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FondaparinSodiuM;Nchọpụta Fondaparinux SodiuM;Fondaparinux sodium N-4;

FondaparinSodiuM;Nchọpụta Fondaparinux SodiuM;Fondaparinux sodium N-4;

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Ọrụ Fondaparinux Biological

Kọwaa Fondaparinux sodium bụ ihe na-egbochi thrombin na-adabere na Xa inhibitor.
Ejikọtara yaOtu Ụzọ mgbaàmà >> Metabolic enzymes/proteases >> Factor Xa Research area >> Ọrịa obi
Ebumnuche Ihe kpatara Xa[1]
In vitroọmụmụ Fondaparinux sodium bụ ọgwụ mgbochi ọhụrụ nke mbụ na-ahọrọ ihe na-achọ Xa.Maka Fondaparinux, uru IC50 (anti-Xa IU / ml) nke monocytes na-arụ ọrụ (ac-M) bụ 0.59 ± 0.05, na ihe ndị sitere na monocyte (MMP) bụ 0.17 ± 0.03 [2].
Na vivonyocha Fondaparinux sodium nwere profaịlụ pharmacokinetic dabere na dose, nke na-enye nzaghachi nke ukwuu.Fondaparinux sodium nwere 100% bioavailability, na-enwe ngwa ngwa mmalite nke omume, nwere ọkara ndụ nke awa 14 ruo 16, ma nwee ike ịga n'ihu na-eguzogide thrombosis n'ime awa 24.Ọgwụ anaghị emetụta oge prothrombin ma ọ bụ oge thromboplastin na-arụ ọrụ, ọ dịghịkwa emetụta ọrụ platelet ma ọ bụ mkpokọta [1].
Ntụaka [1].Bauer KA.et al.Fondaparinux sodium: onye na - egbochi ihe nke Xa.Am J Health Syst Pharm.2001 Nov 1; 58 Nkwado 2: S14-7 .[2].Ben-Hadj-Khalifa S, et al.Mmetụta mgbochi coagulation dị iche iche nke fondaparinux, enoxaparin na heparin na-enweghị isi na ụdị sel nke ọgbọ thrombin.Coagul Fibrinolysis nke ọbara.2011 Jul; 22 (5): 369-73 .

Njirimara chemical na anụ ahụ nke Fondaparinux

Usoro ihe omimi C31H53N3Na10O49S8
Ibu arọ molekụla 1738.16
PSA 900.82000

Ngwa

Fondaparinux bụ ụdị ọgwụ antithrombotic ọhụrụ nke FDA kwadoro mgbe heparin na heparin dị arọ dị ala maka ọgwụgwọ na mgbochi nke thrombosis dị iche iche nke arteriovenous.

Ngosipụta: A na-eji Fondaparinux maka ndị ọrịa na-eme nnukwu ịwa ahụ orthopedic nke akụkụ ụkwụ dị ala, dị ka mgbaji ọkpụkpụ, nnukwu ịwa ahụ ikpere ma ọ bụ ngbanwe hip, iji gbochie thromboembolism venous.A na-eji ya maka ọgwụgwọ nke ndị ọrịa nwere angina na-akwụghị ụgwọ ma ọ bụ na-abụghị ST-ngalaba elu myocardial infarction nke na-enweta ọgwụgwọ ngwa ngwa (<120 nkeji) ọgwụgwọ invasive (PCI) na-enweghị egosi.A na-eji ya maka ọgwụgwọ nke ndị ọrịa nwere myocardial infarction myocardial ST-segment na-eji thrombolysis ma ọ bụ na mbụ anaghị enweta ụdị ọgwụgwọ ọzọ nke reperfusion.

Uru

1) Nkwalite ahịa nke Glaxo na-aga n'ihu ga-etinye ya n'ọnọdụ ọgwụ bụ isi na ụzọ ụlọ ọgwụ na-esote nke Ministry of Health, mgbanwe ọnụahịa nke National Development and Reform Commission, na mkpuchi ahụike nke Ministry of People's Insurance.

