NO175885B - Process for the preparation of a salicylic acid-containing agent for the local treatment of skin diseases with peel - Google Patents
Process for the preparation of a salicylic acid-containing agent for the local treatment of skin diseases with peel Download PDFInfo
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- NO175885B NO175885B NO891220A NO891220A NO175885B NO 175885 B NO175885 B NO 175885B NO 891220 A NO891220 A NO 891220A NO 891220 A NO891220 A NO 891220A NO 175885 B NO175885 B NO 175885B
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- salicylic acid
- weight
- aliphatic
- parts
- diol
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- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 title claims abstract description 50
- 239000003795 chemical substances by application Substances 0.000 title claims abstract description 28
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 title claims abstract description 25
- 229960004889 salicylic acid Drugs 0.000 title claims abstract description 25
- 238000000034 method Methods 0.000 title claims description 9
- 208000017520 skin disease Diseases 0.000 title claims description 8
- 239000010685 fatty oil Substances 0.000 claims abstract description 13
- -1 aliphatic 1,2-diol Chemical class 0.000 claims abstract description 12
- 239000003814 drug Substances 0.000 claims abstract description 4
- 239000000203 mixture Substances 0.000 claims description 10
- DNIAPMSPPWPWGF-GSVOUGTGSA-N (R)-(-)-Propylene glycol Chemical compound C[C@@H](O)CO DNIAPMSPPWPWGF-GSVOUGTGSA-N 0.000 claims description 9
- 206010040844 Skin exfoliation Diseases 0.000 claims description 9
- DNIAPMSPPWPWGF-UHFFFAOYSA-N monopropylene glycol Natural products CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 9
- 235000013772 propylene glycol Nutrition 0.000 claims description 9
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims description 8
- 230000035618 desquamation Effects 0.000 claims description 8
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims description 8
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 6
- 229930195729 fatty acid Natural products 0.000 claims description 6
- 239000000194 fatty acid Substances 0.000 claims description 6
- 150000003626 triacylglycerols Chemical class 0.000 claims description 6
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims description 5
- 235000013311 vegetables Nutrition 0.000 claims description 5
- 239000005632 Capric acid (CAS 334-48-5) Substances 0.000 claims description 4
- 239000005635 Caprylic acid (CAS 124-07-2) Substances 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 229960002446 octanoic acid Drugs 0.000 claims description 4
- 239000000243 solution Substances 0.000 claims description 4
- 238000003756 stirring Methods 0.000 claims description 4
- WERYXYBDKMZEQL-UHFFFAOYSA-N butane-1,4-diol Chemical class OCCCCO WERYXYBDKMZEQL-UHFFFAOYSA-N 0.000 claims description 3
- 150000004665 fatty acids Chemical class 0.000 claims description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 3
- 239000012047 saturated solution Substances 0.000 claims description 2
- 238000001665 trituration Methods 0.000 claims description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 150000001298 alcohols Chemical class 0.000 claims 1
- 201000010099 disease Diseases 0.000 description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 8
- 230000000694 effects Effects 0.000 description 5
- 210000003491 skin Anatomy 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 201000004681 Psoriasis Diseases 0.000 description 3
- 230000009286 beneficial effect Effects 0.000 description 3
- 229920006395 saturated elastomer Polymers 0.000 description 3
- 210000004761 scalp Anatomy 0.000 description 3
- 206010020751 Hypersensitivity Diseases 0.000 description 2
- 206010039792 Seborrhoea Diseases 0.000 description 2
- 208000002474 Tinea Diseases 0.000 description 2
- 241000130764 Tinea Species 0.000 description 2
- 238000011835 investigation Methods 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 206010063409 Acarodermatitis Diseases 0.000 description 1
- 208000001840 Dandruff Diseases 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 206010067482 No adverse event Diseases 0.000 description 1
- 241000447727 Scabies Species 0.000 description 1
- 206010039793 Seborrhoeic dermatitis Diseases 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- NUZWLKWWNNJHPT-UHFFFAOYSA-N anthralin Chemical compound C1C2=CC=CC(O)=C2C(=O)C2=C1C=CC=C2O NUZWLKWWNNJHPT-UHFFFAOYSA-N 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 229960002311 dithranol Drugs 0.000 description 1
- 229920001971 elastomer Polymers 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 230000003779 hair growth Effects 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 229940057917 medium chain triglycerides Drugs 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- CQRYARSYNCAZFO-UHFFFAOYSA-N salicyl alcohol Chemical compound OCC1=CC=CC=C1O CQRYARSYNCAZFO-UHFFFAOYSA-N 0.000 description 1
- 208000005687 scabies Diseases 0.000 description 1
- 208000008742 seborrheic dermatitis Diseases 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/60—Salicylic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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Abstract
Description
Teknisk område Technical area
Oppfinnelsen vedrører en fremgangsmåte for fremstilling av et salicylsyreholdig middel for lokal behandling av hudsykdommer med avskalling innen det human- og veterinærmedisinske område. Til disse hudsykdommene med avskalling hører f.eks. psoriasis, tinea amiantacea og seborrhoea sicca. The invention relates to a method for producing a salicylic acid-containing agent for the local treatment of skin diseases with desquamation in the field of human and veterinary medicine. These skin diseases with desquamation include e.g. psoriasis, tinea amiantacea and seborrhoea sicca.
