Soluble compositions of triphenylethylene antiestrogens

A method for preparing an aqueous solution of a nonsteroidal triphenylethylene antiestrogen or a pharmaceutically acceptable salt thereof, comprising contacting the nonsteroidal triphenylethylene antiestrogen or pharmaceutically acceptable salt thereof with aqueous media and a solubility enhancing agent selected from the group consisting of

• 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, with the proviso that the nonsteroidal triphenylethylene antiestrogen or a pharmaceutically acceptable salt thereof is not in the form of cyclodextrin inclusion complex.

A method for preparing an aqueous solution of a nonsteroidal triphenylethylene antiestrogen or a pharmaceutically acceptable salt thereof comprising contacting the nonsteroidal triphenylethylene antiestrogen or pharmaceutically acceptable salt thereof with aqueous media, an organic water miscible co-solvent and a solubility enhancing agent selected from the group consisting of

• 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, with the proviso that the nonsteroidal triphenylethylene antiestrogen or a pharmaceutically acceptable salt thereof is not in the form of cyclodextrin inclusion complex.