Therapeutic agents complexed with calcium phosphate and...

A - Human Necessities – 61 – K

Patent

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A61K 9/50 (2006.01)

Patent

CA 2435455

The present invention relates generally to an oral drug delivery system which incorporates a therapeutic bioactive agent with biodegradable calcium phosphate particles, the particles then encapsulated by casein. The resulting particles provide a carrier designed to protect the therapeutic agent in the harsh, acidic environment of the stomach before releasing the agent into the small intestine. The therapeutic agent may be any therapeutically effective agent, such as a natural isolate or synthetic chemical or biological agent, such as a therapeutic agent, and in particular, may be a protein or a peptide such as insulin. Also incorporated with the particles may be additional surface modifying agents to assist binding, controlled release, or to otherwise modify the particles. The particles generally support the therapeutic agent for form controlled- or sustained-release particles for the oral or mucosal delivery of the therapeutic agent over time, wherein the therapeutic agent is incorporated into the structure of the particle core, disposed on the surface of the particle, or both.

L'invention porte généralement sur un système d'administration orale de médicament incorporant un principe thérapeutique bio-actif avec des particules de phosphate de calcium biodégradable, les particules étant enrobées de caséine. Les particules résultantes fournissent un support conçu pour protéger le principe thérapeutique contre l'environnement âcre et acide de l'estomac avant sa libération dans le petit intestin. Le principe thérapeutique peut être un quelconque agent thérapeutique efficace, tel qu'un isolat naturel, un produit chimique de synthèse ou un agent biologique, et en particulier peut être une protéine ou un peptide, notamment de l'insuline. Il est aussi possible d'incorporer dans les particules des agents de modification de surface dont les fonctions sont d'aider à la liaison, à la libération prolongée, ou de modifier les particules. Les particules supportent généralement le principe thérapeutique et forment des particules à libération lente ou prolongée destinées à l'administration orale ou par voie de muqueuse du principe thérapeutique dans le temps, ce principe étant incorporé au coeur de la particule ou disposé sur sa surface, ou les deux à la fois.

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