SI21785A - Sestavek estrogena in drugih hormonov z askorbatom, lizinom, s prolinom in z drugimi substancami - Google Patents
Sestavek estrogena in drugih hormonov z askorbatom, lizinom, s prolinom in z drugimi substancami Download PDFInfo
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Abstract
Ta izum se nanasa na sestavke estrogena in sorodnih hormonov v kombinaciji z askorbatom, lizinom, s prolinom in z drugimi substancami, ki vplivajo na vezna tkiva, njihovo zmogljivost in njihovo uporabo v kontracepciji, nadomestnem zdravljenju s hormoni med menopavzo in za drugo rabo v medicini, fiziologiji, farmakologiji, farmacevtski in kozmeticni uporabi.
Description
Sestavek estrogena in drugih hormonov z askorbatom, lizinom, s prolinom in z drugimi substancami
Ta izum se nanaša na sestavke estrogena in sorodnih hormonov v kombinaciji z askorbatom, lizinom, s prolinom in z drugimi substancami, ki vplivajo na vezna tkiva, njihovo zmogljivost in njihovo uporabo v kontracepciji, nadomestnem zdravljenju s hormoni v menopavzi in za drugo rabo v medicini, fiziologiji, farmakologiji, farmacevtski in kozmetični uporabi.
Estrogeni in sorodni hormoni se v medicini široko uporabljajo. Njihova primarna področja uporabe so kontracepcija in nadomestno zdravljenje s hormoni med menopavzo in druga.
Dolgotrajna uporaba estrogena in sorodnih hormonov pa ima občutne in pogoste stranske učinke, vključno raka, zlasti raka dojke, maternice in druge malignosti na organih reproduktivnega sistema, srčna obolenja in druga, ki so povezana z degeneracijo ekstracelularnega matriksa. Po nekaterih virih (Pschyrembel, Klinisches VVorterbuch, 259. izdaja) je zdravljenje z estrogeni kontraindicirano v primerih estrogensko odvisnih tumorjev, akutnih ali kroničnih bolezni jeter, tromboembolije in hipertenzije. V primeru tromboembolitičnih in ishemičnih bolezni je treba nemudoma prekiniti zdravljenje zaradi povišane hipertenzije.
Estrogeni in sorodni hormoni pospešujejo rast raka in eksacerbacijo drugih bolezni z ošibitvijo ekstracelularnega matriksa. Ta učinek estrogena povzroča aktivacija encimov, ki zmanjšujejo vezno tkivo, vključno plazmina, kolagenaz in drugi posredni in neposredni mehanizem, ki destabilizira vezno tkivo.
Iz Evropske patentne prijave 00115643.9, objavljene 17.1.2001 je znano, da so farmacevtski sestavki, ki vsebujejo askorbat, ali sestavke, ki vsebujejo askorbat in inhibitorje fibrinoliz, kot sta lizin in prolin, kombinirana z drugimi substancami, kot so tokoferol, koratin, silen, provitamini in elementi v sledovih primerni farmacevtski sestavki za preprečevanje in zdravljenje bolezni patoloških stanj, povezanih z degradacijo ekstracelularnega matriksa, vključno degenerativnih bolezni, zlasti arterioskleroz, rakov in drugih sorodnih bolezni.
Obstaja očitna potreba po razvoju terapevtskih strategij za zmanjšanje stranskih učinkov zdravljenj z estrogenom pri sicer ugodnih hormonskih terapijah.
Domnevno naj bi dajanje estrogena v kombinaciji z askorbatom, lizinom, s prolinom in z drugimi substancami vsake od teh sestavkov izničilo drugo drugega. Estrogensko zdravljenje privede do degradacije ekstracelularnega matriksa, medtem ko znani sestavki askorbinskih kislin, zlasti v kombinaciji z lizinom in prolinom, zmanjšajo ali inhibirajo take degradacije, pri čemer bi postalo zdravljenje z estrogenom nekoristno. Presenetljivo pa to vsaj delno ni res zaradi sinergističnega učinka takih askorbinskokislinskih sestavkov, zlasti v kombinaciji z lizinom in s prolinom, ki na eni strani preprečuje ali inhibira degeneracijo ekstracelularnega matriksa, po drugi strani pa pospešuje sintezo kolagena, zlasti z askorbinsko kislino, kar ustvarja in podpira ekstracelularni matriks.
