HRP20231343T1 - Liofilizat od treosulfana - Google Patents
Liofilizat od treosulfana Download PDFInfo
- Publication number
- HRP20231343T1 HRP20231343T1 HRP20231343TT HRP20231343T HRP20231343T1 HR P20231343 T1 HRP20231343 T1 HR P20231343T1 HR P20231343T T HRP20231343T T HR P20231343TT HR P20231343 T HRP20231343 T HR P20231343T HR P20231343 T1 HRP20231343 T1 HR P20231343T1
- Authority
- HR
- Croatia
- Prior art keywords
- weight
- lyophilizate
- mbar
- temperature
- mass
- Prior art date
Links
- YCPOZVAOBBQLRI-WDSKDSINSA-N Treosulfan Chemical compound CS(=O)(=O)OC[C@H](O)[C@@H](O)COS(C)(=O)=O YCPOZVAOBBQLRI-WDSKDSINSA-N 0.000 title claims 5
- 229960003181 treosulfan Drugs 0.000 title claims 5
- 238000000034 method Methods 0.000 claims 12
- 238000001035 drying Methods 0.000 claims 10
- 239000000243 solution Substances 0.000 claims 6
- 239000007864 aqueous solution Substances 0.000 claims 5
- 238000007710 freezing Methods 0.000 claims 4
- 230000008014 freezing Effects 0.000 claims 4
- 238000001816 cooling Methods 0.000 claims 3
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Natural products CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 238000002441 X-ray diffraction Methods 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 1
- 210000000601 blood cell Anatomy 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000001143 conditioned effect Effects 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004108 freeze drying Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229940098779 methanesulfonic acid Drugs 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C309/07—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton
- C07C309/08—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton containing hydroxy groups bound to the carbon skeleton
-
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Claims (24)
1. Liofilizat od treosulfana, naznačen time, da liofilizat sadrži najmanje 75% po masi kristalnog oblika B od treosulfana koji prikazuje uzorak rendgenske difrakcije na prahu s karakterističnim maksimumima na 20,87 i 23,47 ± 0,2 stupnja 2Θ, mjereno uporabom Cu-Kα1 = 1,54059 Å, u odnosu na količinu liofilizata.
2. Liofilizat prema patentnom zahtjevu 1, naznačen time, da kristalni oblik B prikazuje uzorak rendgenske difrakcije na prahu s karakterističnim maksimumima na 20,87, 23,47, 26,20, 29,65, 30,81, 34,54, 35,30, 36,87 i 46,24 ± 0,2 stupnja 2Θ.
3. Liofilizat prema patentnom zahtjevu 1 ili 2, naznačen time, da kristalni oblik B prikazuje uzorak rendgenske difrakcije na prahu, uglavnom kako je prikazano na Slici 1.
4. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da kristalni oblik B prikazuje uzorak rendgenske difrakcije na prahu koji nema maksimume u barem jednoj, a poželjno u svim regijama koje slijede od a do f, izraženima u stupnjevima 2Θ:
Regija Stupnjevi 2Θ
a 19,00 – 19,50
b 20,00 – 20,65
c 21,50 – 23,21
d 23,75 – 24,95
e 27,40 – 28,35
f 30,00 – 30,60
5. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time, da sadrži najmanje 96% po masi, prvenstveno najmanje 97% po masi, poželjno najmanje 98% po masi i još poželjnije najmanje 99% po masi kristalnog oblika B, u odnosu na sastavljenu količinu kristalnog oblika B i kristalnog oblika A.
6. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time, da sadrži najmanje 80% po masi, poželjno najmanje 85% po masi, još poželjnije najmanje 90% po masi, i čak još poželjnije najmanje 95% po masi kristalnog oblika B, u odnosu na količinu liofilizata.
7. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 6, naznačen time, da sadrži manje od 20% po masi, prvenstveno manje od 15% po masi, poželjno manje od 10% po masi, i još poželjnije manje od 5% po masi amorfne faze, u odnosu na količinu liofilizata.
8. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time, da sadrži najmanje 95% po masi, prvenstveno najmanje 96% po masi, poželjno najmanje 98% po masi, i još poželjnije najmanje 99% po masi treosulfana.
9. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 8, naznačen time, da sadrži manje od 0,2% po masi, poželjno manje od 0,1% po masi, i još poželjnije manje od 0,05% po masi metansulfonske kiseline.
10. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 9, naznačen time, da sadrži manje od 1% po masi, poželjno manje od 0,5% po masi, i još poželjnije manje od 0,1% po masi vode.
