CA2231404A1 - Novel cyclosporine preparation forms for oral administration of simple composition and high bio-availability, and process for producing them - Google Patents

Novel cyclosporine preparation forms for oral administration of simple composition and high bio-availability, and process for producing them

Info

Publication number
CA2231404A1
CA2231404A1 CA002231404A CA2231404A CA2231404A1 CA 2231404 A1 CA2231404 A1 CA 2231404A1 CA 002231404 A CA002231404 A CA 002231404A CA 2231404 A CA2231404 A CA 2231404A CA 2231404 A1 CA2231404 A1 CA 2231404A1
Authority
CA
Canada
Prior art keywords
cyclosporine
availability
oral administration
preparation forms
simple composition
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CA002231404A
Other languages
French (fr)
Other versions
CA2231404C (en
Inventor
Matthias Olbrich
Heinrich Potter
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2231404A1 publication Critical patent/CA2231404A1/en
Application granted granted Critical
Publication of CA2231404C publication Critical patent/CA2231404C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13Cyclosporins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Dispersion Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Transplantation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

The invention relates to novel preparation forms of cyclosporine of simple composition and high bio-availability for oral administration, containing 0,5 to 2 parts by weight (p/wt) of one or more amorphous cyclosporine(s), preferably cyclosporine A and/or cyclosporine G
and 6 to 9 p/wt of one or mone polyethylene glycol ester(s) of saturated C10-C22 hydroxy fatty acids, especially SOLUTOL® HS 15, and 1-3 p/wt of one or more monovalent or multivalent alcohols, preferably ethanol and propylene glycol. The medical form is produced by first dissolving the amorphous cyclosporing in ethanol and adding under agitation propylene glycol and SOLUTOL® until a clear, viscous solution is obtained, which is packed as a drinking solution or capsules in the prior art manner.
CA002231404A 1994-11-03 1995-07-19 Novel cyclosporine preparation forms for oral administration of simple composition and high bio-availability, and process for producing them Expired - Fee Related CA2231404C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DEP4438861.6 1994-11-03
DE4438861 1994-11-03
PCT/DE1995/000951 WO1996014079A1 (en) 1994-11-03 1995-07-19 Novel cyclosporine preparation forms for oral administration of simple composition and high bio-availability, and process for producing them

Publications (2)

Publication Number Publication Date
CA2231404A1 true CA2231404A1 (en) 1996-05-17
CA2231404C CA2231404C (en) 2009-02-17

Family

ID=6532126

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002231404A Expired - Fee Related CA2231404C (en) 1994-11-03 1995-07-19 Novel cyclosporine preparation forms for oral administration of simple composition and high bio-availability, and process for producing them

Country Status (27)

Country Link
US (1) US6486124B2 (en)
EP (1) EP0789580B1 (en)
JP (1) JP3833248B2 (en)
KR (1) KR970704464A (en)
CN (1) CN1121238C (en)
AT (1) ATE218359T1 (en)
AU (1) AU715165B2 (en)
BG (1) BG62955B1 (en)
BR (1) BR9509550A (en)
CA (1) CA2231404C (en)
CZ (1) CZ287806B6 (en)
DE (2) DE59510233D1 (en)
DK (1) DK0789580T3 (en)
EE (1) EE03425B1 (en)
ES (1) ES2177652T3 (en)
FI (1) FI118722B (en)
HU (1) HUT77283A (en)
LT (1) LT4306B (en)
LV (1) LV11884B (en)
NO (1) NO970741D0 (en)
PL (1) PL183579B1 (en)
PT (1) PT789580E (en)
RU (1) RU2158601C2 (en)
SK (1) SK164796A3 (en)
TR (1) TR199501361A2 (en)
TW (1) TW492876B (en)
WO (1) WO1996014079A1 (en)

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CA2231404C (en) 1994-11-03 2009-02-17 Arzneimittelwerk Dresden Gmbh Novel cyclosporine preparation forms for oral administration of simple composition and high bio-availability, and process for producing them
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US7202209B2 (en) 2005-07-13 2007-04-10 Allergan, Inc. Cyclosporin compositions
US7501393B2 (en) * 2005-07-27 2009-03-10 Allergan, Inc. Pharmaceutical compositions comprising cyclosporins
US7745400B2 (en) * 2005-10-14 2010-06-29 Gregg Feinerman Prevention and treatment of ocular side effects with a cyclosporin
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EP2780358B1 (en) * 2011-11-15 2016-03-23 Allergan, Inc. Cyclosporine a form 2 and method of making same
ES2791751T3 (en) * 2011-11-15 2020-11-05 Allergan Inc Suspensions of cyclosporin A form 2

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Also Published As

Publication number Publication date
ES2177652T3 (en) 2002-12-16
CZ287806B6 (en) 2001-02-14
TR199501361A2 (en) 1996-06-21
LV11884A (en) 1997-12-20
EP0789580B1 (en) 2002-06-05
LV11884B (en) 1998-03-20
JP3833248B2 (en) 2006-10-11
FI970634A (en) 1997-02-14
HUT77283A (en) 1998-03-30
BR9509550A (en) 1997-09-16
EP0789580A1 (en) 1997-08-20
DK0789580T3 (en) 2002-09-09
PL318560A1 (en) 1997-06-23
FI118722B (en) 2008-02-29
NO970741L (en) 1997-02-18
CZ361696A3 (en) 1997-07-16
KR970704464A (en) 1997-09-06
US6486124B2 (en) 2002-11-26
JPH10508306A (en) 1998-08-18
WO1996014079A1 (en) 1996-05-17
CN1121238C (en) 2003-09-17
BG62955B1 (en) 2000-12-29
DE59510233D1 (en) 2002-07-11
LT97002A (en) 1997-11-25
NO970741D0 (en) 1997-02-18
EE03425B1 (en) 2001-06-15
PL183579B1 (en) 2002-06-28
CA2231404C (en) 2009-02-17
US20020025927A1 (en) 2002-02-28
SK164796A3 (en) 1997-06-04
DE19539860A1 (en) 1996-05-09
PT789580E (en) 2002-09-30
LT4306B (en) 1998-03-25
CN1162265A (en) 1997-10-15
ATE218359T1 (en) 2002-06-15
RU2158601C2 (en) 2000-11-10
FI970634A0 (en) 1997-02-14
AU2975195A (en) 1996-05-31
AU715165B2 (en) 2000-01-20
EE9700112A (en) 1997-12-15
TW492876B (en) 2002-07-01
BG101117A (en) 1997-08-29

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