JP2019514976A5 - - Google Patents
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- JP2019514976A5 JP2019514976A5 JP2018558274A JP2018558274A JP2019514976A5 JP 2019514976 A5 JP2019514976 A5 JP 2019514976A5 JP 2018558274 A JP2018558274 A JP 2018558274A JP 2018558274 A JP2018558274 A JP 2018558274A JP 2019514976 A5 JP2019514976 A5 JP 2019514976A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- weight
- anesthetic
- particles
- crystalline
- 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.)
- Pending
Links
- 239000002245 particle Substances 0.000 claims description 36
- 239000000203 mixture Substances 0.000 claims description 35
- 230000003444 anaesthetic effect Effects 0.000 claims description 25
- XPXMKIXDFWLRAA-UHFFFAOYSA-N hydrazinide Chemical compound [NH-]N XPXMKIXDFWLRAA-UHFFFAOYSA-N 0.000 claims description 23
- 238000000034 method Methods 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 14
- 239000002609 medium Substances 0.000 claims description 13
- 239000012453 solvate Substances 0.000 claims description 12
- 239000004034 viscosity adjusting agent Substances 0.000 claims description 12
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 10
- 239000004094 surface-active agent Substances 0.000 claims description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 9
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims description 9
- 238000009472 formulation Methods 0.000 claims description 8
- 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 7
- 229920000642 polymer Polymers 0.000 claims description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 6
- 230000036592 analgesia Effects 0.000 claims description 6
- 239000000243 solution Substances 0.000 claims description 6
- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 claims description 5
- 229920002385 Sodium hyaluronate Polymers 0.000 claims description 5
- JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 claims description 5
- 229940010747 sodium hyaluronate Drugs 0.000 claims description 5
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 claims description 5
- 239000000872 buffer Substances 0.000 claims description 4
- 230000001939 inductive effect Effects 0.000 claims description 4
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 3
- 229920001213 Polysorbate 20 Polymers 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000006184 cosolvent Substances 0.000 claims description 3
- 229960003964 deoxycholic acid Drugs 0.000 claims description 3
- 235000019441 ethanol Nutrition 0.000 claims description 3
- 235000011187 glycerol Nutrition 0.000 claims description 3
- 150000004677 hydrates Chemical class 0.000 claims description 3
- 238000002347 injection Methods 0.000 claims description 3
- 239000007924 injection Substances 0.000 claims description 3
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims description 3
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims description 3
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims description 3
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 3
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 3
- 229940068977 polysorbate 20 Drugs 0.000 claims description 3
- 229920000053 polysorbate 80 Polymers 0.000 claims description 3
- 229940068968 polysorbate 80 Drugs 0.000 claims description 3
- 239000011734 sodium Substances 0.000 claims description 3
- 229910052708 sodium Inorganic materials 0.000 claims description 3
- FHHPUSMSKHSNKW-SMOYURAASA-M sodium deoxycholate Chemical compound [Na+].C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 FHHPUSMSKHSNKW-SMOYURAASA-M 0.000 claims description 3
- 239000012929 tonicity agent Substances 0.000 claims description 3
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims description 2
