Proliposomal and liposomal compositions

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/127 (2006.01) A61K 31/337 (2006.01)

Patent

CA 2681302

Concentrates or proliposomal compositions of poorly water-soluble drugs and compounds, comprising of one or more membrane forming lipids, a membrane stabilizing agent, in a suitable vehicle, and optionally containing a Polyethylene Glycol (PEG)-coupled phospholipid or a mixture thereof and further, optionally containing pharmaceutically acceptable excipients such as antioxidants, buffering agents, acidifying agents etc. are provided, which have superior long term stability. The concentrates of proliposomal compositions instantly form liposomes of the said poorly water-soluble drugs and compounds on rapid injection to a diluting fluid, the liposomal composition so obtained, characterized by a physical stability more than 24 hours, >= 95% drug encapsulation and having a particle size diameter of less than 100 nm. The liposomal compositions so obtained can further be directly administered to patients in need of treatment of the poorly water-soluble drugs and compounds.

La présente invention concerne des concentrés ou des compositions proliposomales de médicaments et de composés faiblement solubles dans l'eau, comprenant un ou plusieurs lipides formant la membrane, un agent de stabilisation de la membrane, dans un excipient adapté, et contenant, en option, un phospholipide couplé à du polyéthylène glycol (PEG) ou un mélange de celui-ci et contenant en outre, en option, des excipients acceptables d'un point de vue pharmaceutique, tels que des antioxydants, des tampons, des agents acidifiants, etc., ayant une stabilité à long terme supérieure. Les concentrés de compositions proliposomales forment instantanément des liposomes desdits médicaments et composés faiblement solubles dans l'eau lors de l'injection rapide dans un fluide diluant, la composition liposomale ainsi obtenue étant caractérisée par une stabilité physique de plus de 24 heures, une encapsulation du médicament >= 95 % et ayant un diamètre de taille de particule inférieure à 100 nm. Les compositions liposomales ainsi obtenues peuvent être ensuite directement administrées à des patients nécessitant un traitement par des médicaments et des composés faiblement solubles dans l'eau.

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