DE1767068A1 - Medical adhesive plaster - Google Patents

Description

D? .. !. M. MAAS D? .. WG? RiliFFER

PATSNTA-! 7 5 LTE β M 'J M CHFN 23 UNOEÜERSTRASSE 25

Eli Lilly and Company

Indianapolis, Indiana,

Mediainisehe3 adhesive plaster

The invention relates to a medical adhesive tape (pressur e ~ seneitive adhesive tape) for direct application the damaged skin

For the topical treatment of stubborn abnormal ones Skin affections, such as 2oB, used to treat psoriasis (Scaly lichen) were occlusive = "bandages with anti-inflammatory steroids used. The inflammatory" - Hemraende steroid in the form of a cream or ointment applied to the diseased skin area and the whole area with a plastic or other airtight material covered to keep both air and clothing away from the diseased area of skin * The edges of the abeohlies-

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Send plastics are then tightly bonded to the neighboring healthy skin with plaster strips or old a bandage mullwicklimg detained »

In this treatment with Qooluaiv dressings, you must Patient wear finger gloves o made of plastic during the treatment «if the edge or the pingers are diseased o Garment bags are currently used to protect injuries to cover the torso or buttocks and fit tightly tight caps are required for the treatment of damage to the scalp The use of has recently received * Borrowed occluaiv dressings with anti-inflammatory steroids is actually based on the pure application of steroids prefers the skin surface, leaves this known type of treatment with Occlueiv dressings or final dressings However, much to be desired »When plastic films, especially items of clothing made from such films, are worn by toddlers and children, there is always a risk of oppression and the children blew during strictly monitored throughout the treatment period o The The inflammation-promoting properties of various plastic films represent a further danger »If beyond that If large areas of the body are covered, the body's heat balance can be affected

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Another undesirable property of the common ooolueiv dressings is that they are very bulky and unsightly, so that patients often do not have their hats when they do I am not in bed to wear Oeclueiv bandages and thereby failing to take advantage of these bandages during long periods of the day currently not possible to cover only the damaged area on a specific part of the body »When ZoB · several diseased areas on an arm or hand in front of » must lie, the whole arm or the whole hand with the closure bandage be covered »Pail, in addition, large areas of the skin are drawn to it difficult to ensure intimate contact of the dressing with the entire diseased skin area

Another disadvantage of conventional treatment methods is that the amount of the agent that is to be applied to the damaged skin area is not precisely adjusted can be »There is also no guarantee that the drug will be in the area where it is most needed is, remains o In those cases in which the OcclusiY associations are not put on during the day, there is a risk that the unprotected medication will come off the clothing » is rubbed o

Admittedly, there were ready-made porous bandages with

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which medication is impregnated and used to treat various skin diseases (see ZoBo Belgian Patent specification 638 231) «these bandages and dressings are suitable eioh, however, absolutely not for the treatment of the Feoria » ice and other persistent abnormal skin diseases, for which a non-porous, non-irritating dressing is used must be o

An occlusive dressing that has the disadvantages listed above does not have, would therefore make a valuable contribution to the technology of treating skin diseases ideally, such a bandage should only be applied to the diseased area of skin? as usual self-adhesive Plasters are stuck on small wounds «. The ideal Bandage should also contain a metered amount of the anti-inflammatory steroid with such a bandage the patient only contains a self-adhesive "drug containing" Apply a tight, tight bandage directly to the area to be treated, eliminating the need for Applying the ointment or cream containing the steroid, wrapping the surrounding area with a plastic film and connecting this plastic film to the healthy skin with an adhesive strip could be avoided o

The invention therefore aims at a new occlusive dressing,

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which does not have the disadvantages of known Ocaluaiv dressings.

