Soluble compositions of triphenylethylene antiestrogens

Details Soluble compositions of triphenylethylene antiestrogens Soluble compositions of triphenylethylene antiestrogens

A - Human Necessities

61

K

A61K 31/138 (2006.01) A61K 31/40 (2006.01) A61K 31/4025 (2006.01) A61K 47/12 (2006.01)

Patent

CA 2355175

The invention relates to aqueous compositions of nonsteroidal triphenylethylene antiestrogens for pharmaceutical use comprising as a solubility enhancing agent a pharmaceutically acceptable mono- or dicarboxylic acid having 1-5 carbon atoms, wherein the carbon chain may further contain 1-4 hydroxyl, 1-3 oxo, or one or several halogen substituents, or a corresponding anion thereof, or methanesulfonic acid or its corresponding anion, in molar excess with respect to the triphenylethylene antiestrogen, optionally together with an organic water miscible co-solvent such as polyethylene glycol (PEG), propylene glycol, ethanol or isopropanol.

Cette invention a trait à des compositions aqueuses à base d'anti-oestrogènes non stéroïdiens de la classe des triphényléthylènes, à usage pharmaceutique, contenant comme agent solubilisant un acide, acceptable du point de vue pharmaceutique, monocarboxylique ou dicarboxylique portant de 1 à 5 atomes de carbone, la chaîne carbonée contenant, en outre, 1-4 hydroxy, 1-3 oxo ou un ou plusieurs substituants halogènes ou bien leur anion correspondant ou un acide méthane-sulfonique ou son anion correspondant en excès molaire relativement à l'anti-oestrogène de la classe des triphényléthylènes, éventuellement, en association avec un co-solvant organique miscible à l'eau notamment du polyéthylène glycol (PEG), du propylène glycol, de l'éthanol ou de l'isopropanol.

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