KR20120050457A - 다비가트란 이텍실레이트 과다복용에 대한 활성 차콜에 의한 응급 중재 - Google Patents
다비가트란 이텍실레이트 과다복용에 대한 활성 차콜에 의한 응급 중재 Download PDFInfo
- Publication number
- KR20120050457A KR20120050457A KR1020127004779A KR20127004779A KR20120050457A KR 20120050457 A KR20120050457 A KR 20120050457A KR 1020127004779 A KR1020127004779 A KR 1020127004779A KR 20127004779 A KR20127004779 A KR 20127004779A KR 20120050457 A KR20120050457 A KR 20120050457A
- Authority
- KR
- South Korea
- Prior art keywords
- charcoal
- formula
- dabigatran
- dabigatran etexilate
- suspension
- 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.)
- Ceased
Links
- 239000003610 charcoal Substances 0.000 title claims abstract description 29
- KSGXQBZTULBEEQ-UHFFFAOYSA-N dabigatran etexilate Chemical compound C1=CC(C(N)=NC(=O)OCCCCCC)=CC=C1NCC1=NC2=CC(C(=O)N(CCC(=O)OCC)C=3N=CC=CC=3)=CC=C2N1C KSGXQBZTULBEEQ-UHFFFAOYSA-N 0.000 title claims abstract description 26
- 229960000288 dabigatran etexilate Drugs 0.000 title claims abstract description 25
- 238000000034 method Methods 0.000 claims abstract description 25
- 239000013543 active substance Substances 0.000 claims abstract description 8
- 150000003839 salts Chemical class 0.000 claims abstract description 7
- 229960003850 dabigatran Drugs 0.000 claims description 17
- YBSJFWOBGCMAKL-UHFFFAOYSA-N dabigatran Chemical compound N=1C2=CC(C(=O)N(CCC(O)=O)C=3N=CC=CC=3)=CC=C2N(C)C=1CNC1=CC=C(C(N)=N)C=C1 YBSJFWOBGCMAKL-UHFFFAOYSA-N 0.000 claims description 17
- 238000006386 neutralization reaction Methods 0.000 claims description 6
- 230000008081 blood perfusion Effects 0.000 claims description 2
- 239000000725 suspension Substances 0.000 description 21
- 239000008188 pellet Substances 0.000 description 20
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 15
- 235000002906 tartaric acid Nutrition 0.000 description 15
- 239000011975 tartaric acid Substances 0.000 description 15
- 239000007921 spray Substances 0.000 description 12
- 239000002253 acid Substances 0.000 description 11
- 239000002245 particle Substances 0.000 description 11
- 238000003756 stirring Methods 0.000 description 11
- 239000000243 solution Substances 0.000 description 10
- 239000000203 mixture Substances 0.000 description 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 7
- 238000005507 spraying Methods 0.000 description 7
- 150000001875 compounds Chemical class 0.000 description 5
- 239000011162 core material Substances 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 238000012216 screening Methods 0.000 description 5
- 239000002775 capsule Substances 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 239000007858 starting material Substances 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- 206010003658 Atrial Fibrillation Diseases 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000010410 layer Substances 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 239000011149 active material Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 230000037406 food intake Effects 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- 238000002955 isolation Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 230000003472 neutralizing effect Effects 0.000 description 2
- 150000007524 organic acids Chemical class 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 238000012545 processing Methods 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- 239000003868 thrombin inhibitor Substances 0.000 description 2
- 230000004580 weight loss Effects 0.000 description 2
- 241000220479 Acacia Species 0.000 description 1
- 206010051055 Deep vein thrombosis Diseases 0.000 description 1
- 229940123900 Direct thrombin inhibitor Drugs 0.000 description 1
- 208000032843 Hemorrhage Diseases 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 235000010643 Leucaena leucocephala Nutrition 0.000 description 1
- 101000712605 Theromyzon tessulatum Theromin Proteins 0.000 description 1
- 229940122388 Thrombin inhibitor Drugs 0.000 description 1
- 206010047249 Venous thrombosis Diseases 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000003146 anticoagulant agent Substances 0.000 description 1
- 229940127219 anticoagulant drug Drugs 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 208000034158 bleeding Diseases 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 239000012792 core layer Substances 0.000 description 1
- 239000002274 desiccant Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 229940008099 dimethicone Drugs 0.000 description 1
- 239000004205 dimethyl polysiloxane Substances 0.000 description 1
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 238000007654 immersion Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 239000004570 mortar (masonry) Substances 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 238000012106 screening analysis Methods 0.000 description 1
- 238000004062 sedimentation Methods 0.000 description 1
- 230000009861 stroke prevention Effects 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
- PJVWKTKQMONHTI-UHFFFAOYSA-N warfarin Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 description 1
- 229960005080 warfarin Drugs 0.000 description 1
