Compositions comprising buprenorphine

Patent metadata

Field	Value
Publication number	US-9295645-B2
Application number	US-201113703015-A
Country	US
Kind code	B2
Filing date	Jun 6, 2011
Priority date	Jun 8, 2010
Publication date	Mar 29, 2016
Grant date	Mar 29, 2016

Abstract

This disclosure relates to a buprenorphine sustained release delivery system for treatment of conditions ameliorated by buprenorphine compounds. The sustained release delivery system includes a flowable composition containing a suspension of buprenorphine, a metabolite, or a prodrug thereof.

First claim

The invention claimed is:

1. An injectable pharmaceutical composition comprising:
(a) 10 wt % to 20 wt % buprenorphine free base having an average particle size of less than 20 μm; and
(b) an aqueous solution comprising polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene (20) sorbitan monooleate, or a combination thereof; and a polyethylene glycol polymer;

wherein the buprenorphine free base is suspended in the aqueous solution, and wherein the composition does not comprise one or both of a polylactide and polyglycolide polymer.

2. The composition of claim 1 , wherein the buprenorphine free base has an average particle size of less than 10 μm.

3. The composition of claim 1 , wherein the aqueous solution comprises polyoxyethylene (20) sorbitan monolaurate and a polyethylene glycol polymer having a molecular weight between 1,000 and 10,000.

4. The composition of claim 1 , wherein the aqueous solution comprises polyoxyethylene (20) sorbitan monooleate and a polyethylene glycol polymer having a molecular weight between 1,000 and 10,000.

5. The composition of claim 1 , wherein the aqueous solution comprises polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene (20) sorbitan monooleate, and a polyethylene glycol polymer having a molecular weight between 1,000 and 10,000.

6. The composition of claim 1 , wherein the polyethylene glycol polymer has a molecular weight between 1,000 and 10,000.

7. The composition of claim 1 , wherein the aqueous solution further comprising a pharmaceutically acceptable salt, a pharmaceutically acceptable sugar, a preservative, or a combination of two or more thereof.

8. An injectable pharmaceutical composition comprising
(a) about 5 wt % to about 20 wt % of buprenorphine free base having an average particle size of less than 50 μm; and
(b) an aqueous solution comprising (i) polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene (20) sorbitan monooleate, a poloxamer, a phospholipid, or a combination thereof, and (ii) a polyethylene glycol polymer, a carboxymethylcellulose, a polyvinylpyrrolidone, a polyvinylalcohol, or a dextran;

wherein the buprenorphine free base is suspended in the aqueous solution, and wherein the composition does not comprise one or both of a polylactide and polyglycolide polymer.

9. The composition of claim 8 comprising about 10 wt % to about 20 wt % buprenorphine free base.

10. The composition of claim 8 , wherein the buprenorphine free base has an average particle size of less than 20 μm.

11. The composition of claim 8 , wherein the aqueous solution comprises (i) polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene (20) sorbitan monooleate, or a combination thereof, and (ii) a polyethylene glycol polymer.

12. The composition of claim 8 , wherein the aqueous solution further comprises a pharmaceutically acceptable salt, a pharmaceutically acceptable sugar, a preservative, or a combination of two or more thereof.

13. A pharmaceutical composition comprising buprenorphine or a pharmaceutically acceptable salt thereof, having an average particle size of less than 200 μm, suspended in an aqueous solution comprising a nonionic surfactant and a water-soluble polymer.

14. The composition of claim 13 , wherein the buprenorphine or the pharmaceutically acceptable salt thereof is present in an amount of about 10 wt % to about 20 wt %.

15. The composition of claim 13 , wherein the buprenorphine or the pharmaceutically acceptable salt thereof has an average particle size of is less than 100 μm.

16. The composition of claim 13 , wherein the buprenorphine is present as the free base (unprotonated) form.

17. The composition of claim 13 , wherein the buprenorphine is present as a pharmaceutically acceptable salt.

18. The composition of claim 13 , wherein the aqueous solution further comprises a pharmaceutically acceptable salt, a pharmaceutically acceptable sugar, a preservative, or a combination of two or more thereof.

19. The composition of claim 13 , wherein the nonionic surfactant is polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene (20) sorbitan monooleate, a poloxamer, a phospholipid, or a combination thereof.

20. The composition of claim 13 , wherein the water-soluble polymer is a polyethylene glycol polymer, a carboxymethylcellulose, a polyvinylpyrrolidone, a polyvinylalcohol, a dextran, or a combination of two or more thereof.

Assignees

• Norton Richard L
• Zhou Mingxing
• Indivior Uk Ltd

Inventors

• Norton Richard L
• Zhou Mingxing

Classifications

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61K47/26

  Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin · CPC title

• A61K47/02

  Inorganic compounds · CPC title

• A61K31/439

  the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46) · CPC title

• A61K9/10 Primary

  Dispersions; Emulsions · CPC title