Matrices formed of polymer and hydrophobic compounds for use...

A - Human Necessities – 61 – K

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A61K 9/22 (2006.01) A61K 9/16 (2006.01) A61K 9/52 (2006.01)

Patent

CA 2329875

A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as "hydrophobic compounds") is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

Un composé lipidique ou autre, hydrophobe ou amphiphile (désigné collectivement par composés hydrophobes ?) est intégré dans une matrice polymère de libération de médicament, de sorte que la cinétique de libération de médicament soit modifiée. Dans des modes de réalisation dans lesquels le médicament est hydrosoluble, le médicament est libéré sur de longues périodes par rapport au cas où il est libéré par une matrice polymère ne contenant pas le composé hydrophobe intégré dans le matériau polymère. A la différence des méthodes dans lesquelles un surfactant ou un lipide est ajouté en tant qu'excipient, le composé hydrophobe est réellement intégré dans la matrice polymère, ce qui modifie la diffusion de l'eau dans la microparticule et la diffusion du médicament solubilisé hors de la matrice. Le composé hydrophobe intégré prolonge également la dégradation des polymères instables au plan hydrolytique, formant la matrice, ce qui retarde encore la libération du médicament encapsulé.

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