11. Postupak za proizvodnju liofilizata prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da postupak obuhvaća sušenje zamrzavanjem vodene otopine koja sadrži treosulfan.
12. Postupak prema patentnom zahtjevu 11, naznačen time, da vodena otopina sadrži vodu i opcionalno jedno ili više organskih otapala.
13. Postupak prema patentnom zahtjevu 12, naznačen time, da organsko otapalo jest octena kiselina.
14. Postupak prema bilo kojem od patentnih zahtjeva 11 do 13, naznačen time, da obuhvaća
(a) pripravljanje vodene otopine koja ima prvu temperaturu,
(b) zamrzavanje vodene otopine, pri čemu se vodena otopina hladi od prve temperature do temperature zamrzavanja, brzinom hlađenja koja nije veća od 3 K/min, i
(c) sušenje zamrznute otopine dobivene u koraku (b) u svrhu dobivanja liofilizata.
15. Postupak prema patentnom zahtjevu 14, naznačen time, da brzina hlađenja u koraku (b) nije veća od 2 K/min, poželjno nije veća od 1,5 K/min i još poželjnije nije veća od 1,3 K/min, ili brzina hlađenja u koraku (b) iznosi od 0,05 do 1,5 i poželjno od 0,1 do 1,3 K/min.
16. Postupak prema bilo kojem od patentnih zahtjeva 11 do 15, naznačen time, da prva temperatura iznosi od 15°C do 95°C, poželjno od 20°C do 50°C, i još poželjnije od 25°C do 35°C.
17. Postupak prema bilo kojem od patentnih zahtjeva 11 do 16, naznačen time, da temperatura zamrzavanja iznosi -40°C ili manje, poželjno od -60°C do -40°C, i još poželjnije od -50°C do -40°C.
18. Postupak prema bilo kojem od patentnih zahtjeva 11 do 17, naznačen time, da se zamrznuta otopina održava na temperaturi zamrzavanja najmanje jedan sat, poželjno jedan do 10 sati i još poželjnije 2 do 8 sati.
19. Postupak prema bilo kojem od patentnih zahtjeva 14 do 18, naznačen time, da sušenje u koraku (c) uključuje primarno sušenje koje se provodi putem podvrgavanja zamrznute otopine temperaturi od -25°C ili više, poželjno temperaturi od -15°C do 0°C, te podvrgavanja zamrznute otopine tlaku od 0,03 do 1,0 mbar, poželjno 0,1 do 0,6 mbar i još poželjnije 0,3 do 0,5 mbar,
ili
sušenje u koraku (c) uključuje primarno sušenje koje se provodi putem podvrgavanja zamrznute otopine temperaturi od 0°C ili više, poželjno temperaturi od 0°C do 60°C, još poželjnije 20°C do 60°C, čak još poželjnije 30°C do 50°C, te podvrgavanja zamrznute otopine tlaku od 0,03 do 1,0 mbar, poželjno 0,1 do 0,6 mbar i još poželjnije 0,3 do 0,5 mbar.
20. Postupak prema patentnom zahtjevu 19, naznačen time, da se primarno sušenje provodi u vremenu od najmanje 5 sati i poželjno najmanje 10 sati.
21. Postupak prema patentnom zahtjevu 19 ili 20, naznačen time, da se nakon primarnog sušenja provodi sekundarno sušenje putem podvrgavanja proizvoda primarnog sušenja temperaturi od najmanje 30°C, poželjno 30°C do 50°C, i podvrgavanje proizvoda primarnog sušenja tlaku od 0,03 do 1,0 mbar, poželjno 0,1 do 0,6 mbar, i još poželjnije 0,3 do 0,5 mbar.
22. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da je za uporabu kao lijek.
23. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da je za uporabu u liječenju raka i prvenstveno raka jajnika.
