HRP20201818T1 - Proces pripreme hidroklorida s niskim udjelom abuk oksimorfona - Google Patents
Proces pripreme hidroklorida s niskim udjelom abuk oksimorfona Download PDFInfo
- Publication number
- HRP20201818T1 HRP20201818T1 HRP20201818TT HRP20201818T HRP20201818T1 HR P20201818 T1 HRP20201818 T1 HR P20201818T1 HR P20201818T T HRP20201818T T HR P20201818TT HR P20201818 T HRP20201818 T HR P20201818T HR P20201818 T1 HRP20201818 T1 HR P20201818T1
- Authority
- HR
- Croatia
- Prior art keywords
- process according
- propanol
- hydrochloric acid
- oxymorphone hydrochloride
- water
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 11
- BCGJBQBWUGVESK-KCTCKCTRSA-N Oxymorphone hydrochloride Chemical compound Cl.O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BCGJBQBWUGVESK-KCTCKCTRSA-N 0.000 title claims 4
- 229960005374 oxymorphone hydrochloride Drugs 0.000 title claims 3
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 15
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 5
- 238000002360 preparation method Methods 0.000 claims 4
- 238000004821 distillation Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- VFNHLTBRAFJQER-ISWURRPUSA-N (4r,4as,7ar,12bs)-4a,9-dihydroxy-3-methyl-2,4,7a,13-tetrahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one Chemical compound O=C([C@@H]1O2)C=C[C@@]3(O)[C@]4([H])N(C)CC[C@]13C1=C2C(O)=CC=C1C4 VFNHLTBRAFJQER-ISWURRPUSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 238000003109 Karl Fischer titration Methods 0.000 claims 1
- UQCNKQCJZOAFTQ-ISWURRPUSA-N Oxymorphone Chemical compound O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O UQCNKQCJZOAFTQ-ISWURRPUSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 229910000041 hydrogen chloride Inorganic materials 0.000 claims 1
- IXCSERBJSXMMFS-UHFFFAOYSA-N hydrogen chloride Substances Cl.Cl IXCSERBJSXMMFS-UHFFFAOYSA-N 0.000 claims 1
- 238000005984 hydrogenation reaction Methods 0.000 claims 1
- 229960005118 oxymorphone Drugs 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 238000010992 reflux Methods 0.000 claims 1
Classifications
-
- 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
-
- 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
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Emergency Medicine (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pain & Pain Management (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (9)
1. Proces za pripremu pripravka oksimorfon hidroklorida koji sadrži:
(i) hidrogeniranje osnovnog pripravka oksimorfona koji ima više od 10 ppm 14-hidroksimorfinona u mješavini koja sadrži 1-propanol, vodu i solnu kiselinu;
(ii) uklanjanje dijela 1-propanola i vode u koraku (i) radi smanjenja sadržaja vode u mješavini;
i
(iii) dodavanje 1-propanola u mješavinu;
pri čemu je pripravak oksimorfon hidroklorida oblik oksimorfon hidroklorid forme I koji ima manje od 10 ppm 14-hidroksimorfinona, i koji je:
• u osnovi bez drugih oblika;
• ima XRPD difrakcijski uzorak kako je prikazano na slici 3; i
• vrijednosti ° 2Θ mogu imati varijacije od + 0.2 ° 2Θ.
2. Proces prema zahtjevu 1, naznačen time što korak hidrogeniranja uključuje uporabu plinovitog vodika.
3. Proces prema zahtjevu 1, naznačen time što je solna kiselina a) koncentrirana solna kiselina; ili b) razrijeđena solna kiselina.
4. Proces prema zahtjevu 1, naznačen time što kiselina je otopina klorovodika u 1-propanolu.
5. Proces prema zahtjevu 1, naznačen time što se dio 1-propanol i vode u koraku (i) uklanjaju destilacijom.
6. Proces prema zahtjevu 5, naznačen time što je destilacija pod vakuumom.
7. Proces prema zahtjevu 1, naznačen time što se proces odvija na povišenoj temperaturi.
8. Proces prema zahtjevu 7, naznačen time što povišena temperatura a) je temperatura refluksa postupka destilacije; ili b) 45 ° C do 65 ° C.
