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Claims for Patent: 5,656,297

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Claims for Patent: 5,656,297

Title: Modulated release from biocompatible polymers
Abstract:The present invention relates to a composition for the modulated release of a biologically active agent. The composition comprises a biocompatible polymeric matrix, a biologically active agent which is dispersed within the polymeric matrix, and a metal cation component which is separately dispersed within the polymeric matrix, whereby the metal cation component modulates the release of the biologically active agent from the polymeric matrix. The present invention also relates to a method for modulating the release of a biologically active agent from a biocompatible polymeric matrix, comprising the steps of dissolving a biocompatible polymer in a solvent to form a polymer solution and also separately dispersing a metal cation component and a biologically active agent within the polymer solution. The polymer solution is then solidified to form a polymeric matrix, wherein at least a significant portion of the metal cation component is dispersed in the polymeric matrix separately from the biologically active protein, and whereby the metal cation component modulates the release of the biologically active agent from the polymeric matrix.
Inventor(s): Bernstein; Howard (Cambridge, MA), Zhang; Yan (Cambridge, MA), Khan; M. Amin (Downingtown, PA), Tracy; Mark A. (Arlington, MA)
Assignee: Alkermes Controlled Therapeutics, Incorporated (Cambridge, MA)
Application Number:08/237,057
Patent Claims: 1. A pharmaceutical composition for the modulated release of a biologically active pharmaceutical agent, comprising:

a) a biocompatible and biodegradable polymeric matrix;

b) an effective amount of a biologically active pharmaceutical agent, the biologically active pharmaceutical agent being dispersed within the polymeric matrix; and

c) a metal cation component for modulating release of the biologically active agent from the polymeric matrix, wherein the metal cation component comprises a cation selected from the group consisting of Zn(II), Mg(II) and a combination of at least two different multivalent metal cations, and wherein the metal cation component is separately dispersed within the polymeric matrix.

2. A modulated release composition of claim 1 wherein said metal cation component is selected from the group consisting of magnesium hydroxide, magnesium carbonate, zinc carbonate, magnesium acetate, zinc acetate, magnesium chloride, zinc chloride, magnesium sulfate, zinc sulfate, magnesium citrate and zinc citrate.

3. A composition for the modulated release of a biologically active pharmaceutical agent, comprising:

a) a biocompatible and biodegradable polymeric matrix;

b) an effective amount of a biologically active pharmaceutical agent, the biologically active pharmaceutical agent being dispersed within the polymeric matrix; and

c) a metal cation component for modulating the release of the biologically active agent from the polymeric matrix, wherein said metal cation component is selected from the group consisting of magnesium hydroxide, magnesium carbonate, calcium carbonate, zinc carbonate, magnesium acetate, zinc acetate, magnesium chloride, zinc chloride, magnesium sulfate, zinc sulfate, magnesium citrate and zinc citrate, and wherein the metal cation component is separately dispersed within the polymeric matrix.

4. A method for significantly stabilizing the glass transition temperature for a polymeric matrix during hydration, comprising the steps of:

a) forming a solution of a polymer;

b) dispersing a metal cation component into said polymer solution; and

c) solidifying said polymer from said polymer solution to form a polymeric matrix, containing the metal cation component dispersed therein, thereby stabilizing the glass transition temperature for a polymeric matrix during hydration.

5. A method for enhancing the initial hydration capacity of a polymeric matrix without significant polymer degradation, comprising the steps of:

a) forming a solution of a biodegradable polymer in a solvent;

b) dispersing a metal cation component within said polymer solution; and

c) solidifying said polymer from said polymer solution to form a polymeric matrix, containing the metal cation component dispersed therein, thereby enhancing the initial hydration capacity of a polymeric matrix without significant polymer degradation.

6. A method for increasing the porosity of a polymeric matrix, comprising the steps of:

a) forming a solution of a polymer and a solvent;

b) dispersing a metal cation component within said polymer solution;

c) solidifying said polymer from said polymer solution, to form a polymeric matrix containing the metal cation component dispersed therein; and

d) hydrating said polymeric matrix to thereby form at least one gap within said polymeric matrix, thereby increasing the porosity of said polymeric matrix.

7. A modulated release composition of claim 3 wherein said biodegradable and biocompatible polymer is selected from the group consisting of poly(lactide) s, poly(glycolide) s, poly(lactide-co-glycolide)s, polyanhydrides, polyorthoesters, polyetheresters, polycaprolactone, polyesteramides, blends and copolymers thereof.

