Methods for providing safe local anesthesia
First Claim
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1. A method for providing local anesthesia at a site in a patient, comprising:
- administering at a site in a patient in need thereof a dose of biocompatible, biodegradable, controlled release microspheres consisting essentially of bupivacaine incorporated at a percent loading from about 60 to about 90% in a polymeric material selected from the group consisting of a polylactide, a polyglycolide, a poly (lactide-co-glycolide), a polyanhydride, a polyorthoester, a polycaprolactone, a polyphosphazene, a polysaccharide, a proteinaceous polymer, a soluble derivative of a polysaccharide, a soluble derivative of a proteinaceous polymer, a polypeptide, a polyester, a polyorthoester, and mixtures thereof contained in a pharmaceutically acceptable carrier, said dose providing local anesthesia to said site for a period of one day, said bupivacaine being present in said dose in an amount effective to induce a localized condition selected from the group consisting of sensory anesthesia, motor anesthesia and combinations thereof, and said dose providing local anesthesia having substantially improved safety relative to a formulation providing a pharmaceutically equivalent effect of bupivacaine administered in immediate release form.
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Abstract
Methods and formulations for inducing substantially safer local anesthesia in a patient are provided. The methods comprise administering, to a patient in need thereof, a substrate containing a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material to safely obtain a reversible nerve blockade when implanted or injected in a patient.
201 Citations
27 Claims
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1. A method for providing local anesthesia at a site in a patient, comprising:
administering at a site in a patient in need thereof a dose of biocompatible, biodegradable, controlled release microspheres consisting essentially of bupivacaine incorporated at a percent loading from about 60 to about 90% in a polymeric material selected from the group consisting of a polylactide, a polyglycolide, a poly (lactide-co-glycolide), a polyanhydride, a polyorthoester, a polycaprolactone, a polyphosphazene, a polysaccharide, a proteinaceous polymer, a soluble derivative of a polysaccharide, a soluble derivative of a proteinaceous polymer, a polypeptide, a polyester, a polyorthoester, and mixtures thereof contained in a pharmaceutically acceptable carrier, said dose providing local anesthesia to said site for a period of one day, said bupivacaine being present in said dose in an amount effective to induce a localized condition selected from the group consisting of sensory anesthesia, motor anesthesia and combinations thereof, and said dose providing local anesthesia having substantially improved safety relative to a formulation providing a pharmaceutically equivalent effect of bupivacaine administered in immediate release form. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)
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25. A method for providing local anesthesia at a site in a patient, comprising:
administering at a site in a patient in need thereof a dose of controlled release microspheres consisting essentially of bupivacaine incorporated at a percent loading from about 60 to about 90% in a biocompatible, biodegradable, polymeric material contained in a pharmaceutically acceptable carrier, said dose providing local anesthesia to said site for a period of one day, said bupivacaine being present in said dose in an amount effective to provide analgesia or anesthesia at the site, said dose providing local anesthesia having substantially improved safety relative to a formulation providing a pharmaceutically equivalent effect of bupivacaine administered in immediate release form.
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26. A method for providing local anesthesia at a site in a patient, comprising:
administering at a site in a patient in need thereof a bupivacaine formulation consisting essentially of a plurality of controlled release microcapsules containing a therapeutically effective amount of bupivacaine free base incorporated at a percent loading from about 60 to about 90% in a biocompatible, biodegradable, polymeric material consisting essentially of a copolymer of lactic acid and glyco lie acid, said formulation providing local anesthesia to said site for a period of one day, said bupivacaine being released from said microcapsules when administered at the site at a rate sufficient to provide analgesia or anesthesia at the site, said formulation having substantially improved safety relative to a formulation providing a pharmaceutically equivalent effect of said bupivacaine administered in immediate release form.
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27. A method for providing local anesthesia at a site in a patient, comprising:
administering at a site in a patient in need thereof a dose of biocompatible, biodegradable, controlled release microparticles consisting essentially of bupivacaine incorporated at a percent loading from about 60 to about 90% in a polymeric material selected from the group consisting of a polylactide, a polyglycolide, a poly (lactide-co-glycolide), a polyanhydride, a polyorthoester, a polycaprolactone, a polyphosphazene, a polysaccharide, a proteinaceous polymer, a soluble derivative of a polysaccharide, a soluble derivative of a proteinaceous polymer, a polypeptide, a polyester, a polyorthoester, and mixtures thereof, contained in a pharmaceutically acceptable carrier, said dose providing local anesthesia to said site for a period of one day, said bupivacaine being present in an amount effective to induce a localized condition selected from the group consisting of sensory anesthesia, motor anesthesia and combinations thereof, and said dose providing local anesthesia having substantially improved safety relative to a formulation providing a pharmaceutically equivalent effect of bupivacaine administered in immediate release form.
Specification