CA2349017A1 - Procedes et compositions d'anesthesie locale prolongee - Google Patents
Procedes et compositions d'anesthesie locale prolongee Download PDFInfo
- Publication number
- CA2349017A1 CA2349017A1 CA002349017A CA2349017A CA2349017A1 CA 2349017 A1 CA2349017 A1 CA 2349017A1 CA 002349017 A CA002349017 A CA 002349017A CA 2349017 A CA2349017 A CA 2349017A CA 2349017 A1 CA2349017 A1 CA 2349017A1
- Authority
- CA
- Canada
- Prior art keywords
- formulation
- local anesthetic
- local
- agent
- controlled release
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 141
- 238000009472 formulation Methods 0.000 title claims abstract description 109
- 238000002690 local anesthesia Methods 0.000 title claims abstract description 69
- 230000002035 prolonged effect Effects 0.000 title claims description 20
- 238000000034 method Methods 0.000 title abstract description 55
- 239000003589 local anesthetic agent Substances 0.000 claims abstract description 174
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 160
- 230000003190 augmentative effect Effects 0.000 claims abstract description 131
- 238000013270 controlled release Methods 0.000 claims abstract description 107
- 239000000758 substrate Substances 0.000 claims abstract description 39
- 239000000463 material Substances 0.000 claims abstract description 31
- 239000003862 glucocorticoid Substances 0.000 claims abstract description 13
- 230000001939 inductive effect Effects 0.000 claims abstract description 8
- 230000002441 reversible effect Effects 0.000 claims abstract description 8
- 230000002459 sustained effect Effects 0.000 claims abstract description 7
- 231100000252 nontoxic Toxicity 0.000 claims abstract description 4
- 230000003000 nontoxic effect Effects 0.000 claims abstract description 4
- 239000004005 microsphere Substances 0.000 claims description 120
- 238000002347 injection Methods 0.000 claims description 61
- 239000007924 injection Substances 0.000 claims description 61
- LEBVLXFERQHONN-UHFFFAOYSA-N 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide Chemical compound CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-UHFFFAOYSA-N 0.000 claims description 49
- 229920000642 polymer Polymers 0.000 claims description 45
- 229960003150 bupivacaine Drugs 0.000 claims description 44
- 239000005526 vasoconstrictor agent Substances 0.000 claims description 38
- -1 ergotoxine Chemical compound 0.000 claims description 24
- 239000000243 solution Substances 0.000 claims description 23
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- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 claims description 16
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- 229920001577 copolymer Polymers 0.000 claims description 15
- 238000011068 loading method Methods 0.000 claims description 15
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- 229920002732 Polyanhydride Polymers 0.000 claims description 14
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- 238000000338 in vitro Methods 0.000 claims description 13
- 150000004676 glycans Chemical class 0.000 claims description 12
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- 239000005017 polysaccharide Substances 0.000 claims description 12
- 239000002207 metabolite Substances 0.000 claims description 11
- 239000002245 particle Substances 0.000 claims description 10
- 238000002513 implantation Methods 0.000 claims description 9
- 239000002552 dosage form Substances 0.000 claims description 8
- GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 claims description 7
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 5
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- RMMXTBMQSGEXHJ-UHFFFAOYSA-N Aminophenazone Chemical compound O=C1C(N(C)C)=C(C)N(C)N1C1=CC=CC=C1 RMMXTBMQSGEXHJ-UHFFFAOYSA-N 0.000 claims description 4
- ZFMITUMMTDLWHR-UHFFFAOYSA-N Minoxidil Chemical compound NC1=[N+]([O-])C(N)=CC(N2CCCCC2)=N1 ZFMITUMMTDLWHR-UHFFFAOYSA-N 0.000 claims description 4
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- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims description 4
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- 229920000728 polyester Polymers 0.000 claims description 4
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- LPMXVESGRSUGHW-UHFFFAOYSA-N Acolongiflorosid K Natural products OC1C(O)C(O)C(C)OC1OC1CC2(O)CCC3C4(O)CCC(C=5COC(=O)C=5)C4(C)CC(O)C3C2(CO)C(O)C1 LPMXVESGRSUGHW-UHFFFAOYSA-N 0.000 claims description 3
