HRP20200029T1 - Kristalni tapentadol fosfat - Google Patents
Kristalni tapentadol fosfat Download PDFInfo
- Publication number
- HRP20200029T1 HRP20200029T1 HRP20200029TT HRP20200029T HRP20200029T1 HR P20200029 T1 HRP20200029 T1 HR P20200029T1 HR P20200029T T HRP20200029T T HR P20200029TT HR P20200029 T HRP20200029 T HR P20200029T HR P20200029 T1 HRP20200029 T1 HR P20200029T1
- Authority
- HR
- Croatia
- Prior art keywords
- crystalline
- tapentadol
- tapentadol phosphate
- phosphate according
- crystalline tapentadol
- Prior art date
Links
- KWTWDQCKEHXFFR-SMDDNHRTSA-N tapentadol Chemical compound CN(C)C[C@H](C)[C@@H](CC)C1=CC=CC(O)=C1 KWTWDQCKEHXFFR-SMDDNHRTSA-N 0.000 title claims 20
- 229960005126 tapentadol Drugs 0.000 title claims 20
- 229910019142 PO4 Inorganic materials 0.000 title claims 15
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 title claims 15
- 239000010452 phosphate Substances 0.000 title claims 15
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
- 150000001768 cations Chemical class 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- FKNQFGJONOIPTF-UHFFFAOYSA-N Sodium cation Chemical compound [Na+] FKNQFGJONOIPTF-UHFFFAOYSA-N 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- XLYOFNOQVPJJNP-ZSJDYOACSA-N heavy water Substances [2H]O[2H] XLYOFNOQVPJJNP-ZSJDYOACSA-N 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 235000019799 monosodium phosphate Nutrition 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims 1
- 229910000162 sodium phosphate Inorganic materials 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 238000002411 thermogravimetry Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C215/48—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups
- C07C215/54—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pain & Pain Management (AREA)
- Pharmacology & Pharmacy (AREA)
- Rheumatology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Claims (15)
1. Kristalni tapentadol fosfat.
2. Kristalni tapentadol fosfat prema patentnom zahtjevu 1 naznačen time što ima sadržaj vode od 0,5 do 4,0% određen termogravimetrijom.
3. Kristalni tapentadol fosfat prema patentnom zahtjevu 1 ili 2, naznačen time što ima karakteristične vrhove rendgenske difrakcije na prahu kod 5,1, 14.,4, 17,7, 18,3 i 21,0 stupnjeva 2θ (± 0,2 stupnjeva 2θ).
4. Kristalni tapentadol fosfat prema bilo kojem od patentnih zahtjeva 1 do 3 u kombinaciji s MHPO4 ili M'2HPO4, pri čemu M je dvovalentni kation i M' je jednovalentni kation.
5. Kristalni tapentadol fosfat prema patentnom zahtjevu 4, naznačen time što M' je natrijev kation.
6. Kristalni tapentadol fosfat prema bilo kojem od patentnih zahtjeva 1 do 5, naznačen time što je prisutan u čvrstom obliku.
7. Kristalni tapentadol fosfat prema bilo kojem od patentnih zahtjeva 1 do 6, naznačen time što je prisutan u izoliranom obliku.
8. Postupak za pripravu kristalnog tapentadol fosfata prema bilo kojem od patentnih zahtjeva 1 do 7 naznačen time što sadrži korake
(a) osiguravanje tapentadola i fosforne kiseline
(b) mljevenje smjese iz koraka (a).
9. Postupak prema patentnom zahtjevu 8, naznačen time što u koraku (a) molarni omjer tapentadola prema fosfornoj kiselini je od 3:1 do 1:1.
10. Postupak za pripravu kristalnog tapentadol fosfata prema bilo kojem od patentnih zahtjeva 1 do 7 naznačen time što sadrži korake
(a') osiguravanje tapentadola i M(H2PO4)2 ili M'H2PO4
(b') mljevenje smjese iz koraka (a)
11. Postupak prema patentnom zahtjevu 10, naznačen time što M'H2PO4 je NaH2PO4×2H2O
12. Postupak prema bilo kojem od patentnih zahtjeva 8 do 11, naznačen time što se u koraku (a) ili (b) dodaje voda, pri čemu je maseni omjer tapentadola i vode od 50:1 do 500:1.
13. Postupak za pripravu kristalnog tapentadol fosfata prema bilo kojem od patentnih zahtjeva 1 do 7 naznačen time što sadrži korake
(a") osiguravanje smjese tapentadola i fosforne kiseline u otapalu,
(b") stvaranje kristala smjese iz koraka (a") s kristalnim tapentadol fosfatom,
(c") izoliranje kristalnog tapentadol fosfata.
14. Farmaceutski pripravak naznačen time što sadrži kristalni tapentadol fosfat prema bilo kojem od patentnih zahtjeva 1 do 7 i nadalje barem jednu farmaceutski prihvatljivu pomoćnu tvar.