Teknikkens stand State of the art
Det er f.eks. fra E. Mutschler, "Arzneimittelwirkungen", Wissenschaftliche Verlagsgesellschaft, Stuttgart 1975, s. It is e.g. from E. Mutschler, "Arzneimittelwirkungen", Wissenschaftliche Verlagsgesellschaft, Stuttgart 1975, p.
373, kjent at salicylsyre bevirker løsgjøring av flass og oppbløtingen av hornstoff, og anvendes i form av salicyl-vasilin, salicylsprit og salicylkollodium. Som ytterligere midler for behandling av de ovenfor nevnte hudsykdommer, er blant andre salicyl-svinefett, salicylleucerin og salicyl- 373, it is known that salicylic acid causes the loosening of dandruff and the softening of the stratum corneum, and is used in the form of salicylic vaseline, salicylic alcohol and salicylic collodion. As additional agents for the treatment of the above-mentioned skin diseases, among others are salicylic lard, salicylic leucerin and salicylic
gel i bruk. gel in use.
Dessuten er det kjent å anvende oppløsninger av salicylsyre i fete oljer, slik som olivenolje, ricinusolje og andre, for behandling av de ovenfor nevnte hudsykdommer. It is also known to use solutions of salicylic acid in fatty oils, such as olive oil, castor oil and others, for the treatment of the above-mentioned skin diseases.
Beskrivelse av oppfinnelsen Description of the invention
Ved bruk av de kjente salicylsyreholdige midler har When using the known salicylic acid-containing agents have
det vist seg at disse kjente midler ved sin anvendelse for de således behandlede pasienter ikke er, eller bare er lite, akseptable av en rekke grunner, deriblant f.eks. en betyde-lig luktbelastning gjennom harskning av fete oljer under behandlingen, og gir i praksis det ønskede resultat egent-lig bare ved vedvarende behandling. For pasientene som be-handles med midlet er imidlertid dette av spesiell betyd-ning, også av psykologiske grunner. it has been shown that these known agents are not, or only marginally, acceptable when used for the patients treated in this way for a number of reasons, including e.g. a significant odor load through the rancidity of fatty oils during treatment, and in practice gives the desired result only with continuous treatment. For the patients who are treated with the agent, however, this is of particular importance, also for psychological reasons.
Formålet ved oppfinnelsen består i å tilveiebringe et salicylsyreholdig middel av den innledningsvis nevnte art, The purpose of the invention is to provide a salicylic acid-containing agent of the type mentioned at the outset,
som ved god forenlighet er uten uheldige virkninger for pasientene og som muliggjør en ikke-vedvarende behandling. which, with good compatibility, have no adverse effects for the patients and which enable a non-persistent treatment.
