组胺H_1受体拮抗剂比拉斯汀.PDF

2010, V o l. 34, N o. 7 331 P rog ress in P ha rm aceu tica l S c iences ,, HCC , + ) , + 52 ( m FOL FOX6 ( ) m FOL FOX6 I HCC ( , ) H1 [] ; [ ] R 976 ; ( bilastine) 2 H1 FA ES , , 2 : , , : CAS: 20218927824 H1 14311 24811 , , : H1 , ( 4411 nmol L - 1 ) ; Ki 30 H1 H1 , 759 282 nmol L - 1 , IC50 9515 2010 34 7 331 , H2 H3 100 mol L - 1 , , ( ED50 = 2145 m g kg- 1 ) 4157 g kg- 1 ) , ( ED50 = 53132 g kg- 1 ) , IgE IgG2 IgE2 ( ED50 5196 3182 H1 IL 24 H1 ( ED50 = - 4115 mg kg- 1 ) , , , (275 mg kg- 1 ) 112 h; , , 81% , 14 C2 ( tmax ) 24 ; : , (10 mg kg- 1 ) , , t1 /2 t1 /2 0159 2102 h; 218 117 L kg- 1 ; 3142 0158 L h - 1 kg- 1 (5 40, 10 50 mg kg- 1 ) 10 0115 0130 h, (Vd ) ( Cl) ( Cmax ) 2 (AUC ) , , AUC 10 , 42% 69% 25% 61% 30 ( , 400 mg) , (Q 2TcN i ) Q 2Tc , 100 mg ( 5 , , ) Q 2T ? 1994-2010 China Academic Journal Electronic Publishing House. All rights reserved. 2010 34 7 332 20 ( , 25 mg) ( 20 40 80 mg) 7 , ,, , , , 18 ( P 01001 ) , H1 , , 20 mg 40 mg 80 mg ( P 01001 ) : , , 20 (p sychomotor perform ance test) , , 80 mg , 40 mg ; : 20 mg , , , 20 mg 21 4 ) (215 5 10 20 ,: 12 , , 50% , 50 mg 50% ; 50% , 1 400 50 m g) 50% , H1 ( 10 mg , 24 , ( SAR ) 332 2010, V o l. 34, N o. 7 P rog ress in P ha rm aceu tica l S c iences 721 3, (5 m g, qd) ( [ (NN SS) 2 01001) , , , , ( SAR ) ( 20 mg, qd) ,2 ) () ] , ( N SS ) ( TSS) , TSS2 (AUC ) : , TSS2 AUC (9814 vs 11814, P (AUC 10015) 2 (2016 % vs 1918% , 1818% ) , 683 SAR (20 mg, qd) ( 10 mg, qd) 2 12 ( ) ( ) NSS NNSS, TSS, 0 14 TSS ( TSS2AUC0214 ) : TSS2AUC0214 , (7615, 7213 vs 10016, P 01001) TSS2AUC0214 , AUC , , 36% , P = 0103) ( 2417% vs ( 2916% ) ; ( 1415% vs 2416% , P = 0103 ) (1915% ) ; , (118% vs 715% , P 01001; 014% vs 418% , P = 0102) , , ,, ? 1994-2010 China Academic Journal Electronic Publishing House. All rights reserved. 2010, V o l. 34, N o. 7 333 P rog ress in P ha rm aceu tica l S c iences 2010 34 7 333 525 ( 20 mg, qd) (5 mg, qd) , 28 , , TSS , 28 , TSS ( - 4123 , - 4163 vs - 2199; P 01001) , , TSS 2 , 6