Steroid monohydrates, formulations containing same and method

C - Chemistry – Metallurgy – 07 – J

Patent

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260/58, 260/69,

C07J 5/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 53/00 (2006.01)

Patent

CA 1195975

Abstract STEROID MONOHYDRATES, FORMULATIONS CONTAINING SAME AND METHOD The invention provides a monohydrate of a steroid having the structure Image and the 1,2-dehydro derivatives thereof, wherein R1 is chlorine, fluorine or hydroxy and R'1 is hydrogen or R1 and R'1 together are =O; R2 is hydrogen or halogen; R3 is hydrogen, methyl or fluorine; R4 is hydrogen, hydroxy, Image or halogen; and R5 and R6 are the same or different and are hydrogen, alkyl, alkylthio, alkoxy, carboalkoxy, formyl, Image hydroxy, halogen, phenyl or cyano, with the proviso that when R5 and R6 are different, one of R5 and R6 is hydrogen, said monohydrate being in the form of a particulate material having a stable average particle size of less than about 20 microns, a method for forming the monohydrate in said particulate form, and cream and lotion formulations containing the said particulate form steroid monohydrate.

419700

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