SK14852003A3 - Farmaceutický a/alebo kozmetický prostriedok a jeho použitie - Google Patents
Farmaceutický a/alebo kozmetický prostriedok a jeho použitie Download PDFInfo
- Publication number
- SK14852003A3 SK14852003A3 SK1485-2003A SK14852003A SK14852003A3 SK 14852003 A3 SK14852003 A3 SK 14852003A3 SK 14852003 A SK14852003 A SK 14852003A SK 14852003 A3 SK14852003 A3 SK 14852003A3
- Authority
- SK
- Slovakia
- Prior art keywords
- phospholipids
- complex
- pharmaceutical
- cellulite
- escin
- Prior art date
Links
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Classifications
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- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- A61K8/63—Steroids; Derivatives thereof
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Description
Oblasť techniky
Predložený vynález sa týka farmaceutických a/alebo kozmetických prípravkov na liečenie lokalizovaných adipozitív a celulitídy.
Doterajší stav techniky
Lokalizované adipozitíva a celulitída postihujú značné a stále sa zvyšujúce percento západnej populácie, predovšetkým ženy. Navyše celulitída tiež postihuje dospelé ženy s normálnou hmotnosťou a postavou, bez problémov s obezitou. Tieto problémy sú spojené s prejavmi panikulopatie, a to oslabenou periférnou cirkuláciou, edémami, fibrózou a zmeneným metabolizmom lipocytov. Preto ideálne liečenie by malo brať do úvahy všetky tieto faktory.
Obrovské množstvo farmaceutických a kozmetických prípravkov určených na liečenie lokalizovaných adipozitív a celulitídy dostupných v súčasnosti na trhu nevyriešilo doposiaľ uspokojivo problém lokalizovaných adipozitív a celulitídy. Uvedené prípravky majú vo všeobecnosti za základ aktívne zložky rastlinného pôvodu, ako sú napríklad brečtan, pagaštan konský, extrakty koly; kofeín, betaadrenergné povzbudzujúce prostriedky, metylxantíny a podobne. Avšak ani jeden z uvedených prípravkov zatiaľ nemal reálne preukázaný účinok a doposiaľ dosiahnuté výsledky sú často skôr výsledkom zmeny stravovacieho režimu, ktorá je často spojená so spomínanými spôsobmi liečby, ako so samotným používaním uvedených prípravkov.
Podstata vynálezu
Zistilo sa, a je to aj predmetom predloženého vynálezu, že farmaceutické a/alebo kozmetické prípravky na lokálne použitie s obsahom kombinácie aktívnych zložiek rastlinného pôvodu vykazujú výborné výsledky pri liečbe lokalizovaných adipozitív a celulitídy a značne redukujú zásoby kožného tuku a takzvanú
-2„pomarančovú“ kožu vďaka kombinácii rôznych aktivít rôznych zložiek, ktoré sa vyznačujú antiedematickými, antifosfodiesterázovými a vazokinetickými vlastnosťami a podporujú tvorbu kolagénu.
Hoci všetky zložky prípravku podľa predloženého vynálezu sú známe a sú používané vo farmaceutickom priemysle a/alebo kozmetike, je nutné poznamenať, že ak sú uvedené jednotlivé komponenty použité osamote, ich aktivita je omnoho nižšia ako pri použití so zložkami podľa predloženého vynálezu; teda spoločne s uvedenými rôznymi zložkami je možné pozorovať synergický efekt.
Podstatou vynálezu je farmaceutický a/alebo kozmetický prípravok na lokálne použitie s obsahom komplexov escín/betasitosterolu s fosfolipidmi, komplexov dimérových flavonoidov z Gingko biloba s fosfolipidmi, etylximeninátu, komplexov extraktov z Coleus forskolii a triterpénov z Centella asiatica s fosfolipidmi.
Konkrétnejšie sa predložený vynález týka farmaceutických a/alebo kozmetických prípravkov s obsahom kombinácie nasledovných aktívnych zložiek:
a) komplex escín/betasitosterolu s fosfolipidmi,
b) komplex dimérových flavonoidov z Gingko biloba s fosfolipidmi,
c) komplex triterpénov z Centella asiatica s fosfolipidmi,
d) etylximeninát,
e) štandardizovaný extrakt z Coleus forskolii.
