SI9420052B - Kristalni brezvodni mikofenolatni mofetil in njegova intravenozna formulacija - Google Patents

Kristalni brezvodni mikofenolatni mofetil in njegova intravenozna formulacija Download PDF

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Publication number
SI9420052B
SI9420052B SI9420052A SI9420052A SI9420052B SI 9420052 B SI9420052 B SI 9420052B SI 9420052 A SI9420052 A SI 9420052A SI 9420052 A SI9420052 A SI 9420052A SI 9420052 B SI9420052 B SI 9420052B
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SI
Slovenia
Prior art keywords
compound
salt
temperature
crystalline anhydrous
range
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SI9420052A
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English (en)
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SI9420052A (en
Inventor
Cherng Roger Fu
De-Mei Leung
S. Jeffrey Fleitman
C.Michele Rizzolio
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Syntex (U.S.A.) Inc.
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Publication of SI9420052A publication Critical patent/SI9420052A/sl
Publication of SI9420052B publication Critical patent/SI9420052B/sl

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Claims (14)

  1. A PATENTNI ZAHTEVKI 1. Kristalna brezvodna spojina s formulo
    kjer je spojina kompleksirana kot sol z anionom, izbranim iz skupine, ki jo sestavljajo klorid, sulfat, fosfat in acetat.
  2. 2. Spojina po zahtevku 1, označena s tem, daje anion klorid.
  3. 3. Kristalna brezvodna spojina po zahtevku 2, označena s tem, da ima tališče od 145°C do 155°C.
  4. 4. Kristalni brezvodni 2-(4-morfolino)etil- E-6-(l,3-dihidro- 4-hidroksi-6-metoksi-7-metil-3-okso-5-izobenzofuranil)-4-metil-4-heksenoat hidroklorid po zahtevku 1.
  5. 5. Sestavek, primeren za pripravo vodne intravenozne formulacije, označen s tem, da obsega spojino s formulo
    kjer je spojina kompleksirana kot sol z anionom, izbranim iz skupine, ki jo sestavljajo klorid, sulfat, fosfat ter acetat in je navedena sol v kristalni brezvodni obliki, in farmacevtsko sprejemljive nosilce.
  6. 6. Sestavek po zahtevku 5, označen s tem, da je edini farmacevtsko sprejemljivi nosilec polisorbat 80. 2
  7. 7. Sestavek po zahtevku 5, označen s tem, da sta farmacevtsko sprejemljiva nosilca polisorbat 80 in citronska kislina.
  8. 8. Postopek za pripravo sestavka, primernega za pripravo intravenozne formulacije, ki obsega spojino s formulo
    kjer je spojina kompleksirana z anionom, izbranim iz skupine, ki jo sestavljajo klorid, sulfat, fosfat ter acetat in je navedena sol v kristalni brezvodni obliki, in farmacevtsko sprejemljive nosilce, označen s tem, da obsega: a) združevanje navedene spojine in farmacevtsko sprejemljivih nosilcev, da dobimo polnilno raztopino, pri čemer je pH navedene polnilne raztopine naravnan na 3,2 do 3,6, b) polnjenje navedene polnilne raztopine v fiole in c) liofiliziranje navedenih napolnjenih fiol, da dobimo navedeni sestavek.
  9. 9. Postopek po zahtevku 8, označen s tem, da liofilizacijska stopnja obsega: a) zniževanje temperature v območju od 25°C do -40°C; b) zniževanje tlaka na 13,3 Pa; c) zviševanje temperature v območju od -40°C do 70°C; in d) zniževanje temperature v območju od 70°C do 25°C.
  10. 10. Postopek po zahtevku 8, označen s tem, da navedena liofilizacijska stopnja 3 obsega: a) zniževanje temperature v območju od 25°C do -10°C pri hitrosti spreminjanja -0,25°C/min; b) vzdrževanje temperature pri -10°C 2 uri in 30 minut; c) zniževanje temperature v območju od -10°C do -40°C pri hitrosti spreminjanja ~0,25°C/min; d) zniževanje tlaka na 13,3 Pa; e) zviševanje temperature v območju od -40°C do -16°C pri hitrosti spreminjanja 0,05°C/min; f) zviševanje temperature v območju od -16°C do 70°C pri hitrosti spreminjanja 0,20°C/min ±0,1°C; in g) zniževanje temperature v območju od 70°C do 25°C.
  11. 11. Uporaba spojine s formulo
    kjer je spojina kompleksirana kot sol z anionom, izbranim iz skupine, ki jo sestavljajo klorid, sulfat, fosfat ter acetat in je navedena sol v njeni kristalni brezvodni obliki, za pripravo zdravila za zdravljenje zavračanja transplantacij, ki vključujejo zlasti zavračanje srčnih transplantacij, zavračanje pankreasnih transplantacij in zavračanje renalnih transplantacij ter za zdravljenje avtoimunskih motenj, psoriaze, vnetnih bolezni, ki vključujejo zlasti revmatoidni artritis, diabetesa, tumorjev in virusnih bolezni.
  12. 12. Uporaba sestavka po zahtevkih 5 - 7 za pripravo intravenozne formulacije, ki nadalje obsega tekoč medij, pri čemer združimo tekoč medij in sestavek pred dajanjem.
  13. 13. Postopek za pripravo intravenozne formulacije, označen s tem, da obsega mešanje a) spojine s formulo
    kjer je spojina kompleksirana kot sol z anionom, izbranim iz skupine, ki jo sestavljajo klorid, sulfat, fosfat ter acetat in je navedena sol v njeni kristalni brezvodni obliki, b) farmacevtsko sprejemljivih nosilcev in c) tekočega medija.
  14. 14. Komplet, uporaben za pripravo intravenozne formulacije, označen s tem, da obsega a) sestavek, ki obsega spojino s formulo 5·
    kjer je spojina kompleksirana kot sol z anionom, izbranim iz skupine, ki jo sestavljajo klorid, sulfat, fosfat ter acetat in je navedena sol v kristalni brezvodni obliki, in farmacevtsko sprejemljive nosilce in b) ustrezno količino tekočega medija.
SI9420052A 1993-09-15 1994-09-12 Kristalni brezvodni mikofenolatni mofetil in njegova intravenozna formulacija SI9420052B (sl)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US12184193A 1993-09-15 1993-09-15
PCT/US1994/010142 WO1995007902A1 (en) 1993-09-15 1994-09-12 Crystalline anhydrous mycophenolate mofetil and intravenous formulation thereof

