System and method for transdermal delivery of an anticoagulant

Details System and method for transdermal delivery of an anticoagulant System and method for transdermal delivery of an anticoagulant

A - Human Necessities

61

K

A61K 31/155 (2006.01) A61K 9/00 (2006.01) A61K 9/70 (2006.01) A61K 31/455 (2006.01) A61N 1/30 (2006.01) A61P 7/02 (2006.01)

Patent

CA 2568625

A device for transdermally delivering an anticoagulant agent by electrotransport. Preferably, the anticoagulant comprises a benzamidine or a naphthamidine derivative. A particularly preferred benzamidine derivative is a 2~-[3-[4-(4-piperidinyloxy) anilino]-1-propenyl]benzamidine derivative. The devices are configured to maintain a plasma concentration of 20-80 ng/mL or providing a flux in the range of approximately 20 - 40 mg/day. Suitable current densities include 0.050 and 0.10 mA/cm2. Methods of the invention include delivering the anticoagulants to precisely maintain the desired plasma concentrations. The invention also comprises treating thromboembolic disease and inhibiting Factor Xa.

La présente invention concerne un dispositif d'administration par voie transdermique d'un anticoagulant par électrotransfert. De préférence, cet anticoagulant comprend un dérivé de benzamidine ou de naphtamidine. Le dérivé de benzamidine particulièrement préféré est un dérivé de 2-[3-[4-(4-pipéridinyloxy)anilino]-1-propényl]benzamidine. Les dispositifs sont configurés pour entretenir une concentration plasmatique de 20-80 ng/ml ou pour garantir un flux tenant dans une fourchette approximative de 20 à 40 mg/jour. Les densités de courant appropriées sont comprises dans une fourchette allant de 0,05 à 0,10 mA/cm?2¿. Les procédés de l'invention portent sur l'administration des anticoagulants de façon à entretenir avec précision les concentrations plasmatiques voulues. L'invention concerne également le traitement d'affections thromboemboliques et l'inhibition du Facteur Xa.

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