JP2019537589A5 - - Google Patents
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- Publication number
- JP2019537589A5 JP2019537589A5 JP2019522974A JP2019522974A JP2019537589A5 JP 2019537589 A5 JP2019537589 A5 JP 2019537589A5 JP 2019522974 A JP2019522974 A JP 2019522974A JP 2019522974 A JP2019522974 A JP 2019522974A JP 2019537589 A5 JP2019537589 A5 JP 2019537589A5
- Authority
- JP
- Japan
- Prior art keywords
- preparation according
- capsaicin
- polyethylene glycol
- solubilizer
- polyethylene
- 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.)
- Granted
Links
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 claims description 134
- 238000002360 preparation method Methods 0.000 claims description 129
- 229960002504 capsaicin Drugs 0.000 claims description 65
- 235000017663 capsaicin Nutrition 0.000 claims description 61
- 239000000203 mixture Substances 0.000 claims description 49
- -1 polyethylene Polymers 0.000 claims description 47
- 239000002202 Polyethylene glycol Substances 0.000 claims description 46
- 229920001223 polyethylene glycol Polymers 0.000 claims description 46
- 239000002904 solvent Substances 0.000 claims description 46
- 239000004698 Polyethylene Substances 0.000 claims description 40
- 229920000573 polyethylene Polymers 0.000 claims description 40
- 125000000350 glycoloyl group Chemical group O=C([*])C([H])([H])O[H] 0.000 claims description 38
- 238000009472 formulation Methods 0.000 claims description 26
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 17
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 17
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 16
- 208000002193 Pain Diseases 0.000 claims description 15
- 230000003204 osmotic effect Effects 0.000 claims description 14
- 238000002347 injection Methods 0.000 claims description 13
- 239000007924 injection Substances 0.000 claims description 13
- 239000003963 antioxidant agent Substances 0.000 claims description 12
- 239000002738 chelating agent Substances 0.000 claims description 12
- 239000007972 injectable composition Substances 0.000 claims description 12
- SPSPIUSUWPLVKD-UHFFFAOYSA-N 2,3-dibutyl-6-methylphenol Chemical group CCCCC1=CC=C(C)C(O)=C1CCCC SPSPIUSUWPLVKD-UHFFFAOYSA-N 0.000 claims description 10
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical group OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 10
- 235000010354 butylated hydroxytoluene Nutrition 0.000 claims description 10
- 239000003795 chemical substances by application Substances 0.000 claims description 9
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims description 8
- 239000002253 acid Substances 0.000 claims description 8
- 239000001632 sodium acetate Substances 0.000 claims description 8
- 235000017281 sodium acetate Nutrition 0.000 claims description 8
- 239000011780 sodium chloride Substances 0.000 claims description 8
- 230000003078 antioxidant effect Effects 0.000 claims description 7
- 239000007853 buffer solution Substances 0.000 claims description 7
- 229920000858 Cyclodextrin Polymers 0.000 claims description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
- 150000002148 esters Chemical class 0.000 claims description 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 6
- 239000003607 modifier Substances 0.000 claims description 6
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 6
- 208000006820 Arthralgia Diseases 0.000 claims description 5
- 239000002552 dosage form Substances 0.000 claims description 4
- 210000000629 knee joint Anatomy 0.000 claims description 4
- 229920000642 polymer Polymers 0.000 claims description 4
- 229950008882 polysorbate Drugs 0.000 claims description 4
- 229920000136 polysorbate Polymers 0.000 claims description 4
- 229910052783 alkali metal Inorganic materials 0.000 claims description 3
- 201000008482 osteoarthritis Diseases 0.000 claims description 3
- 239000011261 inert gas Substances 0.000 claims description 2
- 150000002989 phenols Chemical class 0.000 claims description 2
- 230000002459 sustained effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 16
- 230000003444 anaesthetic effect Effects 0.000 description 3
- 238000010438 heat treatment Methods 0.000 description 3
- 239000003589 local anesthetic agent Substances 0.000 description 3
- 235000010290 biphenyl Nutrition 0.000 description 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N phenylbenzene Natural products C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 description 2
- DYLIWHYUXAJDOJ-OWOJBTEDSA-N (e)-4-(6-aminopurin-9-yl)but-2-en-1-ol Chemical compound NC1=NC=NC2=C1N=CN2C\C=C\CO DYLIWHYUXAJDOJ-OWOJBTEDSA-N 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 1
- 229930013930 alkaloid Natural products 0.000 description 1
- 150000003797 alkaloid derivatives Chemical class 0.000 description 1
- 210000000544 articulatio talocruralis Anatomy 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 125000002843 carboxylic acid group Chemical group 0.000 description 1
- 210000003797 carpal joint Anatomy 0.000 description 1
- 210000002310 elbow joint Anatomy 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 239000003193 general anesthetic agent Substances 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 1
- 210000004394 hip joint Anatomy 0.000 description 1