Podľa výhodného uskutočnenia predloženého vynálezu sú zložky v prípravku podľa predloženého vynálezu obsiahnuté v nasledovných množstvách:
a) komplex escín/betasitosterolu s fosfolipidmi: 0,1 až 2,5 %,
b) komplex dimérových flavonoidov z Gingko biloba s fosfolipidmi: 0,1 až 2,5 %,
c) komplex triterpénov z Centella asiatica s fosfolipidmi: 0,1 až 2,5 % a voliteľne jedna alebo obidve nasledovné zložky:
d) etylximeninát: 0,1 až 2,5 %,
e) štandardizovaný extrakt z Coleus forskolii: 0,1 až 2,5 %.
Escín je saponín nachádzajúci sa v semenách pagaštanu konského, vyznačujúci sa výraznými antiedematickými vlastnosťami, pravdepodobne vďaka zmene kapilárnej permeability: bolo zistené, že escín má schopnosť redukovať množstvo a veľkosť pórov kapilárnych stien, cez ktoré sa uskutočňuje výmena vody.
-3Preto sa vlastnosti escínu považujú za užitočné pri liečbe lokálnych edematických príhod typických pre celulitídu a lokálne adipozitíva.
Komplex escín/betasitosterolu s fosfolipidmi, opísaný v EP 0 283 713, má rovnaké vlastnosti ako escín, ale vyznačuje sa predĺženým uvoľňovaním aktívnych zložiek a lepšou biodostupnosťou.
Komplex dimérových flavonoidov z Gingko biloba s fosfolipidmi, opísaný v EP 0 275 005, má rovnaké účinky ako dimérové flavóny z Gingko biloba vo voľnej forme, ale vyznačuje sa predĺženým uvoľňovaním aktívnych zložiek a lepšou biodostupnosťou. Dimérové flavonoidy z Gingko biloba sú extrémne silné vazoaktívne činidlá vďaka svojmu inhibičnému účinku na uvoľňovanie histamínu a enzýmu cAMP fosfodiesterázy z oporných buniek. Pri inhibícii tohto enzýmu sa zvyšuje množstvo cAMP, molekuly schopnej aktivovať metabolizmus lipocytov. Tento komplex sa teda vyznačuje lipolytickým účinkom a zlepšuje mikrovaskulárnu perfúziu a kutánny trofizmus.
Triterpény zCentella asiatica (kyselina aziatová, aziatikozid a kyselina madekazová) podporujú tvorbu kolagénu (v stabilnej forme) dermálnymi fibroblastami zvyšovaním absorpcie hydroxyprolínu, ktorý je nevyhnutný pre syntézu kolagénu, čím bojuje proti kutánnej skleróze, zodpovednej za tvorbu „pomarančovej“ kože typickej pre celulitídu. Komplex triterpénov z Centella asiatica s fosfolipidmi, opísaný v EP 0 283 713 sa vyznačuje predĺženým uvoľňovaním a lepším prenikaním do kože.
Etylximeninát je etylester kyseliny ximénovej, mastnej kyseliny nachádzajúcej sa v Olax dissitiflora a iných olejnatých rastlinách rodu Ximenia. Dokonalejšie kapilaroskopické techniky ukázali, že etylximeninát má výrazný vazokinetický účinok. Tento účinok je v kombinácii s účinkom ostatných aktívnych zložiek prípravku prospešný pri liečbe celulitídy.
Štandardizovaný extrakt Coleus forskolii, opísaný v príklade 1, obsahuje forskolín, molekulu schopnú stimulovať adenylát-cyklázovú aktivitu a tak zvyšovať koncentráciu cyklických nukleotidov, molekúl stimulujúcich lipolýzu a krvný tok na mikrovaskulárnej úrovni.
Prípravky podľa predloženého vynálezu sa aplikujú lokálne na oblasti tela postihnuté lokálnymi adipozitívami a/alebo celulitídou, po dobu niekoľkých dní až
-4niekoľkých mesiacov v závislosti od závažnosti ochorenia, ktoré sa má liečiť, s opakovaním 1 až 2 aplikácie denne.
Prípravky podľa vynálezu sa pripravujú bežnými technikami, vo forme krémov, olejov, gélov, pien, emulzií, mliek a podobne, výhodne sú uzatvorené v lipozómoch. Uvedené prípravky obsahujú tiež excipienty bežne používané pri farmaceutických a/alebo kozmetických technológiách.
Ďalej sú uvedené príklady zloženia prípravkov.
Príklady uskutočnenia vynálezu
Príklad 1
Príprava štandardizovaného extraktu z Coleus forskolii s 20% obsahom forskolínu kg na jemno pomletých rizómov a koreňov Coleus forskolii sa podrobí extrakcii s postupným použitím 10 I CO2 pri kontinuálnej recyklácii po dobu 2 hodín, pri teplote 45 °C a tlaku 25 MPa (250 barov). Po odparení rozpúšťadla pri 50 °C sa zvyšok rozpustí v 5 dieloch hexánu a spätne extrahuje dvakrát s 2 dielmi 90 % obj. metanolu.
