ZA201808498B - Oral formulations and lipophilic salts of methylnaltrexone - Google Patents
Oral formulations and lipophilic salts of methylnaltrexoneInfo
- Publication number
- ZA201808498B ZA201808498B ZA2018/08498A ZA201808498A ZA201808498B ZA 201808498 B ZA201808498 B ZA 201808498B ZA 2018/08498 A ZA2018/08498 A ZA 2018/08498A ZA 201808498 A ZA201808498 A ZA 201808498A ZA 201808498 B ZA201808498 B ZA 201808498B
- Authority
- ZA
- South Africa
- Prior art keywords
- methylnaltrexone
- oral formulations
- lipophilic salts
- lipophilic
- salts
- Prior art date
Links
- 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 class 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 title 1
- 238000009472 formulation Methods 0.000 title 1
- 229960002921 methylnaltrexone Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
Classifications
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- 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
- 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
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
- C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
- C07D489/08—Oxygen atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Emergency Medicine (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Inorganic Chemistry (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31301810P | 2010-03-11 | 2010-03-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA201808498B true ZA201808498B (en) | 2019-08-28 |
Family
ID=44148539
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA2018/08498A ZA201808498B (en) | 2010-03-11 | 2018-12-18 | Oral formulations and lipophilic salts of methylnaltrexone |
Country Status (32)
| Country | Link |
|---|---|
| US (8) | US8524276B2 (https=) |
| EP (2) | EP3178472B1 (https=) |
| JP (4) | JP6143409B2 (https=) |
| KR (2) | KR101913102B1 (https=) |
| CN (2) | CN102918039B (https=) |
| AR (1) | AR080491A1 (https=) |
| AU (1) | AU2011224275B2 (https=) |
| BR (1) | BR112012022873B1 (https=) |
| CA (1) | CA2789798C (https=) |
| CL (1) | CL2012002192A1 (https=) |
| CO (1) | CO6630134A2 (https=) |
| CR (1) | CR20120476A (https=) |
| EA (1) | EA029096B1 (https=) |
| EC (1) | ECSP12012208A (https=) |
| ES (1) | ES2623926T3 (https=) |
| GE (1) | GEP201606550B (https=) |
| GT (1) | GT201200247A (https=) |
| HU (1) | HUE033133T2 (https=) |
| IL (1) | IL221452A (https=) |
| MA (1) | MA34146B1 (https=) |
| MX (2) | MX349145B (https=) |
| MY (1) | MY160727A (https=) |
| NZ (3) | NZ702826A (https=) |
| PE (1) | PE20130063A1 (https=) |
| PH (1) | PH12012501622A1 (https=) |
| PL (2) | PL2371357T3 (https=) |
| SG (3) | SG183133A1 (https=) |
| TN (1) | TN2012000392A1 (https=) |
| TW (2) | TWI589293B (https=) |
| UA (2) | UA123856C2 (https=) |
| WO (1) | WO2011112816A1 (https=) |
| ZA (1) | ZA201808498B (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20150037T4 (hr) | 2003-04-08 | 2022-09-02 | Progenics Pharmaceuticals, Inc. | Farmaceutske formulacije koje sadrže metilnaltrekson |
| TWI489984B (zh) | 2006-08-04 | 2015-07-01 | Wyeth Corp | 用於非經腸道傳輸化合物之配方及其用途 |
| MX2009010550A (es) | 2007-03-29 | 2009-12-14 | Progenics Pharm Inc | Formas de cristal de bromuro de (r)-n-metilnaltrexona y uso de las mismas. |
| WO2008153725A2 (en) | 2007-05-25 | 2008-12-18 | North Carolina State University | Viral nanoparticle cell-targeted delivery platform |
| UA123856C2 (uk) | 2010-03-11 | 2021-06-16 | Уайт Елелсі | Фармацевтичні композиції метилналтрексону та натрію додецилсульфату для перорального введення |
