SK282435B6 - Farmaceutický a kozmetický prostriedok proti akné obsahujúci antimikrobiálnu zmes a jej použitie - Google Patents
Farmaceutický a kozmetický prostriedok proti akné obsahujúci antimikrobiálnu zmes a jej použitie Download PDFInfo
- Publication number
- SK282435B6 SK282435B6 SK496-99A SK49699A SK282435B6 SK 282435 B6 SK282435 B6 SK 282435B6 SK 49699 A SK49699 A SK 49699A SK 282435 B6 SK282435 B6 SK 282435B6
- Authority
- SK
- Slovakia
- Prior art keywords
- extract
- acid
- krameria
- xymenic
- pharmaceutical
- Prior art date
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- 230000000845 anti-microbial effect Effects 0.000 title claims abstract description 9
- 239000004599 antimicrobial Substances 0.000 title claims abstract description 9
- 239000002537 cosmetic Substances 0.000 title claims abstract description 6
- 238000002360 preparation method Methods 0.000 title claims description 11
- 206010000496 acne Diseases 0.000 title description 7
- 208000002874 Acne Vulgaris Diseases 0.000 title description 5
- 239000000284 extract Substances 0.000 claims abstract description 32
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 claims abstract description 22
- 244000097724 Mesua ferrea Species 0.000 claims abstract description 14
- 235000010931 Mesua ferrea Nutrition 0.000 claims abstract description 14
- VENIIVIRETXKSV-BQYQJAHWSA-N Ximenynic acid Chemical compound CCCCCC\C=C\C#CCCCCCCCC(O)=O VENIIVIRETXKSV-BQYQJAHWSA-N 0.000 claims abstract description 14
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- KNFUWJAIDVAYOV-ONEGZZNKSA-N rataniaphenol II Chemical compound CC=1C2=CC(/C=C/C)=CC=C2OC=1C1=CC=C(O)C=C1 KNFUWJAIDVAYOV-ONEGZZNKSA-N 0.000 claims abstract description 6
- KNFUWJAIDVAYOV-UHFFFAOYSA-N rataniaphenol II Natural products CC=1C2=CC(C=CC)=CC=C2OC=1C1=CC=C(O)C=C1 KNFUWJAIDVAYOV-UHFFFAOYSA-N 0.000 claims abstract description 6
- JXADTNBUTVACPY-UHFFFAOYSA-N 4-(5-propyl-1-benzofuran-2-yl)benzene-1,3-diol Chemical compound OC1=C(C=CC(=C1)O)C=1OC2=C(C1)C=C(C=C2)CCC JXADTNBUTVACPY-UHFFFAOYSA-N 0.000 claims abstract description 5
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- -1 2- (2,4-dihydroxyphenyl) -5-propylbenzofuranate Chemical compound 0.000 claims description 5
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- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
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Classifications
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- A61K36/18—Magnoliophyta (angiosperms)
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
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Abstract
Farmaceutický a kozmetický prostriedok s účinkom proti akné, obsahujúci hydrofilný extrakt z Kramerie sp., výhodne z Kramerie triandra alebo čistú zložku z uvedeného extraktu vybranú zo skupiny pozostávajúcej z eupomatenoidu 6 a 2-(2,4-dihydroxyfenyl)-5-propylbenzofurán a/alebo antimikrobiálny lipofilný extrakt z Mesua ferrea, kyselinu xymenínovú a/alebo kyselinu laurovú a protizápalové saponíny získané z Olax dissitiflora, Aesculus hippocastanum, Centella asiatica, Terminalia sericea, Glycyrrhiza glabra.ŕ
Description
Oblasť techniky
Tento vynález sa týka nových farmaceutických a kozmetických prostriedkov s účinnosťou proti akné, ktoré obsahujú antimikrobiálny hydrofílný extrakt z Kramerie sp. alebo čistú zložku z uvedeného extraktu a/alebo antibakteriálny lipofilný extrakt z Mesua ferrea; kyselinu xymenínovú a/alebo kyselinu laurovú, protizápalové saponíny získané z Olax dissitiflora, Aesculus hippocastanum, Centella asiatica, Terminalia sericea, Glycyrrhiza glabra.
