GB1125410A - Pharmaceutical compositions containing sulphones - Google Patents

Abstract

1,125,410. Compositions containing sulphones. MERCK & CO. Inc. 27 July, 1966 [2 Aug., 1965], No. 33803/66. Headings A5B and A5E. [Also in Division D2] Pharmaceutical and biocidal compositions comprise hydroxy-aliphatic sulphones or their acyl esters, of formula: or their cyclic acetals, of formula: wherein each of R and R<SP>1</SP> is a cycloaliphatic group, or an aliphatic group or R and R<SP>1</SP> together are an alkylene group of at least 3 carbons forming a heterocycle with the sulphur atom, R<SP>1</SP> in the acetals having at least 2 adjacent carbons to which are attached the oxygen atoms; X<SP>1</SP> is hydrogen or an acyl radical, R<SP>2</SP> and R<SP>3</SP> are each alkyl, and n and n' are each 0-2, with n + n' being 1 or 2; together with an inert carrier diluent or coating, which, if other than a solid or an oil, includes one or more sweetening, flavouring, colouring, preserving, suspending or wetting agents; optionally together with other active ingredients. The pharmaceutical compositions may be in forms suitable for oral, parenteral or topical application, and may take the form of tablets, aqueous or oily suspensions, dispersible powders or granules, emulsions, hard or soft capsules, syrups or elixirs, skin penetrant ointments, creams, lotions, or sprays, and mucosally absorbed forms such as suppositories and nasal compositions. The sulphones have tissue penetrant properties and may be included in compositions containing other, non-penetrant active agents, to promote absorption of the latter. Preferred such compositions are anti-perspirant creams, lotions, emulsions, powders or self-propelled aerosols, wherein the further active agent is a metal salt astringent such as zirconium lactate, zinc phenol sulphonate, or an aluminium salt such as the chloride-hydrate, hydroxidedichloride-hydrate, phosphate, sulphonate, or phenolsulphonate. The sulphones have anti-inflamatory activity including analgesic and anti-pyretic properties, and they also relieve respiratory congestion; additionally they have muscle relaxant, microbicidal, (including fungi and viruses), and diuretic properties, and have application in the treatment of burns and circulatory deficiencies and to promote the healing of skin grafts. The invention includes a method for treating animals to relieve pain, fever and inflammation, comprising administering the sulphone. Biocidal compositions of the active sulphones are useful for freeing a non-human locus from micro-organisms, including bacteria, fungi and viruses, and they may be employed as industrial slimicides in re-cycled water, used in air-conditioning units, or the textile or chemical industries.