Método para preparar partículas submicrónicas de paclitaxel o docetaxel

    公开(公告)号:ES2388924T3

    公开(公告)日:2012-10-19

    申请号:ES04810266

    申请日:2004-11-03

    Applicant: BAXTER INT

    Abstract: Método para preparar una composición farmacéutica de partículas submicrónicas de paclitaxel o docetaxel,siendo la solubilidad del paclitaxel o docetaxel mayor en un primer disolvente miscible en agua que en unsegundo disolvente que es acuoso, incluyendo el método los pasos de:i) mezclar un primer modificador superficial que comprende un fosfolípido conjugado con un polímerosoluble en agua o hidrófilo en el primer disolvente miscible en agua o en el segundo disolvente o enambos, el primer disolvente miscible en agua y el segundo disolvente;ii) mezclar un segundo modificador superficial seleccionado de entre el grupo consistente en agentestensioactivos aniónicos, catiónicos, no iónicos y modificadores biológicos con actividad superficial, en elprimer disolvente miscible en agua o en el segundo disolvente o en ambos, el primer disolvente misciblecon agua y el segundo disolvente;iii) disolver el paclitaxel o el docetaxel en el primer disolvente miscible en agua para formar una solución;iv) mezclar la solución con el segundo disolvente para definir una pre-suspensión de partículas; yv) homogeneizar la pre-suspensión para formar una suspensión de partículas pequeñas con un tamaño departícula efectivo medio inferior a aproximadamente 1.000 nm.

    Method for preparing submicron particles of paclitaxel

    公开(公告)号:NZ546439A

    公开(公告)日:2010-04-30

    申请号:NZ54643904

    申请日:2004-11-03

    Applicant: BAXTER INT

    Abstract: Disclosed is a method for preparing a pharmaceutical composition of submicron particles of precipitated paclitaxel or its derivative compounds, the solubility of which is greater in a water miscible first solvent than in a second solvent that is aqueous, the method comprising the steps of: (i) mixing into the water-miscible first solvent or the second solvent or both the water miscible first solvent and the second solvent, a first surface modifier comprising a phospholipid conjugated with a water-soluble or hydrophilic polymer; (ii) mixing into the water-miscible first solvent or the second solvent or both the water miscible first solvent and the second solvent, a second surface modifier selected from the group consisting of: anionic surfactants, cationic surfactants, non ionic surfactants and surface active biological modifiers; (iii) dissolving paclitaxel or its derivative compounds in the water-miscible first solvent to form a solution; (iv) mixing the solution with the second solvent to define a pre-suspension of particles; and (v) homogenizing the pre-suspension to form a suspension of precipitated small particles having an average effective particle size of less than about 1000 nanometres. Also disclosed is a composition of submicron particles of precipitated paclitaxel or its derivative compounds prepared by said method.

    19.
    发明专利
    未知

    公开(公告)号:NO20062378L

    公开(公告)日:2006-05-24

    申请号:NO20062378

    申请日:2006-05-24

    Applicant: BAXTER INT

    Abstract: The present invention is concerned with the formation of small particles of an organic compound by mixing a solution of the organic compound dissolved in a water-miscible organic solvent with an aqueous medium to form a mix and simultaneously homogenizing the mix while continuously removing the organic solvent to form an aqueous suspension of small particles essentially free of the organic solvent. These processes are preferably used to prepare an aqueous suspension of small particles of a poorly water-soluble, pharmaceutically active compound suitable for in vivo delivery by an administrative route such as parenteral, oral, pulmonary, nasal, buccal, topical, ophthalmic, rectal, vaginal, transdermal or the like.

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