# US 2017/0281618 A1 · Injectable flowable composition comprising buprenorphine

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- Number: US 2017/0281618 A1
- Document ID: US20170281618A1
- Status: Published application
- Kind: A1
- Application number: 15/623,191
- Filed: 2017-06-14
- Published: 2017-10-05
- Earliest claimed: 2010-06-08
- Assignees: Indivior UK Limited
- Applicants: Indivior UK Limited
- Inventors: Richard L. Norton; Andrew Watkins; Mingxing Zhou
- Web page: https://patentgrep.com/patent/US20170281618A1

## CPC

- G06F 3/0659: {Command handling arrangements, e.g. command buffers, queues, command scheduling}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0024: {Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L)}
- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/4748: forming part of bridged ring systems (strychnine A61K31/475; morphinan derivatives A61K31/485)
- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- G06F 3/061: {Improving I/O performance}
- G06F 3/0689: {Disk arrays, e.g. RAID, JBOD}
- G06F 9/4881: {Scheduling strategies for dispatcher, e.g. round robin, multi-level priority queues}
- G06F 16/113: {Details of archiving (lifecycle management in storage systems G06F3/0649; point-in-time backing up or restoration of persistent data G06F11/1446)}
- G06F: ELECTRIC DIGITAL DATA PROCESSING (computer systems based on specific computational models G06N)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis.

## Claims

### Claim 1

An injectable composition comprising: (i) 8 wt % to 30 wt % of buprenorphine in the form of a free base or a pharmaceutically acceptable salt; (ii) 20 wt % to 70 wt % of a poly(DL-lactide-co-glycolide) copolymer; and (iii) 30 wt % to 70 wt % of N-methyl-2-pyrrolidone; wherein the composition is transformed in situ into an implant by contact with a bodily fluid.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the composition comprises from 3 milligrams to about 300 milligrams of buprenorphine in the form of the free base or the pharmaceutically acceptable salt.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the polymer is a 50/50 poly (DL-lactide-co-glycolide) copolymer.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the poly(DL-lactide-co-glycolide) copolymer has an average molecular weight from 5,000 Daltons to 40,000 Daltons.

### Claim 5

An injectable composition consisting of: (i) 8 wt % to 30 wt % of buprenorphine in the form of a free base or a pharmaceutically acceptable salt; (ii) 20 wt % to 70 wt % of a poly(DL-lactide-co-glycolide) copolymer; and (iii) 30 wt % to 70 wt % of N-methyl-2-pyrrolidone; wherein the composition is transformed in situ into an implant by contact with a bodily fluid.

### Claim 6 (depends on 5)

The composition of claim 5, wherein the poly(DL-lactide-co-glycolide) copolymer is a 50/50 poly(DL-lactide-co-glycolide) copolymer.

### Claim 7 (depends on 5)

The composition of claim 5, wherein the poly(DL-lactide-co-glycolide) copolymer has an average molecular weight from 5,000 Daltons to 40,000 Daltons.

### Claim 8 (depends on 5)

The composition of claim 5, wherein the composition comprises from 3 milligrams to about 300 milligrams of buprenorphine in the form of a free base or pharmaceutically acceptable salt.

### Claim 9 (depends on 5)

The composition of claim 5, wherein poly(DL-lactide-co-glycolide) copolymer is a 50/50, 55/45, 60/40, 65/35, 70/30, 75/25, 80/20, 85/15, 90/10, or 95/5 poly(DL-lactide-co-glycolide) copolymer.

### Claim 10

An injectable composition comprising: (i) 8 wt % to 30 wt % of buprenorphine in the form of a free base or a pharmaceutically acceptable salt; (ii) 20 wt % to 70 wt % of a poly(DL-lactide-co-glycolide) copolymer; and (iii) 30 wt % to 70 wt % of N-methyl-2-pyrrolidone.

### Claim 11 (depends on 1)

A method for treating opioid dependency in a patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of the composition of claim 1 to treat the opioid dependency.

