Pastes for injection of a therapeutic agent
View Patent ↗Disclosed is a paste for injection of a therapeutic agent, the paste comprising an amount of powder comprising an effective amount of the therapeutic agent, wherein the powder is homogeneously contained within a pharmaceutically acceptable carrier, and wherein the paste comprises an injection volume of 0.1 to 3000 microliters.
1. A paste for injection of a therapeutic agent, said paste comprising an amount of powder comprising an effective amount of a therapeutic agent selected from a protein, peptide, polypeptide, vaccine, or small molecule, wherein said powder is homogeneously contained within a pharmaceutically acceptable carrier that is a non-solvent to the powder, and wherein said paste comprises an injection volume of 0.1 to 3000 microliters.
2. The paste of claim 1 , wherein said paste is a slurry.
3. The paste of claim 1 , wherein said therapeutic agent is a peptide.
4. The paste of claim 3 , wherein said peptide is glucagon.
5. The paste of claim 1 , wherein said therapeutic agent is a vaccine or small molecule.
6. The paste of claim 1 , wherein said powder is prepared by subjecting the therapeutic agent to lyophilization, spray-drying, freeze-drying, spray-freeze drying or a combination thereof prior to incorporation into said pharmaceutically acceptable carrier.
7. The paste of claim 6 , wherein said powder has a mean particle size ranging from 10 nanometers (0.01 microns) to about 100 microns, with no particles being larger than about 500 microns.
8. The paste of claim 1 , further comprising an effective amount of a stabilizing agent.
9. The paste of claim 8 , wherein said stabilizing agent is a member selected from the group consisting of surfactants, polyoxamers, polyols, gels, amphoteric compounds, and mixtures thereof.
10. The paste of claim 1 , wherein the protein, peptide, polypeptide, vaccine, or small molecule is stable in said paste for at least about 2 months when said paste is stored at room temperature.
11. The paste of claim 1 , wherein said pharmaceutically acceptable carrier is a non-aqueous or semi-aqueous carrier.
12. The paste of claim 11 , wherein said pharmaceutically acceptable carrier is a non-aqueous carrier.
13. The paste of claim 12 , wherein said non-aqueous carrier is a hydrophobic non-aqueous carrier.
14. The paste of claim 12 , wherein said pharmaceutically acceptable carrier is a mixture of at least two non-aqueous carriers.
15. The paste of claim 12 , wherein said pharmaceutically acceptable carrier is selected from the group consisting of alkyl benzoates, aryl benzoates, aralkyl benzoates, triacetin, dimethyl sulfoxide (DMSO), N-methyl-2-pyrrolidone (NMP), and mixtures thereof.
16. The paste of claim 1 , comprising an injection volume of 0.3 to 1.2 ml.
17. The paste of claim 1 , comprising an injection volume of 1 μl to 250 μl.
18. The paste of claim 1 , wherein said paste further comprises a pharmaceutically acceptable polymer that imparts thixotropic properties to said paste.
19. The paste of claim 1 , wherein said paste further comprises a pharmaceutically acceptable polymer in an amount effective to slow the release of said therapeutic agent from said paste upon injection.
20. The paste of claim 1 , wherein the protein, peptide, polypeptide, vaccine, or small molecule is incorporated into a liposome or conjugated to or incorporated with a polysaccharide or other another polymer to provide a controlled release of the protein, peptide, polypeptide, vaccine, or small molecule from said paste upon injection.