| US8627816B2 (en) | 2011-02-28 | 2014-01-14 | Intelliject, Inc. | Medicament delivery device for administration of opioid antagonists including formulations for naloxone |
| US8939943B2 (en) | 2011-01-26 | 2015-01-27 | Kaleo, Inc. | Medicament delivery device for administration of opioid antagonists including formulations for naloxone |
| KR20140107540A (ko) * | 2011-12-19 | 2014-09-04 | 샐릭스 파마슈티컬스 리미티드 | 메틸날트렉손의 경구 조성물을 사용하는 오피오이드 유발성 변비의 치료 및 예방 방법 |
| WO2015191686A1 (en) * | 2014-06-10 | 2015-12-17 | Salix Pharmaceuticals, Inc. | Methods of administering methylnaltrexone |
| US10722510B2 (en) * | 2014-07-08 | 2020-07-28 | Hikma Pharmaceuticals Usa Inc. | Liquid naloxone spray |
| US11135155B2 (en) | 2014-07-08 | 2021-10-05 | Hikma Pharmaceuticals Usa Inc. | Liquid naloxone spray |
| CA2954370A1 (en) * | 2014-07-08 | 2016-01-14 | Insys Pharma, Inc. | Sublingual naloxone spray |
| US10617686B2 (en) * | 2014-07-08 | 2020-04-14 | Hikma Pharmaceuticals Usa Inc. | Liquid naloxone spray |
| US10441538B2 (en) * | 2014-07-08 | 2019-10-15 | Hikma Pharmaceuticals Usa Inc. | Liquid naloxone spray |
| WO2016061531A1 (en) | 2014-10-17 | 2016-04-21 | Salix Pharmaceuticals, Inc. | Use of methylnaltrexone to attenuate tumor progression |
| WO2020128583A1 (en) * | 2018-12-19 | 2020-06-25 | Friulchem S.P.A. | Process for the manufacture of a tablet of rifaximin and tablet of rifaximin |
| BR112021022194A2 (pt) * | 2019-05-07 | 2021-12-28 | Bausch Health Ireland Ltd | Formulações líquidas para dosagem oral de metilnaltrexona |
| WO2020245214A1 (en) | 2019-06-03 | 2020-12-10 | Bausch Health Ireland Limited | Use of methylnaltrexone and rifaximin for treatment of increased gut permeability or associated disorders |
| 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 |
| WO2023031955A1 (en) * | 2021-08-28 | 2023-03-09 | Redasani Vijayendrakumar Virendrakumar Ji | Oral pharmaceutical compositions of methylnaltrexone and salt thereof |
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| US4176186A (en) | 1978-07-28 | 1979-11-27 | Boehringer Ingelheim Gmbh | Quaternary derivatives of noroxymorphone which relieve intestinal immobility |
| US4719215A (en) | 1986-03-07 | 1988-01-12 | University Of Chicago | Quaternary derivatives of noroxymorphone which relieve nausea and emesis |
| US4861781A (en) | 1986-03-07 | 1989-08-29 | The University Of Chicago | Quaternary derivatives of noroxymorphone which relieve nausea and emesis |
| CA1297218C (en) | 1986-03-14 | 1992-03-10 | Edward David Weil | Thermally stable diphosphonate-type flame retardant additive for plastics |
| US5102887A (en) | 1989-02-17 | 1992-04-07 | Arch Development Corporation | Method for reducing emesis and nausea induced by the administration of an emesis causing agent |
| US5780012A (en) | 1990-06-21 | 1998-07-14 | Huland; Edith | Method for reducing lung afflictions by inhalation of cytokine solutions |
| AU5171293A (en) | 1992-10-14 | 1994-05-09 | Regents Of The University Of Colorado, The | Ion-pairing of drugs for improved efficacy and delivery |
| US5866154A (en) | 1994-10-07 | 1999-02-02 | The Dupont Merck Pharmaceutical Company | Stabilized naloxone formulations |
| DE19651551C2 (de) | 1996-12-11 | 2000-02-03 | Klinge Co Chem Pharm Fab | Opioidantagonisthaltige galenische Formulierung |
| WO1998035679A1 (de) | 1997-02-14 | 1998-08-20 | Gödecke Aktiengesellschaft | Stabilisierung von naloxonhydrochlorid |
| US6274591B1 (en) | 1997-11-03 | 2001-08-14 | Joseph F. Foss | Use of methylnaltrexone and related compounds |
