Ezetimibe

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Ezetimibe Hyperlipidemia Guriga Gudihiisa / USP 24511  

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Gundhig

Ezetimibe waa karti iyo sheeko-joojiye nuugista nuugista kolestaroolka [1].

Kolestaroolku waa maaddo xayr ah oo loo yaqaan 'lipid molecule' waxaana looga baahan yahay inay dhisto oo ilaaliso xuub-dhismeedka qaab-dhismeedka iyo dheecaanka. Sidoo kale, waxay u adeegtaa sidii horudhac ah fiitamiin D, asiidhyada xiidmaha iyo hormoonnada steroid.

Noocyada kala duwan ee Caco-2 ee lagu shubo carotenoid (1 μM), ezetimibe (10 mg / L) waxay joojisay gaadiidka carotenoid oo leh 50% ka hortag for-carotene iyo β-carotene. Sidoo kale, waxay joojisay gaadiidka β-cryptoxanthin, lycopene iyo lutein: zeaxanthin (1: 1). Isla mar ahaantaana, ezetimibe wuxuu xanibay gaadiidka kolestaroolka 31%. Ezetimibe wuxuu hoos u dhigay muujinta duubayaasha dusha sare SR-BI, ATP xarkaha cajaladda, subfamily A (ABCA1), nooca Niemann-Pick C1 Like 1 protein (NPC1L1) iyo retinoid acid receptor (RAR) γ, walxaha xakamaynta xakamaynta sterol SREBP -1 iyo SREBP-2, iyo beerka X receptor (LXR) β [3].

Jiirka apolipoprotein E knockout (apoE - / -) jiirka, ezetimibe (3 mg / kg) wuxuu joojiyay nuugista kolestaroolka 90%. Ezetimibe wuxuu yareeyay kolestaroolka plasma, wuxuu kordhiyay heerarka HDL, wuxuuna joojiyaa horumarka atherosclerosis [1]. Marxaladda III ee tijaabooyinka aadanaha, Ezetimibe (10 mg) waxay si weyn hoos ugu dhigtay heerarka kalastaroolka LDL, wadarta kolestaroolka iyo triglycerides waxayna kordhisay heerka kolestaroolka HDL [2].

Tixraacyo:
[1]. Davis HR Jr, Compton DS, Hoos L, et al. Ezetimibe, oo ah ka hortagid xoog badan oo kolestarool ah, ayaa horjoogsata horumarinta atherosclerosis ee jiirka ApoE knockout. Arterioscler Thromb Vasc Biol, 2001, 21 (12): 2032-2038.
[2] Caddaynta JW. Soo helitaanka ezetimibe: waa aragti ka timid dib-u-hayaha. J Med Chem, 2004, 47 (1): 1-9.
[3]. Intii lagu gudajiray A, Dawson HD, Harrison EH. Gaadiidka Carotenoid wuu yaraaday muujinta gaadiidleyda xaydha ah ee SR-BI, NPC1L1, iyo ABCA1 ayaa hoos loogu dhigey unugyada Caco-2 ee lagu daweeyey ezetimibe. J Nutr, 2005, 135 (10): 2305-2312.

Sharaxaad

Ezetimibe (SCH 58235) waa ka hortag xoog u nuugista kolestaroolka. Ezetimibe waa ka hortage Niemann-Pick C1-like1 (NPC1L1), waana firfircoon firfircoone Nrf2.

In Vitro

Ezetimibe (Eze) wuxuu u dhaqmaa sidii firfircoon firfircoone Nrf2 isagoon keenin cytotoxicity. Ezetimibe wuxuu xoojiyaa transactivation-ka Nrf2, sida uu shaaca ka qaaday baaritaanka wariye luciferase ah. Ezetimibe wuxuu sidoo kale kor u qaadayaa hiddo-wadaha bartilmaameedka ah ee Nrf2, oo ay ku jiraan GSTA1, heme oxygenase-1 (HO-1) iyo Nqo-1 ee Hepa1c1c7 iyo unugyada MEF. Ezetimibe wuxuu kor u qaadayaa hiddo-wadeyaasha Nrf2 ee unugyada Nrf2 + / + MEF, halka soo-saaristani gebi ahaanba laga xanibay unugyada Nrf2 - / - MEF. Isku soo wada duuboo, Ezetimibe wuxuu u dhaqmaa sidii soo saare Nrf2 sheeko cusub oo ah qaab madax banaan ROS [1]. Bini'aadamka huh7 hepatocytes waxaa lagu daaweynayaa Ezetimibe (10μM, 1 h) oo lagu shubay Palmitic acid (PA, 0.5 mM, 24 h) si loo kiciyo steatosis cagaarshow. Daaweynta Ezetimibe waxay si weyn u xoojineysaa heerarka PA-kordhay triglycerides (TG), taas oo ku habboon daraasaddeena xoolaha. Daaweynta PA waxay keentay ku dhowaad 20% hoos u dhaca muujinta mRNA ee ATG5, ATG6, iyo ATG7, oo lagu kordhiyay daaweynta Ezetimibe. Intaa waxaa dheer, daaweynta Ezetimibe waxay si weyn u kordhisay hoos u dhaca PA-ku-soo-saarka ee borotiinka badan ee LC3 [2].

MCE si madax banaan uma aysan xaqiijin sax ahaanshaha qaababkan. Iyagu waa tixraac keliya.

Maamulka Ezetimibe (Eze) wuxuu yareeyaa culeyska beerka ee jiirka oo laquudiyo cuntada methionine- iyo choline-deficient (MCD). Tani waxay la socotaa saameynta waxtarka leh ee 'Ezetimibe' ee hepatitis steatosis. Beerka histology wuxuu muujinayaa dhibco badan oo dufan macrovesicular ah oo ku jira jiirka cuntada MCD, laakiin daaweynta Ezetimibe waxay si muuqata hoos ugu dhigeysaa tirada iyo cabirka dhibcahaas. Intaas waxaa sii dheer, cagaarshowga beerka ee jiirka ee la siiyo cuntada MCD waxaa si weyn hoos ugu dhigay Ezetimibe [1]. Heerarka dufanka dhiigga iyo beerka oo ay ku jiraan TG, asiidh dufan bilaash ah (FFA), iyo wadarta guud ee kolestaroolka (TC) ayaa si weyn hoos ugu dhacay jiirka Ezetimibe ee lagu daweeyay OLETF. Intaa waxaa dheer, jiirka 'OLETF' waxay muujinayaan heerarka sare ee sonkorta ee sonkorta, insulin, HOMA-IR, TG, FFA, iyo TC marka loo eego xayawaanka LETF, kuwaas oo si weyn hoos ugu dhacay Ezetimibe. Intaa waxaa dheer, falanqaynta taariikhiga ah waxay muujisay in jiirka xakamaynta OLETF ay muujiyeen dhibco buurbuuran oo waaweyn oo ku jira hepatocytes marka loo eego kontoroolka LETO ee da'da la jaanqaadaya, kuwaas oo ay hoos u dhigeen maamulka Ezetimibe [2].

Kaydinta

Budada

-20 ° C

3 sano
 

4 ° C

2 sano
Kala dareeraha

-80 ° C

6 bilood
 

-20 ° C

1 bil

Qaab dhismeedka kiimikada

Ezetimibe

SHAHAADO

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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