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United States Patent (19) 11 4,360,518 Rovee Et Al

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United States Patent (19) 11 4,360,518 Rovee Et Al United States Patent (19) 11 4,360,518 Rovee et al. 45) Nov. 23, 1982 54 TOPICAL ANTI-INFLAMMATORY DRUG Primary Examiner-Stanley J. Friedman THERAPY . 57) ABSTRACT 75) Inventors: David T. Rovee, Bridgewater; John A pharmaceutical composition for topical treatment of R. Marvel; James A. Mezick, both of cutaneous disorders or disruptions characterized by East Brunswick, all of N.J. skin inflammation or hyperproliferative epidermal ac 73) Assignee: Johnson & Johnson, New Brunswick, tivity comprises the combination of a topically active N.J. anti-inflammatory corticosteroid and a non-steroidal 21 Appl. No.: 244,569 anti-inflammatory agent which is an inhibitor of prosta glandin synthetase selected from the group consisting of 22 Filed: Mar. 17, 1981 the hydratropic acid derivatives; acetylsalicylic acid; the pyrazolone derivatives; the fenamic acid deriva Related U.S. Application Data tives; the aroyl-substituted pyrroles and the substituted 60) Division of Ser. No. 64,311, Aug. 6, 1979, abandoned, arylacetohydroxamic acids in a pharmaceutically ac which is a division of Ser. No. 788,453, Apr. 20, 1977, ceptable topical vehicle. Treatment of above cutaneous Pat. No. 4,185, 100, which is a continuation-in-part of disorders may also be effected by concurrent therapy Ser. No. 685,942, May 13, 1976, abandoned. using separate applications of corticosteroid and non 51) Int. Cl. ...................... A61K 31/19; A61K 31/56 steroid. (52) U.S. Cl. ..................................... 424/240; 424/317 58) Field of Search ................................ 424/317, 240 18 Claims, No Drawings 4,360,518 1 2 Ziboh, V. A. and Snyder, D. S. 1974 Naturally occur TOPICAL ANTI-NFLAMMATORY ORUG ring and synthetic inhibitors of prostaglandin synthetase THERAPY of the skin. Prostaglandin Synthetase Inhibitors 353-361. Although it is not understood completely, it is thought CROSS-REFERENCE TO RELATED 5 that these effects related to prostaglandin biosynthesis APPLICATIONS are important components of many dermatopatholo This application is a division of our copending appli gies, so a drug which will interfere with this biosynthe cation Ser. No. 64,311, filed Aug. 6, 1979, now aban sis should be useful in the clinical improvement of the doned, which application is in turn a division of our disease. application Ser. No. 788,453, filed Apr. 20, 1977, (now O There are many non-steroidal compounds or agents U.S. Pat. No. 4,185,100, issued Jan. 22, 1980), which which also have anti-inflammatory effects. Many of application is in turn a continuation-in-part of our appli these are believed to act by blocking the prostaglandin cation Ser. No. 685,942, filed May 13, 1976; now aban synthetase complex of enzymes that is present in normal doned. skin and is necessary for the biosynthetic processes 15 described above. Furthermore, as a general rule, these BACKGROUND OF THE INVENTION drugs are relatively free of unwanted side effects. Ex This invention relates to a pharmaceutical composi amples of such non-steroidal anti-inflammatory com tion for the treatment of cutaneous disorders or disrup pounds include aspirin, indomethacin, suprofen, cli tions characterized by skin inflammation and/or hyper profen and ethyl 5-p-chlorobenzoyl-1,4-dimethylpyr proliferative activity in the epidermis. More specifi 20 role-2-acetate. cally, the invention comprises treatment of such disor ders by concurrent topical application to the affected DESCRIPTION OF THE INVENTION area of an anti-inflammatory steroidal drug and of a We have discovered in the course of investigations selected non-steroidal anti-inflammatory drug, each in a with experimentally induced inflammation that topical suitable vehicle. In one preferred embodiment, the in 25 treatment with a combination of certain steroidal and vention comprises the novel combination of an anti-in non-steroidal anti-inflammatory drugs results in unex flammatory steroidal drug with a selected non-steroidal pectedly improved suppression of inflammation than anti-inflammatory drug in a suitable vehicle for topical occurs when either drug is used alone. That is, either Se. the combination is effective where the drugs used sepa There are many steroidal drugs suitable for treating 30 rately are not, or the combination provides more rapid, particular responsive dermatological disorders. Many dramatic improvement than either drug alone, or the of these steroids must be used systemically. Others ex hibit good activity topically in a suitable vehicle. While combination is equally effective at lower concentrations some steroidal anti-inflammatories are effective both than either drug alone. This effect is postulated to result systemically and topically, there