Claims for Patent: 10,646,572

Summary for Patent: 10,646,572

Title:	Pharmaceutical compositions with enhanced stability
Abstract:	The present invention provides for a stabilized biodegradable polymeric composition useful as a controlled release delivery system for peptide agents. The compositions of the present invention comprise a) a beneficial salt of a luteinizing hormone releasing hormone (LHRH) analogue formed with a strong acid that minimizes or prevents the interaction/reaction between the LHRH and the polymer in an organic solution; b) a biodegradable polymer; c) a pharmaceutically acceptable organic solvent; and d) optionally one or more excipients. The present invention also relates to a method of manufacturing and a method of use thereof.
Inventor(s):	Li; Yuhua (Landenberg, PA), Chien; Benjamin (Woodside, CA)
Assignee:	Foresee Pharmaceuticals Co., Ltd. (Nankang Dist., Taipei, TW)
Application Number:	16/376,028
Patent Claims:	1. A pharmaceutical composition comprising: a) 4% to 40% by weight mesylate salt of leuprolide; b) a polymer selected from the group consisting of polylactide, poly(lactic acid), poly(lactic acid-co-glycolic acid), and poly(lactide-co-glycolide); and c) N-methyl-2-pyrrolidone (NMP). 2. The pharmaceutical composition of claim 1, wherein the polymer has a weight average molecular weight of about 2,000 to about 100,000 daltons. 3. The pharmaceutical composition of claim 1, wherein the composition comprises 30% to 70% by weight of the polymer. 4. The pharmaceutical composition of claim 1, wherein the composition comprises 30% to 80% by weight of N-methyl-2-pyrrolidone. 5. The pharmaceutical composition of claim 1, wherein the polymer comprises at least one of poly(lactide-co-glycolide) and poly(lactic acid-co-glycolic acid), having a monomer ratio of lactide:glycolide or lactic acid:glycolic acid of 50:50 to 100:0, respectively. 6. The pharmaceutical composition of claim 5, wherein the poly(lactide-co-glycolide) or poly(lactic acid-co-glycolic acid) has a monomer ratio of lactide:glycolide or lactic acid:glycolic acid of 80:20 to 90:10, respectively. 7. An injectable pharmaceutical composition comprising: a) 4% to 40% by weight mesylate salt of leuprolide; b) 40% to 60% by weight at least one polymer selected from the group consisting of poly (DL-lactide) and poly(DL-lactide-co-glycolide), and c) 30% to 80% by weight N-methyl-2-pyrrolidone (NMP), wherein the mesylate salt of leuprolide is formed before the salt is combined with the at least one polymer and the NMP. 8. The pharmaceutical composition of claim 7, wherein the polymer has a weight average molecular weight of about 2,000 to about 100,000 daltons. 9. The pharmaceutical composition of claim 8, wherein the at least one polymer is poly (DL-lactide). 10. The pharmaceutical composition of claim 8, wherein the at least one polymer is poly(DL-lactide-co-glycolide) having a monomer ratio of lactide:glycolide of 80:20 to 90:10. 11. A kit comprising a syringe comprising the pharmaceutical composition of claim 1. 12. A kit comprising a syringe comprising the injectable pharmaceutical composition of claim 7. 13. A kit comprising a syringe comprising the injectable pharmaceutical composition of claim 9. 14. A kit comprising a syringe comprising the injectable pharmaceutical composition of claim 10. 15. A method of forming an implant in a subject, comprising administering to the subject an effective amount of the pharmaceutical composition of claim 1. 16. The method of claim 15, wherein the pharmaceutical composition is administered to the subject subcutaneously, intramuscularly, Intrapentoneally, or Intradermally. 17. The method of claim 16, wherein the pharmaceutical composition is administered to fit into a body cavity of the subject to form a depot. 18. A method of forming an implant in a subject, comprising administering to the subject an effective amount of the injectable pharmaceutical composition of claim 7. 19. The method of claim 18, wherein the pharmaceutical composition is administered to the subject subcutaneously, intramuscularly, intraperitoneally, or intradermally. 20. The method of claim 19, wherein the pharmaceutical composition is administered to fit into a body cavity of the subject to form a depot.