Extrakt metanolu sa koncentruje až na sušinu tak, že sa získa 45 g extraktu s obsahom 20 % forskolínu.
Príklad 2
Prípravok vo forme krému
100 g obsahuje:
komplex escín/betasitosterolu s fosfolipidmi 1,50 g komplex triterpénov z Centella asiatica s fosfolipidmi 0,50 g komplex dimérových flavonoidov z Gingko biloba s fosfolipidmi 0,50 g štandardizovaný extrakt z Coleus forskolii (20 % forskolínu) 0,50 g etylximeninát 0,50 g
C12-C15 alkylbenzoát (Finsolv TN - Finetex) 7,50 g cyklometikón (Beisil CMO40 - Wacker) 6,00 g
-5etoxydiglykol (Transcutol CG - Gattefossé) 5,00 g glycerylstearát a PEG-100 stearát (Arlacel 165 V-ICI) 3,00 g
Karité maslo (Shea butter) (Dekarité - Jan Dekker) 3,00 g polysorbát 60 (Tween 60 - ICI) 2,00 g cetylalkohol 1,00 g avokádový olej (Avocado oil - Jan Dekker) 1,00 g acetát vitamínu E 0,20 g askorbylpalmitát 0,10 g polyakrylamid (e) C13-14 izoparafín (e)
Laureth-7 (Sepigel 305 - Seppic) 3,00 g imidazolidinylmočovina 0,30 g metylchlórizotiazolinón a metylizotiazolinón (Kathon CG - Rohm & Haas) 0,05 g dvojsodná sol’EDTA 0,10 g
BHT 0,05 g parfumm (162 - AGF) 0,20 g čistená voda doplnená do množstva 100 g
Claims (4)
- PATENTOVÉ NÁROKY1. Farmaceutický a/alebo kozmetický prípravok, vyznačujúci sa t ý m, že obsahuje:a) komplex escín/betasitosterolu s fosfolipidmi,b) komplex dimérových flavonoidov z Gingko biloba s fosfolipidmi,c) komplex triterpénov z Centella asiatica s fosfolipidmi a voliteľne jednu alebo obidve nasledovné zložky:d) etylximeninát,e) extrakt z Coleus forskolii.
- 2. Farmaceutický a/alebo kozmetický prípravok podľa nároku 1,vyznač uj ú c i sa t ý m, že zložky sa v ňom nachádzajú v nasledovných množstvách:a) komplex escín/betasitosterolu s fosfolipidmi: 0,1 až 2,5 %,b) komplex dimérových flavonoidov z Gingko biloba s fosfolipidmi: 0,1 až 2,5 %,c) komplex triterpénov z Centella asiatica s fosfolipidmi: 0,1 až 2,5 % a voliteľne jedna alebo obidve nasledovné zložky:d) etylximeninát: 0,1 až 2,5 %,e) extrakt z Coleus forskolii: 0,1 až 2,5 %.
- 3. Farmaceutický a/alebo kozmetický prípravok podľa nárokov 1 a 2, v y značujúci sa tým, že obsahuje:a) komplex escín/betasitosterolu s fosfolipidmi 1,50 gb) komplex triterpénov z Centella asiatica s fosfolipidmi 0,50 gc) komplex dimérových flavonoidov z Gingko biloba s fosfolipidmi 0,50 gd) štandardizovaný extrakt z Coleus forskolii (20 % forskolínu) 0,50 ge) etylximeninát 0,50 g
- 4. Farmaceutický a/alebo kozmetický prípravok podľa nárokov 1 a 2, vyzná č u j ú c i sa tým, že extrakt z Coleus forskolii je štandardizovaný extrakt s 20 % forskolínu.-75. Farmaceutický a/alebo kozmetický prípravok podľa nárokov 1 až 4 na kozmetické liečenie lokálnych adipozitív a/alebo celulitídy, aplikovaním na liečené oblasti.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT2001MI001182A ITMI20011182A1 (it) | 2001-06-05 | 2001-06-05 | Composizioni farmaceutiche e/o cosmetiche per il trattamento di adiposita' localizzate e della cellulite |
| PCT/EP2002/005390 WO2002098436A1 (en) | 2001-06-05 | 2002-05-16 | Pharmaceutical and/or cosmetic compositions for the treatment of localised adiposities and cellulite |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SK14852003A3 true SK14852003A3 (sk) | 2004-05-04 |
| SK287612B6 SK287612B6 (sk) | 2011-04-05 |
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| SK1485-2003A SK287612B6 (sk) | 2001-06-05 | 2002-05-16 | Farmaceutický a/alebo kozmetický prípravok a jeho použitie |