This object is achieved by the invention with a medical one Plaster for direct application to skin damage, in the case of the invention a surface of the plaster has a surface that adheres when pressure is applied, with an acrylate ester-acrylic acid copolymer and an anti-inflammatory steroid uniformly distributed in a therapeutically effective concentration

In a preferred embodiment of this invention is the anti-inflammatory steroid Flurandrenoloru

The medical patch according to this invention ensures that the anti-inflammatory steroid is evenly distributed over the appropriate self-adhesive surface of the patch so that a precisely dosed amount of the steroid is available when the patch is applied to the area to be treated ieto the preferred inflammatory steroid Flurandrenolone {6-ÖC -Pluor-16 »QC ~» hydroxyhydroordieeii-i6flC _t 17 06-acetonide) and its concentration is preferably in the range of 14 to 16 micrograms per cm of plaster (0.4 to 1.6 mg per 100 ca » of the plaster).

Other anti-inflammatory steroids that are used for manufacturing

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of the medical patches that can be used according to this invention, are the 16-methyl steroids, KoB ₀ ? ltuoethafton (6 <rf, _e 9ÖC - = Dinuor «16e6 -methyl-i ^ -pregiiadieji-iie ^ iTÖC., 21-triol- = 3 ₈ 20-dione), ß-methasone (98k ~ fluoro-16ß-acetyl-1,4-pregnadien-11fl _s 17ÖG, 21-triol ~ 5,20-dione), dexamethasone (9Ö £ -fluor ~ 16ÖC - methyl-i ^ -pregnadlen-iiaji? &, 21- ^ 101-3,20-dione) and their 17 & -Eeter ₉ in particular the Valerat ™ and caprate esters; other Aoefconlde as Triatacinolon (9ö £ ~ -fluoro-16ÖC hydroxycortison "i6ÖC, 17 QC acetonide)" 9 QL ₈ 11.beta.-dichloro 6ÜC - ■ Iuor ~ 1.4 »pregnadlen" = i6Ö6, 17ÖC, 21-triol ~ 3 _e 20 ~ dlon ~ 16 X, 17 OC -acetonide, 9 J6, 11β-dichloro »6 U *, 21 difluoro-1,4 ~ pregnadiene-16 ^ C» 17 U- diol-3,20 ~ dione ~ i6 & , 17 Ü6 acetonide, 9 OC, 118 "Diohlor-6 G6 ^ f luor -1,4,6 'pregnatrien-16 ÖC, 17 ^ C" 21-triol "20 5 _t-dione OE6 = 16, 17 £ - aoetonide; and the usual corticosteroids, cortisone, hydrocortisone, prednisolone »Medrol (6 & -Metnylprednisolun) u _o like ₀ · dl worshipers of the above anti-inflammatory steroids are also suitable, such as propionates, acetates, phosphates, Piralate These steroids »These steroids are used in a concentration with an activity of 4 to 16 micrograea

Fluorandrenolone per cn plaster equivalent ieto

The novel ooclusive dressing according to this invention is by spraying a solution of one of the above-mentioned steroids onto the eelbathing surface of a plaster.

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one side of which is a layer of one when pressure is applied adhering adhesive is already located, or by mixing one of the above-mentioned steroids with the adhesive prior to application of the same to the plaster carrier will ο

The use of the medicated plaster according to this invention in the therapy of skin affections that respond to anti-inflammatory steroid treatment; has a number of advantages over conventional treatment measures »(1) the peroutane penetration of the anti-inflammatory Steroid is enlarged; (2) a uniform concentration the therapeutically effective agent is given over the entire area of the skin affection to be treated; (3) only the sick area must be covered; (4) an intimate relationship Tact the preparation with the diseased skin is guaranteed at all times and (5) an unnecessary waste of the often very expensive therapeutically effective steroid is prevented because only the area to be treated has to be covered and a Loss of medication on the bandage tissue and normal skin » areas of the body not done <,

According to one embodiment of this invention, the medical patch made by putting a solution of an anti-inflammatory steroid on the self-adhesive top *

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B ~

A plaster is sprayed onto the surface on which there is already a Sahiaht on a string or a binding agent that adheres when pressure is applied, _{or the like}

ßejaäß the preferred Ausführungeform of this invention Fluorandrenolon is introduced into the Bindemitteliaisohung "be ^ or it is applied to a nichtpcrösen, flexible carrier in such a concentration that the Pluorandrenolon τοη in a concentration from about 4 to 16 Mikrogramra per cm patch (O _f O4 Ms 1.6 mg per 100 cm plaster) is present <,

