HRP20120502T1 - Farmaceutske smjese s poboljšanim profilom otapanja za slabo topljive lijekove - Google Patents
Farmaceutske smjese s poboljšanim profilom otapanja za slabo topljive lijekove Download PDFInfo
- Publication number
- HRP20120502T1 HRP20120502T1 HRP20120502TT HRP20120502T HRP20120502T1 HR P20120502 T1 HRP20120502 T1 HR P20120502T1 HR P20120502T T HRP20120502T T HR P20120502TT HR P20120502 T HRP20120502 T HR P20120502T HR P20120502 T1 HRP20120502 T1 HR P20120502T1
- Authority
- HR
- Croatia
- Prior art keywords
- mixture
- oxo
- amino
- carboxylic acid
- fluoro
- Prior art date
Links
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- 229940079593 drug Drugs 0.000 title claims 2
- 239000003814 drug Substances 0.000 title claims 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
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- 150000003839 salts Chemical class 0.000 claims abstract 7
- 238000002425 crystallisation Methods 0.000 claims abstract 3
- 230000008025 crystallization Effects 0.000 claims abstract 3
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- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
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- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims 2
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- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims 2
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- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 claims 1
- BFSVOASYOCHEOV-UHFFFAOYSA-N 2-diethylaminoethanol Chemical compound CCN(CC)CCO BFSVOASYOCHEOV-UHFFFAOYSA-N 0.000 claims 1
- 229930024421 Adenine Natural products 0.000 claims 1
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- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 claims 1
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- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 claims 1
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- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 1
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- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 claims 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 claims 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 claims 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
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- 239000004473 Threonine Substances 0.000 claims 1
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- 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
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Abstract
Smjesa koja sadrži amino difluoropiridin il klor fluor hidroksiazetidin il okso dihidrokinolin karboksilnu kiselinu ili njezinu sol inhibitor kristalizacije izabran iz skupine koja obuhvaća hidroksipropilmetilcelulozu polivinilpirolidon i hidroksipropilcelulozu temodifikator pH naznačena time da smjesa ima mjerljivo poboljšan stupanj otapanja amino difluoropiridin il klor fluor hidroksiazetidin il okso dihidrokinolin karboksilne kiseline ili njezine soli Patent sadrži još patentnih zahtjeva
Claims (6)
1. Smjesa koja sadrži 1-(6-amino-3,5-difluoropiridin-2-il)-8-klor-6-fluor-7-(3-hidroksiazetidin-1- il)-4-okso-1,4-dihidrokinolin-3-karboksilnu kiselinu ili njezinu sol, inhibitor kristalizacije izabran iz skupine koja obuhvaća hidroksipropilmetilcelulozu, polivinilpirolidon i hidroksipropilcelulozu te modifikator pH, naznačena time, da smjesa ima mjerljivo poboljšan stupanj otapanja 1-(6- amino-3,5-difluoropiridin-2-il)-8-klor-6-fluor-7-(3-hidroksiazetidin-1-il)-4-okso-1,4- dihidrokinolin-3-karboksilne kiseline ili njezine soli.
2. Uporaba 1-(6-amino-3,5-difluoropiridin-2-il)-8-klor-6-fluor-7-(3-hidroksiazetidin-1-il)-4-okso-1.4-dihidrokinolin-3-karboksilne kiseline ili njezine soli, inhibitora kristalizacije izabranog iz skupine koja obuhvaća hidroksipropilmetilcelulozu, polivinilpirolidon i hidroksipropilcelulozu te modifikatora pH za proizvodnju smjese, naznačena time, da ima mjerljivo poboljšan stupanj otapanja 1-(6-amino-3,5-difluoropiridin-2-il)-8-klor-6-fluor-7-(3-hidroksiazetidin-1-il)-4-okso-1.4-dihidrokinolin-3-karboksilne kiseline ili njezine soli za liječenje bolesti kod bolesnika kojemu će se dati ta smjesa.
3. Smjesa za uporabu prema zahtjevu 1 ili 2, naznačena time, da sol 1-(6-amino-3,5- difluoropiridin-2-il)-8-klor-6-fluor-7-(3-hidroksiazetidin-1-il)-4-okso-1,4-dihidrokinolin-3-karboksilne kiseline sadrži meglumin.
4. Smjesa za uporabu prema bilo kojem od zahtjeva 1-3, naznačena time, da se modifikator pH izabire iz skupine koja obuhvaća NaOH, LiOH, KOH, Na2CO3, NaHCO3, K2CO3, KHCO3, NaH2PO4, Na2HPO4 Na3PO4, KH2PO4, K2HPO4, K3PO4, Ca(OH)2, Mg(OH)2, Zn(OH)2, Al(OH)3, piridoksin, trietanolamin, amonijev hidroksid, citozin, dietilamin, meglumin, ornitin, glicin, lizin, arginin, valin, prolin, asparaginsku kiselinu, alanin, asparagin, izoleucin, leucin, metionin, treonin, kolin hidroksid, prokain, dietiletanolamin, glukozamin, gvanin, nikotinamid, piperazin, gvanidin, olamin, piperidin, trietilamin, trometamin, benzatin, adenin i njihove smjese.
