Short duration depot formulations
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.
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.