GB794486A - Steroid compositions and the preparation thereof - Google Patents

Abstract

Therapeutic compositions comprise a compound having the formula <FORM:0794486/VI/1> wherein St represents the androstane structure having a 3-keto group and at least a 4(5)-double bond, R represents a lower a ,b - or lower a ,g -alkylene radical having at least one methyl group and each of the carbon atoms adjacent R has a methyl group two atoms removed from it and the salts thereof. An intravenous preparation is obtained by dissolving sodium biphosphate, sodium phosphate and sodium hydrocortisone 21 - hemi - b ,b - dimethylglutarate in water and lyophilizing. The sodium salt may be replaced by an amine or alkaline earth salt in which case the sodium phosphate is replaced by a corresponding phosphate. Aqueous compositions for treatment of the eye are buffered with phosphate and made isotonic with sodium chloride. Merthiolate, chlorobutanol and benzyl alcohol may be added as preservatives. An ointment for application on the skin employs a vehicle comprising 3 parts white petrolatum and 1 part liquid petrolatum or alternatively 55 per cent white petrolatum, 25 per cent white mineral oil and 20 per cent wool fat. The compositions for external use may be in the form of dusting powders (e.g. in an inert base such as lactose), oil-in-water emulsions, lotions and anhydrous water-soluble ointments (e.g. higher molecular weight polyethylene glycols). The compositions may also take the form of suppositories, bougies (e.g. with cocoa butter or polyethylene glycols), vaginal creams, ointments for mastitis and dental cones. Orally the compositions are administered in the forms of tablets, lozenges, gelatine capsules, granules and aqueous solution. Flavouring, colouring, sweetening agents and alcohol may then be present. Effervescent tablets are obtained by the addition of a tartaric acid-citric acid-sodium bicarbonate base. Preparations for injection comprise also the adrenocorticotrophic hormone, and saline solution. In addition, non-antigenic pharmaceutical gelatine or oxypolygelatine may be present. Other therapeutic materials which may be incorporated in the water-soluble compositions are penicillin G, penicillin O, procaine penicillin, N,N1-dibenzylethylenediamine penicillin, bacitracin, tetracycline, chlortetracycline, oxytetracycline, chloramphenicol, streptomycin, dihydrostreptomycin, erythromycin, circulin, endomycin, tyrothrycin, gramicidin, sorbic acid, nitro furazone, chlorazodin, hexachlorophene, undecylenic acid, propionic acid, sodium and/or zinc caprylate, lower alkyl p-hydroxybenzoates, sodium sulphacetamide, sulphisoxazole diethanolamine, sulphamerazine, and sulphamethazine. Similarly thiamine, ribaflavin, pyridoxine, ascorbic acid, pantothenic acid, menadione, nicotinamide or Vitamin B12 can be included in a composition for oral or parenteral use. Specifications 794,483, 794,484 and 794,485 are referred to.