Short duration depot formulations

Patent metadata

Field	Value
Publication number	US-10201496-B2
Application number	US-201615267070-A
Country	US
Kind code	B2
Filing date	Sep 15, 2016
Priority date	Jun 25, 2002
Publication date	Feb 12, 2019
Grant date	Feb 12, 2019

Abstract

Methods and compositions for systemically or locally administering by implantation a beneficial agent to a subject are described, and include, for example, depot gel compositions that can be injected into a desired location and which can provide controlled release of a beneficial agent over a short duration of time. The compositions include a low molecular weight biocompatible polymer, a biocompatible solvent having low water miscibility that forms a viscous gel with the polymer and limits water uptake by the implant, and a beneficial agent.

First claim

We claim:

1. A composition comprising:
(a) a polyorthoester having a weight average molecular weight ranging from about 3000 to about 10,000;
(b); and
(c) bupivacaine base or pharmaceutically acceptable salt thereof in an amount ranging from about 1 wt % to about 20 wt % of the composition,
wherein the ratio of polyorthoester to triacetin ranges from about 40:60 to about 75:25.

2. The composition of claim 1 , wherein the bupivacaine base or pharmaceutically acceptable salt thereof comprises bupivacaine base.

3. The composition of claim 1 , wherein the polyorthoester has a weight average molecular weight ranging from about 4000 to about 8000.

4. The composition of claim 2 , wherein the polyorthoester has a weight average molecular weight ranging from about 4000 to about 8000.

5. The composition of claim 1 , wherein the bupivacaine base or pharmaceutically acceptable salt thereof is present in an amount ranging from about 2 wt % to about 20 wt % of the composition.

6. The composition of claim 2 , wherein the bupivacaine base or pharmaceutically acceptable salt thereof is present in an amount ranging from about 2 wt % to about 20 wt % of the composition.

7. The composition of claim 3 , wherein the bupivacaine base or pharmaceutically acceptable salt thereof is present in an amount ranging from about 2 wt % to about 20 wt % of the composition.

8. The composition of claim 4 , wherein the bupivacaine base or pharmaceutically acceptable salt thereof is present in an amount ranging from about 2 wt % to about 20 wt % of the composition.

9. The composition of claim 1 , wherein the ratio of polyorthoester to triacetin ranges from about 50:50 to about 75:25.

10. The composition of claim 2 , wherein the ratio of polyorthoester to triacetin ranges from about 50:50 to about 75:25.

11. The composition of claim 3 , wherein the ratio of polyorthoester to triacetin ranges from about 50:50 to about 75:25.

12. The composition of claim 4 , wherein the ratio of polyorthoester to triacetin ranges from about 50:50 to about 75:25.

13. The composition of claim 5 , wherein the ratio of polyorthoester to triacetin ranges from about 50:50 to about 75:25.

14. The composition of claim 6 , wherein the ratio of polyorthoester to triacetin ranges from about 50:50 to about 75:25.

15. The composition of claim 7 , wherein the ratio of polyorthoester to triacetin ranges from about 50:50 to about 75:25.

16. The composition of claim 8 , wherein the ratio of polyorthoester to triacetin ranges from about 50:50 to about 75:25.

Assignees

• Durect Corp

Inventors

• Chen Guohua
• Priebe David T

Classifications

• A61P23/02

  Local anaesthetics · CPC title

• A61P23/00

  Anaesthetics · CPC title

• A61K47/34

  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) · CPC title

• A61K38/27

  Growth hormone [GH], i.e. somatotropin · CPC title

• A61K9/0014

  Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00) · CPC title