Must the plaster itself? he was flexible. be to calibration anzupassenο the curvature of the body surface is applied to the as, Further, it must be made of non-porous material, so that the finished product as diaht closing dressing or Ocelusiv dressing can serve _Q The properties of the adhesive need so eein _r that they allow diffusion of the steroid through the adhesive layer. Of course, the adhesive itself must not irritate the skin. The adhesive force should be sufficient "to allow the plaster to adhere to the surface of the skin when light pressure is applied",., The plaster must adhere firmly to the skin during normal use "The The adhesive strength of the adhesive must not be so great that skin

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ait been abgezoger "when the patch τοη might be taken to ^T EN as idelnden area." Plaster backing and paving binder ₉ which meet these conditions are _s described in US Patent RE 24,906 Pateritschrift ".

The invention is explained on the basis of the following examples. These examples describe processes with which pluorandrenolone can be applied to the pavement _c

example 1

A Pflasteretreifen, 3 _S 8 om wide (1.5 inches), was prepared by a Iscaraylaerylatacrylsäure ^ copolymer to a cellulose film in accordance with Example 1 of United States Patent HE was coated 24,906 ". The strip of plaster was wrapped in a spiral with the adhesive side out onto a cylinder with a circumference of 96.5 cm (38 inches) so that it was nowhere on top of one another and no cylinder surface was exposed. The cylinder was 22.9 ca (9 inches) ) tall and a 457 cm (180 inches) plasterate tire roller attached While the cylinder was rotated at a rotational speed of 24 revolutions per minute, 100 cm of an acetone solution containing 10.0 ag of fluoroandrenolone was added; 15 psi pressure was sprayed along the center of the strip using an air brush with an Aranei center probe while the cylinder rotated

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~ 10

The spray was then directed onto the edges "where the windings met" Daa spraying the center and the edges vmrde alternately continued until the geaamte Solution was used up The plaster was then dried for about 20 minutes and then wound onto a spool

Their analysis showed that fluorandrenolone was on the adhesive layer

ο in a concentration of 0.402 days per 100 om plaster present An examination of the plaster 21 days after application of the agent showed. that during the Lagerna the puorandrenolone activity had not decreased

Example 2

A polymer produced by copolymerizing the acrylate ester of commercial fusel oil and acrylic acid in a ratio of 19: 1 in ethyl acetate as solvent using benzyl peroxide as catalyst, was dissolved in a solvent of 70 parts of ethyl acetate and 30 parts of isopropanol, so that there was a concentration of 20 o pluorandrenolone was in this solution dissolved in an amount 0.1 $ equivalent to the amount of the polymer present

Silicone release paper with a uniform layer from the back

2 coated thick enough to give 418 mg of adhesive per 100 on of paper. The solvent was

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ifji anifernä. Thereupon from you a pdyäthyleiif A ¹ "on daa iEi'tmi vtsl with an instruction of warmth and that

tr was withdrawn, analysis showed that

ρ in a range of about O ~ 4 rag per 100 cm

Plaster was present in the adhesive layer *

For the plasters described above, the adhesive is produced by Cc-polymerizing a larger proportion of an acrylic acid ester and a smaller proportion of acrylic acid. In addition to the above-mentioned, ZoBo 2 ethylbutylacrylate, ethyl acrylate and iooootyl acrylate, as described in US Pat. No. RE 24 ₉ 906, are suitable acrylic acid esters described who · = the ₀ How vdrd also described in Flieser specification, acrylic acid can be _f methacrylic acid, itaconic acid, acrylamide and methacrylamide as Ccmonoinsre with the Asrylatestern ver = · turns are _o Da3 ratio τοη acrylate to acrylic acid or dferen equivalent may range from 38 to 97 to 12 to 3sr in particular from 92 to 96 to 8 to 4 ". If desired, a thinner layer of adhesive can be coated on the patch and then a second layer containing both adhesive and pluorandrenolone can be applied to the top of the first layer so that "I gnaw a higher concentration of pluorandrenolone in derje" If the PfIa-B'if.? 8 is applied to the diseased area of the skin directly on the skin