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| US (1) | US7476392B2 (sk) |
| EP (1) | EP1392335B1 (sk) |
| JP (1) | JP4762492B2 (sk) |
| KR (1) | KR100869868B1 (sk) |
| CN (1) | CN100340247C (sk) |
| AT (1) | ATE360427T1 (sk) |
| AU (1) | AU2002304632B2 (sk) |
| CA (1) | CA2449485C (sk) |
| CY (1) | CY1107672T1 (sk) |
| CZ (1) | CZ300576B6 (sk) |
| DE (1) | DE60219782T2 (sk) |
| DK (1) | DK1392335T3 (sk) |
| ES (1) | ES2284870T3 (sk) |
| HK (1) | HK1063295A1 (sk) |
| HU (1) | HU230348B1 (sk) |
| IT (1) | ITMI20011182A1 (sk) |
| NO (1) | NO331789B1 (sk) |
| PL (1) | PL204550B1 (sk) |
| PT (1) | PT1392335E (sk) |
| RU (1) | RU2291683C2 (sk) |
| SI (1) | SI1392335T1 (sk) |
| SK (1) | SK287612B6 (sk) |
| WO (1) | WO2002098436A1 (sk) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20021280A1 (it) * | 2002-06-11 | 2003-12-11 | Carlo Ghisalberti | Metodo di trattamento anticellulite |
| FR2841470B1 (fr) * | 2002-06-27 | 2006-01-13 | Pharmascience Lab | Utilisation d'isoflavones pour la preparation de compositions topiques utiles pour favoriser l'amincissement et methode de traitement cosmetique associee |
| ITMI20031428A1 (it) * | 2003-07-11 | 2005-01-12 | Indena Spa | Combinazioni di agenti vasoattivi e loro uso per il trattamento di disfunzioni sessuali |
| ITMI20031427A1 (it) * | 2003-07-11 | 2005-01-12 | Indena Spa | Combinazioni di agenti vasoattivi, loro uso in campo farmaceutico e cosmetico e formulazioni che li contengono |
| US20050089555A1 (en) * | 2003-10-24 | 2005-04-28 | Aventis Pharma Deutschland Gmbh | Medicinal targeted local lipolysis |
| DE10349979B4 (de) * | 2003-10-24 | 2006-05-18 | Sanofi-Aventis Deutschland Gmbh | Medikamentöse gezielte lokale Lipolyse |
| US20050143347A1 (en) * | 2003-12-22 | 2005-06-30 | Aventis Pharma Deutschland Gmbh | Medicinal lipolysis of accumulations of fat |
| EP1824463A1 (en) * | 2004-12-14 | 2007-08-29 | Menarini Ricerche S.p.A. | Pharmaceutical compositions for the treatment of cellulite |
| WO2006073190A1 (ja) * | 2005-01-07 | 2006-07-13 | Rohto Pharmaceutical Co., Ltd. | 外用組成物 |
| DE102005061071A1 (de) * | 2005-12-21 | 2007-06-28 | Kneipp-Werke Kneipp-Mittel-Zentrale Gmbh & Co. Kg | Wirkstoffkombination aus Santalbinsäure oder Derivate davon und Traubenkernöl zur topischen oder dermatologischen Verwendung |
| DE102007007610A1 (de) * | 2007-02-13 | 2008-08-14 | Beiersdorf Ag | Verfahren zur Steigerung der Hautelastizität und/oder eine Stärkung der Spannkraft der Haut |
| ITTO20070391A1 (it) * | 2007-06-05 | 2008-12-06 | Medestea Res & Production S P | Composizione di integratore alimentare,farmaco o dispositivo medicale e suo impiego per sopprimere l'appetito, migliorare tono ed umore, con attivita antidepressiva naturale e con effetto antiastenico |
| MX337830B (es) * | 2009-04-17 | 2016-03-16 | Lipotec Sa | Peptidos utiles en el tratamiento y/o cuidado de la piel y/o cabello y su uso en composiciones cosmeticas o farmaceuticas. |
| ES2426314T3 (es) * | 2009-08-12 | 2013-10-22 | Horphag Research Ip (Pyc) Ltd. | Combinación de proantocianidinas tales como picnogenol o semillas de uva y centella asiática para el tratamiento de trastornos cardiovasculares tales como la aterosclerosis |
| DE102009028996A1 (de) * | 2009-08-28 | 2011-03-03 | Rovi Cosmetics International Gmbh | Kosmetische Formulierung zur Reduktion der äußeren Erscheinungsbilder von Cellulite oder Orangenhaut |