Publications (2)

Publication Number Publication Date
SI9420052A SI9420052A (en) 1996-12-31
SI9420052B true SI9420052B (sl) 2004-02-29

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ID=22399119

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SI9420052A SI9420052B (sl) 1993-09-15 1994-09-12 Kristalni brezvodni mikofenolatni mofetil in njegova intravenozna formulacija

Country Status (32)

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US (2) US5543408A (sl)
EP (1) EP0724581B1 (sl)
JP (1) JP3411038B2 (sl)
KR (1) KR100349772B1 (sl)
CN (1) CN1060770C (sl)
AT (1) ATE173475T1 (sl)
AU (1) AU677435B2 (sl)
BR (1) BR9407469A (sl)
CA (1) CA2171836C (sl)
CZ (1) CZ292423B6 (sl)
DE (1) DE69414720T2 (sl)
DK (1) DK0724581T3 (sl)
ES (1) ES2123831T3 (sl)
FI (1) FI119639B (sl)
HK (1) HK1012624A1 (sl)
HU (1) HU217300B (sl)
IL (1) IL110970A (sl)
LT (1) LT4052B (sl)
LV (1) LV11326B (sl)
MX (1) MXPA94007099A (sl)
NO (1) NO314727B1 (sl)
NZ (1) NZ273801A (sl)
PH (1) PH30685A (sl)
PL (1) PL178522B1 (sl)
RO (2) RO118075B1 (sl)
RU (1) RU2132849C1 (sl)
SG (1) SG55006A1 (sl)
SI (1) SI9420052B (sl)
TW (1) TW370527B (sl)
UA (1) UA49797C2 (sl)
WO (1) WO1995007902A1 (sl)
ZA (1) ZA947088B (sl)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9512854D0 (en) * 1995-06-23 1995-08-23 Wellcome Found Novel formulation
IN188985B (sl) 1998-12-09 2002-11-30 Biocon Ltd
GB0301259D0 (en) 2003-01-20 2003-02-19 Novartis Ag Organic compounds
GB0307553D0 (en) * 2003-04-01 2003-05-07 Novartis Ag Organic compounds
US20050187170A1 (en) * 2003-06-16 2005-08-25 Biocryst Pharmaceuticals, Inc. Enhancing the efficiency of RNA polymerase inhibitors by using inosine monophosphate dehydrogenase inhibitors
ES2308226T3 (es) * 2003-09-11 2008-12-01 Sandoz Ag Proceso para la produccion de micofenolato mofetil.
US7683188B2 (en) * 2004-04-26 2010-03-23 TEVA Gyógyszergyár Zártkōrūen Mūkōdō Részvénytársaság Process for preparation of mycophenolic acid and ester derivatives thereof
US20050250773A1 (en) * 2004-04-27 2005-11-10 Sandor Molnar Process for preparation of mycophenolate mofetil and other esters of mycophenolic acid
EP1768662A2 (en) 2004-06-24 2007-04-04 Novartis Vaccines and Diagnostics, Inc. Small molecule immunopotentiators and assays for their detection
US7439373B2 (en) * 2004-07-20 2008-10-21 TEVA Gyógyszergyár Zártkörúen Múködö Részvénytársaság Crystalline mycophenolate sodium
CN100383520C (zh) * 2004-09-20 2008-04-23 复旦大学 一种测定人血浆中霉酚酸及其代谢物的方法
US20060235070A1 (en) * 2005-02-08 2006-10-19 Hayden Michael R Compositions and methods for treating vascular, autoimmune, and inflammatory diseases
WO2006086498A2 (en) * 2005-02-08 2006-08-17 Aspreva Pharmaceuticals Sa Treatment of vascular, autoimmune and inflammatory diseases using low dosages of impdh inhibitors
US20080281111A1 (en) * 2005-04-26 2008-11-13 Sandor Molnar Process for preparation of mycophenolate mofetil and other esters of mycophenolic acid
EP2032521B1 (en) 2006-06-27 2009-10-28 Sandoz AG New method for salt preparation
CN101953807A (zh) * 2010-10-09 2011-01-26 山西普德药业有限公司 一种注射用吗替麦考酚酯冻干粉针剂及其制备方法
US8669281B1 (en) 2013-03-14 2014-03-11 Alkermes Pharma Ireland Limited Prodrugs of fumarates and their use in treating various diseases
HUE040044T2 (hu) 2013-03-14 2019-02-28 Alkermes Pharma Ireland Ltd Fumarátok prodrugjai, és azok alkalmazása különbözõ betegségek kezelésében
US9168246B2 (en) 2013-06-27 2015-10-27 Veloxis Pharmaceutical A/S Regimen for suppressing organ rejection
US9604922B2 (en) 2014-02-24 2017-03-28 Alkermes Pharma Ireland Limited Sulfonamide and sulfinamide prodrugs of fumarates and their use in treating various diseases
US11918684B2 (en) 2017-03-13 2024-03-05 Liqmeds Worldwide Limited Pharmaceutical composition of oral suspension of immunosuppressive agents
CA3212370A1 (en) 2021-03-03 2022-09-09 Sana Biotechnology, Inc. Immunosuppressive therapies for use with cardiomyocyte cell therapies, and associated methods and compositions