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42,

_8, the paving O ₉ B 1 and _ε 6 rag Fluorandrenolon per 100 cm hold ent ^ v / ground in an exactly analogous manner by adjusting the Storoidaenge _s eye sets the solutions according to Examples 1 and 2 wirdo

Anti-inflammatory steroids that are used for making τοη Ocelusiv bandages and medicated plasters Suitable for this invention are among various

a. Trade names are made available or can in a known way ₀ A method for preparing certain compositions are disclosed in the US Patents 3,126,375 _s (flurandrenolone); 3,312,590 (β ~ methasone »17« G ester); 3,147,249 and 3,152,154 (general preparation of 17 JL esters); 3,291,815 and 3,264,332 to Flumethaaon; 3,048,158 (general process for the production of aaetonides) and 3,201,391 (process for the production of 11Q-chlorosteroids and general production processes for 21 esters).

P rather known certain derivatives of a basic steroid and can be interchangeable from one steroid to another be applied o

The steroids described above can be included in the adhesive of the plaster introduced or on the adhesive layer dea Patch in the same way as in examples 1 and for fluorandrenolone is described «to be sprayed on

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- '1767 OBB

The amounts of oil of the steroids used in each case

tiirllch corresponds to the 4- actiTit ^ lt oiipQr determniien.

■. '■■■■ BAD 10 98 82 / U39 ^

Claims (1)

Pat entanepr , medisslninsiiea Pf las'5-er f ~ - 'de Application to a skin contact '-seieäneribj. dall a surface of the paving eiiuMi bsi “OruefcanwenduAg adhesive coating with protein Arylic acid polymers and one in one Effective concentration equally divided a steroid 2ο Pflaster nasii Anapruch ^ thereby gefeenr ^ iced "the Sopolymero ciuroh OopaXyfcerißisren wen 88 feis 97 an Aprylatea1; he <= K © nomereii old το« ι 3 tie 12 S ^ Aery3U * acid was produced " 5ο plaster according to claim 1 _9, characterized in that the oopolyraere produced by Gofolyinerisierea τοη 92 to 96 straight AsrylateBter ^ knofflereii old of 4 fcifl δ ο plaster after spray 1 _? 2 or 5, cladureh marked ₉ that the inflammation-free; ai?, Enäe steroid from Flume thaeon, ß = Methaepn ₉ Dexamethason "the fit 17" -Eater ", friamei nolon" 9 $ 6 ₉ 118-dichlor = 6 ° C -fluor- 1 _? 4 "= pregnadi8n-16l & C« '7 flC H ?? ^ triol-3 «20-dione-16 QC -17 OC> -aoetonide, 9 & -11 ß- BAD ORIGINAL 10 ^ 882/1439 Dloh3 © r -u? QL -21 -difluoro-1,4 -pregnadiene-16 ö6 -1? & -die »! = 3o20 -ο1 · -λ-ί6 CC.-17 & -acetonide, '9 it -11ß-Möhlor-6 HL fluor-1 ■ j4 _l 6-pregna.trien- * i6 Ö0 ..- 17 ^ 6 -2i-txiol = 3 _f 20-dione-16D6 = 17fcC -acstonid ,. Oort; ieoii _e Eyarooortiaoaj-. Prednisolone, Medroi or the 21 -Ester of the coigeii steroids beeteht » t? o plaster according to one of the claims 1 to 4? thus germ-proofed .; that öaa steroid is present at a concentration of ₉ illustrates the activity ron 4 bia 16 Mikrogramra PluorandreüPllon per eta of the patch äquiyalent isto ο plaster according to claim 1 «- 2 _S 3 or 5 ₉ characterized _s . that the steroid pluorandrenolone ietc Plaster according to one of the ¹ claims 1 to 6 _? by the fact that the-bei. ! Print application applied adhesive Überaug a * niGhtporb ^v sen $ .flexi ti s support 109882 / U39