- -1 which is a potent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/44—Elemental carbon, e.g. charcoal, carbon black
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- 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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
- A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2121/00—Preparations for use in therapy
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Inorganic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Toxicology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Information Retrieval, Db Structures And Fs Structures Therefor (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23632109P | 2009-08-24 | 2009-08-24 | |
| US61/236,321 | 2009-08-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20120050457A true KR20120050457A (ko) | 2012-05-18 |
Family
ID=42740360
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020127004779A Ceased KR20120050457A (ko) | 2009-08-24 | 2010-08-23 | 다비가트란 이텍실레이트 과다복용에 대한 활성 차콜에 의한 응급 중재 |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US20110206656A1 (https=) |
| EP (1) | EP2470187B1 (https=) |
| JP (1) | JP2013502449A (https=) |
| KR (1) | KR20120050457A (https=) |
| CN (1) | CN102481317B (https=) |
| AR (1) | AR077909A1 (https=) |
| AU (1) | AU2010288601A1 (https=) |
| BR (1) | BR112012004169A2 (https=) |
| CA (1) | CA2767966A1 (https=) |
| CL (1) | CL2012000488A1 (https=) |
| DK (1) | DK2470187T3 (https=) |
| EA (1) | EA201200319A1 (https=) |
| ES (1) | ES2436076T3 (https=) |
| IL (1) | IL216968A0 (https=) |
| MX (1) | MX2012001767A (https=) |
| NZ (1) | NZ597359A (https=) |
| PH (1) | PH12012500388A1 (https=) |
| PL (1) | PL2470187T3 (https=) |
| TW (1) | TW201124143A (https=) |
| WO (1) | WO2011023653A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR079944A1 (es) | 2010-01-20 | 2012-02-29 | Boehringer Ingelheim Int | Anticuerpo neutralizante de la actividad de un anticoagulante |
| SG193552A1 (en) * | 2011-03-30 | 2013-11-29 | Boehringer Ingelheim Int | Anticoagulant antidotes |
| GB201120693D0 (en) * | 2011-12-01 | 2012-01-11 | Convatec Technologies Inc | Wound dressing for use in vacuum therapy |
| CN114452839B (zh) * | 2022-02-10 | 2023-04-21 | 中南大学湘雅医院 | 一种抗凝抗栓血液净化膜及其制备方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5277820A (en) * | 1992-02-06 | 1994-01-11 | Hemocleanse, Inc. | Device and method for extracorporeal blood treatment |
| PE121699A1 (es) | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
| KR101005716B1 (ko) | 2002-03-07 | 2011-01-05 | 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 | ３－［（２－｛［４－（헥실옥시카보닐아미노－이미노-메틸）－페닐아미노］－메틸｝－１－메틸－１ｈ－벤즈이미다졸－５－카보닐）－피리딘－２－일－아미노］ 프로피온산 에틸에스테르의 경구 투여 형태 |
-
2010
- 2010-08-23 JP JP2012526022A patent/JP2013502449A/ja active Pending
- 2010-08-23 WO PCT/EP2010/062229 patent/WO2011023653A1/en not_active Ceased
- 2010-08-23 CN CN201080037665.XA patent/CN102481317B/zh not_active Expired - Fee Related
- 2010-08-23 NZ NZ597359A patent/NZ597359A/en not_active IP Right Cessation
- 2010-08-23 AR ARP100103077A patent/AR077909A1/es active IP Right Grant
- 2010-08-23 EP EP10747022.1A patent/EP2470187B1/en active Active
- 2010-08-23 AU AU2010288601A patent/AU2010288601A1/en not_active Abandoned
- 2010-08-23 BR BR112012004169A patent/BR112012004169A2/pt not_active IP Right Cessation
- 2010-08-23 DK DK10747022.1T patent/DK2470187T3/da active
- 2010-08-23 CA CA2767966A patent/CA2767966A1/en not_active Abandoned
- 2010-08-23 TW TW099128118A patent/TW201124143A/zh unknown
- 2010-08-23 KR KR1020127004779A patent/KR20120050457A/ko not_active Ceased
- 2010-08-23 MX MX2012001767A patent/MX2012001767A/es active IP Right Grant
- 2010-08-23 PL PL10747022T patent/PL2470187T3/pl unknown
- 2010-08-23 EA EA201200319A patent/EA201200319A1/ru unknown
- 2010-08-23 ES ES10747022T patent/ES2436076T3/es active Active
- 2010-08-23 PH PH1/2012/500388A patent/PH12012500388A1/en unknown
- 2010-08-24 US US12/862,110 patent/US20110206656A1/en not_active Abandoned
-
2011
- 2011-12-14 IL IL216968A patent/IL216968A0/en unknown
-
2012
- 2012-02-24 CL CL2012000488A patent/CL2012000488A1/es unknown
-
2013
- 2013-07-22 US US13/947,398 patent/US20130302311A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20130302311A1 (en) | 2013-11-14 |
| JP2013502449A (ja) | 2013-01-24 |
| BR112012004169A2 (pt) | 2016-03-29 |
| CN102481317B (zh) | 2014-09-03 |
| ES2436076T3 (es) | 2013-12-26 |
| MX2012001767A (es) | 2012-02-29 |
| US20110206656A1 (en) | 2011-08-25 |
| DK2470187T3 (da) | 2013-10-28 |
| IL216968A0 (en) | 2012-02-29 |
| CL2012000488A1 (es) | 2012-08-31 |
| CN102481317A (zh) | 2012-05-30 |
| AU2010288601A1 (en) | 2012-02-02 |
| CA2767966A1 (en) | 2011-03-03 |
| WO2011023653A1 (en) | 2011-03-03 |
| TW201124143A (en) | 2011-07-16 |
| AR077909A1 (es) | 2011-09-28 |
| NZ597359A (en) | 2014-01-31 |
| EA201200319A1 (ru) | 2012-09-28 |
| PL2470187T3 (pl) | 2014-01-31 |
| EP2470187A1 (en) | 2012-07-04 |
| EP2470187B1 (en) | 2013-08-21 |
| PH12012500388A1 (en) | 2012-10-22 |
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Legal Events
| Date | Code | Title | Description |
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