Compositions of a polyorthoester and an aprotic solvent
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-047/34
A61K-047/10
A61K-031/439
A61K-047/22
A61K-047/20
출원번호
US-0269806
(2016-09-19)
등록번호
US-9913909
(2018-03-13)
발명자
/ 주소
Ottoboni, Thomas B.
Schillinger, Lee Ann Lynn
출원인 / 주소
Heron Therapeutics, Inc.
대리인 / 주소
McDermott Will & Emery LLP
인용정보
피인용 횟수 :
0인용 특허 :
18
초록▼
Delivery systems and compositions comprised of a biodegradable polyorthoester polymer, an aprotic solvent, and a drug are described. The solvent is selected to modulate release of drug from the composition, where, in some embodiments, the solvent is rapidly released after administration and provides
Delivery systems and compositions comprised of a biodegradable polyorthoester polymer, an aprotic solvent, and a drug are described. The solvent is selected to modulate release of drug from the composition, where, in some embodiments, the solvent is rapidly released after administration and provides a corresponding rapid rate of drug release. Alternatively, in other embodiments, the solvent is slowly released from the composition after its administration, and provides a correspondingly slow rate of drug release.
대표청구항▼
1. A method of administering a therapeutically active agent to a subject in need thereof, comprising: dispensing and administering to the subject a delivery system, wherein the delivery system comprises:a polyorthoester of Formula III; whereA is R1 or R3,R* is C1-4 alkyl,n ranges from 5 to 1000,R1 i
1. A method of administering a therapeutically active agent to a subject in need thereof, comprising: dispensing and administering to the subject a delivery system, wherein the delivery system comprises:a polyorthoester of Formula III; whereA is R1 or R3,R* is C1-4 alkyl,n ranges from 5 to 1000,R1 is: p and q are integers that vary from between about 1 to 20 and the average number of p or the average of the sum of p and q is between 1 and 7;R3 and R6 are each independently: x is an integer of 1-4;R5 is H or methyl, andthe fraction of A units that are of formula R1 is between 10-25 mole percent;an aprotic solvent in which the polyorthoester is miscible to form a single phase, wherein the aprotic solvent is selected from dimethyl sulfoxide, dimethyl acetamide, and N-methyl pyrrolidone; anda local amide- or anilide-type anesthetic dispersed or solubilized in the single phase,wherein the aprotic solvent is present in amounts ranging from about 10-25% by weight of the delivery system and the polyorthoester of formula III is present in amounts ranging from about 45-80% by weight of the delivery system. 2. A method of treating pain in a subject in need thereof, comprising: dispensing and administering to the subject a composition comprised of a therapeutically effective amount of a delivery system, wherein the delivery system comprises:a polyorthoester of Formula III; whereA is R1 or R3,R* is C1-4 alkyl,n ranges from 5 to 1000,R1 is: p and q are integers that vary from between about 1 to 20 and the average number of p or the average of the sum of p and q is between 1 and 7;R3 and R6 are each independently: x is an integer of 1-4;R5 is H or methyl, andthe fraction of A units that are of formula R1 is between 10-25 mole percent;an aprotic solvent in which the polyorthoester is miscible to form a single phase, wherein the aprotic solvent is selected from dimethyl sulfoxide, dimethyl acetamide, and N-methyl pyrrolidone; anda local amide- or anilide-type anesthetic dispersed or solubilized in the single phase. 3. The method of claim 2, wherein the method reduces or prevents pain in the subject. 4. The method of claim 2, wherein the administering comprises administering the composition locally. 5. The method of claim 4, wherein the administering comprises administering the composition intrathecally, at a nerve, into the epidural space, or to a surgical wound. 6. The method of claim 2, wherein the administering comprises administering the composition regionally. 7. The method of claim 6, wherein the administering comprises administering the composition as a nerve block or as a sensory block. 8. The method of claim 2, wherein the active agent is selected from the group consisting of bupivacaine, ropivacaine, levobupivacaine, dibucaine, mepivacaine, procaine, lidocaine, and tetracaine. 9. The method of claim 2, wherein the therapeutically active agent is bupivacaine. 10. The method of claim 2, wherein the therapeutically active agent is ropivacaine. 11. The method of claim 2, wherein the delivery system has a viscosity of less than about 10,000 cP at 37° C. 12. The method of claim 2, wherein the aprotic solvent is dimethyl sulfoxide. 13. The method of claim 1, wherein the method comprises dispensing the delivery system from a tube. 14. The method of claim 1, wherein the method comprises administering to the subject the delivery system in an amount effective to prevent or reduce pain. 15. The method of 1, wherein the aprotic solvent is dimethyl sulfoxide.
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이 특허에 인용된 특허 (18)
Ng, Steven Y.; Heller, Jorge, Bioerodible polyorthoesters containing amine groups.
Heller Jorge (Woodside CA) Ng Steve Y. W. (San Francisco CA) Penhale Donald W. H. (Menlo Park CA), Polymers containing acetal, carboxy-acetal, ortho ester and carboxyortho ester linkages.
Heller Jorge (Woodside CA) Ng Steve Y. W. (San Francisco CA) Penhale Donald W. H. (Menlo Park CA), Polymers containing carboxy-ortho ester and ortho ester linkages.
Heller Jorge (Palo Alto CA) Helwing Robert F. (Sunnyvale CA) Penhale Donald W. (Cupertino CA), Polymers of di- (and higher functionality) ketene acetals and polyols.
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