Hypromellose acetate succinate powder excellent in dissolved state and production method thereof, and production methods for composition for solid dispersion, coating composition, drug-containing particle, and solid

Patent metadata

Field	Value
Publication number	US-11396558-B2
Application number	US-202017066543-A
Country	US
Kind code	B2
Filing date	Oct 9, 2020
Priority date	Apr 5, 2016
Publication date	Jul 26, 2022
Grant date	Jul 26, 2022

Abstract

Provided are HPMCAS powder having high solubility when dissolved in a solvent and being capable of suppressing generation of undissolved materials; and a method for producing the powder. More specifically, provided is hypromellose acetate succinate powder having an average ratio of L to D of from 2.0 to 3.0, wherein L and D mean maximum and minimum diameters of each particle, respectively. Also provided is a method for producing a hypromellose acetate succinate, comprising the steps of: dissolving hypromellose powder in a solvent, esterifying the dissolved hypromellose with succinic anhydride and acetic anhydride in the presence of a catalyst to obtain a reaction mixture, and mixing the reaction mixture with water to precipitate hypromellose acetate succinate, wherein the reaction mixture just before being mixed with the water has a viscosity of from 100 to 200 Pa·s.

First claim

That which is claimed is:

1. A method for producing a coating composition, the method comprising dissolving a hypromellose acetate succinate powder having an average ratio of L to D of from 2.0 to 3.0 in a solvent which is a mixed solution of water and an alcohol, or an aqueous ammonia solution,
wherein L and D mean maximum and minimum diameters, respectively, of each particle in the hypromellose acetate succinate powder.

2. The method for producing a coating composition according to claim 1 , wherein the hypromellose acetate succinate powder has a specific surface area of from 2.0 to 5.0 m 2 /g or more.

3. The method for producing a coating composition according to claim 1 , wherein the hypromellose acetate succinate powder has a loose bulk density of from 0.10 to 0.25 g/mL.

4. The method for producing a coating composition according to claim 1 , wherein the hypromellose acetate succinate powder comprises 10% by weight or less of component not soluble at 20° C. in such a weight of acetone as to be 10 times the weight of the powder.

5. A method for producing a drug-containing particle, comprising:
each step comprised by the method as claimed in claim 1 to obtain a coating composition; and
a step of coating a drug-containing core with the coating composition to form a coat portion over the core.

6. A method for producing a solid preparation, comprising:
the steps comprised by the method as claimed in claim 5 to obtain a drug-containing particle; and
a step of formulating the drug-containing particle into a preparation.

7. The method for producing a solid preparation according to claim 6 , wherein the solid preparation is a tablet, a granule or a fine granule.

Assignees

• Shinetsu Chemical Co

Inventors

• Matsubara Junichi
• Maruyama Naosuke
• Yoshida Mitsuhiro
• Kikuchi Kazuki

Classifications

• A61K9/5042

  Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose · CPC title

• A61K31/525

  Isoalloxazines, e.g. riboflavins, vitamin B2 · CPC title

• C08B13/00 Primary

  Preparation of cellulose ether-esters · CPC title

• A61K9/2866 Primary

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• A61K47/38 Primary

  Cellulose; Derivatives thereof · CPC title