JP2015515982A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2015515982A5 JP2015515982A5 JP2015510266A JP2015510266A JP2015515982A5 JP 2015515982 A5 JP2015515982 A5 JP 2015515982A5 JP 2015510266 A JP2015510266 A JP 2015510266A JP 2015510266 A JP2015510266 A JP 2015510266A JP 2015515982 A5 JP2015515982 A5 JP 2015515982A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- opioid receptor
- receptor antagonist
- phosphatidylcholine
- solvent
- 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.)
- Withdrawn
Links
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims description 98
- 238000000034 method Methods 0.000 claims description 74
- 239000008194 pharmaceutical composition Substances 0.000 claims description 59
- 229940123257 Opioid receptor antagonist Drugs 0.000 claims description 39
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 38
- 239000003401 opiate antagonist Substances 0.000 claims description 38
- 239000002904 solvent Substances 0.000 claims description 36
- 239000000203 mixture Substances 0.000 claims description 33
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 30
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 24
- 230000005764 inhibitory process Effects 0.000 claims description 21
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 20
- 239000003937 drug carrier Substances 0.000 claims description 20
- 238000009472 formulation Methods 0.000 claims description 19
- 230000000694 effects Effects 0.000 claims description 15
- 208000003243 intestinal obstruction Diseases 0.000 claims description 12
- 206010010774 Constipation Diseases 0.000 claims description 11
- 206010000060 Abdominal distension Diseases 0.000 claims description 10
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 10
- 230000030135 gastric motility Effects 0.000 claims description 10
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 10
- 208000003251 Pruritus Diseases 0.000 claims description 8
- 206010046555 Urinary retention Diseases 0.000 claims description 8
- 208000002193 Pain Diseases 0.000 claims description 7
- 230000003247 decreasing effect Effects 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 238000001802 infusion Methods 0.000 claims description 6
- 229940079358 peripheral opioid receptor antagonist Drugs 0.000 claims description 6
- 230000028327 secretion Effects 0.000 claims description 6
- 208000008454 Hyperhidrosis Diseases 0.000 claims description 5
- 206010021518 Impaired gastric emptying Diseases 0.000 claims description 5
- 206010028813 Nausea Diseases 0.000 claims description 5
- 206010047700 Vomiting Diseases 0.000 claims description 5
- 238000012084 abdominal surgery Methods 0.000 claims description 5
- 208000024330 bloating Diseases 0.000 claims description 5
- 230000013872 defecation Effects 0.000 claims description 5
- 238000011010 flushing procedure Methods 0.000 claims description 5
- 230000030136 gastric emptying Effects 0.000 claims description 5
- 238000010438 heat treatment Methods 0.000 claims description 5
- 238000002347 injection Methods 0.000 claims description 5
- 239000007924 injection Substances 0.000 claims description 5
- 230000008991 intestinal motility Effects 0.000 claims description 5
- 230000004899 motility Effects 0.000 claims description 5
- 230000008693 nausea Effects 0.000 claims description 5
- 238000013268 sustained release Methods 0.000 claims description 5
- 239000012730 sustained-release form Substances 0.000 claims description 5
- 230000035900 sweating Effects 0.000 claims description 5
- 230000008673 vomiting Effects 0.000 claims description 5
- INAXVFBXDYWQFN-XHSDSOJGSA-N morphinan Chemical group C1C2=CC=CC=C2[C@]23CCCC[C@H]3[C@@H]1NCC2 INAXVFBXDYWQFN-XHSDSOJGSA-N 0.000 claims description 4
- 230000009467 reduction Effects 0.000 claims description 4
- 206010004663 Biliary colic Diseases 0.000 claims description 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 3
- 208000000094 Chronic Pain Diseases 0.000 claims description 3
- 206010062016 Immunosuppression Diseases 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 102000003840 Opioid Receptors Human genes 0.000 claims description 3
- 108090000137 Opioid Receptors Proteins 0.000 claims description 3
- 208000017442 Retinal disease Diseases 0.000 claims description 3
