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 ??·?×óê??? C13H12F2N6O ??·?×óá??? 306.28 ??D?×'?? ±??·?a?Té???3??÷òoì??? ??ò?àí??àí?? 1.ò?àí×÷ó? ·ú???òê??á??àà?1???úò????1???ú?×??1????ú·t?°?2×?·ú???ò??è?oí?÷?????????ú?Dè???è????é?ú?Dè?(°üà¨?aò??y3??ò?aò?êü?e??è?oí??????è?éíD????é?ú2?)??D?Díòt?é?ú?Dè?(°üà¨?-?ú?Dè?)???·???íà-é??ú??D???×ó?úê????????úê???±í?¤???úê????¤?×??éú?ú??'??é??×ó?ú(°üà¨?-?ú?Dè?)?°???¤×é??°????ú??ì3ê?×?é??ú???¨ê??|???1?èóDD§??·ú???ò??×÷ó??ú???÷òa?a???è????D??éè????ú????°?é???P-450????D???'ó??ò??????ú??°??¤é??ó??1ì'???éú??o?3é?? 2.??àí?D?? ?Y???×±¨?à: ????×÷ó?:'óêó?-?ú??óè·ú???ò20mg/kg???é?á?è?ó3ù·???1y3ì????2?ó°?ì??éúóyá|??'óêó?§2ú?ú?D???á1???'?êó??óè20mg/kgoí40mg/kgê±???3D?????3?????2úoí?ó3ù·??????÷òa±í???a?àì?êyá??á?è???óoí'???D?éúêóêyá???éù??'ó?áá?·ú???ò??'óêó·?????ó°?ì?é?üó????éì?òìD??????í????ê???????'??¤??????óD1??? ??í?±?:amesê??é??D?êóáü°íá?LS178Y??°?ê??é??????1??è??o?ê??é??è?ì?áü°í??°?è?é?ì?ê??é?á1??ù?aò?D??? ??°?×÷ó?:ê??é??DDá?D?êóoí'óêó·?±e°'2.5??5?ò10oá??/1???ì???/è??áá?(???aè?ì?í????áá???2??7±?)?ú·t·ú???ò24??????ìáê?·ú???ò?T??°?×÷ó?????D?D?'óêó?óêü·ú???ò?áá??a5mg/kgoí10mg/kg??á?D???ò?24???????é??????????°??ùá?·?éú?ê?????? ??ò?'ú??á|?§?? ?2????óè·ú???ò100mg?????ù?aò?·??¨?è(Cmax)?a4.5??8mg/L??±í1?·?2?èY?y(Vd)?ó?üóúì?òo×üá???·ú???ò?a???°°×?áo??ê?í(11%??12%)???úì??ú1?·o·?2?óú?¤·?????e?òo???1??òo??ì?òo?è×é??ì?òo?D???òòo?°?¤·??Dò????¨?è???a?aò??¨?è??10±?????e??¤·??D???a2±???íùòo??ì?????e?òo?????×?Dó??aò??¨?è?ó?ü?????¤?×ê±?????1òo?D·ú???ò???¨?è?é'??aò??¨?è??54%??85%??·ú???òéùá??ú???à'úD????÷òa×?é???D1??ò??-Dí×??ò?D??3???ò?á???80%ò?é????a??3y°????ú(t1/2)?a27??27D?ê±??é?1|?ü??í?ê±?÷???ó3¤?? ?aòoí????ò?1?¤í????é2?·???3y·ú???ò?? ?ùí???ò?????á|?§ ò?±¨?à???ùí?ò?????á|?§2?êyè????ùê?:
±??D???ùí????êá? |
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°????ú |
?ú???????y |
(oá??/1???ì???) |
(D?ê±) |
(AUC???????¤D?ê±/oáéy) |
11ìì??11???? |
???áá??2??×?é? 3oá??/1???ì??? |
23 |
110.1 |
9??????13?ê |
???áá??ú·t 2oá??/1???ì??? |
25.0 |
94.7 |
9??????13?ê |
???áá??ú·t 8oá??/1???ì??? |
19.5 |
362.5 |
5?ê??15?ê |
?à?áá??ú·t 2oá??/1???ì??? |
17.4* |
1.3 |
5?ê??15?ê |
?à?áá??ú·t 4oá??/1???ì??? |
15.2* |
1.9 |
5?ê??15?ê |
?à?áá??ú·t 8oá??/1???ì??? |
17.6* |
1.7 |
5?ê??15?ê |
?à?áá??2??×?é? 3oá??/1???ì??? |
15.5 |
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