GB894810A - Aqueous pharmaceutical solutions containing anti-inflammatory steroids - Google Patents

Abstract

Steroids of the general formula <FORM:0894810/IV (b)/1> wherein the 1 : 2 position is saturated or double-bonded, X is a hydrogen or halogen atom, R is lower (C1-6) alkyl and Z is a divalent hydrocarbon radical of less than 10 carbon atoms may be prepared by treating a compound of general <FORM:0894810/IV (b)/2> formula <FORM:0894810/IV (b)/3> in which the 1 : 2 position may be saturated or double-bonded and X and R have the above stated meanings with a polycarboxylic acid anhydride, e.g. succinic, maleic or phthalic anhydride. Alternatively, they may be partially esterified with a polycarboxylic acid, e.g. oxalic, malonic, succinic, glutaric, maleic, malic, tartaric, citramalic, citric, oxalacetic, phthalic, isophthalic, or terephthalic acid. The intermediate compounds of formula II above may be prepared by treating a compound of the general formula <FORM:0894810/IV (b)/4> wherein the 1 : 2 position is saturated or double-bonded and X is a hydrogen or halogen atom with a ketone, e.g. acetone, methyl-ethyl ketone, diethyl ketone or ethylamyl ketone. Examples include preparations of sodium and ammonium hemi-ester salts.ALSO:Clear, stable, aqueous compositions comprise a polyoxyethylene sorbitan mono-oleate non-ionic surfactant and an anti-inflammatory steroid hormone of the 11b -hydroxy-16a ,17a -di - (C1-6 alkyl) - substituted - methylenedioxy-21 - carboxyacyloxy - 4 - pregnene - 3,20 - dione class, e.g. a compound which may be represented by the general formula <FORM:0894810/VI/1> wherein the 1 : 2 position is saturated or double-bonded, X is a hydrogen or halogen atom, R is lower (C1-6) alkyl and Z is a divalent hydrocarbon radical of less than 10 carbon atoms. The compositions may be in forms suitable for topical application, e.g. to the ears, eye, nose and throat and for parenteral administration. Optionally they may also contain other water-soluble drugs, e.g. antibacterial agents, antibiotics, e.g. neomycin sulphate, and sulpha drugs; conventional buffers, preservatives and isotonicizers.