Apixaban

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Sunan API Nuni Musammantawa US DMF EU DMF CEP
Apixaban VTE Cikin-Gida

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Apixaban babban zaɓi ne kuma mai hanawa na Factor Xa tare da ƙimomin Ki na 0.08 nM da 0.17 nM a cikin ɗan adam da zomo, bi da bi [1].

Factor X, wanda kuma aka sanshi da eponym Stuart – Prower factor, enzyme ne na kwaskwarima. An kunna Factor X, ta hanyar hydrolysis, zuwa cikin yanayin Xa ta duka abubuwan IX. Factor Xa shine nau'in da aka kunna na sinadarin coagulation factor thrombokinase. Yin hana Factor Xa zai iya bayar da wata hanya ta daban don maganin tazarar jini. Masu hana Direct Direct shahararrun ƙwayoyin cuta ne [2].

A cikin vitro: Apixabanhas ya nuna babban ƙarfin aiki, zaɓaɓɓe, da inganci a kan Factor Xa tare da Ki na 0.08 nM da 0.17 nM don Humanan Adam Xa da Xa da Rabbit Factor Xa, bi da bi [1]. Apixaban ya tsawaita lokacin daskarewa na jinin plasma na al'ada tare da karfin (EC2x) na 3.6, 0.37, 7.4 da 0.4 μM, waɗanda ake buƙata bi da bi don ninka lokacin prothrombin (PT), gyara lokacin prothrombin (mPT), kunna lokaci na thromboplastin na ɓangare ( APTT) da HepTest. Bayan wannan, Apixaban ya nuna karfin gaske a cikin jinin plasma na mutum da zomo, amma rashin karfi a cikin bera da plasma na kare a duka gwajin PT da APTT [3].

A cikin rayuwa: Apixaban ya fitar da kyawawan magungunan magani tare da rashi mai sauƙi (Cl: 0.02 L kg-1h-1), da ƙarami mai rarraba (Vdss: 0.2 L / kg) a cikin kare. Bayan haka, Apixaban ya kuma nuna matsakaiciyar rayuwa tare da T1 / 2 na awanni 5.8 da kuma kyakkyawar kwayar halittar baki (F: 58%) [1]. A cikin arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) da samfurin rabbit mai kwakwalwa ta hanyar lantarki, Apixaban ya haifar da tasirin antithrombotic tare da EC50 na 270 nM, 110 nM da 70 nM a cikin hanyar dogaro da kashi [3 ]. Apixaban ya haɓaka mahimmancin aikin Xa tare da IC50 na 0.22 μM a cikin zomo ex vivo [4]. A cikin chimpanzee, Apixaban kuma ya nuna ƙaramin juzu'i na rarrabawa (Vdss: 0.17 L kg-1), ƙarancin tsarin tsari (Cl: 0.018 L kg-1h-1), da kyakkyawar kwayar halittar baka (F: 59%) [5].

Nassoshi:
Pinto DJP, Orwat MJ, Koch S, et al. Gano 1- (4-methoxyphenyl) -7-oxo-6- (4- (2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), mai karfin gaske, mai zaba, mai amfani, da kuma mai hana kwayar halittar zubar da jini Xa [J]. Jaridar ilmin sunadarai, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors as Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, mai magana da baki, kai tsaye kuma mai zabi sosai mai hana Xa: in vitro, antithrombotic da antihemostaticstudies [J]. Jaridar Thrombosis da Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics da pharmacodynamics na factor Xa inhibitor apixaban a cikin zomaye [J]. Jaridar thrombosis da thrombolysis, 2010, 29 (1): 70-80.
Shi K, Luettgen JM, Zhang D, et al. Magungunan likitancin magani na yau da kullun da kwayar cutar apixaban, mai tasiri kuma mai zabi Xa inhibitor [J]. Jaridar Turai game da maganin ƙwayoyi da magunguna, 2011, 36 (3): 129-139.

