Sustained-release liposomal anesthetic compositions

Details Sustained-release liposomal anesthetic compositions Sustained-release liposomal anesthetic compositions

A - Human Necessities

61

K

A61K 9/127 (2006.01) A61K 31/167 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61K 45/06 (2006.01)

Patent

CA 2304096

The invention provides a method for obtaining local anesthetics encapsulated in liposomes, such as multivesicular liposomes, with high encapsulation efficiency and slow release in vivo. When the encapsulated anesthetic is administered as a single intracutaneous dose, the duration of anesthesia and half-life of the drug at the local injection site is increased as compared to injection of unencapsulated anesthetic. The maximum tolerated dose of the encapsulated anesthetic is also markedly increased in the liposomal formulation over injection of unencapsulated anesthetic. These results show that the liposomal formulation of local anesthetic is useful for sustained local infiltration and nerve block anesthesia.

L'invention concerne un procédé permettant d'obtenir des anesthésiants locaux encapsulés dans des liposomes; tels que des liposomes multivésiculaires avec une forte efficacité d'encapsulation et une libération lente in vivo. Lorsque l'anesthésiant encapsulé est administré sous forme d'une dose unique par voie intracutanée, la durée de l'anesthésie et la demi-vie du médicament au niveau des sites d'injection locaux est plus longue par rapport à l'injection du même anesthésiant non encapsulé. La dose maximale tolérée de l'anesthésiant encapsulé est fortement accrûe dans la formulation de liposomes par rapport à l'injection du même produit non encapsulé. Ces résultats font apparaître que la formulation de liposomes d'un produit anesthésiant local permet d' assurer une infiltration locale prolongée et une anesthésie par blocage nerveux.

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