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1. WO2011035261 - RECONSTITUTABLE REVERSE THERMAL GELLING POLYMERS

Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

[ EN ]

AMENDED CLAIMS

received by the International Bureau on 03 January 2011 (03.01.2011)

1. An AB-, ABA-, or BAB-block copolymer composition, said block copolymer comprising:

at least a first AB, ABA, or BAB blo'ck copolymer component comprising a first hydrophobic A-block and a first hydrophilic B-block, wherein the first hydrophobic A-block is a biodegradable polyester comprising at least 60% caprolactone and at least one second polyester-forming monomer, and the first hydrophilic B-block has a first average molecular weight and comprises polyethylene glycol;

at least a second AB, ABA, or BAB block copolymer component comprising a second hydrophobic A-block and a second hydrophilic B-block, wherein the second hydrophobic A-block comprises biodegradable polyester, and the second hydrophilic B-block has a second average molecular weight and comprises polyethylene glycol, wherein the second average molecular weight is different from the first average molecular weight;

wherein the block copolymer composition has a total weight average molecular weight from 1500 to 10,000 Daltons, a total A-block content of the composition from about 60 to 85% by weight, and a total B-block content of the composition from about 15% to 40% by weight, wherein the total weight average molecular weight of the B-block in the composition is from 300 to 2000 Daltons,

wherein the block copolymer composition is a powder or wax at room temperature, is capable of exhibiting reverse thermal gellation when formed as an aqueous polymer solution, and is capable of being converted into an aqueous polymer solution in less than thirty minutes by agitating without the use of additives or heat exceeding 60°C.

2. The block copolymer composition of claim 1, wherein the block copolymer composition is an aqueous polymer solution suitable for parenteral administration.

3. The block copolymer composition of claim 1, wherein the total A-block content of the composition ranges from 65 to 80% and the total B-block content of the composition ranges from 20 to 35%.

4. The block copolymer composition of claim 1, wherein the total A-block content of the composition ranges from 67 to 75% and the total B-block content of the composition ranges from 25 to 33%.

5. The block copolymer composition of claim 1, wherein the second polyester monomer comprises residues of at least one of D,L-lactide, D-lactide, L-lactide, D,L-lactic acid, D-lactic acid, L-lactic acid, glycolide, glycolic acid, ε-hydroxy hexonoic acid, γ-butyrolactone, γ-hydroxy butyric acid, δ-valerolactone, δ-hydroxy valeric acid, hydrooxybutyric acids, malic acid, or copolymers thereof.

6. The block copolymer composition of claim 1, wherein the biodegradable polyester of the first A-block comprises at least 85 % caprolactone.

7. The block copolymer composition of claim 1, wherein the total average molecular weight of the B-block in the composition is from 1200 to 1500 Daltons.

8. The block copolymer composition of claim 1, wherein the solid powder block copolymer composition is capable of forming said aqueous polymer solution in less than 30 minutes without exposure to additional agents or temperatures exceeding 60°C, is capable of exhibiting less than 5% swelling after 30 days of aqueous exposure, and is capable of releasing between about 10 to 15% of paclitaxel in five days and 15% to 20% of paclitaxel in 20 days.

9. The block copolymer composition of claim 8, wherein the drug content of said composition is between about 0.01 and 20% by weight.

10. A method for the administration of at least one drug to a warm blooded animal in a controlled release form which comprises:

(1) providing an AB-, ABA-, or BAB-block copolymer composition comprising: i) about 60 to 85% by weight of a biodegradable, hydrophobic A-block comprising a biodegradable polyester, wherein said A-block includes at least 60% caprolactone and at least one second polyester-forming monomer; and

ii) about 15 to 40% by weight of a biodegradable, hydrophilic B-block comprising a polyethylene glycol, wherein the molecular weight of the B-block is between 300 and 2000 Daltons, wherein the block copolymer composition is a powder or wax at room temperature, is capable of exhibiting reverse thermal gellation when formed as an aqueous polymer solution, and is capable of being converted into an aqueous polymer solution in less than thirty minutes by agitating without the use of additives or heat exceeding 60°C.

(2) forming an aqueous polymer solution of said powder or wax composition by combining the copolymer with water without exposing to heat exceeding 60°C; and

(3) administering said aqueous polymer solution to said warm blooded animal.

1 1. The method of claim 10, wherein said aqueous polymer solution is suitable for parenteral administration.

12. The method of claim 10, wherein said copolymer forms a gel upon administering to said warm blooded animal.

13. The method of claim 10, wherein said aqueous polymer solution comprises a drug.

14. The method of claim 13, wherein the drug content of said aqueous polymer solution is between about 0.01 and 20% by weight.

15. A method of making a powder or wax block copolymer composition which comprises:

(1) providing an ABA-block copolymer composition comprising:

i) about 60 to 85% by weight of a biodegradable, hydrophobic A-block comprising a biodegradable polyester, wherein said A-block includes at least 60% caprolactone and at least one second polyester-forming monomer; and

ii) about 15 to 40% by weight of a biodegradable, hydrophilic B-block comprising a polyethylene glycol, wherein the molecular weight of the B-block is between 300 and 2000 Daltons,

(2) freeze drying said block copolymer to form the powder or wax block copolymer composition, wherein the powder or wax block copolymer composition is a solid at room temperature, is capable of exhibiting reverse thermal gellation when formed as an aqueous polymer solution, and is capable of being converted into an aqueous polymer solution in less than thirty minutes by agitating without the use of additives or heat exceeding 60°C.