9. Proces prema zahtjevu 1, naznačen time što se sadržaj vode smanjuje na oko manje od 10% titracijom po Karlu Fischeru.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14/608,544 US9918979B2 (en) | 2015-01-29 | 2015-01-29 | Process of preparing low ABUK oxymorphone hydrochloride |
| EP16703889.2A EP3250574B1 (en) | 2015-01-29 | 2016-01-27 | Process of preparing low abuk oxymorphone hydrochloride |
| PCT/US2016/015096 WO2016123202A1 (en) | 2015-01-29 | 2016-01-27 | Process of preparing low abuk oxymorphone hydrochloride |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20201818T1 true HRP20201818T1 (hr) | 2021-01-22 |
Family
ID=55346212
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20201818TT HRP20201818T1 (hr) | 2015-01-29 | 2020-11-16 | Proces pripreme hidroklorida s niskim udjelom abuk oksimorfona |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9918979B2 (hr) |
| EP (1) | EP3250574B1 (hr) |
| JP (1) | JP6726194B2 (hr) |
| CN (1) | CN107428767B (hr) |
| CA (1) | CA2975470C (hr) |
| DK (1) | DK3250574T3 (hr) |
| ES (1) | ES2836446T3 (hr) |
| HR (1) | HRP20201818T1 (hr) |
| HU (1) | HUE052641T2 (hr) |
| WO (1) | WO2016123202A1 (hr) |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US3916899A (en) | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| GB1478759A (en) | 1974-11-18 | 1977-07-06 | Alza Corp | Process for forming outlet passageways in pills using a laser |
| DE2530563C2 (de) | 1975-07-09 | 1986-07-24 | Bayer Ag, 5090 Leverkusen | Analgetische Arzneimittel mit vermindertem Mißbrauchspotential |
| US4063064A (en) | 1976-02-23 | 1977-12-13 | Coherent Radiation | Apparatus for tracking moving workpiece by a laser beam |
| US4200098A (en) | 1978-10-23 | 1980-04-29 | Alza Corporation | Osmotic system with distribution zone for dispensing beneficial agent |
| US4285987A (en) | 1978-10-23 | 1981-08-25 | Alza Corporation | Process for manufacturing device with dispersion zone |
| US4861598A (en) | 1986-07-18 | 1989-08-29 | Euroceltique, S.A. | Controlled release bases for pharmaceuticals |
| DE3812567A1 (de) | 1988-04-15 | 1989-10-26 | Basf Ag | Verfahren zur herstellung pharmazeutischer mischungen |
| US5215758A (en) | 1991-09-11 | 1993-06-01 | Euroceltique, S.A. | Controlled release matrix suppository for pharmaceuticals |
| US5472712A (en) | 1991-12-24 | 1995-12-05 | Euroceltique, S.A. | Controlled-release formulations coated with aqueous dispersions of ethylcellulose |
| US5273760A (en) | 1991-12-24 | 1993-12-28 | Euroceltigue, S.A. | Stabilized controlled release substrate having a coating derived from an aqueous dispersion of hydrophobic polymer |
| US5286493A (en) | 1992-01-27 | 1994-02-15 | Euroceltique, S.A. | Stabilized controlled release formulations having acrylic polymer coating |
| US5324351A (en) | 1992-08-13 | 1994-06-28 | Euroceltique | Aqueous dispersions of zein and preparation thereof |
| GB9401894D0 (en) | 1994-02-01 | 1994-03-30 | Rhone Poulenc Rorer Ltd | New compositions of matter |
| ATE376832T1 (de) | 2001-07-06 | 2007-11-15 | Penwest Pharmaceuticals Co | Verzögert freisetzende formulierungen von oxymorphon |
| CA2452871C (en) | 2001-07-06 | 2011-10-04 | Endo Pharmaceuticals, Inc. | Oxymorphone controlled release formulations |
| DE10336400A1 (de) | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| TWI483944B (zh) | 2004-03-30 | 2015-05-11 | Euro Celtique Sa | 含有小於２５ｐｐｍ１４-羥可待因酮之羥可酮鹽酸鹽組成物、醫藥劑型、延遲釋出口服劑型及醫藥上可以接受的包裝 |
| JP5695296B2 (ja) * | 2006-03-02 | 2015-04-01 | マリンクロッド エルエルシー | 低レベルのアルファ，ベータ−不飽和ケトン化合物を伴うモルフィナン−６−オン生成物の製造方法 |
| AU2007313103C1 (en) | 2006-10-17 | 2014-01-30 | Penick Corporation | Process for preparing oxymorphone |
| GB0624880D0 (en) * | 2006-12-14 | 2007-01-24 | Johnson Matthey Plc | Improved method for making analgesics |
| CN102116942B (zh) * | 2009-12-31 | 2013-02-13 | 清华大学 | 热致显示元件及热致显示装置 |
| US8563571B2 (en) | 2010-07-22 | 2013-10-22 | Noramco, Inc. | Crystalline forms of oxymorphone hydrochloride |
| EP2714695A1 (en) | 2011-05-27 | 2014-04-09 | Grünenthal GmbH | Crystalline, anhydrous forms of oxymorphone hydrochloride |
| AU2013274407B2 (en) * | 2012-06-11 | 2017-06-22 | Siegfried Ag | Improved method of preparing oxymorphone |
| GB2517000B (en) * | 2013-08-02 | 2018-05-09 | Johnson Matthey Plc | Process for the synthesis of oxymorphone alkaloid and oxymorphone salts |
-
2015
- 2015-01-29 US US14/608,544 patent/US9918979B2/en active Active
-
2016
- 2016-01-27 CN CN201680015394.5A patent/CN107428767B/zh active Active
- 2016-01-27 CA CA2975470A patent/CA2975470C/en active Active
- 2016-01-27 WO PCT/US2016/015096 patent/WO2016123202A1/en active Application Filing
- 2016-01-27 ES ES16703889T patent/ES2836446T3/es active Active
- 2016-01-27 DK DK16703889.2T patent/DK3250574T3/da active
- 2016-01-27 JP JP2017540604A patent/JP6726194B2/ja active Active
- 2016-01-27 EP EP16703889.2A patent/EP3250574B1/en active Active
- 2016-01-27 HU HUE16703889A patent/HUE052641T2/hu unknown
-
2020
- 2020-11-16 HR HRP20201818TT patent/HRP20201818T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3250574A1 (en) | 2017-12-06 |
| HUE052641T2 (hu) | 2021-05-28 |
| EP3250574B1 (en) | 2020-09-09 |
| CN107428767B (zh) | 2019-06-18 |
| US20160220560A1 (en) | 2016-08-04 |
| JP6726194B2 (ja) | 2020-07-22 |
| CA2975470A1 (en) | 2016-08-04 |
| CA2975470C (en) | 2023-03-21 |
| WO2016123202A1 (en) | 2016-08-04 |
| ES2836446T3 (es) | 2021-06-25 |
| CN107428767A (zh) | 2017-12-01 |
| JP2018507193A (ja) | 2018-03-15 |
| US9918979B2 (en) | 2018-03-20 |
| DK3250574T3 (da) | 2020-12-07 |
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