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:
bupivacaine base or salt thereof in an amount ranging from 2 wt % to 20 wt % of the composition; and
a viscous gel comprising:
40 wt % to 70 wt %, based on weight of the viscous gel, of a polyorthoester having a weight average molecular weight ranging from 3000 to 10,000, and
30 wt % to 60 wt %, based on weight of the viscous gel, of a solvent comprising triacetin and dimethyl sulfoxide.
2. The composition of claim 1 , wherein the bupivacaine base or salt thereof consists of bupivacaine base.
3. The composition of claim 1 , wherein the polyorthoester has a weight average molecular weight ranging from 4000 to 8000.
4. The composition of claim 2 , wherein the polyorthoester has a weight average molecular weight ranging from 4000 to 8000.
5. The composition of claim 1 , wherein the viscous gel comprises the polyorthoester in an amount ranging from 40 wt % to 65 wt %, based on weight of the viscous gel.
6. The composition of claim 2 , wherein the viscous gel comprises the polyorthoester in an amount ranging from 40 wt % to 65 wt %, based on weight of the viscous gel.
7. The composition of claim 3 , wherein the viscous gel comprises the polyorthoester in an amount ranging from 40 wt % to 65 wt %, based on weight of the viscous gel.
8. The composition of claim 4 , wherein the viscous gel comprises the polyorthoester in an amount ranging from 40 wt % to 65 wt %, based on weight of the viscous gel.
9. A method of administering bupivacaine base or salt thereof, comprising administering to a subject the composition of claim 1 .
10. A method of administering bupivacaine base, comprising administering to a subject the composition of claim 2 .
11. The composition of claim 1 , wherein the viscous gel comprises the solvent in an amount ranging from 40 wt % to 60 wt %, based on weight of the viscous gel.
12. The composition of claim 2 , wherein the viscous gel comprises the solvent in an amount ranging from 40 wt % to 60 wt %, based on weight of the viscous gel.
13. The composition of claim 3 , wherein the viscous gel comprises the solvent in an amount ranging from 40 wt % to 60 wt %, based on weight of the viscous gel.
14. The composition of claim 4 , wherein the viscous gel comprises the solvent in an amount ranging from 40 wt % to 60 wt %, based on weight of the viscous gel.
15. A method of administering bupivacaine base or salt thereof, comprising administering to a subject the composition of claim 3 .
16. A method of administering bupivacaine base, comprising administering to a subject the composition of claim 4 .
17. A method of administering bupivacaine base or salt thereof, comprising administering to a subject the composition of claim 5 .
18. A method of administering bupivacaine base, comprising administering to a subject the composition of claim 6 .
19. A method of administering bupivacaine base or salt thereof, comprising administering to a subject the composition of claim 7 .
20. A method of administering bupivacaine base, comprising administering to a subject the composition of claim 8 .