Claims for Patent: 9,914,802

Summary for Patent: 9,914,802

Title:	Sustained release polymer
Abstract:	A polymer and a method for its preparation are provided. The polymer comprises poly(lactide), poly(lactide/glycolide) or poly(lactic acid/glycolic acid) segments bonded by ester linkages to both ends of an alkanediol core unit. The polymer is for use in a controlled release formulation for a medicament, preferably leuprolide acetate. The controlled release formulation is administered to a patient as a subcutaneous depot of a flowable composition comprising the polymer, a biocompatible solvent, and the medicament. Controlled release formulations comprising the polymer release leuprolide for treatment of prostate cancer patients over periods of 3-6 months.
Inventor(s):	Dunn; Richard L. (Fort Collins, CO)
Assignee:	Tolmar Therapeutics, Inc. (Fort Collins, CO)
Application Number:	15/695,789
Patent Claims:	1. A method of treatment of prostate cancer in a human male patient, comprising administering to the patient a flowable controlled release composition, wherein the flowable controlled release composition comprises: a. an organic solvent, b. a medicament selected from the group consisting of leuprolide and pharmaceutically acceptable salts thereof, and c. a biodegradable polymer comprising polymer segments selected from the group consisting of 85/15 poly(lactide/glycolide) (PLG) copolymer segments and 85/15 poly(lactic acid/glycolic acid) (PLGA) copolymer segments, wherein the polymer has substantially no titratable carboxylic acid groups and is hydroxyl-terminated at the distal ends of the polymer; and wherein the composition when administered once per about six months reduces the serum testosterone level of the patient to 20 ng/dL or lower. 2. The method of treatment of prostate cancer of claim 1, wherein the biodegradable polymer is 85/15 poly (DL-lactide-co-glycolide). 3. The method of treatment of prostate cancer of claim 1, wherein the organic solvent is a polar, aprotic organic solvent having at least some water solubility. 4. The method of treatment of prostate cancer of claim 1, wherein the step of administering comprises injecting the flowable controlled release composition subcutaneously into the patient to form a depot. 5. A method of preparing a controlled release formulation for the reduction of serum testosterone in a patient and formulated for administration once per about six months, comprising combining: a. an organic solvent, b. a medicament selected from the group consisting of leuprolide and pharmaceutically acceptable salts thereof, and c. a biodegradable polymer comprising polymer segments selected from the group consisting of 85/15 poly(lactide/glycolide) (PLG) copolymer segments and 85/15 poly(lactic acid/glycolic acid) (PLGA) copolymer segments, wherein the polymer has substantially no titratable carboxylic acid groups and is hydroxyl-terminated at the distal ends of the polymer. 6. The method of preparing a controlled release formulation of claim 5, wherein the step of combining comprises combining the organic solvent and the biodegradable polymer to form a polymer solution and combining the polymer solution and the medicament to form the controlled release formulation. 7. A method to reduce serum testosterone levels in a human patient, comprising administering a composition subcutaneously to the human patient, the composition comprising: a. a biodegradable polymer comprising polymer segments selected from the group consisting of 85/15 poly(lactide/glycolide) (PLG) copolymer segments and 85/15 poly(lactic acid/glycolic acid) (PLGA) copolymer segments, wherein the polymer has substantially no titratable carboxylic acid groups and is hydroxyl-terminated at the distal ends of the polymer; b. an organic solvent; and c. a medicament selected from the group consisting of leuprolide and pharmaceutically acceptable salts thereof; and wherein the composition when administered once per about six months reduces the serum testosterone level of the patient is reduced to 20 ng/dL or lower. 8. The method to reduce serum testosterone levels in a human patient of claim 7, wherein the biodegradable polymer is 85/15 poly (DL-lactide-co-glycolide). 9. A syringe comprising a flowable composition consisting essentially of: a. a biodegradable polymer comprising polymer segments selected from the group consisting of 85/15 poly(lactide/glycolide) (PLG) copolymer segments and 85/15 poly(lactic acid/glycolic acid) (PLGA) copolymer segments and the polymer has substantially no titratable carboxylic acid groups and is hydroxyl-terminated at the distal ends of the polymer, b. an organic solvent, and c. leuprolide or a pharmaceutically acceptable salt thereof wherein the composition when administered once per about six months reduces the serum testosterone level of a patient to 20 ng/dL or lower. 10. The syringe comprising a flowable composition of claim 9, wherein the organic solvent is selected from the group consisting of N-methylpyrrolidone, N,N-dimethylformamide, N,N-dimethylacetamide, triacetin, propylene carbonate, and ethyl acetate.