Spojine, uporabljene v tem izumu za kombinirano uporabo ali terapevtsko uporabo z estrogeni in sorodnimi hormoni, so izbrane tako, da delujejo proti šibitvi veznega tkiva, ki ga povzročajo ti hormoni. Znano je, da askorbat stimulira sintezo kolagena, elastina in drugih makromolekul veznega tkiva iz fibroblasta in sorodnih celic. Aminokislini lizin in prolin sta predominantni aminokislini, potrebni za sintezo molekul veznega tkiva. Železo in baker sta elementa v sledovih, ki katalizirata produkcijo teh makromolekul.
Med fiziološkimi stanji, kot sta ovulacija in nosečnost, deluje proti degradaciji veznega tkiva, ki ga povzroča estrogen, regulirani sistem naravnih mehanizmov, da preprečijo degradacijo kolagena. V patoloških pogojih, ki jih povzročajo stranski učinki ugodnih hormonskih terapij, je mogoče naravne mehanizme, ki niso več aktivni med menopavzo in po njej, nadomestiti s terapevtsko uporabo kombinacij po tem izumu. Koristne so za zmanjšanje ali preprečevanje stranskih učinkov dolgotrajnih hormonskih terapij vključno raka in drugih težkih zdravstvenih stanj, medtem ko dopuščajo želeni medicinski ali terapevtski učinek estrogena in sorodnih hormonov.
V zvezi z izumom pojem »estrogen« vsebuje poleg estrogena tudi estradiol, etinilestradiol, estriol, noretisteron in linestrenol. Pojem »lizin« vsebuje poleg lizina tudi lizinske soli, hidroksilizin in hidroksilizinske soli. Pojem »askorbat« vsebuje askorbinsko kislino in askorbatne soli.
V prednostnem izvedbenem primeru izuma, farmacevtski sestavek nadalje vsebuje prolin, prolinske soli, hidroksiprolin ali hidroksiprolinske soli.
V drugem prednostnem izvedbenem primeru izuma, farmacevtski sestavek nadalje vsebuje selen ali selenove soli, baker ali bakrove soli, železo ali železove soli in druge minerale ali elemente v sledovih.
V prednostnem izvedbenem primeru pričujočega izuma, farmacevtski sestavek nadalje vsebuje hondrotin sulfat, glikosaminoglikane, proteoglikane ali glikoproteine ekstracelularnega matriksa.
Nadalje se izum nanaša na uporabo estrogena, estradiola, etinilestradiola, estriola, noretisterona ali linestrenola in lizina, lizinskih soli, hidroksilizina ali hidorksilizinskih soli ter askorbinske kisline ali askorbatnih soli za pripravo farmacevtskega sestavka za nadzor plodnosti (kontracepcijo), nadomestno zdravljenje s hormoni, lajšanje simptomov, povezanih z menopavzo, zdravljenje osteoporoze ali kardiovaskularnih bolezni.
V prednostnem izvedbenem primeru navedene uporabe, farmacevtski sestavek nadalje vsebuje prolin, prolinske soli ali hidroksiprolin ali hidroksiprolinske soli.
V drugem prednostnem izvedbenem primeru navedene uporabe, farmacevtski sestavek nadalje vsebuje selen ali selenove soli, baker ali bakrove soli, železo ali železove soli in druge minerale ali elemente v sledovih.
V drugem prednostnem izvedbenem primeru navedene uporabe, farmacevtski sestavek nadalje vsebuje hondrotin sulfat, glikosaminoglikane, proteoglikane ali glikoproteine ekstracelularnega matriksa.
V posebej prednostnem izvedbenem primeru zgoraj navedene uporabe na podlagi tega izuma, se farmacevtski sestavek daje sublingvalno, intravenozno, subkutano, intramuskularno, transdermalno ali parenteralno.
Različne spojine iz te prijave se lahko uporabljajo skupaj v obliki kovalentno vezanih spojih ali kot fizične mešanice ali v katerikoli drugi kombinaciji.
Claims (9)
- Patentni zahtevki1. Farmacevtski sestavek, ki vsebuje estrogen, estradiol, etinilestradiol, estriol, noretisteron ali linestrenol in lizin, lizinske soli, hidroksilizin ali hidroksilizinske soli, ter askorbinsko kislino ali askorbatne soli.