Apixaban babban zaɓi ne kuma mai hanawa na Factor Xa tare da ƙimomin Ki na 0.08 nM da 0.17 nM a cikin ɗan adam da zomo, bi da bi [1].

Factor X, wanda kuma aka sanshi da eponym Stuart – Prower factor, enzyme ne na kwaskwarima. An kunna Factor X, ta hanyar hydrolysis, zuwa cikin yanayin Xa ta duka abubuwan IX. Factor Xa shine nau'in da aka kunna na sinadarin coagulation factor thrombokinase. Yin hana Factor Xa zai iya bayar da wata hanya ta daban don maganin tazarar jini. Masu hana Direct Direct shahararrun ƙwayoyin cuta ne [2].

A cikin vitro: Apixabanhas ya nuna babban ƙarfin aiki, zaɓaɓɓe, da inganci a kan Factor Xa tare da Ki na 0.08 nM da 0.17 nM don Humanan Adam Xa da Xa da Rabbit Factor Xa, bi da bi [1]. Apixaban ya tsawaita lokacin daskarewa na jinin plasma na al'ada tare da karfin (EC2x) na 3.6, 0.37, 7.4 da 0.4 μM, waɗanda ake buƙata bi da bi don ninka lokacin prothrombin (PT), gyara lokacin prothrombin (mPT), kunna lokaci na thromboplastin na ɓangare ( APTT) da HepTest. Bayan wannan, Apixaban ya nuna karfin gaske a cikin jinin plasma na mutum da zomo, amma rashin karfi a cikin bera da plasma na kare a duka gwajin PT da APTT [3].

A cikin rayuwa: Apixaban ya fitar da kyawawan magungunan magani tare da rashi mai sauƙi (Cl: 0.02 L kg-1h-1), da ƙarami mai rarraba (Vdss: 0.2 L / kg) a cikin kare. Bayan haka, Apixaban ya kuma nuna matsakaiciyar rayuwa tare da T1 / 2 na awanni 5.8 da kuma kyakkyawar kwayar halittar baki (F: 58%) [1]. A cikin arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) da samfurin rabbit mai kwakwalwa ta hanyar lantarki, Apixaban ya haifar da tasirin antithrombotic tare da EC50 na 270 nM, 110 nM da 70 nM a cikin hanyar dogaro da kashi [3 ]. Apixaban ya haɓaka mahimmancin aikin Xa tare da IC50 na 0.22 μM a cikin zomo ex vivo [4]. A cikin chimpanzee, Apixaban kuma ya nuna ƙaramin juzu'i na rarrabawa (Vdss: 0.17 L kg-1), ƙarancin tsarin tsari (Cl: 0.018 L kg-1h-1), da kyakkyawar kwayar halittar baka (F: 59%) [5].

Nassoshi:
Pinto DJP, Orwat MJ, Koch S, et al. Gano 1- (4-methoxyphenyl) -7-oxo-6- (4- (2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), mai karfin gaske, mai zaba, mai amfani, da kuma mai hana kwayar halittar zubar da jini Xa [J]. Jaridar ilmin sunadarai, 2007, 50 (22): 5339-5356.
Sidhu P S. Direct Factor Xa Inhibitors as Anticoagulants [J].
Wong PC, Crain EJ, Xin B, et al. Apixaban, mai magana da baki, kai tsaye kuma mai zabi sosai mai hana Xa: in vitro, antithrombotic da antihemostaticstudies [J]. Jaridar Thrombosis da Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, et al. Metabolism, pharmacokinetics da pharmacodynamics na factor Xa inhibitor apixaban a cikin zomaye [J]. Jaridar thrombosis da thrombolysis, 2010, 29 (1): 70-80.
Shi K, Luettgen JM, Zhang D, et al. Magungunan likitancin magani na yau da kullun da kwayar cutar apixaban, mai tasiri kuma mai zabi Xa inhibitor [J]. Jaridar Turai game da maganin ƙwayoyi da magunguna, 2011, 36 (3): 129-139.

Tsarin sunadarai

Apixaban

TABBATARWA

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

KYAUTA MANAGEMENT

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