Fondaparinux Biological Activity
Chaza | I-Fondaparinux sodium yi-antithrombin-dependent factor Xa inhibitor. |
EyeleleneyoIindidi | indlela yomqondiso >> Metabolic enzymes/proteases >> Factor Xa Iindawo zophando >> Izifo zentliziyo |
Ekujoliswe kuko | Factor Xa[1] |
I-In vitroizifundo | I-Fondaparinux i-sodium yi-anticoagulant yokuqala entsha ejolise ngokukhethekileyo kwi-factor Xa.Kwi-Fondaparinux, ixabiso le-IC50 (i-anti-Xa IU/ml) ye-monocytes esebenzayo (ac-M) yi-0.59±0.05, kunye ne-monocyte-derived particles (MMP) yi-0.17±0.03 [2]. |
Kwi-vivouphando | I-Fondaparinux sodium ine-linear, iprofayili ye-pharmacokinetic exhomekeke kwidosi, enika impendulo eqikelelweyo kakhulu.I-Fondaparinux sodium ine-100% ye-bioavailability, inokuqala ngokukhawuleza kwesenzo, inesiqingatha sobomi be-14 kwiiyure ze-16, kwaye inokuqhubeka nokumelana ne-thrombosis kwiiyure ezingama-24.Ichiza alichaphazeli ixesha leprothrombin okanye ixesha le-thromboplastin elisebenzayo, kwaye alichaphazeli ukusebenza kweplatelet okanye ukuhlanganiswa [1]. |
Iimbekiselo | [1].Bauer KA.okqhubekayo.I-Fondaparinux sodium: inhibitor ekhethiweyo ye-factor Xa.Am J Health Syst Pharm.2001 Nov 1;58 Suppl 2:S14-7.[2].UBen-Hadj-Khalifa S, et al.Ukwahlukana kwe-coagulation inhibitory effect ye-fondaparinux, i-enoxaparin kunye ne-heparin engaxutywanga kwiimodeli zeeseli zesizukulwana se-thrombin.Igazi le-Coagul Fibrinolysis.2011 Jul;22(5):369-73. |
Iimpawu zeMichiza kunye nezomzimba zeFondaparinux
Ifomula yemolekyuli | C31H53N3Na10O49S8 |
Ubunzima bemolekyuli | 1738.16 |
PSA | 900.82000 |
I-Fondaparinux luhlobo olutsha lwechiza le-antithrombotic elivunywe yi-FDA emva kwe-heparin kunye ne-heparin ephantsi ye-molecular weight kunyango kunye nokuthintela iintlobo ezahlukeneyo ze-arteriovenous thrombosis.
Izibonakaliso: I-Fondaparinux isetyenziselwa izigulane ezenza utyando olukhulu lwamathambo emilenze ephantsi, njengokuphuka kwe-hip, utyando olukhulu lwamadolo okanye ukutshintshwa kwe-hip, ukukhusela i-thromboembolism ye-venous.Isetyenziselwa unyango lwezigulane ezine-angina engazinzanga okanye i-non-ST-segment elevation myocardial infarction ehamba ngokukhawuleza (<120 imizuzu) unyango olungenayo (PCI) ngaphandle kokubonisa.Isetyenziselwa unyango lwezigulane ezine-ST-segment elevation myocardial infarction abasebenzisa i-thrombolysis okanye ekuqaleni abafumani ezinye iindlela zonyango zonyango.
1)Intengiso eqhubekayo ye-Glaxo yemarike iya kuyibeka kwindawo engundoqo yechiza kwindlela elandelayo yezonyango yoMphathiswa wezeMpilo, uhlaziyo lwexabiso leKomishoni yoPhuhliso noHlengahlengiso lweSizwe, kunye ne-inshurensi yezonyango yoBuphathiswa be-Inshurensi yaBantu.
A, Imveliso ayikangeni kwi-inshurensi yezonyango yesizwe.Ngo-2010, uhlengahlengiso lwe-inshorensi yezonyango lusanda kungena kwi-inshurensi yezonyango yasekuhlaleni yamaphondo ali-16.Iintengiso zikwinqanaba lokuqala kwaye ngokuthe ngcembe ziya kuthatha indawo yemarike ye-heparin ephantsi-molekyuli;amaphondo inshorensi yezonyango: Shaanxi, Shanxi, Inner Mongolia, Liaoning, Tibet, Yunnan, Guangdong , Guangxi, Hainan, Jiangsu, Gansu, Fujian, Jiangxi, Henan, Hubei, Beijing.
B, Iimpawu zisakhula.I-GSK okwangoku inezalathisi ezi-3 ekliniki.Ngokomzekelo, iimpawu ze-stents zivunyiwe kuphela.Ezinye iiheparin azikho.Ukusetyenziswa kweklinikhi ye-stents kwandisa ngama-30% ngonyaka.Ngokuvunywa kwezibonakaliso ezintsha, ukuthengisa kuya kwanda.Kwithiyori, zonke izifo eziphathwa yimveliso ye-heparin zinganyangwa yile mveliso.
C, Ixabiso inzuzo, ixabiso elisezantsi le mveliso kwimarike US 132 US dollar ngalinye, e China yi 168 yuan, ixabiso lasekhaya akayi kuhla.Ukuba uthumela ngaphandle, imarike yamazwe ngamazwe inendawo ebanzi;
2) Umda wezobuchwephesha uphezulu, izinto eziluhlaza zenziwe ngamanyathelo angama-75, kwaye i-patent iphelile iminyaka emi-5 (inqaku ngo-2014).Ayivunywanga ngabanye abavelisi.I-synthesis inzima kakhulu.Ayizukwenziwa ngaphantsi kweminyaka eli-10.Umjikelo mde, unzima, kwaye utyalo-mali.phezulu.Bambalwa abakhuphisana basekhaya, kwaye abakhuphisana bamazwe angaphandle baneendleko eziphezulu zempahla ekrwada.Injongo yethu kukunciphisa ngokuqhubekayo iindleko zempahla kunye nokubuyisela i-Glaxo kwimveliso yempahla ekrwada.
I-Hengrui Pharmaceuticals Fondaparinux yamkelwe njengomzekelo wokuqala e-China ngo-2018.
I-Guangdong Runxing Biotechnology Co., Ltd. inemveliso yonyaka ye-210 kg ye-fondaparinux sodium ephakathi kwe-N3 ephakathi, eya kufakwa kwi-2018.
IFondaparinux yaphuhliswa kuqala yiMYLAN IRELAND.Okwangoku, iHengrui Pharmaceuticals, iBorui Pharmaceuticals, iHaisco.
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I-TECHNOL OGY I-ADVANTAGES
●Uxinzelelo oluPhezulu lweCatalytic Hydrogenation.Uxinzelelo oluPhezulu lwe-Hydrogenolysis Reaction.I-Cryogenic Reaction (<-78%C)
● I-Aromatic Heterocyclic Synthesis
● Ukusabela ngokutsha
● IsiGqibo seChiral
●Heck, Suzuki,Negishi,Sonogashira .Giignard Reaction
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