Doterajší stav techniky
Z literatúry (Martindaie, „The extrafarmacopeía“, 28 th Ed. (1982); Cannizaro, Boli. Soc. Ital. Biol. Sperim. 1,22, 1964; V. Hoppe, Drogenkunde dl Walter De Gruyter Ed., 1975; a britský patent 2.184.353 A) je známe, že extrakty získané extrakciou, pomocou chlórovaných rozpúšťadiel, alifatických éterov a ketónov, ako aj alifatických a aromatických éterov, z koreňov, kôry kmeňov stromov a listov rôznych druhov Kramerie, výhodne Kramerie triandra obohatenej o neolignany (hlavne eupomatenoid 6 a 2-(2,4-dihydroxyfenyl)-5-propylbenzofúrán) majú antimikróbny účinok proti grampozitívnym (+), gramnegatívnym (-) baktériám, hubám a anaeróbnym kmeňom.
Tieto extrakty, aj keď získané extrakciou dokonca aj s protickými rozpúšťadlami sú prirodzene hydrofilné vďaka fenolovému charakteru ich aktívnych zložiek.
Čisté zložky eupomatenoid 6 a 2-(2,4-dihydroxyfenyl)-5-propylbenzofurán je možné získať z týchto extraktov použitím chromatografických techník na silikagéli, ako sú opísané v EP 0 464 297 Bl.
Extrakciou kvetov, hlavne púčikov Mesua ferrea použitím aprotických rozpúšťadiel, ako je hexán, metylénchlorid alebo použitím oxidu uhličitého v hyperkritických podmienkach, napríklad extrakciou rastlinných materiálov pod tlakom v rozpätí od 11 MPa do 26 MPa a pri teplote v rozpätí od 35 do 65 °C, výhodne pri 45 °C je možné získať lipofilný extrakt obsahujúci substituované kumaríny a xantóny, ktoré majú najmä účinok na gram +, gram - a anaeróbne bakteriálne kmene, s účinkom porovnateľným s účinkom extraktu pripraveného z Krameria triandra.
Podstata vynálezu
Prekvapivo bolo zistené, že kombinácia extraktov, z niektorých rastlín, ktoré majú prirodzenú antimikrobiálnu aktivitu, najmä extrakty alebo čisté zlúčeniny rôznych druhov Kramérií, výhodne Kramerie triandra a z Mesua ferrea s látkami, ako je kyselina xymeninová, a so saponínmi, ako sú tie získané z Olax dissitiflora, Aesculus hippocastanum, Centella asiatica, Terminalia sericea, Glycyrrhiza glabra s prídavkom alebo bez prídavku nízkomolekulových mastných kyselín, ako sú kyselina laurová, kyselina myristová, kyselina izomyristová a podobne, je vysoko aktívna pri liečbe akné.
Kombinácia tejto zmesi antimikrobiálnych činidiel s kyselinou xymenínovou a s prírodnými zlúčeninami s protizápalovým účinkom vyvolá skoro úplné zmiznutie prejavov akné a pôsobí ako účinná prevencia tvorby a rozvoja akné. Dobré účinky dosiahla najmä kombinácia antimikrobiálnych činidiel s kyselinou xymeninovou, kyselinou laurovou (jeden z hlavných komponentov lipofilického extraktu z Serenoa repens) a saponinom získaným z tých, ktoré sú extrahovateľné z Olax dissitiflora, Aesculus hippocasta num, Centella asiatica, Terminalia sericea, Glycyrrhiza glabra výhodne z Aesculum hippocastanum a Centella asiatica.
