Hypromellose acetate succinate for use as hot-melt extrusion carrier, hot-melt extrusion composition, and method for producing hot-melt extrudate

Patent metadata

Field	Value
Publication number	US-11090295-B2
Application number	US-201414453935-A
Country	US
Kind code	B2
Filing date	Aug 7, 2014
Priority date	Aug 12, 2013
Publication date	Aug 17, 2021
Grant date	Aug 17, 2021

Abstract

Provided are hypromellose acetate succinates (HPMCAS) for use as a hot-melt extrusion carrier having a volume average particle size (D 50 ) of from 70 to 300 as measured by dry laser diffraction and a loose bulk density of from 0.25 to 0.40 g/cm 3 ; and a hot-melt extrusion composition comprising the HPMCAS and a drug. Also provided is a method for producing a hot-melt extrudate including the steps of: hot-melting the hot-melt extrusion composition at a hot-melt temperature equal to or higher than a melting temperature of the HPMCAS, or at a hot-melt temperature equal to or higher than a temperature at which both of the HPMCAS and the drug become melt; and extruding the hot-melted composition.

First claim

The invention claimed is:

1. Hypromellose acetate succinate for use as a hot-melt extrusion carrier having a volume-average particle size (D 50 ) as measured by dry laser diffraction of from 70 to 300 μm and a loose bulk density of from 0.25 to 0.40 g/cm 3 , wherein the hypromellose acetate succinate has a degree of compaction of from 15 to 40 %.

2. A hot-melt extrusion composition comprising the hypromellose acetate succinate as claimed in claim 1 and a drug.

3. The hot-melt extrusion composition according to claim 2 , wherein the drug is a poorly water-soluble drug.

4. A method for producing a hot-melt extrudate, comprising the steps of:
hot-melting a hot-melt extrusion composition comprising hypromellose acetate succinate having a volume-average particle size (D 50 ) as measured by dry laser diffraction of from 70 to 300 μm a loose bulk density of from 0.25 to 0.40 g/cm 3 , and a degree of compaction of from 15 to 40 %, and a drug at a hot-melt temperature equal to or higher than a melting temperature of the hypromellose acetate succinate, or at a hot-melt temperature equal to or higher than a temperature at which both of the hypromellose acetate succinate and the drug become melt to provide a hot-melted composition; and
extruding the hot-melted composition.

5. The method for producing a hot-melt extrudate according to claim 4 , wherein the hot-melt temperature is from 50 to 250° C.

6. The hypromellose acetate succinate according to claim 1 , wherein the degree of compaction is from 20.2 to 28.2%.

7. The hypromellose acetate succinate according to claim 1 , wherein the hypromellose acetate succinate has an angle of repose from 30 to 45°.

8. The hypromellose acetate succinate according to claim 1 , wherein the hypromellose acetate succinate has an angle of repose from 30 to 40° .

9. A composition comprising the hypromellose acetate succinate according to claim 1 and a plasticizer or a surfactant, wherein the composition is a hot-melt extrusion composition.

10. The hypromellose acetate succinate according to claim 1 , wherein the degree of compaction is from 15 to 35%.

11. A hot-melt extrusion composition comprising the hypromellose acetate succinate as claimed in claim 10 and a drug.

12. The hot-melt extrusion composition according to claim 11 , wherein the drug is a poorly water-soluble drug.

Assignees

• Shinetsu Chemical Co

Inventors

• Maruyama Naosuke
• Warashina Shogo
• Kusaki Fumie
• Obara Sakae
• Kikuchi Kazuki

Classifications

• A61K9/20

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• A61K9/146

  with organic macromolecular compounds · CPC title

• A61K31/4422 Primary

  1,4-Dihydropyridines, e.g. nifedipine, nicardipine · CPC title

• Y10T428/2982

  Particulate matter [e.g., sphere, flake, etc.] · CPC title