A, Ngwaahịa abanyebeghị na mkpuchi ahụike mba.Na 2010, mgbanwe mkpuchi ahụike ka abanyela na mkpuchi ahụike mpaghara nke mpaghara iri na isii.Ịre ahịa dị na mbido mbụ ma ga-eji nwayọọ nwayọọ dochie ahịa heparin dị arọ nke dị ala;mpaghara mkpuchi ahụike: Shaanxi, Shanxi, Mongolia ime, Liaoning, Tibet, Yunnan, Guangdong, Guangxi, Hainan, Jiangsu, Gansu, Fujian, Jiangxi, Henan, Hubei, Beijing.

B, Ngosipụta ka na-abawanye.GSK nwere ihe ngosi 3 ugbu a na ụlọọgwụ ahụ.Dịka ọmụmaatụ, ihe ngosi maka stent ka akwadoro naanị.Heparins ndị ọzọ adịghị.Ngwa ụlọ ọgwụ nke stent na-abawanye site na 30% kwa afọ.Site na nkwado nke ihe ngosi ọhụrụ, ahịa ga-abawanye.Na tiori, a na-agwọ ọrịa niile nke ngwaahịa usoro heparin na-agwọ site na ngwaahịa a.

C, Uru ọnụahịa, ọnụahịa kacha nta nke ngwaahịa a na ahịa US bụ 132 US dollar ọ bụla, na China bụ yuan 168, ọnụahịa ụlọ agaghị ada.Ọ bụrụ na ị na-ebupụ, ahịa mba ụwa nwere ohere sara mbara;

2) Ọnụ ụzọ teknụzụ dị elu, akụrụngwa akụrụngwa na-arụ ọrụ na usoro 75, yana patent agwụla afọ 5 (isiokwu na 2014).Ndị nrụpụta ndị ọzọ akwadobeghị ya.Ngwakọta ahụ siri ike nke ukwuu.Agaghị eme ya n'ihe na-erughị afọ 10.Usoro ahụ dị ogologo, siri ike, yana itinye ego.elu.Enwere ndị asọmpi ụlọ ole na ole, ndị asọmpi si mba ọzọ nwere ọnụ ahịa akụrụngwa dị elu.Ebumnuche anyị bụ ibelata ọnụ ahịa akụrụngwa ma dochie Glaxo na mmepụta akụrụngwa.
A kwadoro Hengrui Pharmaceuticals Fondaparinux dị ka nṅomi mbụ na China 2018.
Guangdong Runxing Biotechnology Co., Ltd. nwere mmepụta kwa afọ nke 210 n'arọ nke fondaparinux sodium Advanced intermediate N3, nke a ga-ede akwụkwọ na 2018.

MYLAN IRELAND mepụtara Fondaparinux na mbụ.Ugbu a, Hengrui Pharmaceuticals, Borui Pharmaceuticals, Haisco.

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Uru dị na nhazi nhazi ahụike

TECHNOL OGY URU
● Nnukwu nrụgide catalytic Hydrogenation.Mmeghachi omume Hydrogenolysis nrụgide dị elu.Mmeghachi omume Cryogenic (<-78%C)
●Aromatic Heterocyclic Synthesis
●Mmeghachi omume
● Mkpebi Chiral
●Heck, Suzuki,Negishi,Sonogashira .Mmeghachi omume Gignard

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Ụdị imekọ ihe ọnụ

1.Hazie ndị etiti ọhụrụ ma ọ bụ API.Otu dị ka nkesa nke dị n'elu, ndị ahịa nwere ihe achọrọ maka Intermediates ma ọ bụ API, na ha enweghị ike ịchọta ngwaahịa ndị dị mkpa na ahịa, mgbe ahụ anyị nwere ike inye aka hazie.

2.Usoro nkwalite maka ngwaahịa ochie.Ndị otu anyị ga-enyere aka ịkwalite ma melite mmepụta dị otú ahụ nke ụzọ mmeghachi omume ya mere ochie, ọnụ ahịa mmepụta dị elu, na arụmọrụ dị ala.Anyị nwere ike ịnye akwụkwọ zuru oke maka ịnyefe teknụzụ na nkwalite usoro, nyere ndị ahịa aka maka mmepụta nke ọma.

Site na ebumnuche ọgwụ ruo IND, JIN DUN Medical na-enye gịngwọta R&D ahaziri otu nkwụsị.

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