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痴夷子皮: 金币+3, 谢谢提供信息，辛苦了，欢迎常来新药研发版哦。 2012-09-13 13:41:48
感谢参与，应助指数 +1
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??????????10mg????????????50mg????????????100mg ????????????? **2009??6????????8?棬?????a???????????????餦????? *2007??3???? ????????????????? 874291 ?????????????????? ?????Y???????????????? 2007??3?? ?a???????? ???????[???? ???J?? ????? ??????????10mg ????????`?? 4291405F1025 ???J・?S????? ???J???? 20700AMZ00529 ????? Aqupla ?a????????d???? 1995??8?? ????_????? 1995??9?? ?A??・???????? ?A?????? ???・???±??? ??????? ????????????????g3?? ???????** ???a ?I????????a? ?????????I????????????????? ???????????顸?????a??????????? ?M?? ???・??????1??У??? ?????????10mg ?????? ?????????70??10mg ??? ???・???Σ? ?????????????X?|??K???????????? pH?? 6.5??7.5 0.02g/mL???? ????R???????????c???????????? ?s0.1 0.02g/mL???? ????? ??????????50mg ????????`?? 4291405F2021 ???J・?S????? ???J???? 20700AMZ00531 ????? Aqupla ?a????????d???? 1995??8?? ????_????? 1995??9?? ?A??・???????? ?A?????? ???・???±??? ??????? ????????????????g3?? ???????** ???a ?I????????a? ?????????I????????????????? ???????????顸?????a??????????? ?M?? ???・??????1??У??? ?????????50mg ?????? ?????????70??50mg ??? ???・???Σ? ?????????????X?|??K???????????? pH?? 6.5??7.5 0.02g/mL???? ????R???????????c???????????? ?s0.1 0.02g/mL???? ????? ??????????100mg ????????`?? 4291405F3028 ???J・?S????? ???J???? 20700AMZ00533 ????? Aqupla ?a????????d???? 1995??8?? ????_????? 1995??9?? ?A??・???????? ?A?????? ???・???±??? ??????? ????????????????g3?? ???????** ???a ?I????????a? ?????????I????????????????? ???????????顸?????a??????????? ?M?? ???・??????1??У??? ?????????100mg ?????? ?????????70??100mg ??? ???・???Σ? ?????????????X?|??K???????????? pH?? 6.5??7.5 0.02g/mL???? ????R???????????c???????????? ?s0.1 0.02g/mL???? ???????? ????????????? ???? 1. ???????????H???????l????R?????????????ΙC??????I?C?????????Ф??????????B???????Q???????????J????????????m?Ф?I????Ф??????????@?A?ο???????????????????????????????????l??????????I?C?????????????Ф????a????????R????Y?????????????v?B??????????????????????????J?????????R????Y????????????????????????28.5??????V???С??p?????21.1??????V??????p????k?F??????????νY????????????????????????????????????????? 2. ????????????o???r?????????????????O???????????????????????U?Y????????Τ????Ф?????????????????????x?k??????????????m?Ф??ж??????????Τ???????????????ɡ???????? 3. ??????????????????????????????i??????? ???? ???Τλ???????????????? 1. ??V????l????Τ????????l??????????????? 2. ??V???I????Τ???????I??????????????? 3. ????????????????a?????????V???^????μ????s?Τ????? 4. ?ыD??????路??????????Τ???D?????ыD???b?D??????D?????????????? ??????τ??????÷????????? ??????τ??? ?^?i????????С?????????η?С?????????????????????????z????裩?[?????юz??????m?i?? ?÷????????? 1. ???????????????????????1??1??80??100mg/m2???????e????????????????4?L?g???a?????????1???`????????????R?????? ????????????????h???????????????m?ˉ??p???? 2. ???????r?????????????300mL???????????c????5?????????`?????????????60????????????ξ?????? 3. ???????????????A??1000mL??????????ξ?????? ?????????* ??????? ???Τλ?????????????????? 1. ???l????Τ????????l????????????????????????????桹????????? 2. ?I????Τ???????I????????????????????????????桹????????? 3. ??????Τ?????????????????????????????? 4. ???????Τ???????????????????????????????? 5. ?????????????????????ι??l??????????????????????????????????? 6. ??????????????????????????????????????? 7. ???h?????l????????????????????????????h???????????????? ????????????? 1. ???l??????I?C??????????V??????????????????????Τ???l????R?????????????ΙC??????I?C?????????Ф????????????B???????Q??????????????J????????????p???????a????m?Ф?I????Ф??????????????????????????????????????????l?C????I?C??????¤????????????l??????I?C????¤???????????????????Τ???????λ????????????????m??p???????????????I?C???????????????????????L???g??錄????????????????????w???????????????????Τ????????????Ф?????? 2. ??????????A???k?F??ω???????????????? 3. ?I??????????