Apixaban

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Apixaban waa xakameyn heer sare ah oo la celin karo oo ah Factor Xa oo leh qiyamka Ki ee 0.08 nM iyo 0.17 nM ee aadanaha iyo bakaylaha, siday u kala horreeyaan [1].

Factor X, oo sidoo kale loo yaqaan 'epuym' Stuart – Prower factor, waa enzyme of xinjirowga qulqulka. Xaqiijinta X waa la shaqeysiiyay, by hydrolysis, oo loo yaqaan 'Xa' labadaba IX. Factor Xa waa qaabka firfircoon ee cuncunka xinjirowga thrombokinase. Ka-hortagga Factor Xa wuxuu bixin karaa qaab kale oo looga hortago xinjirowga xinjirowga. Toosinta Xa-xajiyeyaasha waa dawooyinka xinjirowga lidka ku ah ee caanka ah [2].

In vitro: Apixabanhas waxay ku soo bandhigtay awood sare, xulasho, iyo waxtar ku saabsan Factor Xa oo leh Ki ee 0.08 nM iyo 0.17 nM oo loogu talagalay Xaqiiqda Aadanaha Xa iyo Bakayle Xaas Xa, siday u kala horreeyaan [1]. Apixaban wuxuu dheereeyay waqtiyada xinjirowga ee plasma-ka caadiga ah ee dadka oo leh uruurinta (EC2x) ee 3.6, 0.37, 7.4 iyo 0.4 μM, kuwaas oo looga baahan yahay siday u kala horreeyaan inay u labanlaabaan waqtiga prothrombin (PT), waqtiga prothrombin ee wax laga beddelay (mPT), oo firfircoon waqtiga tromboplastin qayb ahaan ( APTT) iyo HepTest. Ka sokow, Apixaban wuxuu muujiyay awoodda ugu sareysa ee ku jirta bini-aadamka iyo bakaylaha, laakiin awood yar oo ku jirta jiirka iyo eeyga plasma labadaba baaritaanka PT iyo APTT [3].

In vivo: Apixaban wuxuu kahelay farmasokokinetik aad u fiican oo leh nadiifin aad uyar (Cl: 0.02 L kg-1h-1), iyo mugga hoose ee qaybinta (Vdss: 0.2 L / kg) eeyga. Ka sokow, Apixaban sidoo kale wuxuu muujiyay nolol nus dhexaad ah oo leh T1 / 2 oo ah saacadaha 5.8 iyo bioavailability afka oo wanaagsan (F: 58%) [1]. Qaabka xididdada dhiigga loo yaqaan 'arteriovenous-shunt thrombosis' (AVST), venous thrombosis (VT) iyo koronto dhexdhexaad ah carotid arterial thrombosis (ECAT) moodooyinka bakaylaha, Apixaban waxay soo saartay saameyn antithrombotic leh EC50 oo ah 270 nM, 110 nM iyo 70 nM qaab ku tiirsan qiyaasta [3 ]. Apixaban wuxuu si weyn u joojiyay cunsuriyada Xa ee leh IC50 ee 0.22 μM ee bakaylaha ex vivo [4]. In chimpanzee, Apixaban sidoo kale wuxuu muujiyey mug yar oo qaybinta (Vdss: 0.17 L kg-1), nadiifin nidaamsan oo hooseysa (Cl: 0.018 L kg-1h-1), iyo bioavailability afka ah (F: 59%) [5].

Tixraacyo:
Pinto DJP, Orwat MJ, Koch S, iyo al. Soo helidda 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), oo ah mid aad u karti badan, xul ah, waxtar leh, iyo ka hortag bioavailable factor of coagulation factor Xa [J]. Joornaalka kiimikada daawada, 2007, 50 (22): 5339-5356.
Sidhu P S. Xaqiiqda Tooska ah ee Xaasidada Xawaareyaasha sida Anticoagulants [J].
Wong PC, Crain EJ, Xin B, iyo al. Apixaban, oo ah cunsur hadal, toos ah oo aad u xulasho badan Xa joojiye: in vitro, antithrombotic iyo antihemostaticstudies [J]. Wargeyska Thrombosis iyo Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, iyo al. Dheef-shiid kiimikaadka, farmasokokinetikada iyo farmasiga firfircoonida ee cunsurka Xa inhibitor apixaban ee bakaylaha [J]. Joornaalka xinjirowga iyo dhiig-baxa, 2010, 29 (1): 70-80.
Isaga K, Luettgen JM, Zhang D, et al. Daawooyinka daawooyinka takhasuska leh iyo dawooyinka dawooyinka ee apixaban, oo ah awood xoog leh oo xulasho leh Xa inhibitor [J]. Joornaalka Yurub ee dheef-shiid kiimikaadka iyo farmasokokinetics, 2011, 36 (3): 129-139.