5. Smjesa ili uporaba prema bilo kojem od zahtjeva 1-4, naznačena time, da je s barem 5% povećanim stupnjem topljivosti.
6. Smjesa ili uporaba prema bilo kojem od zahtjeva 1-5, naznačena time, da je doza lijeka od 0,03 do 200 mg/kg tjelesne težine.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US67020705P | 2005-04-11 | 2005-04-11 | |
| PCT/US2006/013651 WO2006110815A1 (en) | 2005-04-11 | 2006-04-11 | Pharmaceutical compositions having improved dissolution profiles for poorly soluble drugs |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120502T1 true HRP20120502T1 (hr) | 2012-07-31 |
Family
ID=36648686
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120502TT HRP20120502T1 (hr) | 2005-04-11 | 2012-06-14 | Farmaceutske smjese s poboljšanim profilom otapanja za slabo topljive lijekove |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US20060228411A1 (hr) |
| EP (2) | EP1868581B1 (hr) |
| JP (2) | JP5284777B2 (hr) |
| AT (1) | ATE549016T1 (hr) |
| CA (1) | CA2603783C (hr) |
| CY (1) | CY1112980T1 (hr) |
| DK (1) | DK1868581T3 (hr) |
| ES (1) | ES2384333T3 (hr) |
| HR (1) | HRP20120502T1 (hr) |
| ME (1) | ME02003B (hr) |
| MX (1) | MX2007012642A (hr) |
| PL (1) | PL1868581T3 (hr) |
| PT (1) | PT1868581E (hr) |
| RS (1) | RS52354B (hr) |
| SI (1) | SI1868581T1 (hr) |
| WO (1) | WO2006110815A1 (hr) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2009297085B2 (en) | 2008-09-24 | 2015-07-09 | Melinta Subsidiary Corp. | Process for making quinolone compounds |
| JP2012508773A (ja) * | 2008-11-14 | 2012-04-12 | ポートラ ファーマシューティカルズ， インコーポレイテッド | 低いｐＨでの難水溶性のイオン化活性薬剤の制御放出のための固体組成物およびその使用方法 |
| WO2010056872A2 (en) | 2008-11-15 | 2010-05-20 | Rib-X Pharmaceuticals, Inc. | Antimicrobial compositions |
| WO2011088152A1 (en) * | 2010-01-12 | 2011-07-21 | Portola Pharmaceuticals, Inc. | Pharmaceutical composition and dosage forms of elinogrel and methods of use thereof |
| WO2012043696A1 (ja) | 2010-09-30 | 2012-04-05 | 富山化学工業株式会社 | ６－フルオロ－３－ヒドロキシ－２－ピラジンカルボキサミドのメグルミン塩 |
| CN104098548B (zh) * | 2013-04-11 | 2017-07-18 | 上海医药工业研究院 | 一种Delafloxacin的精制方法 |
| TWI732337B (zh) * | 2014-06-20 | 2021-07-01 | 美商梅琳塔有限責任公司 | 醫藥組成物及其用途 |
| TW201605447A (zh) * | 2014-06-20 | 2016-02-16 | 美林塔治療學有限公司 | 處理感染的方法 |
| AU2015346023A1 (en) | 2014-11-14 | 2017-06-01 | Melinta Subsidiary Corp. | Method for treating, preventing, or reducing the risk of skin infection |
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| DE2213275C3 (de) * | 1972-03-18 | 1979-11-15 | Desitin-Werk, Carl Klinke Gmbh, 2000 Hamburg | Verfahren zur Herstellung von 5,5-Diphenylhydantoin-Natrium-Lösungen als Infusionskonzentrate |
| JPS5221575B2 (hr) * | 1972-03-18 | 1977-06-11 | ||
| FR2525108B1 (fr) * | 1982-04-19 | 1989-05-12 | Elan Corp Ltd | Medicaments a haut degre de solubilite et procede pour leur obtention |
| DE3420743A1 (de) * | 1984-06-04 | 1985-12-05 | Bayer Ag, 5090 Leverkusen | 7-amino-1-cyclopropyl-6,8-dihalogen-1,4-dihydro-4-oxo-3-chinolincarbonsaeuren, verfahren zu ihrer herstellung sowie diese enthaltende antibakterielle mittel |
| US4696814A (en) * | 1985-08-21 | 1987-09-29 | Warner-Lambert Company | Parenteral phenytoin compositions |
| IT1207994B (it) * | 1986-01-03 | 1989-06-01 | Therapicon Srl | Sali idrosulubili di composti adattivita' antiinfiammatoria ed analgesica, loro preparazione ed utilizzo in composizioni farmaceutiche. |
| DE3626868A1 (de) * | 1986-08-08 | 1988-02-11 | Bayer Ag | Parenterale loesung |
