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1. WO1996019242 - COMPLEXES OF DERMATAN SULFATE AND DRUGS, GIVING IMPROVED PHARMACOKINETICS

Publication Number WO/1996/019242
Publication Date 27.06.1996
International Application No. PCT/US1994/014776
International Filing Date 22.12.1994
Chapter 2 Demand Filed 22.07.1996
IPC
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
CPC
A61K 47/61
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
61the organic macromolecular compound being a polysaccharide or a derivative thereof
Applicants
  • ACCESS PHARMACEUTICALS, INC. [US]/[US]
Inventors
  • RANNEY, David, F.
Agents
  • HODGINS, Daniel, S.
  • GLAWE, DELFS, MOLL & PARTNER
Priority Data
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPLEXES OF DERMATAN SULFATE AND DRUGS, GIVING IMPROVED PHARMACOKINETICS
(FR) COMPLEXES DE SULFATE DE DERMATAN ET DE MEDICAMENTS, AMELIORANT LA PHARMACOCINETIQUE
Abstract
(EN)
A drug carrier composition comprising a drug complexed with dermatan sulfate is disclosed. The drug is preferably an antitumor drug and may be taxol, a peptide onco-agent or vincristine. The most preferred antitumor drug is doxorubicin. The dermatan sulfate is essentially purified dermatan sulfate with a sulfur content of up to 9 % (w/w) and with selective oligosaccharide oversulfation. The compositions are administered in a fashion that allows efficient vascular access and induced the following $i(in vivo) effects: 1) rapid, partial or total endothelial envelopment of the drug (diagnostic) carrier; 2) sequestration of the carrier and protection of the entrapped agent from blood vascular clearance at an early time (2 minutes) when the endothelial pocket which envelops the carrier still invaginates into the vascular compartment; 3) acceleration of the carrier's transport across and/or through the vascular endothelium or subendothelial structures into the tissue compartment (intestitium); and 4) improvement of the efficiency with which the drug migrates across the endothelium, or epi-endothelial or subendothelial barriers, such that a lower total drug dose is required to obtain the desired effect relative to that required for standard agents. Analogous tissue uptake is described for transepithelial migration into the lungs, bladder and bowel.
(FR)
Compositions supports de médicaments consistant en un médicament complexé à un sulfate de dermatan. Le médicament est de préférence un antitumoral tel que le taxol, un peptide oncoagent ou la vincristine, ou mieux, la doxorubicine. Le sulfate de dermatan, pratiquement pur, contient jusqu'à 9 % en poids de soufre et présente une sursulfatation sélective par les oligosaccharides. Ces compositions qui s'administrent de manière à accéder facilement au système vasculaire y induisent $i(in vivo) les effets suivants: (1) enveloppement endothélial rapide, partiel ou total du support (diagnostique) du médicament; (2) emprisonnement du support, et protection de l'agent captif vis-à-vis de la clairance sanguine vasculaire anticipée (2 minutes) alors que la cavité endothéliale enveloppant le support s'invagine encore dans le compartiment vasculaire; (3) accélération du transport du support dans et/ou à travers les structures vasculaires endothéliales ou sous-endothéliales en direction du compartiment tissulaire (intersticium); et (4) amélioration de l'efficacité de migration du médicament à travers l'endothélium ou les barrières épi-endothéliales ou sous-endothéliales permettant de diminuer la dose nécessaire pour obtenir les effets désirée, par rapport à l'utilisation d'agents usuels. L'absorption par des tissus analogues et la migration trans-épithéliale dans les poumons, la vessie ou les intestins sont également décrits.
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