IL31289A - Pharmaceutical preparation containing a dermatologically active difluorinated corticoid and dithranol - Google Patents

Abstract

1,225,830. Anti-psoriasis compositions. CIBA Ltd. 31 Dec., 1968 [8 Jan., 1968], No. 61909/ 68. Heading A5B. Pharmaceutical preparations, e.g. ointments, creams, pastes, foams, lotions and aerosol sprays, for the treatment of psoriasis, contain a dermatologically active steroid, and a triester of dithranol (1,8,9-trihydroxyanthracene) with a C 1-6 alkanoic acid unsubstituted or substituted by halogen and/or C 1-6 alkyl, in admixture or conjunction with a pharmaceutically suitable carrier. Triacetyldithranol is preferred. Suitable steroids include hydrocortisone, prednisolone, fluocortolone, fluorohydrocortisone, dexamethasone, betamethasone, triamcinoline and its acetonide, fluorometholone, 3, 20-dioxo- 6-fluoro-11, 16, 17, 21-tetrahydroxypregna-#<SP>4</SP>- en-16, 17-acetonide, fluocinolone acetonide and flumethasone or their esters with alkanecarboxylic acids or with inorganic acids, e.g. phosphoric or sulpuric acid, such as flumethasone pivalate. The preparations may also contain a keratolytic, e.g. salicyclic acid, antibiotics, antimycotics or antiseptics.

Description

Pharmacoutical preparations containing a corticoid and dxthranol 29551 la The present invention is concerned with new pharmaceutical preparations for the treatment of which are characterized in that they contain in addition to a dermatologically active difiuorinated corticoid a triester of dithranol in conjunction with a pharmaceutical has been known for 4507c and to treat psoriasis with clinical trials have shown that good results can te achieved in of the cases with of flumethasone pivalate I has further been known to treat psoriasis with dithranol or a triester thereof for British Patent Specification and In clinical trials good results were achieved in of the cases with a triacetyl dithranol It observed that compositions with a triester dithranol or pure dithranol as the only active ingredient cause irreversible coloration of linen and skin and rise to conjunctivitis and kerato unctivitis which occur in about of the cases with triacetyl dithranol and in about the cases with dithranol It has now been unexpectedly found that combination of a difiuorinated corticoid with a triester of dithranol produces a synergistic effect which is manifested in a higher activity and absence of the disadvantages inherent in compositions containing only an ointment according to the invention containing of triacetyl dithranol Suitable dermatologically active difluorinated corticoids are fluocinolone acetonide or or their esters with lower alkanecarboxylic or with inorganic acids phosphoric or sulphuric in the first place the flumethasone of dithranol are especially alkanoyl in the first place The new preparations contain the dermatologically active steroid in the usual more especially in a concentration from to especially from to The esters of dithranol are present in i the preparations named preferably in a concentration j from to especially from j 1 to above all from 2 to The new preparations may be in any form that can be applied to the such as aerosol sprays or especially the may further preferably contain a such as salicylic advantageously in a concentration from 1 to especially The new preparations are formulated in the tional using assistants that do not react with the active stearic stearyl vegetable benzyl polyalkylene or other medicinal If they may further contain other assistants such as colouring or aromatic They may also contain further therapeutically ful compounds such as antimycotics or The new preparations may used only in human medicine but also in veterinary medicine for the treatment of similar diseases in dogs or The invention is also concerned with the manufacture of the new wherein the active if desired together with are made up in the usual manner into the desired form of The following Examples illustrate the invention without restricting Example 1 Paste grams Flumethasone pivalate purified white petroleum to make 0 The paste is prepared by melting the white petroleum jelly together with the pasting the active ingredients with part of this fat adding the zinc and mixing and thoroughly homogenizing the The resulting genizate is added to the remainder of the fat melt and the whole is thoroughly The g of flumethasone pivalate used above be replaced by 0 03 g of fluocinolone acetonide or by 08 g of botnmcthaoonc valerate or by g of 2 Cream grams Flumethasone pivalate 0 triacetyldithranol white wax 0 spermaceti 0 arachis oil 22 lanolin 5 castor oil 5 0 deionized water to make 100 grams The white arachis oil and lanolin are melted the resulting fat melt is emulsified in warm the active ingredients are pasted with part of the resulting emulsion and the remainder of the emulsion is ously stirred The castor oil is then stirred cold into the resulting emulsion and the whole is Example purified white petroleum jelly to make grams The ointment is obtained by melting the suint togethe with the white petroleum pasting the active ingredients with part of the resulting fat stirring until cold and In a similar manner an ointment of the following composition can be grams Flurnethasone pivalate triacetyldithranol salicylic acid purified white petroleum jelly to make grams The g of flurnethasone pivalate used in these ointments may be replaced by of fluocinolone or by g of betamethasone valerate or by g dcxamcthaoono Example Ointment grams Flurnethasone pivalate triacetyldithranol salicylic acid purified white petroleum jelly to make grams The ointment is obtained by melting the suint gether with the white petroleum pasting the active 0ι02 g of flumothaeone pivalate used in this ointment may be replaoed by g of prednieolon by g of o The triacetyldithranol used in these Examples may be replaced by a corresponding of an other triester of dithranol the thranol or the tricoproyldithranol Example alcoholic solution Flumethasone pivalate triacetyldithranol salicylic acid polyethyleneglycol ethanol to make The solution may be obtained by dissolving the flumethasone pivalate on the polyethylene glycol and the triacetyldithranol and the salicylic acid in The two solutions are thoroughly mixed and 312 insufficientOCRQuality

Claims (1)

1. CLAIMS A pharmaceutical preparation for the treatment of psoriasie containing in addition to a active corticoid a of dithranolp and a ceutical A pharmaceutical preparation according to Claim as a a alkanoic acid ester of Λ pharmaceutical preparation according to Claim containing a of dithranol the A preparation according to any of Claims 1 to 3 containing to 15 cent of the pharmaceutical preparation according to one of Claims 1 to containing 1 to 10 per cent the A pharmaceutical preparation according to one of 1 to 3 containing 2 to 5 cent of the A pharmaceutical preparation according to any one of 1 to containing pharmaceutical preparation according to Claiai 7 containing the corticoi in a concentration from to per A pharmaceutical preparation according to 7 containing the luorinated corticoid in a concentration from to per pharmaceutical preparation according to any one of 1 to containing a Q A pharmaceutical preparation according to Claim containing salicylic acid as A pharmaceutical preparation according to Claim containing salicylic acid in a concentration from 1 to A pharmaceutical preparation according to any of Claims 1 to 12 in the of an ointment A pharmaceutical preparation according to any one of Claims 1 to 12 in the form of a pharmaceutical preparation according to any one of Claims 1 to 12 in the form of a A pharmaceutical preparation according to any one of Claims 1 to 12 in the form of a A pharmaceutical preparation according to any one of Claims 1 to 12 in the form of an aerosol For the Applicants AMD PARTNERS insufficientOCRQuality