| AU6001790A (en) * | 1989-08-02 | 1991-02-07 | Warner-Lambert Company | Formulations of phenytoin sodium for intravenous administration |
| JP2613139B2 (ja) * | 1990-07-19 | 1997-05-21 | エスエス製薬 株式会社 | キノロンカルボン酸誘導体 |
| GB9121316D0 (en) * | 1991-10-09 | 1991-11-20 | Wellcome Found | Heterocyclic compounds |
| EP0563697B1 (en) * | 1992-04-03 | 2001-07-04 | Nippon Kayaku Kabushiki Kaisha | Cytarabine ocfosfate hard capsule |
| US5811558A (en) * | 1994-04-12 | 1998-09-22 | Chiroscience Limited | Process for the resolution of etodolac using glucamine derivatives |
| TW487582B (en) * | 1995-08-11 | 2002-05-21 | Nissan Chemical Ind Ltd | Method for converting sparingly water-soluble medical substance to amorphous state |
| RU2171252C2 (ru) * | 1995-09-22 | 2001-07-27 | Вакунага Фармасьютикал КО., Лтд. | Аминосоединение для получения новых производных пиридонкарбоновой кислоты или их солей |
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| SI3056492T1 (sl) * | 2004-10-08 | 2022-03-31 | Abbvie Inc. | Sol meglumina in njene kristalinične oblike zdravila (delafloksacin) |
-
2006
- 2006-04-11 MX MX2007012642A patent/MX2007012642A/es active IP Right Grant
- 2006-04-11 WO PCT/US2006/013651 patent/WO2006110815A1/en active Application Filing
- 2006-04-11 AT AT06740898T patent/ATE549016T1/de active
- 2006-04-11 ES ES06740898T patent/ES2384333T3/es active Active
- 2006-04-11 EP EP06740898A patent/EP1868581B1/en active Active
- 2006-04-11 ME MEP-2012-250A patent/ME02003B/me unknown
- 2006-04-11 RS RS20120250A patent/RS52354B/en unknown
- 2006-04-11 SI SI200631326T patent/SI1868581T1/sl unknown
- 2006-04-11 CA CA2603783A patent/CA2603783C/en active Active
- 2006-04-11 DK DK06740898.9T patent/DK1868581T3/da active
- 2006-04-11 PT PT06740898T patent/PT1868581E/pt unknown
- 2006-04-11 JP JP2008506637A patent/JP5284777B2/ja active Active
- 2006-04-11 EP EP20100178627 patent/EP2286800A1/en not_active Withdrawn
- 2006-04-11 US US11/401,746 patent/US20060228411A1/en not_active Abandoned
- 2006-04-11 PL PL06740898T patent/PL1868581T3/pl unknown
-
2010
- 2010-06-02 US US12/792,171 patent/US20100324018A1/en not_active Abandoned
-
2012
- 2012-06-12 CY CY20121100531T patent/CY1112980T1/el unknown
- 2012-06-14 HR HRP20120502TT patent/HRP20120502T1/hr unknown
- 2012-08-14 US US13/585,081 patent/US20120309740A1/en not_active Abandoned
-
2013
- 2013-02-01 JP JP2013018095A patent/JP2013121976A/ja active Pending
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2014
- 2014-10-31 US US14/529,907 patent/US20150057266A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2006110815A1 (en) | 2006-10-19 |
| CY1112980T1 (el) | 2016-04-13 |
| US20150057266A1 (en) | 2015-02-26 |
| CA2603783C (en) | 2014-11-18 |
| ES2384333T3 (es) | 2012-07-03 |
| EP1868581B1 (en) | 2012-03-14 |
| PT1868581E (pt) | 2012-06-22 |
| MX2007012642A (es) | 2008-01-11 |
| JP2008535925A (ja) | 2008-09-04 |
| EP2286800A1 (en) | 2011-02-23 |
| SI1868581T1 (sl) | 2012-06-29 |
| EP1868581A1 (en) | 2007-12-26 |
| ATE549016T1 (de) | 2012-03-15 |
| PL1868581T3 (pl) | 2012-08-31 |
| ME02003B (me) | 2012-12-31 |
| DK1868581T3 (da) | 2012-07-09 |
| US20100324018A1 (en) | 2010-12-23 |
| CA2603783A1 (en) | 2006-10-19 |
| US20060228411A1 (en) | 2006-10-12 |
| JP2013121976A (ja) | 2013-06-20 |
| JP5284777B2 (ja) | 2013-09-11 |
| US20120309740A1 (en) | 2012-12-06 |
| RS52354B (en) | 2012-12-31 |
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