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1. WO2000040219 - DISPERSIBLE CONCENTRATE FOR THE DELIVERY OF CYCLOSPORIN

Publication Number WO/2000/040219
Publication Date 13.07.2000
International Application No. PCT/IL1999/000710
International Filing Date 30.12.1999
Chapter 2 Demand Filed 25.07.2000
IPC
A61K 9/107 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions
A61K 38/13 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
12Cyclic peptides
13Cyclosporins
CPC
A61K 9/1075
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions ; ; Emulsion preconcentrates; Micelles
1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 37/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
A61P 37/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
06Immunosuppressants, e.g. drugs for graft rejection
Applicants
  • DEXCEL LTD. [IL/IL]; P.O. Box 50 38100 Hadera, IL (AllExceptUS)
  • DOMB, Abraham, J. [IL/IL]; IL (UsOnly)
Inventors
  • DOMB, Abraham, J.; IL
Agents
  • BRASS, Daniel; 10 Dizengoff Street 64281 Tel-Aviv, IL
Priority Data
09/223,37830.12.1998US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) DISPERSIBLE CONCENTRATE FOR THE DELIVERY OF CYCLOSPORIN
(FR) CONCENTRE DISPERSABLE DESTINE A L'ADMINISTRATION D'UNE CYCLOSPORINE
Abstract
(EN)
A formulation for the administration of a cyclosporin. This formulation features a hydrophilic solvent which is characterized by being a lower alkyl ester of hydroxyalkanoic acid; and a surfactant, preferably a combination of a surfactant with a high HLB (hydrophilic/lipophilic balance) of at least about 8 and a surfactant with a low HLB of less than about 5. Other ingredients are optional, such as a fatty acid ester such as tricaprin, a phospholipid, and an ethoxylated fat such as Cremophor or another similar substance. Optionally, the ethoxylated fat is substituted for the surfactant. The preferred particle size of the resultant formulation is less than about 100 nm, more preferably less than about 60 nm, and most preferably from about 5 nm to about 50 nm. The formulation of the present invention is characterized by having high bioavailability.
(FR)
L'invention concerne une préparation destinée à l'administration d'une cyclosporine. Cette préparation contient un solvant hydrophile caractéristique en tant qu'ester d'alkyle inférieur d'acide hydroxyalcanoïque, et un tensioactif constitué de préférence d'un tensioactif ayant un HLB (rapport hydrophile-lipophile) élevé d'au moins environ 8 combiné à un tensioactif ayant un HLB faible inférieur à environ 5. D'autres ingrédients facultatifs peuvent être un ester d'acide gras (tricaprine, par exemple), un phospholipide, ou un corps gras éthoxylé (Cremophor ou autre substance similaire). Le corps gras éthoxylé est éventuellement substituée au tensioactif. La taille des particules préférée de la préparation résultante est inférieure à environ 100 nm. De préférence, cette taille est inférieure à environ 60 nm ou, mieux encore, à environ 5 à 50 nm. La préparation de l'invention est caractérisée par une biodisponibilité élevée.
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