Ifølge oppfinnelsen løses denne oppgave ved en fremgangsmåte for fremstilling av et salicylsyreholdig middel for lokal behandling av hudsykdommer med avskalling innen det human- og veterinærmedisinske område, som er kjennetegnet ved at 4-10 vektdeler salicylsyre tritureres med 1-7 vektdeler av en alifatisk 1,2-diol og deretter blandes med 83-95 vektdeler av en fet olje valgt fra gruppen av vegetabilske fete oljer og triglycerider med middels kjedelengde, det vil si C8-C12-fettsyrer, under omrøring til en klar, oljeaktig oppløsning. According to the invention, this task is solved by a method for the production of a salicylic acid-containing agent for the local treatment of skin diseases with desquamation in the field of human and veterinary medicine, which is characterized by 4-10 parts by weight of salicylic acid being triturated with 1-7 parts by weight of an aliphatic 1, 2-diol and then mixed with 83-95 parts by weight of a fatty oil selected from the group of vegetable fatty oils and medium chain triglycerides, i.e. C8-C12 fatty acids, with stirring to a clear, oily solution.
Metningskonsentrasjonen av salicylsyre i fete oljer eller blandinger derav ligger i området fra 3% til maksimalt 5%, noe som er for lavt for mange anvendelsestilfeller. Overraskende ble det nå funnet at høyere metningskonsentra-sjoner kan oppnåes når midlet fremstilt ifølge oppfinnelsen i tillegg inneholder en alifatisk 1,2-diol. Således kan det anvendes forskjellige alifatiske 1,2-dioler, idet 1,2-propandiol og de forskjellige butylenglycoler med hydroxylgrupper i nabostillinger har vist seg å være særlig gunstige. The saturation concentration of salicylic acid in fatty oils or mixtures thereof lies in the range from 3% to a maximum of 5%, which is too low for many applications. Surprisingly, it was now found that higher saturation concentrations can be achieved when the agent produced according to the invention additionally contains an aliphatic 1,2-diol. Thus, various aliphatic 1,2-diols can be used, 1,2-propanediol and the various butylene glycols with hydroxyl groups in adjacent positions having proven to be particularly favorable.
I midlet fremstilt ifølge oppfinnelsen anvendes altså vegetabilske fete oljer eller triglycerider med middels kjedelengde. Særlig pålitelig har således triglyceridene av fettsyrer med middels kjedelengde og blandinger derav vist seg å være, idet triglycerider av caprylsyre, caprinsyre eller blandinger derav, er særlig foretrukket. In the agent produced according to the invention, therefore, vegetable fatty oils or triglycerides with a medium chain length are used. Thus, the triglycerides of fatty acids with medium chain length and mixtures thereof have proven to be particularly reliable, with triglycerides of caprylic acid, capric acid or mixtures thereof being particularly preferred.
Midlet fremstilt ifølge oppfinnelsen er også godt forenlig ved langtidsanvendelse, hittil har det heller ikke ved langtidsanvendelse blitt iakttatt noen allergiske reaksjoner. Derved oppnåes en høy aktivitet, særlig nåes det allerede etter forholdsvis kort anvendelsestid alt etter sykdommens alvorlighet, en fullstendig avskalling, dvs. at det nåes en symptomfrihet, som beholdes ved tilsvarende etterbehand-ling. The agent produced according to the invention is also well compatible with long-term use, so far no allergic reactions have been observed with long-term use either. Thereby, a high activity is achieved, in particular a complete desquamation is achieved already after a relatively short period of use, depending on the severity of the disease, i.e. a freedom from symptoms is achieved, which is maintained by corresponding post-treatment.
Et særlig virkningsfullt, foretrukket middel fremstilt ifølge oppfinnelsen inneholder 4 til 10 g salicylsyre, 1 til 7 g 1,2-propandiol og 83 til 95 g av triglyceridet av caprylsyre, caprinsyre eller blandingen derav. A particularly effective, preferred agent prepared according to the invention contains 4 to 10 g of salicylic acid, 1 to 7 g of 1,2-propanediol and 83 to 95 g of the triglyceride of caprylic acid, capric acid or the mixture thereof.
En viktig årsak til den høye aktivitet av midlet fremstilt An important reason for the high activity of the agent produced
ifølge oppfinnelsen ligger muligens i at de utvalgte opp-løsningsmiddelblandinger virker inn på den syke hud på terapeutisk særlig gunstig måte og derved utgjør en svært virksom bærer som bringer salicylsyren til dens virknings-sted. according to the invention possibly lies in the fact that the selected solvent mixtures act on the diseased skin in a therapeutically particularly beneficial way and thereby constitute a very effective carrier that brings the salicylic acid to its site of action.
