Composition and method of preparing microparticles of...

A - Human Necessities – 61 – K

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A61K 9/51 (2006.01) A61K 9/14 (2006.01) A61K 9/16 (2006.01) A61K 47/10 (2006.01) A61K 47/24 (2006.01)

Patent

CA 2326456

Compositions and procedures that yield sub-micron and micron-size stable particles of water-insoluble or poorly soluble drugs or other industrially useful insoluble compounds are prepared using combinations of natural or synthetic phospholipids, a charged surface modifier such as a highly purified charged phospholipid and a block copolymer coated or adhered onto the surfaces of the water insoluble-compound particles. The combination of charged surface modifier and block copolymer allows the formation and stabilization of the sub-micron and micron size compound particles - stabilized by the charged phospholipid to provide electrostatic stabilization and the block copolymer to provide steric stabilization - and therefore prevents these particles from particle growth, aggregation or flocculation.

La présente invention concerne des compositions et des procédés de préparation de particules stables, de tailles micronique et sub-micronique, de principes actifs qui sont peu ou pas solubles dans l'eau ou d'autres composés industriels utiles et insolubles. Ces compositions et ces procédés sont réalisés par l'utilisation de combinaisons de phospholipides naturels ou synthétiques, d'un agent de surface chargé, tel qu'un phospholipide chargé hautement purifié, et d'un copolymère séquencé qui revêt ou adhère à la surface des particules des composés insolubles dans l'eau. La combinaison d'un copolymère séquencé et d'un agent de surface chargé permet la formation et la stabilisation de particules de composés de tailles micronique et sub-micronique. Le phospholipide chargé procure la stabilisation de nature électrostatique et le copolymère séquencé celle de nature stérique, ce qui permet d'éviter une croissance des particules, leur agrégation ou leur floculation.

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