Podstatou vynálezu je farmaceutický a kozmetický prostriedok s účinkom proti akné, ktoiý obsahuje:
a) hydrofílný extrakt z Kramerie sp., výhodne z Kramerie triandra alebo čistú zložku z uvedeného extraktu vybranú zo skupiny pozostávajúcej z eupomatenoidu 6 a 2-(2,4-dihydroxyfenyl)-5-propylbenzofiirán a/alebo antimikrobiálny lipofilný extrakt z Mesua ferrea,
b) kyselinu xymenínovú a/alebo kyselinu laurovú a
c) protizápalové saponiny získané z Olax dissitiflora, Aesculus hippocastanum, Centella asiatica, Terminalia sericea, Glycyrrhiza glabra..
Medzi rôznymi testovanými kombináciami, najlepšie klinické výsledky dosiahli tie, ktoré obsahovali od 0,1 do 0,5 % extraktu z Kramerie triandra, výhodne 0,2 %, 0,1 do 0,5 % extraktu Mesua ferrea, výhodne 0,25 %, 0,2 do 1 % kyseliny xymenínovej, výhodne 0,2 % a od 0,35 do 1 % escínu, výhodne 0,5 %.
Účinnosť proti akné bola testovaná na 30 pacientoch oboch pohlaví, vo veku od 18 do 35 rokov. Pacienti boli liečení s 0,5 cm prostriedku dvakrát denne počas 45 po sebe nasledujúcich dní.
Neošetrovaná časť tváre bola použitá na kontrolu. Na konci liečby bol vyhodnotený počet pupencov, pľuzgierov a komedónov (A), koncentrácia mazu (B) a prítomnosť Propionibacterium acnes vo výlučku z pľuzgierov a komedónov (C).
Zistené výsledky sú uvedené v nasledujúcej tabuľke.
| Liečba | % zníženia | ||
| A | B | C | |
| Žiadna | 5 | 2,3 | 0 |
| Prípravok 1 (Pr. 4) | 70 | 13,1 | 80 |
| Prípravok 2 (Pr. 5) | 50 | 12,1 | 70 |
| Prípravok 3 * | 20 | 4 | 20 |
* formulácia obsahuje kyselinu xymenínovú a escín sitosterol(EP 283713).
Vynález sa preto týka farmaceutických a kozmetických prostriedkov s účinkom proti akné, ktoré sa môžu podávať lokálne (gély, krémy, lotiony, mlieka a tuhé preparáty). Uvedené prostriedky sú pripravované podľa bežných metód známych vo farmaceutických technikách, ako sú opísané v „Remington's Pharmaceutical Handbook“, Mack Publishing Co., N. Y., USA, spolu s vhodnými excipientmi, najmä antioxidantmi.
Nasledujúce príklady ilustrujú vynález v ďalších detailoch.
Príklady uskutočnenia vynálezu
Príklad 1
Príprava lipofilného extraktu z Mesua ferrea kg jemne namletých púčikov Mesua ferrea bol extrahovaný pomocou CO2 za hyperkritických podmienok v extraktore s objemom 5 litrov. Prvá extrakcia bola uskutočnená pri teplote 34 °C a tlaku 9 MPa, použitím 25 1 oxidu uhličitého. Výsledný extrakt bol odložený a na druhú extrakciu sa pripravil rastlinný materiál. Táto sa uskutočňovala pri zvýšenej teplote na 45 °C a tlaku na 22 MPa. Získalo sa 15,6 g veľmi hustého oleja oranžovej farby. Tento olej je možné použiť priamo samotný alebo je podrobený ďalším frakcionáciám prostriedkami bežných chemických separácií. Extrakt sa prednostne použije bez ďalších úprav.