| FR2962907B1 (fr) * | 2010-07-21 | 2015-05-08 | Ephyla Sas | Extrait de vegetal pour la fabrication de composition amincissante et procede de controle pour mincir mettant en oeuvre une telle composition |
| BE1022293B1 (nl) | 2012-11-21 | 2016-03-14 | Wendy Angrave | Methode en composities om toxines te verwijderen uit het lichaam |
| CA2905756C (en) | 2013-03-15 | 2016-11-29 | Mary Kay Inc. | Cosmetic compositions for reducing the appearance of cellulite or improving skin texture |
| CN103432045B (zh) * | 2013-09-06 | 2015-06-24 | 雅露拜尔生物科技（杭州）有限公司 | 健美瘦身组合物及健美瘦身霜 |
| WO2022178967A1 (zh) * | 2021-02-24 | 2022-09-01 | 中国药科大学 | 佛司可林-异佛司可林与五环三萜类化合物的药物组合物及其应用 |
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|---|---|---|---|---|
| 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 |
| FR2669537B1 (fr) * | 1990-11-28 | 1993-02-19 | Oreal | Composition amincissante a base d'alpha-2-bloqueurs. |
| FR2684300B1 (fr) * | 1991-11-29 | 1994-03-11 | Lvmh Recherche | Composition cosmetique ou pharmaceutique, notamment dermatologique, destinee en particulier a favoriser la pigmentation de la peau ou des cheveux, contenant un extrait de ballote, et son procede de fabrication. |
| JPH10182473A (ja) * | 1996-12-25 | 1998-07-07 | Lion Corp | 皮下脂肪代謝促進剤及びそれを含む外用組成物 |
| AU776037B2 (en) * | 1999-09-10 | 2004-08-26 | Ceteris Holding B.V.-Amsterdam (Olanda) -Succursale Di Lugano | An anti-oxidant preparation based on plant extracts for the treatment of circulation and adiposity problems |
-
2001
- 2001-06-05 IT IT2001MI001182A patent/ITMI20011182A1/it unknown
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2002
- 2002-05-16 AU AU2002304632A patent/AU2002304632B2/en not_active Ceased
- 2002-05-16 US US10/477,923 patent/US7476392B2/en not_active Expired - Lifetime
- 2002-05-16 JP JP2003501475A patent/JP4762492B2/ja not_active Expired - Fee Related
- 2002-05-16 SI SI200230545T patent/SI1392335T1/sl unknown
- 2002-05-16 EP EP02732718A patent/EP1392335B1/en not_active Expired - Lifetime
- 2002-05-16 CA CA2449485A patent/CA2449485C/en not_active Expired - Fee Related
- 2002-05-16 CN CNB028112911A patent/CN100340247C/zh not_active Expired - Fee Related
- 2002-05-16 RU RU2003135427/15A patent/RU2291683C2/ru not_active IP Right Cessation
- 2002-05-16 AT AT02732718T patent/ATE360427T1/de active
- 2002-05-16 HU HU0400119A patent/HU230348B1/hu not_active IP Right Cessation
- 2002-05-16 DK DK02732718T patent/DK1392335T3/da active
- 2002-05-16 CZ CZ20033293A patent/CZ300576B6/cs not_active IP Right Cessation
- 2002-05-16 PL PL366914A patent/PL204550B1/pl unknown
- 2002-05-16 PT PT02732718T patent/PT1392335E/pt unknown
- 2002-05-16 WO PCT/EP2002/005390 patent/WO2002098436A1/en active IP Right Grant
- 2002-05-16 KR KR1020037015485A patent/KR100869868B1/ko not_active IP Right Cessation
- 2002-05-16 ES ES02732718T patent/ES2284870T3/es not_active Expired - Lifetime
- 2002-05-16 SK SK1485-2003A patent/SK287612B6/sk not_active IP Right Cessation
- 2002-05-16 DE DE60219782T patent/DE60219782T2/de not_active Expired - Lifetime
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2003
- 2003-12-04 NO NO20035389A patent/NO331789B1/no not_active IP Right Cessation
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2004
- 2004-08-13 HK HK04106092A patent/HK1063295A1/xx not_active IP Right Cessation
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2007
- 2007-06-14 CY CY20071100788T patent/CY1107672T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Patent lapsed due to non-payment of maintenance fees |
Effective date: 20170516 |