15. Kristalni tapentadol fosfat prema bilo kojem od patentnih zahtjeva 1 do 7 naznačen time što je za uporabu za liječenje bola.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16166101 | 2016-04-19 | ||
| EP16166099 | 2016-04-19 | ||
| EP16170781 | 2016-05-23 | ||
| EP16170780 | 2016-05-23 | ||
| EP17716933.1A EP3445742B1 (en) | 2016-04-19 | 2017-04-18 | Crystalline tapentadol phosphate |
| PCT/EP2017/059125 WO2017182438A1 (en) | 2016-04-19 | 2017-04-18 | Crystalline tapentadol phosphate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20200029T1 true HRP20200029T1 (hr) | 2020-03-20 |
Family
ID=58537027
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20200029TT HRP20200029T1 (hr) | 2016-04-19 | 2020-01-09 | Kristalni tapentadol fosfat |
Country Status (7)
| Country | Link |
|---|---|
| EP (3) | EP3653599B1 (hr) |
| DK (3) | DK3445742T3 (hr) |
| ES (3) | ES2966219T3 (hr) |
| HR (1) | HRP20200029T1 (hr) |
| PL (3) | PL3819287T3 (hr) |
| PT (1) | PT3445742T (hr) |
| WO (1) | WO2017182438A1 (hr) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3650439T (pt) | 2010-07-23 | 2021-03-03 | Gruenenthal Gmbh | Sais ou cocristais de 3-(3-dimetilamino-1-etil-2-metilpropil)fenol |
| AU2020100441B4 (en) * | 2020-03-02 | 2020-06-18 | Grünenthal GmbH | Dosage form providing prolonged release of tapentadol phosphoric acid salt |
| AU2020100442B4 (en) * | 2020-03-02 | 2020-06-18 | Grünenthal GmbH | Dosage form providing prolonged release of tapentadol phosphoric acid salt |
| EP3875080A1 (en) | 2020-03-02 | 2021-09-08 | Grünenthal GmbH | Dosage form providing prolonged release of tapentadol phosphoric acid salt |
| EP4003318A1 (en) | 2020-03-02 | 2022-06-01 | Grünenthal GmbH | Dosage form providing prolonged release of tapentadol phosphoric acid salt |
| PL3875077T3 (pl) * | 2020-03-02 | 2024-03-11 | Grünenthal GmbH | Postać dawkowania zapewniająca przedłużone uwalnianie soli kwasu fosforowego tapentadolu |
| DE202020104285U1 (de) | 2020-07-24 | 2020-12-18 | Grünenthal GmbH | Ethylcellulose-beschichtete Partikel enthaltend ein Salz aus Tapentadol und Phosphorsäure |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4426245A1 (de) | 1994-07-23 | 1996-02-22 | Gruenenthal Gmbh | 1-Phenyl-3-dimethylamino-propanverbindungen mit pharmakologischer Wirkung |
| DK1612203T3 (da) | 2004-06-28 | 2007-12-03 | Gruenenthal Gmbh | Krystallinske former af (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenolhydrochlorid |
| CN101939287B (zh) | 2007-12-07 | 2014-10-22 | 格吕伦塔尔有限公司 | (1r,2r)-3-(3-二甲基氨基-1-乙基-2-甲基-丙基)-苯酚的结晶变体 |
| PT3650439T (pt) | 2010-07-23 | 2021-03-03 | Gruenenthal Gmbh | Sais ou cocristais de 3-(3-dimetilamino-1-etil-2-metilpropil)fenol |
| WO2012051246A1 (en) | 2010-10-12 | 2012-04-19 | Ratiopharm Gmbh | Tapentadol hydrobromide and crystalline forms thereof |
-
2017
- 2017-04-18 ES ES20216224T patent/ES2966219T3/es active Active
- 2017-04-18 PL PL20216224.4T patent/PL3819287T3/pl unknown
- 2017-04-18 ES ES19208228T patent/ES2937740T3/es active Active
- 2017-04-18 PL PL17716933T patent/PL3445742T3/pl unknown
- 2017-04-18 PT PT177169331T patent/PT3445742T/pt unknown
- 2017-04-18 PL PL19208228.7T patent/PL3653599T3/pl unknown
- 2017-04-18 ES ES17716933T patent/ES2772806T3/es active Active
- 2017-04-18 DK DK17716933.1T patent/DK3445742T3/da active
- 2017-04-18 EP EP19208228.7A patent/EP3653599B1/en active Active
- 2017-04-18 WO PCT/EP2017/059125 patent/WO2017182438A1/en active Application Filing
- 2017-04-18 DK DK19208228.7T patent/DK3653599T3/da active
- 2017-04-18 EP EP17716933.1A patent/EP3445742B1/en active Active
- 2017-04-18 DK DK20216224.4T patent/DK3819287T3/da active
- 2017-04-18 EP EP20216224.4A patent/EP3819287B1/en active Active
-
2020
- 2020-01-09 HR HRP20200029TT patent/HRP20200029T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017182438A1 (en) | 2017-10-26 |
| EP3653599B1 (en) | 2022-12-14 |
| PL3819287T3 (pl) | 2024-03-11 |
| ES2937740T3 (es) | 2023-03-30 |
| EP3445742B1 (en) | 2019-11-13 |
| PT3445742T (pt) | 2020-02-19 |
| DK3819287T3 (da) | 2023-12-18 |
| PL3653599T3 (pl) | 2023-03-20 |
| EP3819287A1 (en) | 2021-05-12 |
| DK3445742T3 (da) | 2020-02-24 |
| EP3445742A1 (en) | 2019-02-27 |
| EP3653599A1 (en) | 2020-05-20 |
| PL3445742T3 (pl) | 2020-05-18 |
| ES2966219T3 (es) | 2024-04-19 |
| EP3819287B1 (en) | 2023-09-20 |
| ES2772806T3 (es) | 2020-07-08 |
| DK3653599T3 (da) | 2023-01-30 |
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