Príklad 2
Príprava extraktu z Kramerie triandra kg kôry koreňa Kramerie triandra sú po rozomletí 3-krát extrahované použitím vždy 5 litrov acetónu, spojené extrakty boli zahustené na malý objem a koncentrát sa pridal do 0,8 1 acetónu a vody v pomere 1:1. Výsledná suspenzia je dvakrát extrahovaná použitím 0,5 1 metylénchloridu, chlórmetylénová fáza sa vysušila bezvodým síranom sodným, potom sa zahustila na sucho. Získalo sa 85 g červenkastej tuhej látky, ktorá obsahuje približne 26 % eupomatenoidu 6 a 14 % 2-(2,4-dihydroxyfenyl)-5-propylbenzofúránu.
Príklad 3
Príprava extraktu z Mesua ferrea použitím hexánu kg jemne mletých púčikov Mesua ferrea sa extrahovalo 4-krát pomocou 3 1 hexánu pod refluxom. Spojené hexánové extrakty boli dekolorizované pomocou aktívneho dreveného uhlia (5 g) a vo vákuu sa zahustili na olej. Získalo sa 14,5 g extraktu, ktorý je možné použiť bez ďalšej frakcionácie.
Príklad 4
Príprava emulzie voda-silikón
Mesua ferrea 0,25 g
Krameria triandra0,2 g
Kyselina xymenínová 0,60 g
Kyselina laurová 0,20 g
Kyselina 18- glycynhetic 0,50 g
Propylén glykol 5,0g
Coccoylglutamát sodný 25 % roztok 2,0g
Minerálny olej alkoholy lanolínu 2,5g
Octyl octanoat 5,0g
Octododecyl myristate 7,5g
Cetyl dímetycone copolyol 2,5g
Tetramer cyclometycone 5,0g
Chlorid sodný 2,0g
Glycerín 2,5g
Imidurea 0,3g
Metylparaben 0,1g
Čistená voda q. s. do 100,0g
Príklad 5
Príprava emulzie olej/voda
Krameria triandria 0,20g
Escin B- Sitosterol fítosoma ® 0,50g
Kyselina ximeninová 0,50g
Kyselina laurová 0,20g
Glyceryl monosterarát 3,00g
Alkyl Ci2- benzoát 7,00g
Silikónový olej 0,50g
Carbomer 0,50g
Akrylát/C10.}() alkylakrylát sieť, polymér 0,20 g Laurylsulfát sodný 1,00 g
Propylén glykol 5,00g
Hydroxid sodný 10 % roztok 1,50 g
Imidurea 0,30g
Metylparaben 0,10g
Čistená voda q. s. do 100,00g stearoyl laktylát sodný (Nikkhomulese 41 -Nikkho)
Behenyl alkohol 1,5g
Squalane 7,00g
Trioktanoine 6,00g
PPG-12/SMDI 2,00g
Butenyl glykol 5,00g
Xantanová guma 0,30g
Konzervačné látky q. s.
Destilovaná voda q. s. do 100,00 g
Claims (4)
- PATENTOVÉ NÁROKY1. Farmaceutický a kozmetický prostriedok s účinkom proti akné, vyznačujúci sa tým, že obsahuje:a) hydroftlný extrakt z Kramerie sp., výhodne z Kramerie triandra alebo čistú zložku z uvedeného extraktu vybranú zo skupiny pozostávajúcej z eupomatcnoidu 6 a 2-(2,4-dihydroxyfenyl)-5-propylbenzofurán a/alebo antimikrobiálny lipoftlný extrakt z Mesua ferrea,b) kyselinu xymenínovú a/alebo kyselinu laurovú ac) protizápalové saponíny získané z Olax dissitiflora, Aesculus hippocastanum, Centella asiatica, Terminalia sericea, Glycyrrhiza glabra.
- 2. Prostriedok podľa nároku 1, vyznačujúci sa tým, že obsahuje: 0,1 do 0,5 % extraktu z Kramerie triandra, 0,1 do 0,5 % extraktu z Mesua ferrea, 0,2 do 1 % kyseliny xymenínovej, 0,1 do 0,4 % kyseliny laurovej, 0,35 do 1 % escínu.