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4328213A (en) * 1979-11-28 1982-05-04 Schering Corporation Stable injectable labetalol formulation
US4478829A (en) * 1983-04-28 1984-10-23 Armour Pharmaceutical Company Pharmaceutical preparation containing purified fibronectin
US4753935A (en) * 1987-01-30 1988-06-28 Syntex (U.S.A.) Inc. Morpholinoethylesters of mycophenolic acid and pharmaceutical compositions

Also Published As

Publication number Publication date
EP0724581A1 (en) 1996-08-07
JP3411038B2 (ja) 2003-05-26
EP0724581B1 (en) 1998-11-18
LT96028A (en) 1996-08-26
SI9420052A (en) 1996-12-31
PL178522B1 (pl) 2000-05-31
LT4052B (en) 1996-10-25
DE69414720D1 (de) 1998-12-24
UA49797C2 (uk) 2002-10-15
AU677435B2 (en) 1997-04-24
MXPA94007099A (es) 2004-01-23
IL110970A0 (en) 1994-11-28
TW370527B (en) 1999-09-21
LV11326B (en) 1996-10-20
AU7723894A (en) 1995-04-03
DE69414720T2 (de) 1999-04-08
NO961075D0 (no) 1996-03-15
DK0724581T3 (da) 1999-08-02
PL313480A1 (en) 1996-07-08
HU217300B (hu) 1999-12-28
FI961169A (fi) 1996-03-13
ATE173475T1 (de) 1998-12-15
WO1995007902A1 (en) 1995-03-23
LV11326A (lv) 1996-06-20
FI961169A0 (fi) 1996-03-13
CZ292423B6 (cs) 2003-09-17
NZ273801A (en) 1997-10-24
RU2132849C1 (ru) 1999-07-10
JPH09502721A (ja) 1997-03-18
PH30685A (en) 1997-09-16
NO961075L (no) 1996-03-15
CZ78896A3 (en) 1996-10-16
KR100349772B1 (ko) 2002-12-28
RO118075B1 (ro) 2003-01-30
CA2171836C (en) 2006-11-14
RO118427B1 (ro) 2003-05-30
BR9407469A (pt) 1996-11-12
ES2123831T3 (es) 1999-01-16
HK1012624A1 (en) 1999-08-06
SG55006A1 (en) 1998-12-21
US5545637A (en) 1996-08-13
FI119639B (fi) 2009-01-30
US5543408A (en) 1996-08-06
CN1060770C (zh) 2001-01-17
IL110970A (en) 1999-01-26
HU9600652D0 (en) 1996-05-28
CA2171836A1 (en) 1995-03-23
ZA947088B (en) 1996-03-14
NO314727B1 (no) 2003-05-12
CN1131420A (zh) 1996-09-18
HUT75119A (en) 1997-04-28

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