Drug complex

Details Drug complex Drug complex

A - Human Necessities

61

K

A61K 31/70 (2006.01) A61K 31/335 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2251742

Disclosed is a drug complex of a drug having a hydroxyl group, which is capable of controlling the rate of the release of the drug therefrom in blood, the drug complex being represented by the following formula (1): A-B-C (1) wherein A represents at least one carrier selected from the group consisting of saccharides each having a car- boxyl group, polyethylene glycols each having a carboxyl group, aliphatic carboxylic acids each having a carboxyl group, and derivatives thereof each having a carboxyl group; B represents at least one spacer comprised of a compound having a amino group and a carboxyl group; C represents at least one drug having a hydroxyl group, wherein the carrier A is bonded to the spacer B through an amide bond formed between the carboxyl group of the carrier A and the amino group of the spacer B; and the spacer B is bonded to the drug C through an ester bond formed between the carboxyl group of the spacer B and the hydroxyl group of the drug C. The drug complex of the present invention is capable of not only surely controlling the rate of release of the drug therefrom, but also enhancing the transferability of the drug to target tissues and the pharmacological effect of the drug.

Composite médicamenteux dont chacun des médicaments présente un groupe hydroxyle, ledit composite correspondant à la formule générale suivante: A-B-C dans laquelle A représente un véhicule sélectionné dans des saccharides possédant chacun un groupe carboxyle, polyéthylèneglycol, des acides carboxyliques aliphatiques et leurs dérivés, B représente un espaceur dont la molécule possède des groupes amino et carboxyle et C représente un médicament possédant un groupe hydroxyle. Dans ce cas, le véhicule A et l'espaceur B sont liés l'un à l'autre par l'intermédiaire de la liaison amide formée entre le groupe carboxyle du véhicule A et le groupe amino de l'espaceur B, tandis que ce dernier et le médicament C sont liés l'un à l'autre par l'intermédiaire de la liaison ester formée entre le groupe carboxyle de l'espaceur B et le groupe hydroxyle du médicament C. Ce composite présente une vitesse de libération contrôlé fiable permettant d'augmenter la migration du médicament vers un tissu ciblé et/ou d'améliorer l'efficacité du médicament.

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