- 3. Prostriedok podľa nároku 2, vyznačujúci sa tým, že obsahuje: 0,2 % extraktu z Kramerie triandra, 0,25 % extraktu z Mesua ferrea, 0,6 % kyseliny xymenínovej, 0,2 % kyseliny laurovej, 0,5 % escínu.
- 4. Použitie a) antimikrobiálneho hydrofilného extraktu z Kramerie sp., výhodne z Kramerie triandra alebo čistej zložky z uvedeného extraktu, vybranú zo skupiny pozostávajúcej z eupomatenoidu 6 a 2-(2,4-dihydroxyfenyl)-5propylbenzofiiránu a/alebo antimikrobiálneho lipofilného extraktu z Mesua ferrea, b) kyseliny xymenínovej a/alebo kyseliny laurovej a c) protizápalových saponínov získaných z Olax dissitiflora, Aesculus hippocastanum, Centella asiatica, Terminalia sericea, Glycyrrhiza glabra na prípravu liečiva s účinkom proti akné.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT96MI002149A IT1284971B1 (it) | 1996-10-17 | 1996-10-17 | Formulazioni farmaceutiche e cosmetiche ad attivita' antiacne |
| PCT/EP1997/005510 WO1998017293A1 (en) | 1996-10-17 | 1997-10-07 | Pharmaceutical and cosmetic antiacne formulations containing plant extracts (krameria triandra or mesua ferrea) |
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| Publication Number | Publication Date |
|---|---|
| SK49699A3 SK49699A3 (en) | 2000-03-13 |
| SK282435B6 true SK282435B6 (sk) | 2002-02-05 |
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| SK496-99A SK282435B6 (sk) | 1996-10-17 | 1997-10-07 | Farmaceutický a kozmetický prostriedok proti akné obsahujúci antimikrobiálnu zmes a jej použitie |
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| EP (1) | EP0930888B1 (sk) |
| JP (1) | JP3725557B2 (sk) |
| KR (1) | KR100325317B1 (sk) |
| CN (1) | CN1136859C (sk) |
| AT (1) | ATE218357T1 (sk) |
| AU (1) | AU717760B2 (sk) |
| CA (1) | CA2268908C (sk) |
| CZ (1) | CZ289844B6 (sk) |
| DE (1) | DE69713116T2 (sk) |
| DK (1) | DK0930888T3 (sk) |
| ES (1) | ES2177953T3 (sk) |
| HK (1) | HK1022277A1 (sk) |
| HU (1) | HU228300B1 (sk) |
| IT (1) | IT1284971B1 (sk) |
| NO (1) | NO320407B1 (sk) |
| PL (1) | PL189441B1 (sk) |
| PT (1) | PT930888E (sk) |
| RU (1) | RU2194524C2 (sk) |
| SI (1) | SI0930888T1 (sk) |
| SK (1) | SK282435B6 (sk) |
| WO (1) | WO1998017293A1 (sk) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU6315300A (en) * | 1999-07-26 | 2001-02-13 | Shionogi & Co., Ltd. | Benzene derivatives and immunopotentiating compositions or drug-sensitivity restoring agents containing the same |
| KR20010097631A (ko) * | 2000-04-25 | 2001-11-08 | 김국남 | 스킨로션 조성물 |
| FR2813194A1 (fr) * | 2000-08-22 | 2002-03-01 | Oreal | Utilisation d'une sapogenine pour traiter les desordres lies a une suractivite de la 5a-reductase |
| JP4611565B2 (ja) * | 2001-03-30 | 2011-01-12 | 株式会社ナリス化粧品 | 脂肪合成促進剤および化粧料 |
