Pharmaceutical compositions with enhanced performance and improved processability

• US 9,492,550 B2
• Filed: 02/21/2014
• Issued: 11/15/2016
• Est. Priority Date: 03/01/2013
• Status: Active Grant

• Current Assignee: Hercules, LLC (Ashland Global Holdings, Inc.)
• Original Assignee: Hercules, LLC (Ashland Global Holdings, Inc.)
• Inventors: Brugel, Todd A., Nguyen, Tuyen T., Sahoo, Sangrama, Tewari, Divya, Zong, Yuda
• Primary Examiner(s): GOON, SCARLETT Y
• Application Number:
  US14/186,147
• Publication Number:
  US 20140249235A1
• Time in Patent Office: 998 Days
• Field of Search: 424/484, 424/488, 514/781, 536/69
• US Class Current: 1/1
• CPC Class Codes: A61K 31/397 having four-membered rings, e.g. azetidine
• CPC Class Codes: A61K 31/4418 having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: C08B 13/00 Preparation of cellulose ether-esters
• CPC Class Codes: C08L 1/32 Cellulose ether-esters

Abstract

The presently disclosed and claimed inventive concept(s) relates to a polymer for enhancing drug performance and improving processability. Specifically, the polymer comprises hydroxypropyl methyl cellulose acetate succinate (HPMC-AS). On the HPMC-AS, the percentage of total succinoyl degree of substitution is less than 12% at C6-OH position and greater than 53% at C3-OH, and the percentage of total acetyl degree of substitution is greater than 32% at C6-OH position.

Claims

1. A polymer for enhancing drug performance and improving processability, wherein the polymer is hydroxypropyl methyl cellulose acetate succinate having:

a percentage of a total degree of substitution (DS) of succinoyl less than or equal to 6% at a C6-OH position (%C₆DS_Suc≦

6%) and from 58% to 84% at a C3-OH position (58% <

%C₃DS_Suc<

84%), and

a percentage of a total DS of acetyl from 33% to 51% at a C6-OH position (33%<

%C₆DS_Ac<

51%) and from 16% to 20% at the C3-OH position (16%<

%C₃DS_Ac<

20%).

2. A composition comprising a drug and a polymer, wherein the polymer is hydroxypropyl methyl cellulose acetate succinate having:

a percentage of a total degree of substitution (DS) of succinoyl less than or equal to 6% at a C6-OH position (%C₆DS_Suc≦

6%) and from 58% to 84% at a C3-OH position (58%<

%C₃DS_Suc<

84%), and

a percentage of a total DS of acetyl from 33% to 51% at a C6-OH position (33%<

%C₆DS_Ac<

51%) and from 16% to 20% at the C3-OH position (16% <

%C₃DS_Ac<

20%).

3. The composition of claim 2, wherein the drug is a low-solubility drug having a solubility equal to or less than about 0.5 mg/mL in an aqueous solution at a pH from 1 to 8.

4. The composition of claim 3, wherein the composition comprises a solid amorphous dispersion comprising the low-solubility drug and the polymer.

5. The composition of claim 3, wherein the composition comprises a physical mixture of the low-solubility drug and the polymer.