- 2. Farmacevtski sestavek po zahtevku 1, ki nadalje vsebuje prolin ali prolinske soli, hidroksiprolin ali hidroksiprolinske soli.
- 3. Farmacevtski sestavek po zahtevku 1 ali 2, ki nadalje vsebuje selen ali selenove soli, baker ali bakrove soli, železo ali železove soli in druge minerale ali elemente v sledovih.
- 4. Farmacevtski sestavek po kateremkoli zahtevku od 1 do 3, ki nadalje vsebuje hondrotin sulfat, glikosaminoglikane, proteoglikane ali glikoproteine ekstracelularnega matriksa.
- 5. Uporaba estrogena, estradiola, etinilestradiola, estriola, noretisterona ali linestrenola in lizina, lizinskih soli, hidroksilizina ali hidroksilizinskih soli ter askorbinske kisline ali askorbatnih soli za pripravo farmacevtskega sestavka za nadzor plodnosti (kontracepcijo), nadomestno zdravljenje s hormoni, lajšanje tipičnih simptomov, povezanih z menopavzo, zdravljenje osteoporoze ali kardiovaskularnih bolezni.
- 6. Uporaba po zahtevku 5, v katerem omenjeni farmacevtski sestavek nadalje vsebuje prolin, prolinske soli, hidroksiprolin ali hidroksiprolinske soli.
- 7. Uporaba po zahtevku 5 ali 6, v katerem omenjeni farmacevtski sestavek nadalje vsebuje selen ali selenove soli, baker ali bakrove soli, železo ali železove soli in druge minerale ali elemente v sledovih.
- 8. Uporaba po kateremkoli zahtevku od 5 do 7, v katerem omenjeni farmacevtski sestavek nadalje vsebuje hondrotin sulfat, glikosaminoglikane, proteoglikane ali glikoproteine ekstracelularnega matriksa.
- 9. Uporaba po kateremkoli zahtevku od 5 do 8, v katerem se omenjeni farmacevtski sestavki dajejo sublingvalno, intravenozno, subkutano, intramuskularno, transdermalno ali parenteralno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2001/014726 WO2003051371A1 (en) | 2001-12-14 | 2001-12-14 | Composition of estrogen and other hormones with ascorbate, lysine, proline and other substances |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SI21785A true SI21785A (sl) | 2005-12-31 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI200120070A SI21785A (sl) | 2001-12-14 | 2001-12-14 | Sestavek estrogena in drugih hormonov z askorbatom, lizinom, s prolinom in z drugimi substancami |
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| Country | Link |
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| EP (1) | EP1453520B1 (sl) |
| JP (1) | JP2005511768A (sl) |
| KR (1) | KR20040063950A (sl) |
| CN (1) | CN1582152A (sl) |
| AT (1) | ATE338555T1 (sl) |
| AU (1) | AU2002233257B2 (sl) |
| BR (1) | BR0116856A (sl) |
| CA (1) | CA2467964C (sl) |
| CZ (1) | CZ2004809A3 (sl) |
| DE (1) | DE60122943T2 (sl) |
| DK (1) | DK1453520T3 (sl) |
| EE (1) | EE200300310A (sl) |
| ES (1) | ES2272555T3 (sl) |
| HR (1) | HRP20040611B1 (sl) |
| HU (1) | HUP0500896A3 (sl) |
| IL (1) | IL162013A0 (sl) |
| MX (1) | MXPA04005771A (sl) |
| NO (1) | NO20033555L (sl) |
| NZ (1) | NZ532976A (sl) |
| PT (1) | PT1453520E (sl) |
| SI (1) | SI21785A (sl) |
| WO (1) | WO2003051371A1 (sl) |
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| US20040253319A1 (en) * | 2003-06-11 | 2004-12-16 | Shrirang Netke | Pharmaceutical compositions and method for alleviating side-effects of estrogen replacement therapy |
| KR100903984B1 (ko) * | 2005-02-01 | 2009-06-25 | 주식회사 이매진 | Aimp1 폴리펩티드 또는 이의 단편을 유효성분으로 포함하는 피부 노화 방지, 주름 개선, 피부 유연 증진 및 탄력 증진용 화장료 조성물 |
