Esterified cellulose ethers of low viscosity

Patent metadata

Field	Value
Publication number	US-9486532-B2
Application number	US-201414766997-A
Country	US
Kind code	B2
Filing date	Feb 28, 2014
Priority date	Mar 7, 2013
Publication date	Nov 8, 2016
Grant date	Nov 8, 2016

Abstract

Esterified cellulose ethers which comprise (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA, wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation, or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, which have a viscosity of up to 2.33 mPa·s, measured as a 2.0 wt % solution of the esterified cellulose ether in 0.43 wt % aqueous NaOH at 20° C., and which have a viscosity of up to 13 mPao·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C. are useful for preparing solid dispersions comprising drugs.

First claim

The invention claimed is:

1. A hydroxypropyl methyl cellulose acetate succinate (HPMCAS)
having a viscosity of up to 2.33 mPa·s, measured as a 2.0 wt % solution of the HPMCAS in 0.43 wt % aqueous NaOH at 20° C., and
having a viscosity of up to 13 mPa·s, measured as a 10 wt % solution of the HPMCAS in acetone at 20° C.

2. The HPMCAS of claim 1 having a viscosity of from 1.20 to 1.80 mPa·s, measured as a 2.0 wt % solution of the HPMCAS in 0.43 wt % aqueous NaOH at 20° C.

3. The HPMCAS of claim 1 having a viscosity of up to 10 mPa·s, measured as a 10 wt % solution of the HPMCAS in acetone at 20° C.

4. The HPMCAS of claim 3 having a viscosity of up to 3 mPa·s, measured as a 10 wt % solution of the HPMCAS in acetone at 20° C.

5. The HPMCAS of claim 1 having a weight average molecular weight of M w of from 90,000 to 350,000 Dalton.

6. The HPMCAS of claim 1 having a weight average molecular weight of M w of from 10,000 to 90,000 Dalton.

7. A composition comprising a liquid diluent and at least one HPMCAS of claim 1 .

8. The composition of claim 7 additionally comprising at least one active ingredient and optionally one or more adjuvants.

9. The composition of claim 7 comprising from 10 to 25 percent of at least one HPMCAS, from 70 to 89 percent of a liquid diluent, and from 1 to 15 percent of an active ingredient, based on the total weight of the composition.

10. A solid dispersion comprising at least one active ingredient and at least one HPMCAS of claim 1 .

11. The solid dispersion of claim 10 wherein the solid dispersion has been formulated into tablets, pills, granules, pellets, caplets, microparticles, fillings of capsules, or into a paste, cream, suspension or slurry.

12. A dosage form being coated with at least one HPMCAS of claim 1 .

13. A capsule shell comprising at least one HPMCAS of claim 1 .

Assignees

• Dow Global Technologies Llc

Inventors

• Brackhagen Meinolf
• Guillaudeu Steven J
• Grasman Nicholas S
• Petermann Oliver
• Schmitt Robert L
• Sprehe Matthias

Classifications

• A61K9/4891

  Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004) · CPC title

• A61K9/2866

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

• A61K47/38 Primary

  Cellulose; Derivatives thereof · CPC title

• C08B13/00

  Preparation of cellulose ether-esters · CPC title