Μp??r????????????????????p???????a??????????????N?????a????ν???r?g???L????Τ???????ζ????????????Τ?????????r????????_???????????????????m????????D-?????`???????????????????????????????????????????????????Ф????????I????????????????????????????a???椵??????Τ?????????????a?o??????Ф????????????U???????????????y??????????・?I????????????????Τ?????????????????? 4. ????・?I????????????????????????????????????Τ?????????B???????Q?????m?Ф?I????Ф?????? 5. С?????????????????h?λ????????????????????????????????????]??????? 6. ???????R????Y????????632??????????????????2?????????????・????`?????k??????????????????????1????????椵????????????1??????A???????????????????R????????????????1???????????????????????????}????????????×???z????γ?????????????????・????`?????k????1???????????????????ST???¤??????????????????????????????????k?????T??????????????????????????????????????????v?B?????餫?????? ?????? ??????? ??????????????? 1. ?a?????????ο??????[???? ?????????????????x??????????????|?????????????? ???侀???? ?R????・???÷??? ???l?????????????????????Τ?????????J??????????p???????a????m?Ф?I????Ф?????? ?C??・Σ????? ?C?????? ??????l??????????Ф??? 2. ?a?????????Υ???????????????| ?R????・???÷??? ?I???????????????????????????????Τ?????????J?????????????a???????m?Ф?I????Ф?????? ?C??・Σ????? ?C?????? ?????I????????????????Ф??? 3. ?a??????Х???????c??c ?R????・???÷??? ?I???????????????????????????????Τ?????????J?????????????a???????m?Ф?I????Ф?????? ?C??・Σ????? ?C?????? ?????I????????????????Ф??? ?????? ???????k?F??r?θ?? ???J?r???????????u????????597???У??R?????????????????????569????95.3???????J?????? ?????K??r???????????u????????3091???У??R?????????????????????2339????75.67???????J?????? ???????????????224????7.25???????I??138????4.46?????????????105????3.40????????????????????73????2.36???????????????Τ?????V????????????8????0.26???????I??7????0.23?????????12????0.39????????????? ?????R?????????????????????p??1521????49.21??????????????p??729????23.58???????С??p??1329????43.00??????ι??l??????????????Τ?????V?????????????p??379????12.26???????С??p??340????11.00?????????????????????????????????????I?C???????BUN??N201????6.50????????奯?????????N95????3.07????????????V????????BUN??N18????0.58???????????????????ΙC???????AST??GOT????N221????7.15??????ALT??GPT????N259????8.38????????????? ?????????k?F?l?????J?r???????K??r?γ???????????? ????????? 1. ???????????????饭???`??????1??5??δ?????????????????????饭???`?????????t?????????y??????????R??????????????????????Τ???Q????????Ф??????????J??????????????????????m?Ф?I????Ф?????? 2. ???l??????????p???1??5??δ???????????????p?????????p????С??p???????A??0.1??1??δ?????????????????????Τ??????????Q????????Ф??????????J???????????????g???????L???p???????a????m?Ф?I????Ф?????? 3. ?I?????0.1??1??δ???????I????????V???I???????????????????Τ???Q????????Ф??????????J??????????????@?A?ο????????????????????? 4. ??????・????`?????k??????????・????`?????k????????????????????????椵????????????????????????????? 5. ?y?・????????1??5??δ?????????Q??0.1??1??δ???????y?????????????????????Q?????????????????Τ???m??????????Ф??????????B???????Q???????????J?????????????a???????m?Ф?I????Ф???????????????????u???????????????????????????????????I?C????¤Τ?????????????????? 6. ?g?|??????0.1??δ???????k??????????????y?????X?????????餦?g?|????????????????????Τ???Q????????Ф??????????J????????????????????????I??|????????????m?Ф?I????Ф?????? 7. ???????????m???????????SIADH?????l?????????????????????????R???????Х???????й?????????????????R??????餦???????????m???????????SIADH??????????????????Τ?????Τ褦??????????????????????????????????????????m?Ф?I????Ф?????? ???????θ????? ??????U??? 0.1??5??δ?? ?^?????????????Τ???????????U?????ζ????? ??????U??? 0.1??δ?? ?d?? ?I??? 5?????? BUN??N?????????????N ?I??? 0.1??5??δ?? ???????????????????2???????????????N???????????????????N ?I??? 0.1??δ?? ???x???????`??????NAG??N ???????? 5?????? ????・?I?????????? ???????? 0.1??5??δ?? ?????????????????????????????? ??h???? 0.1??5??δ?? ???????????l?}??ST????? ??h???? 0.1??δ?? ?????? ???????? 