KR102258043B1 - 날트렉손 요법에서 약물 생체이용률의 증가 - Google Patents
날트렉손 요법에서 약물 생체이용률의 증가 Download PDFInfo
- Publication number
- KR102258043B1 KR102258043B1 KR1020207011510A KR20207011510A KR102258043B1 KR 102258043 B1 KR102258043 B1 KR 102258043B1 KR 1020207011510 A KR1020207011510 A KR 1020207011510A KR 20207011510 A KR20207011510 A KR 20207011510A KR 102258043 B1 KR102258043 B1 KR 102258043B1
- Authority
- KR
- South Korea
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- naltrexone
- bupropion
- amount
- 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.)
- Active
Links
- DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 title claims abstract description 312
- 229960003086 naltrexone Drugs 0.000 title claims abstract description 305
- 230000001965 increasing effect Effects 0.000 title claims abstract description 35
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- 239000000203 mixture Substances 0.000 claims abstract description 65
- 238000000034 method Methods 0.000 claims abstract description 50
- 150000003839 salts Chemical class 0.000 claims description 232
- SNPPWIUOZRMYNY-UHFFFAOYSA-N bupropion Chemical compound CC(C)(C)NC(C)C(=O)C1=CC=CC(Cl)=C1 SNPPWIUOZRMYNY-UHFFFAOYSA-N 0.000 claims description 231
- 229960001058 bupropion Drugs 0.000 claims description 223
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- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 16
- 235000021471 food effect Nutrition 0.000 description 15
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- JLVNEHKORQFVQJ-PYIJOLGTSA-N 6alpha-Naltrexol Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@H]3O)CN2CC1CC1 JLVNEHKORQFVQJ-PYIJOLGTSA-N 0.000 description 5
- 230000008859 change Effects 0.000 description 5
- ZFSXKSSWYSZPGQ-UHFFFAOYSA-N (2-hydroxycyclopentyl)azanium;chloride Chemical compound Cl.NC1CCCC1O ZFSXKSSWYSZPGQ-UHFFFAOYSA-N 0.000 description 4
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- NDPTTXIBLSWNSF-JOYOIKCWSA-N (1s,2s)-2-(tert-butylamino)-1-(3-chlorophenyl)propan-1-ol Chemical compound CC(C)(C)N[C@@H](C)[C@@H](O)C1=CC=CC(Cl)=C1 NDPTTXIBLSWNSF-JOYOIKCWSA-N 0.000 description 3
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- NDPTTXIBLSWNSF-BXKDBHETSA-N (1s,2r)-2-(tert-butylamino)-1-(3-chlorophenyl)propan-1-ol Chemical compound CC(C)(C)N[C@H](C)[C@@H](O)C1=CC=CC(Cl)=C1 NDPTTXIBLSWNSF-BXKDBHETSA-N 0.000 description 2
- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 description 2
- 206010013710 Drug interaction Diseases 0.000 description 2
- AKOAEVOSDHIVFX-UHFFFAOYSA-N Hydroxybupropion Chemical compound OCC(C)(C)NC(C)C(=O)C1=CC=CC(Cl)=C1 AKOAEVOSDHIVFX-UHFFFAOYSA-N 0.000 description 2
- 206010028813 Nausea Diseases 0.000 description 2
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- 230000002708 enhancing effect Effects 0.000 description 2
- 229960002464 fluoxetine Drugs 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- IUBSYMUCCVWXPE-UHFFFAOYSA-N metoprolol Chemical compound COCCC1=CC=C(OCC(O)CNC(C)C)C=C1 IUBSYMUCCVWXPE-UHFFFAOYSA-N 0.000 description 2
- 229960002237 metoprolol Drugs 0.000 description 2
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- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 2
- FSQFFCPJTDFOAN-CDHBEYIESA-N (4r,4as,7r,7ar,12bs)-3-(cyclopropylmethyl)-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,7,9-triol;hydrochloride Chemical compound Cl.C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@H]3O)CN2CC1CC1 FSQFFCPJTDFOAN-CDHBEYIESA-N 0.000 description 1
- IKBZAUYPBWFMDI-UHFFFAOYSA-N 5-bromo-4-methoxy-7-methyl-2,3-dihydro-1h-indene Chemical compound C1=C(Br)C(OC)=C2CCCC2=C1C IKBZAUYPBWFMDI-UHFFFAOYSA-N 0.000 description 1
- 206010010774 Constipation Diseases 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
- 206010019233 Headaches Diseases 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 102000004877 Insulin Human genes 0.000 description 1
- 108090001061 Insulin Proteins 0.000 description 1
- 238000008214 LDL Cholesterol Methods 0.000 description 1
- 235000014443 Pyrus communis Nutrition 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 208000037063 Thinness Diseases 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 238000000540 analysis of variance Methods 0.000 description 1
- 230000036528 appetite Effects 0.000 description 1
- 235000019789 appetite Nutrition 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 229960004367 bupropion hydrochloride Drugs 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 238000011260 co-administration Methods 0.000 description 1
- 238000011284 combination treatment Methods 0.000 description 1
- 239000011162 core material Substances 0.000 description 1
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- 235000020931 dietary conditions Nutrition 0.000 description 1