- 206010038923 Retinopathy Diseases 0.000 claims description 3
- 206010052428 Wound Diseases 0.000 claims description 3
- 208000027418 Wounds and injury Diseases 0.000 claims description 3
- 230000009471 action Effects 0.000 claims description 3
- 230000033115 angiogenesis Effects 0.000 claims description 3
- 210000000941 bile Anatomy 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 208000037976 chronic inflammation Diseases 0.000 claims description 3
- 230000006020 chronic inflammation Effects 0.000 claims description 3
- 239000006071 cream Substances 0.000 claims description 3
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims description 3
- 238000007654 immersion Methods 0.000 claims description 3
- 230000001506 immunosuppresive effect Effects 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 3
- 238000007913 intrathecal administration Methods 0.000 claims description 3
- 238000001990 intravenous administration Methods 0.000 claims description 3
- 230000002262 irrigation Effects 0.000 claims description 3
- 238000003973 irrigation Methods 0.000 claims description 3
- 150000002632 lipids Chemical class 0.000 claims description 3
- 230000001404 mediated effect Effects 0.000 claims description 3
- 230000001769 paralizing effect Effects 0.000 claims description 3
- 230000010412 perfusion Effects 0.000 claims description 3
- 230000002980 postoperative effect Effects 0.000 claims description 3
- 208000007056 sickle cell anemia Diseases 0.000 claims description 3
- 210000002784 stomach Anatomy 0.000 claims description 3
- 230000002792 vascular Effects 0.000 claims description 3
- PCSQOABIHJXZMR-MGQKVWQSSA-O (4r,4as,7ar,12bs)-4a,9-dihydroxy-3-methyl-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-3-ium-7-one Chemical compound O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CC[N+](C)(CC=C)[C@@H]3CC5=CC=C4O PCSQOABIHJXZMR-MGQKVWQSSA-O 0.000 claims description 2
- HJDWPCLBBHHTIG-NNJWZEOZSA-O (4r,7s,7ar,12bs)-3-methyl-3-prop-2-enyl-2,4,4a,7,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-3-ium-7,9-diol Chemical compound O([C@H]1[C@H](C=CC23)O)C4=C5[C@@]12CC[N+](C)(CC=C)[C@@H]3CC5=CC=C4O HJDWPCLBBHHTIG-NNJWZEOZSA-O 0.000 claims description 2
- JVLBPIPGETUEET-GAAHOAFPSA-O methylnaltrexone Chemical group C[N+]1([C@@H]2CC=3C4=C(C(=CC=3)O)O[C@@H]3[C@]4([C@@]2(O)CCC3=O)CC1)CC1CC1 JVLBPIPGETUEET-GAAHOAFPSA-O 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical group C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 230000000699 topical effect Effects 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- JVLBPIPGETUEET-WIXLDOGYSA-O (3r,4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-3-ium-7-one Chemical compound C([N@+]1(C)[C@@H]2CC=3C4=C(C(=CC=3)O)O[C@@H]3[C@]4([C@@]2(O)CCC3=O)CC1)C1CC1 JVLBPIPGETUEET-WIXLDOGYSA-O 0.000 description 38
- 229960002921 methylnaltrexone Drugs 0.000 description 38
- 230000005176 gastrointestinal motility Effects 0.000 description 4
- 239000011343 solid material Substances 0.000 description 4
- 238000001356 surgical procedure Methods 0.000 description 4
- 229940005483 opioid analgesics Drugs 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 2
- 239000005557 antagonist Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 230000001684 chronic effect Effects 0.000 description 2
- 239000000796 flavoring agent Substances 0.000 description 2
- 235000013355 food flavoring agent Nutrition 0.000 description 2
- 238000004108 freeze drying Methods 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 239000002502 liposome Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261642837P | 2012-05-04 | 2012-05-04 | |
| US61/642,837 | 2012-05-04 | ||
| PCT/US2013/031078 WO2013165577A1 (en) | 2012-05-04 | 2013-03-13 | Bioavailability of oral methylnaltrexone increases with a phosphatidylcholine-based formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015515982A JP2015515982A (ja) | 2015-06-04 |
| JP2015515982A5 true JP2015515982A5 (https=) | 2016-05-12 |
Family
ID=49514721
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015510266A Withdrawn JP2015515982A (ja) | 2012-05-04 | 2013-03-13 | 経口メチルナルトレキソンのバイオアベイラビリティはホスファチジルコリンベースの製剤で増加する |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20150190523A1 (https=) |
| EP (1) | EP2854537A4 (https=) |
| JP (1) | JP2015515982A (https=) |