Videre er behandlingen med midlene fremstilt ifølge oppfinnelsen ikke forbundet med uønskede og uakseptable belast-ninger for pasientene, samtidig som midlet fremstilt ifølge oppfinnelsen hurtig og fullstendig resorberes i huden. For pasientene fremkommer det derved ikke uutholdelige luktbelast-ninger gjennom harskning av fett eller fete oljer, og den uønskede tilsmussing av klær eller sengklær skjer ikke. En ytterligere ganske vesentlig fordel ved midlet fremstilt ifølge oppfinnelsen består i at det i de fleste tilfeller ikke lenger er nødvendig med et sykehusopphold. Derved oppnåes det en svært høy aksept hos pasientene. Furthermore, the treatment with the agents manufactured according to the invention is not associated with unwanted and unacceptable burdens for the patients, while the agent manufactured according to the invention is quickly and completely resorbed in the skin. For the patients, there are no unbearable odor burdens through the rancidity of fat or fatty oils, and the unwanted soiling of clothes or bedclothes does not occur. A further rather significant advantage of the agent produced according to the invention consists in the fact that in most cases a hospital stay is no longer necessary. Thereby, a very high level of acceptance by the patients is achieved.
Foretrukne utførelsesformer av oppfinnelsen Preferred embodiments of the invention
Foretrukne utførelseseksempler på oppfinnelsen be-lyses nedenunder i forbindelse med fremstillingsbeskrivel-sen. De anvendte stoffer tilfredsstiller renhetsfordringene til D.A.B. Preferred embodiments of the invention are explained below in connection with the manufacturing description. The substances used satisfy the purity requirements of D.A.B.
Salicylsyre ble oppveid i mengder på 4, 5, 7,5 og 10 Salicylic acid was weighed in amounts of 4, 5, 7.5 and 10
g og triturert med en mengde på henholdsvis 1, 2, 4, 5 og g and triturated with an amount of 1, 2, 4, 5 and
7 g 1,2-propandiol på vanlig måte. Deretter ble det til de 5, 7, 12 og 17 g av en 1,2-propandiol-triturering tilsatt henholdsvis 95, 93, 88 og 83 g av en vegetabilsk fet olje henholdsvis triglycerid og blandingen omrørt inntil det opp-sto en klar oljeaktig oppløsning. Dette middel inneholder dermed i vekt% og beregnet ut fra en totalvekt = 100, 7 g of 1,2-propanediol in the usual way. Then 95, 93, 88 and 83 g of a vegetable fatty oil and triglyceride respectively were added to the 5, 7, 12 and 17 g of a 1,2-propanediol trituration and the mixture was stirred until a clear oily resolution. This agent thus contains in % by weight and calculated on the basis of a total weight = 100,
Fortrinnsvis gåes det derved frem slik at det, idet man går ut fra metningskonsentrasjonen til salicylsyre i triglyceridet, direkte tilsettes så mye 1,2-propandiol at en mettet eller nesten mettet oppløsning av den ønskede salicylsyremengde i 1,2-propandiol-triglyceridblandingen fåes. Det har i alle tilfeller vist seg gunstig for behandlingen når det anvendes mettede eller nesten mettede oppløs- Preferably, this is done so that, starting from the saturation concentration of salicylic acid in the triglyceride, so much 1,2-propanediol is directly added that a saturated or almost saturated solution of the desired amount of salicylic acid in the 1,2-propanediol-triglyceride mixture is obtained. In all cases, it has proven beneficial for the treatment when saturated or almost saturated solvents are used.
ninger av salicylsyre. nings of salicylic acid.