| WO2008139314A1 (en) * | 2007-05-11 | 2008-11-20 | Horphag Research (Luxembourg) Holding Sa | Compositions and methods for treating joint disorders |
| WO2010146078A2 (en) * | 2009-06-16 | 2010-12-23 | Bergen Teknologioverføring As | Novel uses of hydroxyproline compositions |
| EP2857028A4 (en) * | 2012-05-25 | 2016-04-06 | Lion Corp | AGENT CONTAINING ASCORBIC ACID DERIVATIVE AND USE THEREOF |
| JP6125899B2 (ja) * | 2012-05-25 | 2017-05-10 | ライオン株式会社 | 骨粗鬆症予防および／または改善剤 |
| JP6018800B2 (ja) * | 2012-05-25 | 2016-11-02 | ライオン株式会社 | 経口投与組成物 |
| CN113244227B (zh) * | 2020-02-12 | 2022-09-02 | 浙江医药股份有限公司新昌制药厂 | 一种17β-雌二醇与维生素C的分子复合物及其制备方法及应用 |
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| GB888631A (en) * | 1959-02-24 | 1962-01-31 | Upjohn Co | Improvements in or relating to oral therapeutic compositions comprising steroids |
| US4980358A (en) * | 1988-04-04 | 1990-12-25 | George D. McAdory | Method employing gonadal hormones and dopamine agonist intended for combined use in the improvement of lymphocyte function |
| CA2078804C (en) * | 1991-10-01 | 2003-02-25 | Takehiko Suzuki | Manufacture and use of novel glycosides of catechol estrogens |
| EP1068868A3 (en) * | 1997-07-08 | 2001-01-31 | Rath, Matthias, Dr. med. | Synergistic compositions comprising ascorbate and lysine for states related to extracellular matrix degeneration |
| DE29916231U1 (de) * | 1999-09-15 | 2000-02-17 | Renner Jobst | Multivitamin- und -mineralpräparat |
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- 2001-12-14 AU AU2002233257A patent/AU2002233257B2/en not_active Ceased
- 2001-12-14 PT PT01984842T patent/PT1453520E/pt unknown
- 2001-12-14 MX MXPA04005771A patent/MXPA04005771A/es active IP Right Grant
- 2001-12-14 CA CA002467964A patent/CA2467964C/en not_active Expired - Fee Related
- 2001-12-14 CZ CZ2004809A patent/CZ2004809A3/cs unknown
-
2003
- 2003-08-11 NO NO20033555A patent/NO20033555L/no not_active Application Discontinuation
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2004
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Also Published As
| Publication number | Publication date |
|---|---|
| CA2467964C (en) | 2008-06-03 |
| HUP0500896A2 (en) | 2007-02-28 |
| CZ2004809A3 (cs) | 2004-12-15 |
| CN1582152A (zh) | 2005-02-16 |
| EP1453520A1 (en) | 2004-09-08 |
| NZ532976A (en) | 2006-02-24 |
| BR0116856A (pt) | 2004-08-03 |
| KR20040063950A (ko) | 2004-07-14 |
| NO20033555L (no) | 2003-10-02 |
| WO2003051371A1 (en) | 2003-06-26 |
| DE60122943D1 (de) | 2006-10-19 |
| AU2002233257B2 (en) | 2008-08-14 |
| MXPA04005771A (es) | 2004-09-10 |
| IL162013A0 (en) | 2005-11-20 |
| DK1453520T3 (da) | 2007-01-15 |
| DE60122943T2 (de) | 2007-04-26 |
| ES2272555T3 (es) | 2007-05-01 |
| AU2002233257A1 (en) | 2003-06-30 |
| HUP0500896A3 (en) | 2008-04-28 |
| EP1453520B1 (en) | 2006-09-06 |
| JP2005511768A (ja) | 2005-04-28 |
| PT1453520E (pt) | 2006-12-29 |
| ATE338555T1 (de) | 2006-09-15 |
| HRP20040611A2 (en) | 2005-04-30 |
| HRP20040611B1 (en) | 2008-03-31 |
| CA2467964A1 (en) | 2003-06-26 |
| NO20033555D0 (no) | 2003-08-11 |
| EE200300310A (et) | 2003-10-15 |
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Legal Events
| Date | Code | Title | Description |
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| OO00 | Grant of patent |
Effective date: 20051111 |
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| KO00 | Lapse of patent |
Effective date: 20090717 |