- 230000000917 hyperalgesic effect Effects 0.000 description 1
- 244000145841 kine Species 0.000 description 1
- 229960004194 lidocaine Drugs 0.000 description 1
- 210000001872 metatarsal bone Anatomy 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 125000001483 monosaccharide substituent group Chemical group 0.000 description 1
- 150000002894 organic compounds Chemical group 0.000 description 1
- 210000000323 shoulder joint Anatomy 0.000 description 1
- YKPUWZUDDOIDPM-VURMDHGXSA-N zucapsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C/C(C)C)=CC=C1O YKPUWZUDDOIDPM-VURMDHGXSA-N 0.000 description 1
- 229960002860 zucapsaicin Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662416345P | 2016-11-02 | 2016-11-02 | |
| US62/416,345 | 2016-11-02 | ||
| PCT/US2017/059628 WO2018085476A1 (en) | 2016-11-02 | 2017-11-02 | Stable aqueous capsaicin injectable formulations and medical uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019537589A JP2019537589A (ja) | 2019-12-26 |
| JP2019537589A5 true JP2019537589A5 (enExample) | 2020-12-10 |
| JP7100635B2 JP7100635B2 (ja) | 2022-07-13 |
Family
ID=62077165
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019522974A Active JP7100635B2 (ja) | 2016-11-02 | 2017-11-02 | 安定な水性カプサイシン注射製剤およびその医学的使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (7) | US11000490B2 (enExample) |
| EP (1) | EP3534961A4 (enExample) |
| JP (1) | JP7100635B2 (enExample) |
| KR (1) | KR102657458B1 (enExample) |
| CN (1) | CN110035740B (enExample) |
| AU (1) | AU2017353782B2 (enExample) |
| CA (1) | CA3041121A1 (enExample) |
| IL (1) | IL266279B2 (enExample) |
| MX (1) | MX2019005202A (enExample) |
| NZ (1) | NZ752750A (enExample) |
| WO (1) | WO2018085476A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7100635B2 (ja) | 2016-11-02 | 2022-07-13 | セントレクシオン セラピューティクス コーポレイション | 安定な水性カプサイシン注射製剤およびその医学的使用 |
| IL272036B2 (en) | 2017-07-20 | 2025-01-01 | Centrexion Therapeutics Corp | Methods and compositions for treating pain using capsaicin |
| JP2021534207A (ja) * | 2018-08-24 | 2021-12-09 | セントレクシオン セラピューティクス コーポレイション | 膝関節痛の治療のためのカプサイシン連続投薬方法 |
| CN114641485A (zh) | 2020-04-05 | 2022-06-17 | 辉瑞大药厂 | 用于治疗covid-19的化合物和方法 |
| CN113855626B (zh) * | 2020-08-07 | 2023-03-24 | 北京泰德制药股份有限公司 | 一种用于骨关节炎治疗的辣椒碱注射剂及其制备方法 |
| WO2023027670A2 (en) * | 2021-08-23 | 2023-03-02 | Tum Ekip Ilac Anonim Sirketi | Lyophilized levosimendan compositions |
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| US5021450A (en) | 1989-05-30 | 1991-06-04 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | New class of compounds having a variable spectrum of activities for capsaicin-like responses, compositions and uses thereof |
| US5431914A (en) | 1992-04-17 | 1995-07-11 | Adekunle; Michael | Method of treating an internal condition by external application of capsaicin without the need for systemic absorption |
| US5318960A (en) | 1992-06-03 | 1994-06-07 | Frank Toppo | System for transdermal delivery of pain relieving substances |
| US5985860A (en) | 1992-06-03 | 1999-11-16 | Toppo; Frank | System for transdermal delivery of pain relieving substances |
| EP0646372B1 (de) | 1993-09-30 | 1999-03-31 | Medichemie Ag | Capsaicin enthaltendes Arzneimittel zur Behandlung chronischer Rhinopathie |
| US6248788B1 (en) | 1996-11-06 | 2001-06-19 | The Regents Of The University Of California | Therapeutic method with capsaicin and capasicin analogs |
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| JP2002514221A (ja) | 1997-05-27 | 2002-05-14 | アルゴス ファーマシューティカル コーポレーション | カプサイシノイド及びその強化薬を含有する鎮痛薬組成物 |
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| WO2017205534A1 (en) | 2016-05-25 | 2017-11-30 | Concentric Analgesics, Inc. | Prodrugs of phenolic trpv1 agonists in combination with local anesthetics and vasoconstrictors for improved local anesthesia |
| JP7100635B2 (ja) | 2016-11-02 | 2022-07-13 | セントレクシオン セラピューティクス コーポレイション | 安定な水性カプサイシン注射製剤およびその医学的使用 |
| WO2018217937A1 (en) | 2017-05-24 | 2018-11-29 | Concentric Analgesics, Inc. | Prodrugs of phenolic trpv1 agonists in combination with local anesthetics and vasoconstrictors for improved local anesthesia |
-
2017
- 2017-11-02 JP JP2019522974A patent/JP7100635B2/ja active Active
- 2017-11-02 EP EP17868308.2A patent/EP3534961A4/en active Pending
- 2017-11-02 US US16/342,652 patent/US11000490B2/en active Active
- 2017-11-02 AU AU2017353782A patent/AU2017353782B2/en active Active
- 2017-11-02 MX MX2019005202A patent/MX2019005202A/es unknown
- 2017-11-02 NZ NZ752750A patent/NZ752750A/en unknown
- 2017-11-02 CA CA3041121A patent/CA3041121A1/en active Pending
- 2017-11-02 WO PCT/US2017/059628 patent/WO2018085476A1/en not_active Ceased
- 2017-11-02 KR KR1020197015747A patent/KR102657458B1/ko active Active
- 2017-11-02 CN CN201780075307.XA patent/CN110035740B/zh active Active
-
2019
- 2019-04-28 IL IL266279A patent/IL266279B2/en unknown
- 2019-05-01 US US16/400,278 patent/US10493047B2/en active Active
- 2019-11-26 US US16/695,831 patent/US10765649B2/en active Active
- 2019-11-26 US US16/695,824 patent/US10772853B2/en active Active
-
2020
- 2020-09-11 US US17/018,148 patent/US11344516B2/en active Active
-
2022
- 2022-03-22 US US17/701,160 patent/US11992470B2/en active Active
-
2024
- 2024-05-24 US US18/674,288 patent/US20240423931A1/en active Pending
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