Gas-filled amino acid block co-polymer microspheres

A - Human Necessities – 61 – K

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A61K 49/00 (2006.01) A61K 49/22 (2006.01)

Patent

CA 2220712

The present invention relates to gas-filled microspheres useful as ultrasound contrast agents. More particularly, the present invention relates to gas- filled microspheres prepared from amphiphilic poly amino acid block co- polymers and a pharmacologically acceptable water-insoluble gas. The hydrophobic block of the co-polymer is formed from amino acids possessing hydrophobic side-chains, for example, leucine, isoleucine, valine and phenylalanine, and the hydrophilic block of the co-polymer is formed from amino acids possessing hydrophilic side-chains, for example, glutamic acid (and its ionized form, glutamate), aspartic acid (and its ionized form, aspartate), and lysine.

L'invention concerne des microsphères remplies de gaz utiles en tant qu'agents de contraste d'échographie. Plus particulièrement, l'invention concerne des microsphères remplies de gaz préparées à partir de copolymères alternés de polyacides aminés amphiphiles et d'un gaz hydrosoluble pharmacologiquement acceptable. Le bloc hydrophobe du copolymère est formé à partir d'acides aminés possédant des chaînes latérales hydrophobes, par exemple, la leucine, l'isoleucine, la valine et la phénylalanine, et le bloc hydrophile du copolymère est formé à partir d'acides aminés possédant des chaînes latérales hydrophiles, par exemple, l'acide glutamique (et sa forme ionisée, le glutamate), l'acide aspartique (et sa forme ionisée, l'aspartate), et la lysine.

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