| ATE210983T1 (de) | 1997-11-03 | 2002-01-15 | Stada Arzneimittel Ag | Stabilisiertes kombinationsarzneimittel enthaltend naloxone und ein opiatanalgetikum |
| US20030158220A1 (en) | 1997-11-03 | 2003-08-21 | Foss Joseph F. | Use of methylnaltrexone and related compounds to treat chronic opioid use side effects |
| US5972954A (en) | 1997-11-03 | 1999-10-26 | Arch Development Corporation | Use of methylnaltrexone and related compounds |
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| US20030022909A1 (en) | 2001-06-05 | 2003-01-30 | University Of Chicago | Use of methylnaltrexone to treat immune suppression |
| ES2654819T3 (es) | 2001-10-18 | 2018-02-15 | Nektar Therapeutics | Conjugados poliméricos de antagonistas de opioides |
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| MXPA05010819A (es) | 2003-04-08 | 2006-03-30 | Progenics Pharm Inc | Uso de antagonistas de opioide perifericos, especialmente metilnaltrexona para tratar sindrome de intestino irritable. |
| HRP20150037T4 (hr) | 2003-04-08 | 2022-09-02 | Progenics Pharmaceuticals, Inc. | Farmaceutske formulacije koje sadrže metilnaltrekson |
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| JP5165239B2 (ja) * | 2003-07-15 | 2013-03-21 | ピーアール ファーマシューティカルズ， インコーポレイテッド | 制御放出処方物の調製のための方法 |
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| CN101061073A (zh) | 2004-09-30 | 2007-10-24 | 贝克顿·迪金森公司 | 减少或消除玻璃容器中残余物的方法以及根据该方法制成的玻璃容器 |
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| AR057035A1 (es) * | 2005-05-25 | 2007-11-14 | Progenics Pharm Inc | SíNTESIS DE (R)-N-METILNALTREXONA, COMPOSICIONES FARMACÉUTICAS Y USOS |
| TWI489984B (zh) * | 2006-08-04 | 2015-07-01 | Wyeth Corp | 用於非經腸道傳輸化合物之配方及其用途 |
| WO2008021394A2 (en) * | 2006-08-15 | 2008-02-21 | Theraquest Biosciences, Llc | Pharmaceutical formulations of cannabinoids and method of use |
| JP4970542B2 (ja) * | 2006-08-16 | 2012-07-11 | ノバルティス アーゲー | 有色レンズケア溶液の時間的光漂白及びその使用 |
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| JP5525247B2 (ja) * | 2009-08-04 | 2014-06-18 | 株式会社神戸製鋼所 | 高強度で曲げ加工性に優れた銅合金 |
| UA123856C2 (uk) | 2010-03-11 | 2021-06-16 | Уайт Елелсі | Фармацевтичні композиції метилналтрексону та натрію додецилсульфату для перорального введення |
| TW201235609A (en) * | 2010-07-13 | 2012-09-01 | Koninkl Philips Electronics Nv | Low cost mounting of LEDs in TL-retrofit tubes |
-
2011
- 2011-03-10 UA UAA201602306A patent/UA123856C2/uk unknown
- 2011-03-10 TW TW100108143A patent/TWI589293B/zh active
- 2011-03-10 US US13/045,108 patent/US8524276B2/en active Active
- 2011-03-10 NZ NZ702826A patent/NZ702826A/en unknown
- 2011-03-10 MA MA35290A patent/MA34146B1/fr unknown
- 2011-03-10 PE PE2012001538A patent/PE20130063A1/es active IP Right Grant
- 2011-03-10 GE GEAP201112868A patent/GEP201606550B/en unknown
- 2011-03-10 WO PCT/US2011/027913 patent/WO2011112816A1/en not_active Ceased
- 2011-03-10 KR KR1020127026488A patent/KR101913102B1/ko active Active
- 2011-03-10 AU AU2011224275A patent/AU2011224275B2/en active Active
- 2011-03-10 SG SG2012057261A patent/SG183133A1/en unknown
- 2011-03-10 NZ NZ601595A patent/NZ601595A/en unknown
- 2011-03-10 JP JP2011052316A patent/JP6143409B2/ja active Active
- 2011-03-10 TW TW105105359A patent/TWI605814B/zh active
- 2011-03-10 AR ARP110100757A patent/AR080491A1/es unknown
- 2011-03-10 EA EA201270741A patent/EA029096B1/ru unknown
- 2011-03-10 BR BR112012022873-0A patent/BR112012022873B1/pt active IP Right Grant
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2012
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