Method for the formulation of substances having a low...

A - Human Necessities – 61 – K

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A61K 31/28 (2006.01) A61K 9/127 (2006.01) A61K 9/51 (2006.01)

Patent

CA 2389147

The present invention relates to a method for encapsulating substances, in particular drugs, that have a low water-solubility and lipophilicity, which method comprises providing a lipid system comprising one or more negatively charged lipid(s); combining the lipid system with the substance(s) in a medium at a low total solutes concentration; subjecting the mixture thus obtained to one or more cycles of freezing and thawing to produce lipid-coated aggregates of the substance(s), and optionally removing the free (non-enclosed) substance(s). The method is in particular suitable for encapsulating cisplatin.

La présente invention concerne un procédé d'encapsulation de substances, notamment des médicaments, ayant une hydrosolubilité et une lipophilie faibles, lequel procédé consiste à prendre un système lipidique comprenant au moins un lipide de charge négative ; à combiner ce système lipidique avec la substance dans un milieu à faible concentration totale de solutés ; à soumettre le mélange ainsi obtenu à un ou plusieurs cycles de gel et de dégel en vue de l'obtention d'agrégats enrobés de lipides ; et éventuellement à éliminer les substances libres (non encapsulées). Ce procédé est particulièrement indiqué dans l'encapsulation du cisplatine.

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