Colloidal suspension of submicronic particles for carrying...

A - Human Necessities – 61 – K

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A61K 9/51 (2006.01) B01J 13/00 (2006.01)

Patent

CA 2424981

The invention concerns a suspension of particles for carrying hydrophilic active principles (insulin). Said carrier particles are based on a polyethylene glycol/hydrophobic neutral polyminoacid double-block polymer. Said polyethylene glycol/hydrophobic neutral polyaminoacid particles are associated with a hydrophilic active principle (insulin). The invention also concerns, a powdery solid from which the transporting particles are derived and the preparation of said solid and said suspension of transporting particles based on polyethylene glycol/hydrophobic neutral polyminoacid particles and insulin. Said preparation consists in copolymerising N-carboxy-anhydrides of hydrophobic neutral polyminoacid particles, in the presence of N-methyl/pyrrolidone, methanol, and amine-functionalised polyethylene glycol, thereby obtaining polyethylene glycol/hydrophobic neutral polyaminoacids, associating the latter with insulin; precipitating with water so as to obtain the carrier particles; optionally carrying out neutralisation, dialysis, concentration and elimination of water, thereby producing a powdery solid or suspended carrier particles and preparing pharmaceutical specialties.

L'invention concerne une suspension de particules de vectorisation (PV) de principes actifs (PA) hydrophiles (insuline). Ces PV sont à base d'un copolymère dibloc PolyEthylèneGlycol/polyaminoacides neutres hydrophobes polyAANO. Ces particules de PEG/polyAANO sont associés à un PA hydrophile (insuline). 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 à base de PEG/polyAANO-insuline. Cette préparation consiste à copolymériser les N-CarboxyAnhydrides d'AANO, en présence de N- méthylpyrrolidone, de méthanol et de PEG fonctionnalisé amine. On obtient du PEG/polyAANO, que l'on associe avec l'insuline. On précipite à l'aide d'eau de façon à obtenir les PV. Eventuellement, on neutralise, on dialyse, on concentre et on élimine l'eau. On produit ainsi un solide pulvérulent ou des PV en suspension chargé en insuline et on prépare des spécialités pharmaceutiques.

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