is not ordinarily any 35 from the two drugs acting upon different aspects of the predictable relationship between systemic and topical inflammatory response. Particularly in the case of UV activity of a drug, particularly an anti-inflammatory induced erythema, significant therapeutic effects (ame steroidal drug. In addition to having a broad range of lioration of the condition) are produced by combina applicable biological activities (e.g., cell membrane tions of the two types of drugs at concentration levels at stabilization, vasoconstrictor activity, antimitotic effect, 40 which either drug alone has low or minimal effect. The suppression of DNA and protein synthesis, etc.), the steroid/non-steroid drug combination treatment of the steroids often exhibit undesired local and systemic side present invention can also be used in the therapeutic effects when used for prolonged periods. These may be treatment of a wide variety of dermatological disorders manifested in the form of local skin atrophy, or in adre in which inflammation is a component. Examples of nal atrophy in the most severe case. Furthermore, a 45 these diseases are psoriasis, eczema, contact dermatitis, reduction in host defense mechanisms to infection may atopic dermatitis, etc. Inflammation accompanying accompany their use. thermal or chemical burns as well as sunburn are other Beyond the potential undesired side effects, steriods areas for application of the combination therapy of this do not interact with the complete biological spectrum invention, as are diaper rash, insect bite inflammation, of inflammation. For example, ultraviolet (UV) light 50 gingival inflammation and pruritus. Also, vesicular dis induced erythema is not amenable to treatment by ste eases, especially those characterized by acantholysis, roidal anti-inflammatories. UV-induced early changes and other blistering conditions, appear to be particu in skin such as vasodilatation are related to the conver larly susceptible to this therapy. sion of arachidonic acid to E prostaglandins or to inter In accordance with one aspect of the present inven mediate forms such as HETE (12L-hydroxy-5,8,10,14 55 tion, there is provided a topical composition for the eicosatetraenoic acid) or the endoperoxides which are treatment of inflammatory conditions of the skin com vasoactive and are believed to have cutaneous activity, prising a pharmaceutically acceptable topical vehicle such as triggering hyperproliferative epidermal activ containing, in combination, an anti-inflammatory corti ity. See, for example, Bem, J. L. and Greaves, M. W. costeroid and a non-steroidal anti-inflammatory agent 1974 Prostaglandin E1 effects on epidermal cell growth 60 which is an inhibitor of prostaglandin synthetase se "in vitro." Arch. Derm. Forsch. 251:35-41; Snyder, D. S. lected from the group consisting of acetylsalicylic acid; and Eaglstein, W. H. 1974 Topical indomethacin and the hydratropic acid derivatives; the pyrazolone deriva sunburn. Brit. J. Dern. 90:91-93; Snyder, D. S. and tives; the fenamic acid derivatives; the aroyl-substituted Eaglstein, W. H. 1974 Intradermal anti-prostaglandin pyrroles; and the substituted arylacetohydroxamic agents and sunburn. J. Invest. Derm. 62:47-50; and Gol 65 acids. dyne, M. E. et al. 1973 Prostaglandin activity in human The topically useful anti-inflammatory corticoster cutaneous inflammation: Detection by radio-immunoas oids are generally classified as being either halogenated say. Prostaglandins 4:737-749. See also Hsia, S. L., or non-halogenated. Examples of suitable non 4,360,518 3. 4. halogenated ones include hydrocortisone and its 17- and In general, treatment is effected by applying the com 21- esters, such as the 21-acetate and the 17-butyrate, position or compositions to the affected area from one and desonide. Examples of suitable halogenated steroids to about four times daily until the inflammation is re include dexamethasone, triancinolone acetonide, fluo lieved. The duration of treatment will vary with the cinolone acetonide, fluocinonide and betamethasone 17-valerate. severity of the condition, and will be about the same Suitable hydratropic acid type non-steroidal anti-in whether combination compositions are used or separate flammatory prostaglandin synthetase inhibitors that compositions of the different active ingredients are may be used in the compositions of the present inven applied simultaneously. tion are suprofen, cliprofen, cicloprofen, fenoprofen, O TYPICAL COMBINATION FORMULATIONS flurbiprofen, ibuprofen, ketoprofen, naproxen and pir profen. Phenylbutazone is an example of a suitable py (Unless otherwise indicated, throughout this specifi razolone derivative, while flufenamic acid and mefe cation, all amounts are by weight.) namic acid are examples of suitable fenamic acid deriva tives. Suitable aroyl-substituted pyrroles
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