Bioerodible poly (orthoesters) from dioxolane-based diketene acetals
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/335
A61F-002/00
출원번호
US-0330781
(2002-12-24)
발명자
/ 주소
Ng, Steven Y.
Heller, Jorge
출원인 / 주소
AP Pharma, Inc.
대리인 / 주소
Heller Ehrman White & McAuliffe LLP
인용정보
피인용 횟수 :
13인용 특허 :
129
초록
Bioerodible poly(orthoesters) useful as orthopedic implants or vehicles for the sustained delivery of pharmaceutical, cosmetic and agricultural agents contain hydrogen bonding groups and α-hydroxy acid-containing groups.
대표청구항▼
1. A pharmaceutical composition comprising:(a) an active agent; and(b) as a vehicle, a poly(orthoester) that is the product of a reaction between:(i) a diketene acetal of formula II:where:R is a bond, —(CH 2 ) a —, or —(CH 2 ) b —O—(CH 2 ) c —; where a
1. A pharmaceutical composition comprising:(a) an active agent; and(b) as a vehicle, a poly(orthoester) that is the product of a reaction between:(i) a diketene acetal of formula II:where:R is a bond, —(CH 2 ) a —, or —(CH 2 ) b —O—(CH 2 ) c —; where a is an integer of 1 to 10, and b and c are independently integers of 1 to 5; andL is hydrogen or a C 13 alkyl, and(ii) a polyol or mixture of polyols in which at least 0.1 mole percent of the total polyol content is a diol of the formula HO—R 1 —OH, whereR 1 is:where:p is an integer of 1 to 20;R 5 is hydrogen or C 1-4 alkyl; andR 6 is:where:s is an integer of 0 to 30;t is an integer of 2 to 200; andR 7 is hydrogen or C 1-4 alkyl. 2. The composition of claim 1 where the poly(orthoester) is of formula I:where:R is a bond, —(CH 2 ) a —, or —(CH 2 ) b —O—(CH 2 ) c —; where a is an integer of 1 to 10, and b and c are independently integers of 1 to 5;R* is a C 1-4 alkyl;n is an integer of at least 5; andA is R 1 , R 2 , R 3 , or R 4 , whereR 1 is:where:p is an integer of 1 to 20;R 5 is hydrogen or C 1-4 alkyl; andR 6 iswhere:s is an integer of 0 to 30;t is an integer of 2 to 200; andR 7 is hydrogen or C 1-4 alkyl;R 2 is:R 3 is:where:x is an integer of 0 to 30;y is an integer of 2 to 200;R 8 is hydrogen or C 1-4 alkyl;R 9 and R 10 are independently C 1-12 alkylene;R 11 is hydrogen or C 1-6 alkyl and R 12 is C 1-6 alkyl; or R 11 and R 12 together are C 3-10 alkylene; andR 4 is the residue of a diol containing at least one functional group independently selected from amide,imide, urea, and urethane groups;in which at least 0.1 mol % of the A units are R 1 . 3. The composition of claim 2 where n is about 5 to about 1000. 4. The composition of claim 2 where the poly(orthoester) comprises about 1 to about 50 mole percent of units in which A is R 1 . 5. The composition of claim 2 where p is 1 to 2. 6. The composition of claim 2 where R 5 is hydrogen or methyl. 7. The composition of claim 2 where the poly(orthoester) comprises up to about 20 mole percent of units in which A is R 2 . 8. The composition of claim 2 where the poly(orthoester) comprises about 60 to about 99.9 mole percent of units in which A is R 2 . 9. The pharmaceutical composition of claim 1 where the fraction of the active agent is from 1% to 60% by weight of the composition. 10. The pharmaceutical composition of claim 9 where the fraction of the active agent is from 5% to 30% by weight of the composition. 11. The pharmaceutical composition of claim 9 where the active agent is selected from anti-infectives, antiseptics, steroids, therapeutic polypeptides, anti-inflammatory agents, cancer chemotherapeutic agents, narcotics, local anesthetics, antiangiogenic agents, vaccines, antigens, DNA, and antisense oligonucleotides. 12. The pharmaceutical composition of claim 11 where the active agent is a therapeutic polypeptide. 13. The pharmaceutical composition of claim 11 where the active agent is a local anesthetic. 14. The pharmaceutical composition of claim 13 further comprising a glucocorticosteroid. 15. The pharmaceutical composition of claim 11 where the active agent is an antiangiogenic agent. 16. A method of treating a disease state treatable by controlled release local administration of an active agent, comprising locally administering a therapeutically effective amount of the active agent in the form of a pharmaceutical composition of claim 1. 17. The method of claim 16 where the active agent is selected from anti-infectives, antiseptics, steroids, therapeutic polypeptides, anti-inflammatory agents, cancer chemotherapeutic agents, narcotics, local anesthetics, antiangiogenic agents, vaccines, antigens, DNA, and antisense oligonucleotides. 18. A method of preventing or relieving local pain at a site in a mammal, comprising administering to the site a therapeutically effective amo unt of a local anesthetic in the form of a pharmaceutically acceptable composition of claim 1. 19. A device for orthopedic restoration or tissue regeneration comprising a poly(orthoester) that is the product of a reaction between:(i) a diketene acetal of formula II: where:R is a bond, —(CH 2 ) a —, or —(CH 2 ) b —O—(CH 2 ) c —; where a is an integer of 1 to 10, and b and c are independently integers of 1 to 5; andL is hydrogen or a C 1-3 alkyl, and(ii) a polyol or mixture of polyols in which at least 0.1 mole percent of the total polyol content is a diol of the formula HO—R 1 —OH, whereR 1 is: where:p is an integer of 1 to 20;R 5 is hydrogen or C 1-4 alkyl; andR 6 is: where:s is an integer of 0 to 30;t is an integer of 2 to 200; andR 7 is hydrogen or C 1-4 alkyl. 20. A bioerodible implant comprising a poly(orthoester) that is the product of a reaction between:(i) a diketene acetal of formula II: where:R is a bond, —(CH 2 ) a —, or —(CH 2 ) b —O—(CH 2 ) c —; where a is an integer of 1 to 10, and b and c are independently integers of 1 to 5; andL is hydrogen or a C 1-3 alkyl, and(ii) a polyol or mixture of polyols in which at least 0.1 mole percent of the total polyol content is a diol of the formula HO—R 1 —OH, whereR 1 is: where:p is an integer of 1 to 20;R 5 is hydrogen or C 1-4 alkyl; andR 6 is: where:s is an integer of 0 to 30;t is an integer of 2 to 200; andR 7 is hydrogen or C 1-4 alkyl.
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