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OwnerJohan Adriaan Martens, Christine Eva Antonia Kirschhock +4inventors
InventorsJohan Adriaan Martens, Christine Eva Antonia Kirschhock, Sebastien Philippe Brigitte Kremer, Alexander Jan Maria Herman Eugeen Aerts, Guy Van Den Mooter, Jan Van Humbeeck
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The invention describes a new class of crystalline silica material having two levels of porosity and structural order. At the first level, building units are nanoslabs of uniform size having zeolite framework. At the second structural level, nanoslabs are assembled, e.g. linked through their corners, edges or faces following patterns imposed by interaction with cationic surfactant or triblock copolymer molecules. After evacuation of these molecules, microporosity is obtained inside the nanoslabs, and a precise mesoporosity between the nanoslabs depending on the tiling pattern of the zeolite nanoslabs, as evidenced by X-ray diffraction. These materials are useful for the fixation of biologically active species, such as poorly soluble drugs.
A pharmaceutical composition for the immediate release of a poorly soluble drug, comprising said poorly soluble drug and a substantially ordered mesoporous silica, wherein the drug molecules are loaded on the mesoporous silica material, wherein the water solubility of said biologically active species is below 2.5 mg/ml, wherein the molecular weight of said poorly soluble drug is between about 200 and 1,000 Daltons, and wherein said ordered silica has one level of porosity or structural order, has a highly ordered, two-dimensional hexagonal (P6mm) honeycomb mesostructure, which upon calcination at 500° C. yields porous structures with high BET surface areas of 690 to 1040 m2/g and pore volumes up to 2.5 cm3/g, ultra large d(100) spacings of 7.45-45 nm, and silica wall thicknesses of 3.1 to 6.4 nm, and has a pore size in the range 6 nm to 14 nm and is obtained in the absence of an alpha-tocopherol polyethylene glycol ester templating biomolecule.
A process for producing a pharmaceutical composition comprising a poorly soluble drug loaded on a substantially ordered mesoporous silica, wherein the water solubility of said poorly soluble drug is below 2.5 mg/ml, wherein the molecular weight of said poorly soluble drug is between about 200 and 1,000 Daltons, and wherein said ordered silica has a highly ordered, two-dimensional hexagonal (P6 mm) honeycomb mesostructure, which upon calcination at 500° C. yields porous structures with high BET surface areas of 690 to 1040 m2/g and pore volumes up to 2.5 cm3/g, ultra large d(100) spacings of 7.45-45 nm, and silica wall thicknesses of 3.1 to 6.4 nm, and wherein said ordered silica has one level of porosity or structural order, has a pore size in the range of 6 nm to 14 nm, and is obtained in the absence of an alpha-tocopherol polyethylene glycol ester templating biomolecule, wherein a physical mixture of said biologically active species and said substantially ordered mesoporous silica is suspended in an appropriate solvent other than a supercritical fluid, and the suspended mixture is stirred until the poorly soluble drug is substantially entirely fixed or entrapped within the pores of the ordered mesoporous silica.
Dependencies are inferred from the claim text.