to 5. The results are shown in Table 3.

[0143]

[0144] The results of Examples 1 to 5 sh...

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Abstract

There are provided an enteric coating composition having an excellent film-forming property, being capable of forming a film at a lower temperature than conventional compositions, and / or being capableof avoiding decomposition of a drug due to a high temperature and operational troubles due to or nozzle clogging; and others. More specifically, there are provided an enteric coating composition containing hypromellose acetate succinate having a molar substitution of hydroxypropoxy groups of 0.40 or more, and water; a method for producing a solid preparation including steps of coating a drug-containing core with the enteric coating composition to obtain a coating layer, and drying the coating layer; and a solid preparation containing a drug-containing core, and a coating layer directly or indirectly on the core, the coating layer containing a hypromellose acetate succinate having a molar substitution of hydroxypropoxy groups of 0.40 or more.

Description

technical field [0001] The invention relates to an enteric coating composition, which is an aqueous dispersion comprising hypromellose acetate succinate and water; and an application of the composition. Background technique [0002] Drugs for pharmaceutical applications include those that degrade under acidic conditions. When such drugs are administered, they are broken down in the stomach, which has acidic conditions, and then reach the site of absorption in the small intestine. Therefore, it is difficult to exert the effect of administration. Acid resistant dosage forms are widely used to deliver such drugs into the intestine. For example, coating with an enteric coating composition is a technique for coating tablets, granules and powders with polymers to protect them from breakdown in the stomach and dissolve rapidly in the intestine. [0003] Examples of polymers used as enteric substrates include polymers with methoxy groups (-OCH 3 ) and hydroxypropoxyl (-OC 3 h ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K9/36A61K9/50A61K9/48
CPCA61K47/38A61K9/2866A61K9/5042A61K9/4891A61K9/5015A61K9/282A61K9/5047A61K47/10
Inventor 藁品彰吾平间康之
Owner SHIN ETSU CHEM CO LTD
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