Composition comprising highly-concentrated α1 proteinase inhibitor and method for obtaining thereof

Patent metadata

Field	Value
Publication number	US-11701412-B2
Application number	US-202117448509-A
Country	US
Kind code	B2
Filing date	Sep 22, 2021
Priority date	Aug 2, 2018
Publication date	Jul 18, 2023
Grant date	Jul 18, 2023

Abstract

Compositions include highly-concentrated Alpha-1 Proteinase Inhibitor (A1PI) in a concentration greater than or equal to 100 mg/ml. Pharmaceutical compositions can be prepared from these compositions. The pharmaceutical compositions can be suitable for subcutaneous administration. The highly-concentrated A1PI solutions can be obtained by single-pass tangential flow filtration (SPTFF).

First claim

What is claimed is:

1. A composition comprising Alpha1-Proteinase Inhibitor (A1PI) in an aqueous solution, wherein the concentration of A1PI is greater than 200 mg/ml, wherein the composition further comprises one or more uncharged excipient.

2. The composition of claim 1 , wherein further comprises one or more uncharged excipient.

3. The composition of claim 2 , wherein said one or more uncharged excipient is at a concentration to achieve an osmolality between 220 and 410 mOsm/kg H 2 O.

4. The composition of claim 3 , wherein said one or more uncharged excipient is at a concentration to achieve an osmolality of about 300 mOsm/kg H 2 O.

5. A pharmaceutical composition comprising the composition according to claim 1 and a pharmaceutically acceptable carrier.

6. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition is formulated for intravenous, subcutaneous, aerosol, or intradermal administration.

7. The pharmaceutical composition of claim 6 , wherein the pharmaceutical composition is formulated for subcutaneous administration.

8. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition is encapsulated in nanoparticles.

9. The pharmaceutical composition of claim 5 , wherein the pharmaceutical composition comprises a time-release polymer.

10. A method for preparing a composition according to claim 1 , comprising a step of preparing a solution of A1PI by concentrating an initial solution of A1PI by single-pass tangential flow filtration (SPTFF).

11. A method for preparing a composition according to claim 10 , wherein said step of SPTFF is carried out against water for injection (WFI).

12. A method for preparing a composition according to claim 10 , wherein after the SPTFF step the solution of A1PI is formulated with one or more uncharged excipients selected from the group consisting of sorbitol, serine, trehalose, alanine, sucrose, and mannitol, and combinations thereof.

13. A method for preparing a composition according to claim 12 , wherein after the SPTFF step the solution of A1PI is formulated with sorbitol, trehalose, alanine, or a combination thereof.

Assignees

• Grifols Worldwide Operations Ltd

Inventors

• Rebbeor James
• Miller Charles
• Klos Anthony
• Allgaier Eric
• Zimmerman Thomas P
• Wee Kevin
• StPETER MICHELLE
• Glancy Kelly

Classifications

• A61K38/57 Primary

  from animals; from humans {(A61K38/553, A61K38/556 take precedence)} · CPC title

• A61K47/183

  Amino acids, e.g. glycine, EDTA or aspartame · CPC title

• A61K9/08

  Solutions {(composition of solutions A61K47/00)} · CPC title

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · CPC title

• A61P1/16

  for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics · CPC title