Dette middel ble på den nedenunder beskrevne måte an-vendt til behandling av hudsykdommer med avskalling, slik som psoriasis, tinea amiantacea og seborrhoea sicca hos mennesker, og av sommerskurv og andre sykdommer med avskalling, f.eks. hos ponnier. Totalt har det vist seg ved disse og andre sammenlignbare undersøkelser at, med hensyn til forenlighet, aktivitet og behandlingsvarighet inntil symptomfrihet, utviser midlene som inneholder 4 vekt% til 7,5 vekt% salicylsyre, 1 vekt% til 4,5 vekt% av den alifatiske 1,2-diol og 88 vekt% til 93 vekt% av den fete olje, den relativt beste virkning. This agent was used in the manner described below for the treatment of skin diseases with scaling, such as psoriasis, tinea amiantacea and seborrhoea sicca in humans, and of summer scabies and other diseases with scaling, e.g. in ponies. Overall, it has been shown by these and other comparable investigations that, with regard to compatibility, activity and duration of treatment until symptom-free, the agents containing 4% to 7.5% by weight of salicylic acid exhibit 1% to 4.5% by weight of the aliphatic 1,2-diol and 88% by weight to 93% by weight of the fatty oil, the relatively best effect.
Ved ytterligere undersøkelser ble det funnet at i stedet for 1,2-propandiol kan også de forskjellige butylenglycoler med hydroxylgrupper i nabostillinger og even-tuelt også andre alifatiske 1,2-dioler anvendes. Likeså kan det i stedet for de vegetabilske fete oljer eller triglycerider eller blandinger derav, anvendes triglycerider av fettsyrer med middels kjedelengde, dvs. Cg- til C^2~sYrer eller blandinger derav. During further investigations, it was found that instead of 1,2-propanediol, the various butylene glycols with hydroxyl groups in neighboring positions and possibly other aliphatic 1,2-diols can also be used. Likewise, instead of the vegetable fatty oils or triglycerides or mixtures thereof, triglycerides of fatty acids of medium chain length, i.e. Cg- to C^2-acids or mixtures thereof, can be used.
Den terapeutiske anvendelse av et utførelseseksempel som inneholder 5 vekt% salicylsyre, 2 vekt% 1,2-propandiol og 93 vekt% triglycerid av middels kjedelengde (totalvekt av midlet = 100), ble illustrert som vist nedenunder ved hjelp av en pasientgruppe på 150 personer som hovedsakelig led av psoriasis og for en mindre dels vedkommende av andre hud- og hodehudsykdommer med avskalling, f.eks. seborré-eksem. Behandlingen besto i at The therapeutic use of an embodiment containing 5% by weight of salicylic acid, 2% by weight of 1,2-propanediol and 93% by weight of medium chain triglyceride (total weight of the agent = 100) was illustrated as shown below using a patient group of 150 subjects who mainly suffered from psoriasis and to a lesser extent from other skin and scalp diseases with scaling, e.g. seborrhoeic eczema. The treatment consisted of
a) ved sykdommer i hodehuden ble midlet påført to til tre ganger ukentlig på de angrepne steder av hodehuden; behandlingen kan skje under benyttelse av en dusjhette av plast med tilsluttende gummikant og en konvensjonell operasjonshette for fiksering over natten, og b) ved sykdommer på kroppen påføres midlet en til to ganger daglig på de angrepne steder; etter 10 til 15 minutters påvirkningstid fjernes midlet fra huden. a) for diseases of the scalp, the remedy was applied two to three times a week to the affected areas of the scalp; the treatment can take place using a plastic shower cap with a connecting rubber edge and a conventional surgical cap for fixation overnight, and b) in the case of diseases of the body, the agent is applied once or twice a day to the affected areas; after 10 to 15 minutes of exposure, the agent is removed from the skin.
Hos 8 personer i pasientgruppen ble behandlingen av-brudt for tidlig av grunner som ikke hadde å gjøre med den egentlige behandling. Hos 50 personer i pasientgruppen ble det, avhengig av alvorligheten av den opprinnelige sykdom, oppnådd total avskalling og dermed den ønskede symptomfrihet etter en behandlingstid på In 8 people in the patient group, the treatment was stopped prematurely for reasons that had nothing to do with the actual treatment. In 50 people in the patient group, depending on the severity of the original disease, total desquamation and thus the desired freedom from symptoms was achieved after a treatment period of
1 måned ved lettere opprinnelig sykdom, 1 month in case of mild original illness,
inntil 3 måneder ved middels opprinnelig sykdom og up to 3 months in the case of moderate original disease and
inntil 4 måneder ved alvorlig opprinnelig sykdom, idet oppstartingen av avskallingen inntrådte allerede i den første uke av behandlingen. up to 4 months in the case of severe original disease, as the initiation of peeling occurred already in the first week of treatment.
