CN103932973B - 包含丁卡因和血管收缩剂的用于鼻内给药的牙麻醉剂 - Google Patents
包含丁卡因和血管收缩剂的用于鼻内给药的牙麻醉剂 Download PDFInfo
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
- A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
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- A—HUMAN NECESSITIES
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- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
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Landscapes
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- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
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- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16668009P | 2009-04-03 | 2009-04-03 | |
| US61/166,680 | 2009-04-03 | ||
| CN201080020599.5A CN102421416B (zh) | 2009-04-03 | 2010-04-02 | 包含丁卡因和血管收缩剂的用于鼻内给药的牙麻醉剂 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080020599.5A Division CN102421416B (zh) | 2009-04-03 | 2010-04-02 | 包含丁卡因和血管收缩剂的用于鼻内给药的牙麻醉剂 |
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|---|---|
| CN103932973A CN103932973A (zh) | 2014-07-23 |
| CN103932973B true CN103932973B (zh) | 2017-08-11 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410169695.6A Expired - Fee Related CN103932973B (zh) | 2009-04-03 | 2010-04-02 | 包含丁卡因和血管收缩剂的用于鼻内给药的牙麻醉剂 |
| CN201080020599.5A Expired - Fee Related CN102421416B (zh) | 2009-04-03 | 2010-04-02 | 包含丁卡因和血管收缩剂的用于鼻内给药的牙麻醉剂 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080020599.5A Expired - Fee Related CN102421416B (zh) | 2009-04-03 | 2010-04-02 | 包含丁卡因和血管收缩剂的用于鼻内给药的牙麻醉剂 |
Country Status (18)
| Country | Link |
|---|---|
| US (7) | US8580282B2 (enExample) |
| EP (1) | EP2413899B1 (enExample) |
| JP (3) | JP5788864B2 (enExample) |
| KR (2) | KR20170026639A (enExample) |
| CN (2) | CN103932973B (enExample) |
| AU (2) | AU2010232995C1 (enExample) |
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| EP2413899B1 (en) | 2009-04-03 | 2021-01-27 | St. Renatus, LLC | Dental anesthetic comprising tetracaine and a vasoconstrictor for intranasal administration |
| WO2014052859A1 (en) * | 2012-09-28 | 2014-04-03 | St. Renatus, Llc | Pharmaceutical composition comprising benzyl alcohol for the treatment of migraines |
| EP3086785A4 (en) * | 2014-01-01 | 2017-08-30 | Real Time Imaging Technologies, LLC | Improved local anesthetic solution for dental and/or contrast media use |
| CA2952622A1 (en) * | 2014-06-16 | 2015-12-23 | Loewi LLC | Methods of anesthetizing nerve tissue in the trigeminal nerve pathway and medical uses thereof |
| CA2971156A1 (en) * | 2014-12-23 | 2016-06-30 | St. Renatus, Llc | Tetracaine-based anesthetic |
| EP3244800A1 (en) | 2015-01-12 | 2017-11-22 | Real Time Imaging Technologies, LLC | Low-dose x-ray imaging system |
| US10039830B2 (en) * | 2016-03-04 | 2018-08-07 | Cetylite Industries, Inc. | Topical anesthetic composition |
| US20170360718A1 (en) * | 2016-06-01 | 2017-12-21 | St. Renatus, Llc | Intranasal dental anesthetic |
| AU2019403903A1 (en) | 2018-12-19 | 2021-06-24 | Acasti Pharma U.S., Inc. | Therapeutic composition of intranasal lidocaine |
| CN111494310A (zh) * | 2020-04-29 | 2020-08-07 | 周晓玲 | 一种局部麻醉药物的制备及使用方法 |
| EP4355313A1 (en) * | 2021-06-14 | 2024-04-24 | Pharmavax AS | Combinations of local anesthetics for improved pain relief |
| EP4648760A1 (en) * | 2023-01-13 | 2025-11-19 | Smilanich, Michael D. | Composition for local anesthesia and uses thereof |
| GB2628149A (en) * | 2023-03-16 | 2024-09-18 | Lee Nathaniel Wurie | Nasal spray for performing sphenopalatine ganglion block |
Citations (1)
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| US6413499B1 (en) * | 2000-01-06 | 2002-07-02 | Bryan M. Clay | Methods and kits for maxillary dental anesthesia by means of a nasal deliverable anesthetic |
Family Cites Families (15)
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|---|---|---|---|---|
| US3832460A (en) * | 1971-03-19 | 1974-08-27 | C Kosti | Anesthetic-vasoconstrictor-antihistamine composition for the treatment of hypertrophied oral tissue |
| US5209724A (en) | 1988-04-11 | 1993-05-11 | Dhaliwal Avtar S | Composite anesthetic article and method of use |
| BR9306816A (pt) | 1992-07-28 | 1998-12-08 | Procter & Gamble | Composição farmaceutica para uso tópico contendo um polímero catiônico reticulado e um eter alcoxilado |
| US5854269A (en) | 1993-11-19 | 1998-12-29 | Schering-Plough Healthcare Products, Inc. | Nasal spray compositions |
| US5585398A (en) * | 1994-07-15 | 1996-12-17 | Ernst; Amy A. | Topical anesthetic comprising lidocaine, adrenaline, and tetracaine, and its method of use |
| US6075059A (en) | 1999-02-24 | 2000-06-13 | The Ohio State University | Compositions for dental anesthesia |
| US20040131665A1 (en) * | 1999-10-22 | 2004-07-08 | Wepfer Scott T. | Topical anesthetic formulation |
| US20040045546A1 (en) | 2002-09-05 | 2004-03-11 | Peirce Management, Llc | Pharmaceutical delivery system for oral inhalation through nebulization consisting of inert substrate impregnated with substance (S) to be solubilized or suspended prior to use |
| JP4591746B2 (ja) | 2002-12-03 | 2010-12-01 | 大正製薬株式会社 | 難溶性抗ウイルス成分含有水溶性外用剤組成物 |
| ES2223277B1 (es) * | 2003-06-19 | 2006-03-01 | Fernando Bouffard Fita | Composicion anestesica para administracion topica. |
| WO2005065696A1 (en) | 2004-01-01 | 2005-07-21 | Panacea Biotec Ltd. | Pharmaceutical compositions comprising an extract of euphorbia prostrata |
| US20060052305A1 (en) * | 2004-05-10 | 2006-03-09 | Nastech Pharmaceutical Company Inc. | Method of treating osteoporosis using intranasal parathyroid hormone |
| US20070154402A1 (en) | 2005-10-24 | 2007-07-05 | Collegium Pharmaceutical, Inc. | Topical Pharmaceutical Foam Composition |
| US9252862B2 (en) | 2008-09-17 | 2016-02-02 | Qualcomm Incorporated | MIMO preamble for initial access with an unknown number of transmit antennas |
| EP2413899B1 (en) * | 2009-04-03 | 2021-01-27 | St. Renatus, LLC | Dental anesthetic comprising tetracaine and a vasoconstrictor for intranasal administration |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US6413499B1 (en) * | 2000-01-06 | 2002-07-02 | Bryan M. Clay | Methods and kits for maxillary dental anesthesia by means of a nasal deliverable anesthetic |
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