- ZKMNUMMKYBVTFN-HNNXBMFYSA-N (S)-ropivacaine Chemical compound CCCN1CCCC[C@H]1C(=O)NC1=C(C)C=CC=C1C ZKMNUMMKYBVTFN-HNNXBMFYSA-N 0.000 claims description 2
- QTGIAADRBBLJGA-UHFFFAOYSA-N Articaine Chemical compound CCCNC(C)C(=O)NC=1C(C)=CSC=1C(=O)OC QTGIAADRBBLJGA-UHFFFAOYSA-N 0.000 claims description 2
- VTUSIVBDOCDNHS-UHFFFAOYSA-N Etidocaine Chemical compound CCCN(CC)C(CC)C(=O)NC1=C(C)C=CC=C1C VTUSIVBDOCDNHS-UHFFFAOYSA-N 0.000 claims description 2
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 2
- 239000012736 aqueous medium Substances 0.000 claims description 2
- 229960003831 articaine Drugs 0.000 claims description 2
- 229960003150 bupivacaine Drugs 0.000 claims description 2
- 229960001747 cinchocaine Drugs 0.000 claims description 2
- PUFQVTATUTYEAL-UHFFFAOYSA-N cinchocaine Chemical compound C1=CC=CC2=NC(OCCCC)=CC(C(=O)NCCN(CC)CC)=C21 PUFQVTATUTYEAL-UHFFFAOYSA-N 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- 229960003976 etidocaine Drugs 0.000 claims description 2
- 229920002674 hyaluronan Polymers 0.000 claims description 2
- 229960003160 hyaluronic acid Drugs 0.000 claims description 2
- 230000008595 infiltration Effects 0.000 claims description 2
- 238000001764 infiltration Methods 0.000 claims description 2
- 229960004288 levobupivacaine Drugs 0.000 claims description 2
- LEBVLXFERQHONN-INIZCTEOSA-N levobupivacaine Chemical compound CCCCN1CCCC[C@H]1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-INIZCTEOSA-N 0.000 claims description 2
- 229960004194 lidocaine Drugs 0.000 claims description 2
- 229960002409 mepivacaine Drugs 0.000 claims description 2
- INWLQCZOYSRPNW-UHFFFAOYSA-N mepivacaine Chemical compound CN1CCCCC1C(=O)NC1=C(C)C=CC=C1C INWLQCZOYSRPNW-UHFFFAOYSA-N 0.000 claims description 2
- 229960001807 prilocaine Drugs 0.000 claims description 2
- MVFGUOIZUNYYSO-UHFFFAOYSA-N prilocaine Chemical compound CCCNC(C)C(=O)NC1=CC=CC=C1C MVFGUOIZUNYYSO-UHFFFAOYSA-N 0.000 claims description 2
- 230000002035 prolonged effect Effects 0.000 claims description 2
- 229960001549 ropivacaine Drugs 0.000 claims description 2
- 239000006172 buffering agent Substances 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 description 5
- 230000001953 sensory effect Effects 0.000 description 2
- 210000003127 knee Anatomy 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 210000002414 leg Anatomy 0.000 description 1
- 229940083542 sodium Drugs 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662332015P | 2016-05-05 | 2016-05-05 | |
| US62/332,015 | 2016-05-05 | ||
| US201662440088P | 2016-12-29 | 2016-12-29 | |
| US62/440,088 | 2016-12-29 | ||
| US201762443318P | 2017-01-06 | 2017-01-06 | |
| US62/443,318 | 2017-01-06 | ||
| US201762463206P | 2017-02-24 | 2017-02-24 | |
| US62/463,206 | 2017-02-24 | ||
| US201762472885P | 2017-03-17 | 2017-03-17 | |
| US62/472,885 | 2017-03-17 | ||
| PCT/US2017/031397 WO2017193066A1 (en) | 2016-05-05 | 2017-05-05 | Precision controlled load and release particles for post-operative pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019514976A JP2019514976A (ja) | 2019-06-06 |
| JP2019514976A5 true JP2019514976A5 (enExample) | 2020-06-18 |
Family
ID=60203445
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018558274A Pending JP2019514976A (ja) | 2016-05-05 | 2017-05-05 | 負荷と放出が正確に制御された術後疼痛用粒子 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20190209538A1 (enExample) |
| EP (1) | EP3452031A4 (enExample) |
| JP (1) | JP2019514976A (enExample) |
| WO (1) | WO2017193066A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021146215A1 (en) | 2020-01-13 | 2021-07-22 | Durect Corporation | Sustained release drug delivery systems with reduced impurities and related methods |
| CN116669717A (zh) * | 2020-08-17 | 2023-08-29 | 美国人福制药公司 | 长效原位成型/胶凝组合物 |
| CA3203561A1 (en) | 2021-01-12 | 2022-07-21 | Adrian Neil Verity | Sustained release drug delivery systems and related methods |