Hos de fleste av de gjenværende 92 pasienter var avskallingen etter inntil 1 års behandlingsvarighet svært langt fremskredet og ga også her forventning om total avskalling og dermed denønskede symptomfrihet. Allergiske reaksjoner ble ikke iakttatt og behandlingen ble utmerket akseptert av pasientene. Til dette bidrar sikkert at midlet er luktnøytralt og trekker hurtig inn i huden, hvorved det ikke skjer noen tilsmussing av klær eller lakener, samt den kjensgjerning at det bare er ved særlige omstendigheter og svært alvorlige sykdommer at et sykehusopphold er nød-vendig . In most of the remaining 92 patients, the desquamation was very far advanced after up to 1 year of treatment, and here too gave the expectation of total desquamation and thus the desired freedom from symptoms. Allergic reactions were not observed and the treatment was excellently accepted by the patients. This is certainly helped by the fact that the agent is odor neutral and absorbs quickly into the skin, whereby no soiling of clothes or sheets occurs, as well as the fact that it is only in special circumstances and very serious illnesses that a hospital stay is necessary.
Som svært fordelaktig bivirkning, ble det fastslått tydelig merkbar forøkt hårvekst, også på det veterinærmedisinske område. As a very beneficial side effect, clearly noticeable increased hair growth was established, also in the veterinary medical field.
Den først oppnådde symptomfrihet kan også opprett-holdes i ettertid. Til dette anbefales en etterfølgende behandling under anvendelse av konvensjonelt middel som redu-serer en fornyet skjelldannelse, slik som dithranol av-vekslende med de før beskrevne midler. The initially achieved freedom from symptoms can also be maintained afterwards. For this, a subsequent treatment is recommended using a conventional agent that reduces a renewed scale formation, such as dithranol alternating with the previously described agents.
Claims (7)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE3724691A DE3724691C2 (en) | 1987-07-25 | 1987-07-25 | Pharmaceutical agent for the local therapy of flaking skin diseases |
| PCT/EP1988/000649 WO1989000853A1 (en) | 1987-07-25 | 1988-07-19 | Agent containing salicylic acid for treating lepidosis |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| NO891220L NO891220L (en) | 1989-03-20 |
| NO891220D0 NO891220D0 (en) | 1989-03-20 |
| NO175885B true NO175885B (en) | 1994-09-19 |
| NO175885C NO175885C (en) | 1994-12-28 |
Family
ID=6332361
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO891220A NO175885C (en) | 1987-07-25 | 1989-03-20 | Process for the preparation of a salicylic acid-containing agent for the local treatment of skin diseases with peel |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP0325628B1 (en) |
| JP (1) | JPH02500106A (en) |
| AT (1) | ATE69550T1 (en) |
| AU (1) | AU2072088A (en) |
| DE (2) | DE3724691C2 (en) |
| DK (1) | DK173547B1 (en) |
| FI (1) | FI94314C (en) |
| NO (1) | NO175885C (en) |
| WO (1) | WO1989000853A1 (en) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GR1001303B (en) * | 1989-01-23 | 1993-07-30 | Wolff Chem Pharm Gmbh | Method for preparation of a means that contains salicyloxyd against scaling sick |
| WO1990008547A1 (en) * | 1989-01-25 | 1990-08-09 | Dr. August Wolff Chemisch-Pharmazeutische Fabrik Gmbh & Co. Kg | Preparation containing salicylic acid for treating desquamative skin diseases |
