A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 9/16 (2006.01) A61K 9/51 (2006.01) B01J 13/00 (2006.01)
Patent
CA 2391986
The invention concerns a suspension of particles as carriers (PV) for active principles (PA). Said vector particles (PV) are based on polyamino acids (PAA). They have a mean hydrodynamic diameter (Dh) ranging between 30 and 120 nm and have an insulin load factor (Ta) ranging between 5 and 25 % of associated insulin volume relative to the polyamino acid volume forming the carrier principles. The polyamino acids are double-block polymers comprising hydrophilic (AAI) and hydrophobic (AAO) monomers. The invention also concerns a solid powder substance from which are derived the carrier particles and the preparation of said solid powder substance and said suspension of carrier particles. Said preparation consists in copolymerising N-carboxy anhydrides of hydrophobic monomers and precursors of hydrophilic monomers, in the presence of N-methyl pyrrolidone and methanol. The precursors of the hydrophilic monomers are then transformed into hydrophilic monomers by acid hydrolysis. Optionally the copolymer is neutralised, subjected to dialysis, concentrated and the water is eliminated. Thus a solid powder substance or suspended carrier particles are produced. Active principles (such as insulin or vaccines) are associated with said carrier particles for preparing special pharmaceutical products.
L'invention concerne une suspension de particules de vectorisation (PV) de principes actifs (PA). Ces PV sont à base de polyaminoacides PAA. Elles ont un diamètre hydrodynamique moyen Dh compris entre 30 et 120 nm et présentent un taux de chargement Ta avec l'insuline compris entre 5 et 25 % de masse d'insuline associée par rapport à la masse de PAA formant les PV. Les PAA sont des copolymères diblocs comprenant des monomères hydrophiles AAI et hydrophobes AAO. L'invention vise, également, un solide pulvérulent à partir duquel sont issues les PV ainsi que la préparation de ce solide et de cette suspension de PV. Cette préparation consiste à copolymériser les N- CarboxyAnhydrides d'AAO et de précurseurs d'AAI, en présence de N- méthylpyrrolidone et de méthanol. On transforme ensuite des précurseurs d'AAI en AAI par hydrolyse acide. Eventuellement, on neutralise, on dialyse, on concenre et on élimine l'eau. On produit ainsi un solide pulvérulent ou des PV en suspension. On associe des PA (comme l'insuline ou des vaccins) à ces PV et on prépare des spécialités pharmaceutiques.
Bryson Nathan
Touraud Franck
Flamel Technologies
Robic
LandOfFree
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