IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
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| 국제특허분류(IPC7판) |
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| 출원번호 |
US-0237387
(2002-09-09)
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발명자
/ 주소 |
- Chasin, Mark
- Goldenheim, Paul
- Sackler, Richard
- Tigner, Joseph
- Burch, Ronald M
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| 출원인 / 주소 |
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| 대리인 / 주소 |
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| 인용정보 |
피인용 횟수 :
121 인용 특허 :
114 |
초록
▼
A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obt
A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.
대표청구항
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1. A formulation for inducing sustained regional local anesthesia or analgesia in a patient comprising:a plurality of substrates in a pharmaceutically acceptable medium, said substrates comprising a local anesthetic and an effective amount of a biocompatible, biodegradable controlled release materia
1. A formulation for inducing sustained regional local anesthesia or analgesia in a patient comprising:a plurality of substrates in a pharmaceutically acceptable medium, said substrates comprising a local anesthetic and an effective amount of a biocompatible, biodegradable controlled release material comprising a polymer selected from the group consisting of polyanhydrides, copolymers of lactic acid and glycolic acid, poly(lactic) acid, poly(glycolic) acid, polyesters, polyorthoesters, proteins, polysaccharides and combinations thereof to provide a controlled release of said local anesthetic when said formulation is implanted or injected in a patient, said biocompatible, biodegradable controlled release material being capable of degrading at least fifty percent in less than two years following implantation or injection into the patient and prolonging the release of said local anesthetic from said substrates in-vitro, when measured using the United States Pharmacopeia/National Formulary Paddle Method II, said substrates being included in said formulation in an amount sufficient to obtain reversible local numbness and/or analgesia when said formulation is implanted or injected in a patient, and taxol in an amount effective to augment the local anesthetic, said taxol being (i) incorporated into and/or onto said substrates; or (ii) incorporated into said pharmaceutically acceptable medium, or (iii) incorporated into said substrates and also incorporated into said pharmaceutically acceptable medium. 2. The formulation of claim 1, wherein said substrates are microspheres.3. The formulation of claim 1, wherein said substrates are microcapsules.4. The formulation of claim 1, wherein at least a portion of said taxol is incorporated in said substrates.5. The formulation of claim 1, wherein said taxol is incorporated in the pharmaceutically acceptable medium in a concentration of from about 0.01% to about 1%, by weight.6. The formulation of claim 1, wherein said taxol is incorporated in the pharmaceutically acceptable medium in a concentration of from about 0.05% to about 0.5%, by weight.7. The formulation of claim 1, wherein the local anesthetic is incorporated into said controlled release material at a percent loading of 0.1% to about 90% by weight.8. The formulation of claim 1, wherein the local anesthetic is selected from the group consisting of bupivacaine, ropivacaine, dibucaine, etidocaine, tetracaine, lidocaine, xylocaine, procaine, chloroprocaine, prilocaine, mepivacaine, mixtures thereof, and salts thereof.9. The formulation of claim 1, wherein the substrates are in a form selected from slabs, rods, beads, pellets, microparticles, spheroids and pastes.10. The formulation of claim 1, wherein said substrates include from about 65% to about 80% local anesthetic, by weight.11. The formulation of claim 1, wherein said formulation is injected.12. The formulation of claim 1, wherein said formulation is implanted.13. The formulation of claim 1, wherein the local anesthetic is bupivacaine.14. The formulation of claim 1, wherein the taxol is incorporated in said substrates.15. The formulation of claim 1, wherein a further amount of said taxol is on said substrates.16. The formulation of claim 1, wherein the taxol is on said substrates.17. The formulation of claim 1, wherein the substrates are in a pharmaceutically acceptable medium and wherein the taxol is incorporated in the pharmaceutically acceptable medium.18. The formulation of claim 1, wherein the taxol is provided in an amount effective to prolong the duration of the local anesthetic effect for a time period greater than that possible by the use of the local anesthetic in controlled release form by itself.19. A formulation for inducing sustained regional local anesthesia or analgesia in a patient comprising:a plurality of substrates in a pharmaceutically acceptable medium, said substrates comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material comprising a polymer selected from the group consisting of polyanhydrides, copolymers of lactic acid and glycolic acid, poly(lactic) acid, poly(glycolic) acid, polyesters, polyorthoesters, proteins, polysaccharides and combinations thereof to provide a controlled release of said local anesthetic when said formulation is implanted or injected in a patient, said biocompatible, biodegradable controlled release material being capable of degrading at least fifty percent in less than two years following implantation or injection into the patient, and prolonging the release of said local anesthetic from said substrates in-vitro, said substrates being included in said formulation in an amount sufficient to obtain reversible local numbness and/or analgesia when said formulation is implanted or injected in a patient; and taxol in an amount effective to augment the local anesthetic, said taxol being (i) incorporated into and/or onto said substrates; or (ii) incorporated into said pharmaceutically acceptable medium, or (iii) incorporated into said substrates and also incorporated into said pharmaceutically acceptable medium, said formulation providing an in vitro release of said local anesthetic using the United States Pharmacopeia/National Formulary Paddle Method II of from about 10 to about 60 percent after 24 hours, from about 20 to about 80 percent release after 48 hours and from about 40 to about 100 percent release after 72 hours, said formulation providing a reversible local anesthesia at the site when administered in vivo of at least about 24 hours. 20. The formulation of claim 19, wherein the local anesthetic is selected from the group consisting of bupivacaine, ropivacaine, dibucaine, etidocaine, tetracaine, lidocaine, xylocaine, procaine, chloroprocaine, prilocaine, mepivacaine, mixtures thereof, and salts thereof.21. The formulation of claim 19, wherein said Substrates are microspheres.22. The formulation of claim 19, wherein said Substrates are microcapsules.23. A formulation for inducing sustained regional local anesthesia or analgesia in a patient comprising a plurality of substrates comprising a local anesthetic, taxol in an amount effective to augment the local anesthetic, and an effective amount of a biocompatible, biodegradable controlled release material comprising a polymer selected from the group consisting of polyanhydrides, copolymers of lactic acid and glycolic acid, poly(lactic) acid, poly(glycolic) acid, polyesters, polyorthoesters, proteins, polysaccharides and combinations thereof to provide a controlled release of said local anesthetic when said formulation is implanted or injected in a patient, said biocompatible, biodegradable controlled release material being capable of degrading at least fifty percent in less than two years following implantation or injection into the patient and prolonging the release of said local anesthetic from said substrates in vitro, when measured using the United States Pharmacopeia/National Formulary Paddle Method II, said substrates being included in said formulation in an amount sufficient to obtain reversible local numbness and/or analgesia when said formulation is implanted or injected in a patient.24. The formulation of claim 23, wherein the local anesthetic is selected from the group consisting of bupivacaine, ropivacaine, dibucaine, etidocaine, tetracaine, lidocaine, xylocaine, procaine, chloroprocaine, prilocaine, mepivacaine, mixtures thereof, and salts thereof.
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