| KR (1) | KR20150006877A (https=) |
| CN (1) | CN104470361A (https=) |
| AU (1) | AU2013257211A1 (https=) |
| BR (1) | BR112014027496A2 (https=) |
| CA (1) | CA2872400A1 (https=) |
| HK (1) | HK1207940A1 (https=) |
| IL (1) | IL235390A0 (https=) |
| IN (1) | IN2014DN09359A (https=) |
| MX (1) | MX2014013425A (https=) |
| WO (1) | WO2013165577A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016061531A1 (en) * | 2014-10-17 | 2016-04-21 | Salix Pharmaceuticals, Inc. | Use of methylnaltrexone to attenuate tumor progression |
| CA3177250A1 (en) * | 2020-05-02 | 2021-11-11 | Bausch Health Ireland Limited | Methods of reducing mortality risk in subjects suffering from an underlying disease or condition by administration of methylnaltrexone |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7846478B2 (en) * | 2002-01-31 | 2010-12-07 | Henkel Ag & Co. Kgaa | Bioadhesive composition |
| CN101432011A (zh) * | 2006-02-27 | 2009-05-13 | 亚历山大·米哈洛 | 通过诱导逆适应调节神经递质系统的方法 |
| EP2079456B1 (en) * | 2007-04-04 | 2012-12-05 | Sigmoid Pharma Limited | Pharmaceutical cyclosporin compositions |
| CA2729582C (en) * | 2008-07-01 | 2017-09-19 | University Of Chicago | Particles containing an opioid receptor antagonist and methods of use |
| US20110190267A1 (en) * | 2010-01-05 | 2011-08-04 | Shire Pharmaceuticals, Inc. | Prodrugs of opioids and uses thereof |
| US20120053130A1 (en) * | 2010-08-30 | 2012-03-01 | Bristol-Myers Squibb Company | Composition for enhancing absorption of a drug and method |
-
2013
- 2013-03-13 CA CA2872400A patent/CA2872400A1/en not_active Abandoned
- 2013-03-13 IN IN9359DEN2014 patent/IN2014DN09359A/en unknown
- 2013-03-13 JP JP2015510266A patent/JP2015515982A/ja not_active Withdrawn
- 2013-03-13 US US14/398,914 patent/US20150190523A1/en not_active Abandoned
- 2013-03-13 EP EP13785315.6A patent/EP2854537A4/en not_active Withdrawn
- 2013-03-13 HK HK15108676.7A patent/HK1207940A1/xx unknown
- 2013-03-13 AU AU2013257211A patent/AU2013257211A1/en not_active Abandoned
- 2013-03-13 KR KR20147034096A patent/KR20150006877A/ko not_active Withdrawn
- 2013-03-13 BR BR112014027496A patent/BR112014027496A2/pt not_active IP Right Cessation
- 2013-03-13 MX MX2014013425A patent/MX2014013425A/es unknown
- 2013-03-13 CN CN201380028597.4A patent/CN104470361A/zh active Pending
- 2013-03-13 WO PCT/US2013/031078 patent/WO2013165577A1/en not_active Ceased
-
2014
- 2014-10-29 IL IL235390A patent/IL235390A0/en unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR101230804B1 (ko) | 향상된 흡수를 갖는 경점막 전달 장치 | |
| ES2745210T3 (es) | Película oral que contiene cuentas de liberación entérica de opiáceos | |
| JP5985824B2 (ja) | オピオイド受容体アンタゴニスト含有の粒子および使用方法 | |
| EP2574167B1 (en) | Liquid nasal spray containing low-dose naltrexone | |
| CA2661759A1 (en) | Buprenophine-wafer for drug substitution therapy | |
| KR20100063106A (ko) | 난용성 약물의 전달을 위한 입상 조성물 | |
| CN103889508A (zh) | 用于传递丁丙诺啡的防滥用性粘膜粘附剂装置 | |
| CN102711759B (zh) | 胆道疾病的治疗或预防药 | |
| TW200418474A (en) | Method of treating post-operative nausea and vomiting | |
| JP2010520185A (ja) | ブプレノルフィンとナロキソンを含む改良医薬組成物 | |
| RU2683317C2 (ru) | Конъюгаты оксикодона с бензойной кислотой, производными бензойной кислоты и гетероарилкарбоновой кислотой | |
| CA2579378C (en) | Treatment of diseases using nalmefene and its analogs | |
| JP2015515982A5 (https=) | ||
| US20120164139A1 (en) | Dopamine 3 receptor agonist and antagonist treatment of gastrointestinal motility disorders | |
| KR20170091775A (ko) | 정맥 내 투여용 이부프로펜의 투여 | |
| CN1674903A (zh) | 经鼻吸收用组合物 | |
| RU2683274C2 (ru) | Бензойная кислота, производные бензойной кислоты и конъюгаты гетероарилкарбоновой кислоты и оксиморфона, их пролекарства, способы получения и применение | |
| JP2014505113A (ja) | 末梢作用性μオピオイドアンタゴニスト | |
| US10874658B2 (en) | Sublingual opioid formulations containing naloxone | |
| RU2561873C2 (ru) | Применение антагонистов опиоидных рецепторов при заболеваниях желудочно-кишечного тракта | |
| JPH0225427A (ja) | 慢性痛あるいは慢性咳を治療する経口用組成物 | |
| JP2013505260A5 (https=) | ||
| Neyens et al. | Novel opioid antagonists for opioid-induced bowel dysfunction and postoperative ileus | |
| JP2015515982A (ja) | 経口メチルナルトレキソンのバイオアベイラビリティはホスファチジルコリンベースの製剤で増加する | |
| AU2011254554B2 (en) | Liquid nasal spray containing low-dose naltrexone |