### Claim 12 (depends on 5)

A method for treating opioid dependency in a patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of the composition of claim 5 to treat the opioid dependency.

### Claim 13 (depends on 10)

A method for treating opioid dependency in a patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of the composition of claim 10 to treat the opioid dependency.

### Claim 14

An injectable composition consisting of: (i) 8 wt % to 30 wt % of buprenorphine in the form of a free base or a pharmaceutically acceptable salt; (ii) 20 wt % to 70 wt % of a poly(DL-lactide-co-glycolide) copolymer; and (iii) 30 wt % to 70 wt % of N-methyl-2-pyrrolidone.

### Claim 15 (depends on 14)

A method for treating opioid dependency in a patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of the composition of claim 14 to treat the opioid dependency.

### Claim 16 (depends on 1)

The composition of claim 1, wherein the buprenorphine is in the form of the free base.

### Claim 17 (depends on 5)

The composition of claim 5, wherein the buprenorphine is in the form of the free base.

### Claim 18 (depends on 17)

The composition of claim 17, wherein the composition comprises from 3 milligrams to about 300 milligrams of the buprenorphine.

### Claim 19 (depends on 10)

The composition of claim 10, wherein the buprenorphine is in the form of the free base.

### Claim 20 (depends on 10)

The composition of claim 10, wherein the poly(DL-lactide-co-glycolide) copolymer is a 50/50 poly(DL-lactide-co-glycolide) copolymer.

### Claim 21 (depends on 14)

The composition of claim 14, wherein the buprenorphine is in the form of the free base.

### Claim 22 (depends on 21)

The composition of claim 21, wherein the composition comprises from 3 milligrams to about 300 milligrams of the buprenorphine.

### Claim 23 (depends on 14)

The composition of claim 14, wherein the poly(DL-lactide-co-glycolide) copolymer is a 50/50 poly(DL-lactide-co-glycolide) copolymer.

### Claim 24 (depends on 11)

The method of claim 11, comprising subcutaneously administering the composition to the patient once per month.

### Claim 25 (depends on 12)

The method of claim 12, comprising subcutaneously administering the composition to the patient once per month.

### Claim 26 (depends on 13)

The method of claim 13, comprising subcutaneously administering the composition to the patient once per month.

### Claim 27 (depends on 15)

The method of claim 15, comprising subcutaneously administering the composition to the patient once per month.

### Claim 28

An injectable composition comprising: (i) 8 wt % to about 22 wt % of buprenorphine free base; (ii) 25 wt % to 50 wt % of a poly(DL-lactide-co-glycolide) copolymer having an average molecular weight of about 5,000 Daltons to about 40,000 Daltons; and (iii) 30 wt % to 70 wt % of N-methyl-2-pyrrolidone.

### Claim 29 (depends on 28)

The composition of claim 28, wherein the composition is transformed in situ into an implant by contact with a bodily fluid.

### Claim 30 (depends on 28)

The composition of claim 28, wherein the polymer is a 50/50 poly(DL-lactide-co-glycolide) copolymer.

### Claim 31 (depends on 28)

The composition of claim 28, wherein the polymer has an average molecular weight of 5,000 Daltons to 40,000 Daltons.

### Claim 32 (depends on 28)

The composition of claim 28, wherein the polymer has a carboxy terminal group.

### Claim 33 (depends on 28)

The composition of claim 28, wherein the weight ratio of buprenorphine to polymer is between about 0.01:1 and about 2:1.

### Claim 34 (depends on 28)

A method for treating opioid dependency in a patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of the composition of claim 28 to treat the opioid dependency.

### Claim 35 (depends on 34)

The method of claim 34, comprising subcutaneously administering the composition to the patient once per month.

### Claim 36 (depends on 28)

The composition of claim 28, wherein the composition comprises from 3 milligrams to about 300 milligrams of the buprenorphine.