Apixaban waa xakameyn heer sare ah oo la celin karo oo ah Factor Xa oo leh qiyamka Ki ee 0.08 nM iyo 0.17 nM ee aadanaha iyo bakaylaha, siday u kala horreeyaan [1].

Factor X, oo sidoo kale loo yaqaan 'epuym' Stuart – Prower factor, waa enzyme of xinjirowga qulqulka. Xaqiijinta X waa la shaqeysiiyay, by hydrolysis, oo loo yaqaan 'Xa' labadaba IX. Factor Xa waa qaabka firfircoon ee cuncunka xinjirowga thrombokinase. Ka-hortagga Factor Xa wuxuu bixin karaa qaab kale oo looga hortago xinjirowga xinjirowga. Toosinta Xa-xajiyeyaasha waa dawooyinka xinjirowga lidka ku ah ee caanka ah [2].

In vitro: Apixabanhas waxay ku soo bandhigtay awood sare, xulasho, iyo waxtar ku saabsan Factor Xa oo leh Ki ee 0.08 nM iyo 0.17 nM oo loogu talagalay Xaqiiqda Aadanaha Xa iyo Bakayle Xaas Xa, siday u kala horreeyaan [1]. Apixaban wuxuu dheereeyay waqtiyada xinjirowga ee plasma-ka caadiga ah ee dadka oo leh uruurinta (EC2x) ee 3.6, 0.37, 7.4 iyo 0.4 μM, kuwaas oo looga baahan yahay siday u kala horreeyaan inay u labanlaabaan waqtiga prothrombin (PT), waqtiga prothrombin ee wax laga beddelay (mPT), oo firfircoon waqtiga tromboplastin qayb ahaan ( APTT) iyo HepTest. Ka sokow, Apixaban wuxuu muujiyay awoodda ugu sareysa ee ku jirta bini-aadamka iyo bakaylaha, laakiin awood yar oo ku jirta jiirka iyo eeyga plasma labadaba baaritaanka PT iyo APTT [3].

In vivo: Apixaban wuxuu kahelay farmasokokinetik aad u fiican oo leh nadiifin aad uyar (Cl: 0.02 L kg-1h-1), iyo mugga hoose ee qaybinta (Vdss: 0.2 L / kg) eeyga. Ka sokow, Apixaban sidoo kale wuxuu muujiyay nolol nus dhexaad ah oo leh T1 / 2 oo ah saacadaha 5.8 iyo bioavailability afka oo wanaagsan (F: 58%) [1]. Qaabka xididdada dhiigga loo yaqaan 'arteriovenous-shunt thrombosis' (AVST), venous thrombosis (VT) iyo koronto dhexdhexaad ah carotid arterial thrombosis (ECAT) moodooyinka bakaylaha, Apixaban waxay soo saartay saameyn antithrombotic leh EC50 oo ah 270 nM, 110 nM iyo 70 nM qaab ku tiirsan qiyaasta [3 ]. Apixaban wuxuu si weyn u joojiyay cunsuriyada Xa ee leh IC50 ee 0.22 μM ee bakaylaha ex vivo [4]. In chimpanzee, Apixaban sidoo kale wuxuu muujiyey mug yar oo qaybinta (Vdss: 0.17 L kg-1), nadiifin nidaamsan oo hooseysa (Cl: 0.018 L kg-1h-1), iyo bioavailability afka ah (F: 59%) [5].

Tixraacyo:
Pinto DJP, Orwat MJ, Koch S, iyo al. Soo helidda 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), oo ah mid aad u karti badan, xul ah, waxtar leh, iyo ka hortag bioavailable factor of coagulation factor Xa [J]. Joornaalka kiimikada daawada, 2007, 50 (22): 5339-5356.
Sidhu P S. Xaqiiqda Tooska ah ee Xaasidada Xawaareyaasha sida Anticoagulants [J].
Wong PC, Crain EJ, Xin B, iyo al. Apixaban, oo ah cunsur hadal, toos ah oo aad u xulasho badan Xa joojiye: in vitro, antithrombotic iyo antihemostaticstudies [J]. Wargeyska Thrombosis iyo Haemostasis, 2008, 6 (5): 820-829.
Zhang D, He K, Raghavan N, iyo al. Dheef-shiid kiimikaadka, farmasokokinetikada iyo farmasiga firfircoonida ee cunsurka Xa inhibitor apixaban ee bakaylaha [J]. Joornaalka xinjirowga iyo dhiig-baxa, 2010, 29 (1): 70-80.
Isaga K, Luettgen JM, Zhang D, et al. Daawooyinka daawooyinka takhasuska leh iyo dawooyinka dawooyinka ee apixaban, oo ah awood xoog leh oo xulasho leh Xa inhibitor [J]. Joornaalka Yurub ee dheef-shiid kiimikaadka iyo farmasokokinetics, 2011, 36 (3): 129-139.

Qaab dhismeedka kiimikada

Apixaban

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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