- KXDROGADUISDGY-UHFFFAOYSA-N Benzamil hydrochloride Chemical compound C=1C=CC=CC=1CN=C(N)NC(=O)C1=NC(Cl)=C(N)N=C1N KXDROGADUISDGY-UHFFFAOYSA-N 0.000 claims description 3
- FMGSKLZLMKYGDP-UHFFFAOYSA-N Dehydroepiandrosterone Natural products C1C(O)CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CC=C21 FMGSKLZLMKYGDP-UHFFFAOYSA-N 0.000 claims description 3
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 3
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- 229930012538 Paclitaxel Natural products 0.000 claims description 3
- 244000166550 Strophanthus gratus Species 0.000 claims description 3
- 150000003943 catecholamines Chemical class 0.000 claims description 3
- FMGSKLZLMKYGDP-USOAJAOKSA-N dehydroepiandrosterone Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 FMGSKLZLMKYGDP-USOAJAOKSA-N 0.000 claims description 3
- NIJJYAXOARWZEE-UHFFFAOYSA-N di-n-propyl-acetic acid Natural products CCCC(C(O)=O)CCC NIJJYAXOARWZEE-UHFFFAOYSA-N 0.000 claims description 3
- GFMHGFPPCYBUCK-HBUFSDLISA-N dnc012382 Chemical compound C([C@@H](C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C(O)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H]1N(CC(Cl)C1Cl)C(=O)[C@H](C)NC(=O)[C@H]1N(CCC1C=1C=NC=CC=1)C(=O)[C@H](CCCCN)NC(=O)C=1C=NC=CC=1)C1=CC=CC=C1 GFMHGFPPCYBUCK-HBUFSDLISA-N 0.000 claims description 3
- LPMXVESGRSUGHW-HBYQJFLCSA-N ouabain Chemical compound O[C@@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@H]1O[C@@H]1C[C@@]2(O)CC[C@H]3[C@@]4(O)CC[C@H](C=5COC(=O)C=5)[C@@]4(C)C[C@@H](O)[C@@H]3[C@@]2(CO)[C@H](O)C1 LPMXVESGRSUGHW-HBYQJFLCSA-N 0.000 claims description 3
- 229960003343 ouabain Drugs 0.000 claims description 3
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- 102000004169 proteins and genes Human genes 0.000 claims description 3
- 108090000623 proteins and genes Proteins 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
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- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 3
- MSRILKIQRXUYCT-UHFFFAOYSA-M valproate semisodium Chemical compound [Na+].CCCC(C(O)=O)CCC.CCCC(C([O-])=O)CCC MSRILKIQRXUYCT-UHFFFAOYSA-M 0.000 claims description 3
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 claims description 2
- YKFCISHFRZHKHY-NGQGLHOPSA-N (2s)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid;trihydrate Chemical compound O.O.O.OC(=O)[C@](N)(C)CC1=CC=C(O)C(O)=C1.OC(=O)[C@](N)(C)CC1=CC=C(O)C(O)=C1 YKFCISHFRZHKHY-NGQGLHOPSA-N 0.000 claims description 2
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- SYGWGHVTLUBCEM-TUJFWAKLSA-N (3r,5s,8s,9s,10s,13s,14s,17r)-3,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,3,4,5,6,7,8,9,12,14,15,16-dodecahydro-1h-cyclopenta[a]phenanthren-11-one Chemical compound C1[C@H](O)CC[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CC[C@H]21 SYGWGHVTLUBCEM-TUJFWAKLSA-N 0.000 claims description 2
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- LTMHDMANZUZIPE-AMTYYWEZSA-N Digoxin Natural products O([C@H]1[C@H](C)O[C@H](O[C@@H]2C[C@@H]3[C@@](C)([C@@H]4[C@H]([C@]5(O)[C@](C)([C@H](O)C4)[C@H](C4=CC(=O)OC4)CC5)CC3)CC2)C[C@@H]1O)[C@H]1O[C@H](C)[C@@H](O[C@H]2O[C@@H](C)[C@H](O)[C@@H](O)C2)[C@@H](O)C1 LTMHDMANZUZIPE-AMTYYWEZSA-N 0.000 claims description 2
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Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US10595P | 1995-06-09 | 1995-06-09 | |
US60/000,105 | 1995-06-09 | ||
CA002195119A CA2195119C (fr) | 1995-06-09 | 1996-06-07 | Procedes et compositions d'anesthesie locale prolongee |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA002195119A Division CA2195119C (fr) | 1995-06-09 | 1996-06-07 | Procedes et compositions d'anesthesie locale prolongee |
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Publication Number | Publication Date |
---|---|
CA2349017A1 true CA2349017A1 (fr) | 1996-12-27 |
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ID=25678983
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA002349017A Abandoned CA2349017A1 (fr) | 1995-06-09 | 1996-06-07 | Procedes et compositions d'anesthesie locale prolongee |
Country Status (1)
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---|---|
CA (1) | CA2349017A1 (fr) |
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1996
- 1996-06-07 CA CA002349017A patent/CA2349017A1/fr not_active Abandoned
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