| TW202308595A (zh) * | 2021-08-13 | 2023-03-01 | 大陸商江西濟民可信集團有限公司 | 一種微球懸液、微粒製劑及其製備方法 |
| JP7768735B2 (ja) * | 2021-11-16 | 2025-11-12 | 新田ゼラチン株式会社 | 生体吸収性粒子 |
| WO2025015011A1 (en) * | 2023-07-10 | 2025-01-16 | Nevakar Injectables Inc. | Bupivacaine compositions and methods |
| US12648940B2 (en) | 2023-09-12 | 2026-06-09 | Fresenius Kabi Austria Gmbh | Bupivacaine liquid formulations |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5922340A (en) * | 1992-09-10 | 1999-07-13 | Children's Medical Center Corporation | High load formulations and methods for providing prolonged local anesthesia |
| AU733867B2 (en) * | 1996-06-24 | 2001-05-31 | Euro-Celtique S.A. | Methods for providing safe local anesthesia |
| US6046187A (en) * | 1996-09-16 | 2000-04-04 | Children's Medical Center Corporation | Formulations and methods for providing prolonged local anesthesia |
| IL129951A0 (en) * | 1997-07-02 | 2000-02-29 | Euro Celtique Sa | Prolonged anesthesia in joints and body spaces |
| US7582311B1 (en) * | 1999-10-15 | 2009-09-01 | Genentech, Inc. | Injection vehicle for polymer-based formulations |
| WO2002032398A2 (en) * | 2000-10-16 | 2002-04-25 | Massachusetts Institute Of Technology | Lipid-protein-sugar particles for drug delivery |
| US20030152637A1 (en) * | 2001-01-25 | 2003-08-14 | Mark Chasin | Local anesthetic, and method of use |
| US8986736B2 (en) * | 2003-06-24 | 2015-03-24 | Baxter International Inc. | Method for delivering particulate drugs to tissues |
| US20050106214A1 (en) * | 2003-11-14 | 2005-05-19 | Guohua Chen | Excipients in drug delivery vehicles |
| US20060127468A1 (en) * | 2004-05-19 | 2006-06-15 | Kolodney Michael S | Methods and related compositions for reduction of fat and skin tightening |
| DK2767292T3 (en) * | 2004-09-17 | 2016-12-19 | Durect Corp | RENEWABLE local anesthetic COMPOSITION CONTAINING SAIB |
| CA2611985C (en) * | 2005-06-17 | 2016-08-16 | The University Of North Carolina At Chapel Hill | Nanoparticle fabrication methods, systems, and materials |
| WO2008063204A2 (en) * | 2006-01-27 | 2008-05-29 | The University Of North Carolina At Chapel Hill | Taggants and methods and systems for fabricating |
| US20080102123A1 (en) * | 2006-10-27 | 2008-05-01 | Schachter Deborah M | Self-gelling tunable drug delivery system |
| US8846068B2 (en) * | 2008-04-18 | 2014-09-30 | Warsaw Orthopedic, Inc. | Methods and compositions for treating post-operative pain comprising a local anesthetic |
| WO2009132153A2 (en) * | 2008-04-22 | 2009-10-29 | Angiotech Pharmaceuticals, Inc. | Biocompatible crosslinked hydrogels, drug-loaded hydrogels and methods of using the same |
| WO2012075447A2 (en) * | 2010-12-03 | 2012-06-07 | Warsaw Orthopedic, Inc. | Compositions and methods for delivering clonidine and bupivacaine to a target tissue site |
| US10188772B2 (en) * | 2011-10-18 | 2019-01-29 | Micell Technologies, Inc. | Drug delivery medical device |
| BR112015015439A2 (pt) * | 2012-12-28 | 2017-07-11 | Otsuka Pharma Co Ltd | formulação injetável depot, processo para produzir uma formulação injetável depot, e, kit para prevenção ou tratamento de doença renal policística, uso de uma combinação |
| JP6723162B2 (ja) * | 2014-04-21 | 2020-07-15 | ヘロン セラピューティクス, インコーポレイテッドHeron Therapeutics, Inc. | ポリオルトエステルおよび有機酸添加剤の組成物 |
| WO2015164840A1 (en) * | 2014-04-24 | 2015-10-29 | Georgia Tech Research Corporation | Microneedles and methods of manufacture thereof |
-
2017
- 2017-05-05 WO PCT/US2017/031397 patent/WO2017193066A1/en not_active Ceased
- 2017-05-05 US US16/099,118 patent/US20190209538A1/en not_active Abandoned
- 2017-05-05 JP JP2018558274A patent/JP2019514976A/ja active Pending
- 2017-05-05 EP EP17793498.1A patent/EP3452031A4/en not_active Withdrawn
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