| DE10121090A1 (de) * | 2001-04-26 | 2002-10-31 | Beiersdorf Ag | Wirkstoffkombinationen aus Tetrahydrocurcuminoiden und Sericosid und/oder Pflanzenextrakten |
| DE10121092A1 (de) * | 2001-04-26 | 2002-10-31 | Beiersdorf Ag | Kosmetische oder dermatologische Formulierungen mit einem Gehalt an Sericosid und/oder Pflanzenextrakten, dasselbe enthaltend |
| DE10232774B4 (de) * | 2002-07-18 | 2004-07-15 | Cognis Deutschland Gmbh & Co. Kg | Kosmetische Zubereitungen mit antibakteriellen Eigenschaften |
| EP1402787A1 (en) | 2002-09-27 | 2004-03-31 | Loders Croklaan B.V. | Ximenynic acid |
| JP4589663B2 (ja) * | 2004-06-16 | 2010-12-01 | 株式会社マンダム | 抗男性ホルモン剤原料 |
| JP5665276B2 (ja) * | 2008-02-27 | 2015-02-04 | 花王株式会社 | 皮膚老化予防又は改善剤 |
| US8496975B2 (en) * | 2008-04-24 | 2013-07-30 | Indena S.P.A. | Compositions for the treatment and prevention of infections of the oral cavity |
| DE102008052520A1 (de) * | 2008-10-21 | 2010-04-22 | Cognis Ip Management Gmbh | Kosmetische und/oder pharmazeutische Zubereitungen |
| WO2011147768A1 (en) * | 2010-05-24 | 2011-12-01 | Indena S.P.A. | Tamarind seed polysaccharide for use in the treatment of inflammatory diseases |
| KR20140132005A (ko) * | 2012-03-12 | 2014-11-14 | 피라말 엔터프라이지즈 리미티드 | 여드름 치료 방법 및 항-여드름 제형 |
| CN102949461B (zh) * | 2012-10-25 | 2014-06-11 | 北京华夏众芳生物科技有限公司 | 治疗结节型痤疮的外用中药组合物、制剂及其制备方法 |
| JP6815006B2 (ja) * | 2016-11-01 | 2021-01-20 | 株式会社桃谷順天館 | アクネ菌株選択的抗菌剤 |
| CN108272740B (zh) * | 2018-03-28 | 2019-03-12 | 湖南御家化妆品制造有限公司 | 组合物及含有该组合物的痤疮修复化妆品 |
| CN109010390A (zh) * | 2018-08-20 | 2018-12-18 | 林爵文 | 一种提高男性性功能和治疗性功能障碍的保健品 |
| KR102253095B1 (ko) | 2020-11-06 | 2021-05-17 | 주식회사 허브테라피 | 여드름 피부 개선 화장료, 이의 제조방법 및 이를 포함하는 여드름 피부 개선 기능성 화장품 |
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| JPS62126128A (ja) * | 1985-11-27 | 1987-06-08 | Sato Seiyaku Kk | 抗菌剤 |
| IT1203515B (it) * | 1987-02-26 | 1989-02-15 | Indena Spa | Complessi di saponine con fosfolipidi e composizioni farmaceutiche e cosmetiche che li contengono |
| IT1223290B (it) * | 1987-07-27 | 1990-09-19 | Indena Spa | Acidi poliinsaturi ad azione vasocinetica e relative formulazioni farmaceutiche e cosmetiche |
| EP0464297B1 (en) * | 1990-07-05 | 1995-05-17 | INDENA S.p.A. | Complexes of neolignane derivatives with phospholipids, the use thereof and pharmaceutical and cosmetic formulations containing them |
| GB2304050B (en) * | 1992-11-26 | 1997-06-25 | Eladevi Shah | Herbal Compositions |
| JPH0812565A (ja) * | 1994-06-29 | 1996-01-16 | Shiseido Co Ltd | 皮膚外用剤 |
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1996
- 1996-10-17 IT IT96MI002149A patent/IT1284971B1/it active IP Right Grant
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| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Patent lapsed due to non-payment of maintenance fees |
Effective date: 20131007 |