Composition for hot-melt extrusion and method for producing hot-melt extrusion product using same

Patent metadata

Field	Value
Publication number	US-10016508-B2
Application number	US-201414294258-A
Country	US
Kind code	B2
Filing date	Jun 3, 2014
Priority date	Jun 3, 2013
Publication date	Jul 10, 2018
Grant date	Jul 10, 2018

Abstract

Provided are a composition for hot-melt extrusion which can be hot-melt extruded at a temperature lower than a conventional temperature and therefore free of heat-induced deactivation of a drug; and a method for producing a hot-melt extrusion product which is simpler than a spray-drying method. More specifically, provided is a composition for hot-melt extrusion including a drug and hypromellose acetate succinate (HPMCAS) having a hydroxypropoxy molar substitution of 0.40 or more. Also provided is a method for producing a hot-melt extrusion product including a step of hot-melt extruding a composition for hot-melt extrusion including a drug and hypromellose acetate succinate having a hydroxypropoxy molar substitution of 0.40 or more at a hot-melt temperature of melting temperature of the hypromellose acetate succinate or higher, or at a hot-melt temperature equal to or higher than a temperature at which both the hypromellose acetate succinate and the drug become melted.

First claim

The invention claimed is:

1. A composition for hot-melt extrusion, comprising a drug and hypromellose acetate succinate having a hydroxypropoxy molar substitution of 0.40 to 1.00.

2. The composition for hot-melt extrusion according to claim 1 , wherein the hydroxypropoxy molar substitution is from 0.40 to 0.90.

3. The composition for hot-melt extrusion according to claim 1 , wherein the hypromellose acetate succinate has a glass transition temperature (Tg) of 115° C. or lower.

4. The composition for hot-melt extrusion according to claim 1 , wherein the hypromellose acetate succinate has a glass transition temperature (Tg) of 70 to 100° C.

5. The composition for hot-melt extrusion according to claim 1 , wherein the hypromellose acetate succinate has a methoxy molar substitution from 1.4 to 1.9.

6. The composition for hot-melt extrusion according to claim 1 , wherein the hypromellose acetate succinate has an acetyl molar substitution from 0.40 to 0.95.

7. The composition for hot-melt extrusion according to claim 1 , wherein the hypromellose acetate succinate has a succinyl molar substitution from 0.10 to 0.60.

8. The composition for hot-melt extrusion according to claim 1 , wherein a molar ratio of acetyl groups to succinyl groups in the hypromellose acetate succinate is from 1.6 to 4.0.

9. The composition for hot-melt extrusion according to claim 1 , wherein a molar ratio of acetyl groups to succinyl groups in the hypromellose acetate succinate is from 1.8 to 3.8.

10. The composition for hot-melt extrusion according to claim 1 , wherein the drug is poorly water-soluble.

11. The composition for hot-melt extrusion according to claim 1 , wherein a weight ratio of hypromellose acetate succinate to drug is preferably from 1:0.2 to 1:5.

12. The composition for hot-melt extrusion according to claim 1 further comprising a plasticizer.

13. The composition for hot-melt extrusion according to claim 1 further comprising a surfactant.

14. A method for producing a hot-melt extrusion product, comprising a step of hot-melt extruding a composition for hot-melt extrusion comprising a drug and hypromellose acetate succinate having a hydroxypropoxy molar substitution of 0.40 to 1.0 at a hot-melt temperature of melting temperature of the hypromellose acetate succinate or higher, or at a hot-melt temperature equal to or higher than a temperature at which both the hypromellose acetate succinate and the drug become melted.

15. The method for producing a hot-melt extrusion product according to claim 14 , wherein a molar ratio of acetyl groups to succinyl groups in the hypromellose acetate succinate is from 1.6 to 4.0.

16. The method for producing a hot-melt extrusion product according to claim 14 , wherein the hot-melting temperature is from 50 to 250° C.

17. The method for producing a hot-melt extrusion product according to claim 14 , wherein the hot-melting temperature is from 90 to 190° C.

18. The method for producing a hot-melt extrusion product according to claim 14 , wherein the hot-melt extrusion is performed at an extrusion rate of 10 to 100 mm/min.

19. The method for producing a hot-melt extrusion product according to claim 14 further comprising a step of cooling the composition after extrusion.

Assignees

• Shinetsu Chemical Co

Inventors

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

Classifications

• C08L1/32

  Cellulose ether-esters · CPC title

• C08J2301/32

  Cellulose ether-esters · CPC title

• C08J3/201

  Pre-melted polymers · CPC title

• C08B13/00

  Preparation of cellulose ether-esters · CPC title

• C08B11/20

  Post-etherification treatments of chemical or physical type, {e.g. mixed etherification in two steps}, including purification · CPC title