8. A composition for the modulated release of a biologically active protein, comprising:

a) a biocompatible polymeric matrix;

b) an effective amount of a biologically active protein, the biologically active protein being dispersed within the polymeric matrix; and

c) a metal cation component for modulating release of the biologically active protein from the polymeric matrix, wherein the metal cation component comprises a cation selected from the group consisting of Zn(II), Mg(II) and a combination of at least two different multivalent metal cations, and wherein the metal cation component is separately dispersed within the polymeric matrix.

9. A modulated release composition of claim 8 wherein said polymer is biodegradable.

10. A modulated release composition of claim 7 wherein said biologically active agent comprises a protein.

11. A modulated release composition of claim 10 wherein said protein is selected from the group consisting of nucleases, erythropoietin, human growth hormone, interferons, interleukins, growth factors, tumor necrosis factor, adrenocorticotropic hormone, and colony-stimulating factors.

12. A method for modulating the release of a biologically active agent from a polymeric matrix, comprising:

a) dissolving a biocompatible polymer in a solvent to form a polymer solution;

b) dispersing a metal cation component in said solvent, wherein the metal cation component comprises a metal cation selected from the group consisting of Zn(II), Mg(II) and a combination of at least two different multivalent metal cations;

c) separately dispersing a biologically active agent in said polymer solution; and

d) solidifying said polymer from said polymer solution to form a polymeric matrix, whereby the metal cation component modulates the release of the biologically active agent from the polymeric matrix.

13. A composition for the modulated release of a biologically active agent, comprising:

a) a biocompatible polymeric matrix of a polymer selected from the group consisting of poly(lactide)s, poly(glycolide)s, poly(lactide-co-glycolide)s and blends thereof;

b) an effective amount of a biologically active protein, said biologically active protein being dispersed within the polymeric matrix; and

c) a metal cation component for modulating release of the biologically active agent from the polymeric matrix, wherein said metal cation component is selected from the group consisting of magnesium hydroxide, magnesium carbonate, calcium carbonate, zinc carbonate, magnesium acetate, zinc acetate, magnesium sulfate, zinc sulfate, magnesium chloride, zinc chloride, zinc citrate and magnesium citrate, and wherein the metal cation component is separately dispersed within the polymeric matrix.

14. A modulated release composition of claim 13 wherein said biologically active protein is selected from the group consisting of nucleases, erythropoietin, human growth hormone, interferons, interleukins, growth factors, adrenocorticotropic hormone, tumor necrosis factor and colony-stimulating factors.

15. A method of claim 12, further comprising the step of suspending particles of said metal cation component in a second solvent before dispersing the metal cation component in the polymer solution, wherein the second solvent is miscible with said first solvent, and wherein said polymer is soluble in the second solvent.

16. A method for modulating the release of a biologically active agent from a polymeric matrix, comprising:

a) dissolving a biocompatible polymer in a solvent to form a polymer solution;

d) dispersing a metal cation component in said solvent wherein said metal cation component is selected from the group consisting of magnesium hydroxide, magnesium carbonate, calcium carbonate, zinc carbonate, magnesium acetate, zinc acetate, magnesium sulfate, zinc sulfate, magnesium chloride, zinc chloride, zinc citrate and magnesium citrate;

c) separately dispersing a biologically active agent in said polymer solution; and

d) solidifying said polymer from said polymer solution to form a polymeric matrix, whereby the metal cation component modulates the release of the biologically active agent from the polymeric matrix.

17. A method of claim 16 wherein said biologically active agent comprises a protein.

18. A method of claim 17 wherein said protein is selected from the group consisting of nucleases, erythropoietin, human growth hormone, interferons, interleukins, growth factors, adrenocorticotropic hormone, tumor necrosis factor and colony-stimulating factors.

19. A method of claim 18 wherein said polymer is biodegradable.

20. A method of claim 19 wherein said biodegradable polymer is selected from the group consisting of poly(lactide)s, poly(glycolide) s, poly(lactide-co-glycolide)s, polyanhydrides, polyorthoesters, polyetheresters, polycaprolactone, polyesteramides, blends and copolymers thereof.

21. A method of claim 18 wherein said polymer is non-biodegradable.

22. A method of claim 21 wherein said non-biodegradable polymer is selected from the group consisting of polyacrylates, polymers of ethylene-vinyl acetates, and acyl substituted cellulose acetates, non-degradable polyurethanes, polystyrenes, polyvinyl chloride, polyvinyl fluoride, poly(vinyl imidazole), chlorosulphonate polyolefins, polyethylene oxide, blends and copolymers thereof.

23. A method of claim 15, further comprising the step of dissolving said metal cation component in a second solvent before dispersing the metal cation component in the polymer solution, wherein the second solvent is miscible with the first solvent, and wherein said polymer is soluble in the second solvent.
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