Compositions emitting positrons and containing inorganic...

A - Human Necessities – 61 – K

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A61K 51/12 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2691580

The invention relates to pharmaceutical agents containing a particulate inorganic matrix having a diameter of from 0.1 nm to 100 µm, preferably 1 nm to 10 µm, particularly preferably 1 nm to 1 µm, such as, for example, topaz, (Al2F2)[SiO4], and chiolite, Na[Al3F4], preferably wavellite, Al3(PO4)2(OH, F)2, calcium carbonate, CaCO3, maghemite, Y-Fe2O3, particularly preferably zeolites, gen. formula Mn[(AlO2)x(SiO2)y](M = metal, e.g. Na), magnetite, Fe3O4, and barium sulphate, BaSO4, and very particularly preferably gallium phosphate, GaPO4, apatite or fluorohydroxyapatite, Ca5(PO4)3(OH, F) = 3Ca3(PO4)2 * Ca(OH, F)2, and fluorspar, CaF2, which, in addition to the natural isotope distribution of the structure type--forming elements of the anions and cations, also contain medically usable contents of positron-emitting nuclides, such as, for example, [15]O, [30]P, [13]N, preferably [65]Ga, [11]C, particularly preferably [131]Ba, [26]Al, and very particularly preferably [68]Ga and [18]F, the preparation thereof, and the use of these composition in medicine, particularly preferably in diagnostic imaging, in particular positron emission tomography (PET), on animals and humans, and in vitro diagnostics.

La présente invention concerne des agents pharmaceutiques contenant une matrice minérale particulaire ayant un diamètre de 0,1 nm à 100 µm, de préférence de 1 nm à 10 µm, de préférence encore de 1 nm à 1 µm, par exemple de la topaze, (Al2F2)[SiO4] et de la chiolithe, Na[Al3F4], de préférence de la wavellite, Al3(PO4)2(OH, F)2, du carbonate de calcium, CaCO3, de la maghémite, ? -Fe2O3 en particulier de préférence de la zéolithe, de formule générale Mn[(AlO2)x(SiO2)y] (M= métal par ex. Na), de la magnétite, Fe3O4, et du sulfate de baryum, BaSO4, et tout particulièrement du phosphate de gallium, GaPO4, de l'apatite ou de la fluorhydroxylapatite, Ca5(PO4)3(OH, F)=3Ca3(PO4)2 *Ca(OH, F)2, et du spath fluor, CaF2, qui contiennent, en plus des éléments des anions ou cations, formant la répartition isotopique naturelle des types structurels, également des proportions médicalement utiles en nucléides émettant des positrons, tels que [15]O, [30]P, [13]N, de préférence [65]Ga,[11]C, de préférence encore [131]Ba, [26]A1, idéalement [68]Ga ou [18]F. L'invention concerne également le préparation de ces agents pharmaceutiques, l'utilisation de ces compositions en médecine, de préférence pour l'imagerie diagnostique, en particulier la tomographie par émission de positrons (TEP), chez l'animal et chez l'homme ainsi que pour le diagnostic in vitro.

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