24. Liofilizat prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da je za uporabu u kondicioniranoj terapiji za pripremu prije transplantacije koštane srži ili matičnih krvnih stanica.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18196967 | 2018-09-26 | ||
| EP19778493.7A EP3856151B1 (en) | 2018-09-26 | 2019-09-25 | Lyophilisate of treosulfan |
| PCT/EP2019/075832 WO2020064819A1 (en) | 2018-09-26 | 2019-09-25 | Lyophilisate of treosulfan |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20231343T1 true HRP20231343T1 (hr) | 2024-02-16 |
Family
ID=63685769
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20231343TT HRP20231343T1 (hr) | 2018-09-26 | 2019-09-25 | Liofilizat od treosulfana |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20220031620A1 (hr) |
| EP (2) | EP3856151B1 (hr) |
| JP (2) | JP2022509904A (hr) |
| CN (1) | CN112752569A (hr) |
| CA (1) | CA3113705A1 (hr) |
| DK (1) | DK3856151T3 (hr) |
| EA (1) | EA202190616A1 (hr) |
| ES (1) | ES2964602T3 (hr) |
| FI (1) | FI3856151T3 (hr) |
| HR (1) | HRP20231343T1 (hr) |
| HU (1) | HUE064508T2 (hr) |
| LT (1) | LT3856151T (hr) |
| PL (1) | PL3856151T3 (hr) |
| PT (1) | PT3856151T (hr) |
| WO (1) | WO2020064819A1 (hr) |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1188583B (de) | 1960-02-22 | 1965-03-11 | Leo Pharm Prod Ltd | Verfahren zur Herstellung der Steroisomeren und des Racemats von Butan-1, 2, 3, 4-tetrol-1, 4-di-(methansulfonat) |
| GB896052A (en) * | 1960-02-22 | 1962-05-09 | Knud Abildgaard | The stereo-isomers and the racemate of butane-1,2,3,4-tetrol-1,4-di-(methanesulphonate) |
| DE1193938B (de) | 1961-10-02 | 1965-06-03 | Leo Pharm Prod Ltd | Verfahren zur Herstellung des Racemats und der Stereoisomeren einschliesslich des Mesoisomeren von Butan-1, 2, 3, 4-tetrol-1, 4-di-(methansulfonat) |
| DE19936281C2 (de) * | 1999-08-02 | 2002-04-04 | Bayer Ag | Verfahren zur Gefriertrocknung |
| DE19953517C1 (de) | 1999-11-05 | 2001-08-09 | Medac Klinische Spezialpraep | Verwendung von Treosulfan zur Konditionierung von Patienten vor Knochemarktransplantation oder Blutstammzelltransplantation |
| US8793895B2 (en) * | 2006-02-10 | 2014-08-05 | Praxair Technology, Inc. | Lyophilization system and method |
| IN2013MU03491A (hr) * | 2013-11-04 | 2015-07-31 | Emcure Pharmaceuticals Ltd |
-
2019
- 2019-09-25 HU HUE19778493A patent/HUE064508T2/hu unknown
- 2019-09-25 ES ES19778493T patent/ES2964602T3/es active Active
- 2019-09-25 EP EP19778493.7A patent/EP3856151B1/en active Active
- 2019-09-25 FI FIEP19778493.7T patent/FI3856151T3/fi active
- 2019-09-25 PT PT197784937T patent/PT3856151T/pt unknown
- 2019-09-25 CN CN201980062324.9A patent/CN112752569A/zh active Pending
- 2019-09-25 PL PL19778493.7T patent/PL3856151T3/pl unknown
- 2019-09-25 EA EA202190616A patent/EA202190616A1/ru unknown
- 2019-09-25 CA CA3113705A patent/CA3113705A1/en active Pending
- 2019-09-25 DK DK19778493.7T patent/DK3856151T3/da active
- 2019-09-25 LT LTEPPCT/EP2019/075832T patent/LT3856151T/lt unknown
- 2019-09-25 HR HRP20231343TT patent/HRP20231343T1/hr unknown
- 2019-09-25 JP JP2021516733A patent/JP2022509904A/ja active Pending
- 2019-09-25 WO PCT/EP2019/075832 patent/WO2020064819A1/en unknown
- 2019-09-25 US US17/279,200 patent/US20220031620A1/en active Pending
- 2019-09-25 EP EP23192810.2A patent/EP4257122A3/en active Pending
-
2023
- 2023-08-24 JP JP2023136343A patent/JP2023153362A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2022509904A (ja) | 2022-01-25 |
| EP3856151B1 (en) | 2023-08-23 |
| ES2964602T3 (es) | 2024-04-08 |
| EP4257122A2 (en) | 2023-10-11 |
| PT3856151T (pt) | 2023-10-27 |
| LT3856151T (lt) | 2023-11-27 |
| US20220031620A1 (en) | 2022-02-03 |
| CA3113705A1 (en) | 2020-04-02 |
| CN112752569A (zh) | 2021-05-04 |
| EA202190616A1 (ru) | 2021-06-25 |
| PL3856151T3 (pl) | 2024-02-19 |
| WO2020064819A1 (en) | 2020-04-02 |
| JP2023153362A (ja) | 2023-10-17 |
| HUE064508T2 (hu) | 2024-03-28 |
| FI3856151T3 (fi) | 2023-11-15 |
| EP3856151A1 (en) | 2021-08-04 |
| DK3856151T3 (da) | 2023-11-27 |
| EP4257122A3 (en) | 2024-01-10 |
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