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- 208000035475 disorder Diseases 0.000 description 1
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- 239000003937 drug carrier Substances 0.000 description 1
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- 206010013781 dry mouth Diseases 0.000 description 1
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- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 229960004715 morphine sulfate Drugs 0.000 description 1
- GRVOTVYEFDAHCL-RTSZDRIGSA-N morphine sulfate pentahydrate Chemical compound O.O.O.O.O.OS(O)(=O)=O.O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O.O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O GRVOTVYEFDAHCL-RTSZDRIGSA-N 0.000 description 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 description 1
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- RCOBKSKAZMVBHT-TVQRCGJNSA-N radafaxine Chemical compound C[C@@H]1NC(C)(C)CO[C@@]1(O)C1=CC=CC(Cl)=C1 RCOBKSKAZMVBHT-TVQRCGJNSA-N 0.000 description 1
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Classifications
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61M21/00—Other devices or methods to cause a change in the state of consciousness; Devices for producing or ending sleep by mechanical, optical, or acoustical means, e.g. for hypnosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Acoustics & Sound (AREA)
- Biomedical Technology (AREA)
- Anesthesiology (AREA)
- Physics & Mathematics (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Medicinal Preparation (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020217015625A KR102391511B1 (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41939510P | 2010-12-03 | 2010-12-03 | |
| US61/419,395 | 2010-12-03 | ||
| KR1020197014576A KR102105857B1 (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
| PCT/US2011/063177 WO2012075459A1 (en) | 2010-12-03 | 2011-12-02 | Increasing drug bioavailability in naltrexone therapy |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197014576A Division KR102105857B1 (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020217015625A Division KR102391511B1 (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20200044158A KR20200044158A (ko) | 2020-04-28 |
| KR102258043B1 true KR102258043B1 (ko) | 2021-05-28 |
Family
ID=46172304
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020207011510A Active KR102258043B1 (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
| KR1020137017317A Ceased KR20140035320A (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
| KR1020197014576A Active KR102105857B1 (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
| KR1020217015625A Active KR102391511B1 (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
| KR1020187016354A Active KR101984500B1 (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020137017317A Ceased KR20140035320A (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
| KR1020197014576A Active KR102105857B1 (ko) | 2010-12-03 | 2011-12-02 | 날트렉손 요법에서 약물 생체이용률의 증가 |
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| PT2316456T (pt) | 2003-04-29 | 2017-09-05 | Orexigen Therapeutics Inc | Composições para afetar a perda de peso compreendendo naltrexona e bupropion |
| CN101370488B (zh) | 2005-11-22 | 2012-07-18 | 奥雷西根治疗公司 | 增加胰岛素敏感性的组合物 |
| WO2007089318A2 (en) * | 2005-11-23 | 2007-08-09 | Orexigen Therapeutics, Inc. | Compositions and methods for reducing food cravings |
| MX2010012909A (es) | 2008-05-30 | 2011-02-25 | Orexigen Therapeutics Inc | Metodos para tratamiento de condiciones de grasa visceral. |
| KR101841442B1 (ko) | 2010-01-11 | 2018-03-23 | 오렉시젠 세러퓨틱스 인크. | 주우울증 환자들에 있어서 체중 감량 치료를 제공하는 방법 |
| JP6008866B2 (ja) * | 2010-12-03 | 2016-10-19 | オレキシジェン・セラピューティクス・インコーポレーテッド | ナルトレキソン療法における薬物バイオアベイラビリティの増加 |
| IL300868A (en) | 2012-06-06 | 2023-04-01 | Orexigen Therapeutics Inc | Methods for treating overweight and obesity |
| EP3253379A4 (en) * | 2015-02-07 | 2018-10-10 | Intas Pharmaceuticals Limited | Pharmaceutical composition for the treatment of obesity |
| KR20200072445A (ko) * | 2017-03-28 | 2020-06-22 | 엘디엔 파마 리미티드 | 암의 치료를 위한 세포 사멸의 bcl2-관련 효능제의 발현을 증가시키는 제제 |
| EP3482751A1 (en) * | 2017-11-14 | 2019-05-15 | LDN Pharma Limited | Cancer treatment |
| US12303604B1 (en) | 2024-10-16 | 2025-05-20 | Currax Pharmaceuticals Llc | Pharmaceutical formulations comprising naltrexone and/or bupropion |
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| US20080013026A1 (en) | 2006-06-30 | 2008-01-17 | Lg Philips Lcd Co., Ltd. | In-plane switching mode liquid crystal display device and method of fabricating the same |
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