Compositions for oral administration of campothecin and its...

A - Human Necessities – 61 – K

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Details

A61K 47/16 (2006.01) A61K 47/48 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2569585

Pharmaceutical compositions are provided which comprise a lactone form of camptothecin, or a lactone form analog thereof that is effective for controlling abnormal cell proliferation; and at least one amphiphilic block copolymer that, upon oral administration to a patient, increases oral bioavailability of the lactone form significantly more than that of a directly related carboxylate form of the camptothecin or analog thereof. Compositions are also provided that further comprise at least one bioadhesive polymer that protects a closed alpha-hydroxy lactone structure of the lactone form of camptothecin or analog thereof, and provides a controlled release of the lactone form of camptothecin or lactone form analog thereof, in GI, upon oral administration to a patient. Methods are described for the prevention and/or treatment of a condition related to abnormal cell proliferation comprising orally administering to a patient in need of thereof an effective amount of a composition of the present invention.

Compositions pharmaceutiques comportant une forme lactone de la campothécine ou un analogue de ladite forme lactone permettant de contrôler efficacement une prolifération cellulaire anormale, ainsi qu'un copolymère séquencé amphiphile qui, lorsqu'il est administré par voie orale à un patient, accroît la biodisponibilité orale de ladite forme lactone de manière significative par rapport à une forme carboxylate directement apparentée de la campothécine ou d'un de ses analogues. L'invention concerne également des compositions comportant en outre au moins un polymère bioadhésif qui protège une structure lactone alpha-hydroxy fermée de la forme lactone de la campothécine ou d'un analogue, et permet une libération contrôlée de la forme lactone de la campothécine ou d'un analogue de ladite forme lactone dans le tractus gastro-intestinal, lorsque lesdites compositions sont administrées par voie orale à un patient. Des procédés de prévention et/ou de traitement d'un état lié à une prolifération cellulaire anormale sont également décrits, lesdits procédés consistant à administrer par voie orale à un patient nécessitant un tel traitement une quantité efficace d'une composition selon la présente invention.

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