| GB9223034D0 (en) * | 1992-11-03 | 1992-12-16 | Surtech Int Ltd | Method and composition for prevention and/or treatment of dandruff and seborrhoeic dermatitis |
| SE9403541L (en) * | 1994-10-14 | 1996-04-15 | Sven Moberg | Antimicrobial composition |
| US5736580A (en) * | 1994-11-14 | 1998-04-07 | Alza Croporation | Composition, device, and method for electrotransport agent delivery |
| US5990179A (en) * | 1995-04-28 | 1999-11-23 | Alza Corporation | Composition and method of enhancing electrotransport agent delivery |
| US5985316A (en) * | 1995-04-28 | 1999-11-16 | Alza Corporation | Composition and method of enhancing electrotransport agent delivery |
| US6623724B2 (en) | 1996-09-18 | 2003-09-23 | Applied Genetics Incorporated Dermatics | Dermatological compositions and methods |
| ES2245465T3 (en) * | 1996-09-18 | 2006-01-01 | Applied Genetics Incorporated Dermatics | NORBORNENE AND NORBORNAN COMPOUND DIOLS FOR THE TREATMENT OF PIGMENTATION DISORDERS, NEURODEGENERATIVE DISEASES OR PROLIFERATIVE SKIN DISEASES. |
| DE10205193A1 (en) * | 2002-02-08 | 2003-08-21 | Beiersdorf Ag | Cleaning preparations containing diol |
| DE10341179A1 (en) † | 2003-09-06 | 2005-03-31 | Beiersdorf Ag | Cosmetic or dermatological preparations containing synergistic combination of alpha- or beta-hydroxyacid and alkanediol, useful for combating acne and/or Propionibacterium acnes infection |
| KR102009698B1 (en) | 2011-12-20 | 2019-08-13 | 바이옴 테라퓨틱스 리미티드 | Topical oil compositions for the treatment of fungal infections |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE762726C (en) * | 1942-05-02 | 1952-09-15 | Hydrierwerke A G Deutsche | Solvent or solubilizer for salicylic acid |
| JPS57171912A (en) * | 1981-04-14 | 1982-10-22 | Sumitomo Chem Co Ltd | Cream |
| FR2585575B1 (en) * | 1985-08-01 | 1989-03-03 | Pf Medicament | PHARMACEUTICAL COMPOSITIONS WITH KERATOLYTIC ACTIVITY IN GEL FORM COMPRISING HYDROALCOHOLIC SALICYLIC ACID |
-
1987
- 1987-07-25 DE DE3724691A patent/DE3724691C2/en not_active Expired - Fee Related
-
1988
- 1988-07-19 DE DE8888905833T patent/DE3866344D1/en not_active Expired - Lifetime
- 1988-07-19 WO PCT/EP1988/000649 patent/WO1989000853A1/en active IP Right Grant
- 1988-07-19 EP EP88905833A patent/EP0325628B1/en not_active Expired - Lifetime
- 1988-07-19 JP JP63505873A patent/JPH02500106A/en active Pending
- 1988-07-19 AU AU20720/88A patent/AU2072088A/en not_active Abandoned
- 1988-07-19 AT AT88905833T patent/ATE69550T1/en not_active IP Right Cessation
-
1989
- 1989-03-20 NO NO891220A patent/NO175885C/en not_active IP Right Cessation
- 1989-03-21 DK DK198901375A patent/DK173547B1/en not_active IP Right Cessation
- 1989-03-22 FI FI891357A patent/FI94314C/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| FI891357A (en) | 1989-03-22 |
| FI891357A0 (en) | 1989-03-22 |
| NO175885C (en) | 1994-12-28 |
| FI94314C (en) | 1995-08-25 |
| DE3724691A1 (en) | 1989-02-02 |
| ATE69550T1 (en) | 1991-12-15 |
| NO891220L (en) | 1989-03-20 |
| DE3724691C2 (en) | 1999-03-18 |
| FI94314B (en) | 1995-05-15 |
| DK137589D0 (en) | 1989-03-21 |
| EP0325628B1 (en) | 1991-11-21 |
| EP0325628A1 (en) | 1989-08-02 |
| AU2072088A (en) | 1989-03-01 |
| NO891220D0 (en) | 1989-03-20 |
| DE3866344D1 (en) | 1992-01-02 |
| WO1989000853A1 (en) | 1989-02-09 |
| DK137589A (en) | 1989-05-19 |
| JPH02500106A (en) | 1990-01-18 |
| DK173547B1 (en) | 2001-02-19 |
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