0.1??5??δ?? ???????y ???????? 0.1??δ?? ?????????????? ?^????? 0.1??5??δ?? ??????`?????????k?????k?? ????? 5?????? AST??GOT????N??ALT??GPT????N??LDH??N??Al-P??N ????? 0.1??5??δ?? ????????N?????t????p?????奢???????? ???|?? 5?????? ?????????????????`???????|???? ???????? 0.1??5??δ?? ???????????У??k?????[????w???t???g??????????????^??? ???????? 0.1??δ?? ???}?????? ???h??????? 1. ???????????????I???????й???????????h?????I?C??????¤????????й???W???????飬???l?????k?F??????????????J???????????????????_?J????????????Ф?????????g????????????? 2. ???h?????????1??1??80mg/m2???????e???????????_????????????????? 3. ?????γ??J?r????????65?r????θ??h??194???У??????p???153????78.9???????С??p???117????60.3??????????????p???130????67.0???????J???????? ???????????K??r????????65?r????θ??h??1113???У??????p???560????50.31???????С??p???525????47.17??????????????p???257????23.09???????J???????? ?ыD???b?D??????D??????? 1. ?ыD??????路??????????Τ???D??????????????????????Y???????????????????ü????????????????????????????????????????????椵???????? 2. ????D???????????????????????????????????a???????????????Ф?????Ф???椵???????? С????????? С?????????????_?????????????????U?Y????????????????????????????????? ?m???????? 1. ?{?u???????????????????????????????? 2. ?{?u?r (1) ????????e??????????Τ?????ο??????[??????????????????? (2) ???????ξ???????H?????????????pH5???¤????????????|?a??????????`??????????5??????????????????????????Τ???????? (3) ?????????????????????????????γ????????????¤???Τ????????????????????????????????????????? (4) ???????????????????Τ???????????¤???????? 3. ???r?????}???????H?????a??????????????????λ????Y・??????????????????Τ???a???????????????褦??????????????? ??????????? 1. ?????????????????????Y????????????????????????B???????????????l????????????????????Y??????????????????νY??????椵?????? 2. ??????????????Y???L1??6?????g?g????}????????????????k??????椵?????? ?a???B 1. ??{????? (1) ?????[??????7?????????????????80mg/m2????100mg/m2??s60???g??ξ?????????????????y????????{?оt?????????????g??Х?????????ΤΣ???νK??r???????????2????????????AUC?????????????????????????????p???T1/2??????s0.1??1?r?g????????????p???T1/2?????s2??13?r?g?????? 1)?? ??1 ?a???B????`?????? (2) ?????[???????????????No.7??????{????????^???????[?x??????y???????????????{?а?????????[?x???????????????????? 1)?? ??2 ?a???B????`?????? 2. ??? ???ο??? ?????????????3mg/kg??g????}????????????M????????????????10?????й?U·??????I????????????{????????????????????????νM???????{??????????????????M?????????????????{??????W???????24?r?g??????????????θ?????I?????????????????I??????????? 3. ???x ???ο??? ??????????????????????????x???????????{?Ф??δ?仯?????????????? 4. ??й ?????[????????????????????80mg/m2????100mg/m2??s60???g??ξ???????????????????y??????24?r?g??????????л?????40??69???????? 1)?? ?a???B?α? ??1 ?a???B????`?? ??? ????? (mg/m2) ???h ???r?? ?? Cmax (??g/mL) AUC0-24 (??g・hr/mL) T1/2?? (hr) T1/2?? (hr) 1 80 33 ?? 8.45 15.47 0.10 1.88 2 80 50 ? 4.95 15.05 1.01 13.13 3 80 77 ? 5.27 28.01 0.75 7.53 4 80 61 ?? 6.51 17.94 0.26 1.89 5 80 66 ? 5.31 20.79 0.89 4.03 6 100 68 ?? 5.96 31.92 0.99 5.78 7 100 50 ? 6.72 28.08 0.79 4.82 ??2 ?a???B????`?? Cmax(??g/mL) AUC0-24(??g・hr/mL) T1/2??(hr) T1/2??(hr) ?t?????? 6.72 28.08 0.79 4.82 ?[?x??????? 6.50 22.77 0.90 2.71 ?R????? ???J?r????g???????2???R????Y 2)??9)?????????u????????418????????????e????????±??Τ??????????? ??3 ?R????????? ?R??????α? ??3 ?R????? ?????? ??????CR??PR??????/??????u?????????? ??????????? ?^?i???? 2),3) (11??27)/90 42.2 ??С?????? 4) (0??9)/22 40.9 ?η?С?????? 4),9) (1??16)/103 16.5 ????? 5) (0??15)/29 51.7 ????? 6) (2??6)/21 38.1 ???z????裩?[?? 6) (6??6)/15 80.0 ?юz?? 7) (4??18)/59 37.3 ??m?i?? 7),8) (8??24)/79 40.5 CR??complete response???????? PR??partial response??????? ?a???a?? 1. ???[?????? (1) ??????[????????Lewis??????K??????[???????B???????δ??????Lu-99???α?????????RERF-LC-AI?????????50???????????????????1??g/mL??????????????A549????????1.6??g/mL??????????μ???????μ??????2?????????6.5??12.5??g/mL??????????in vitro?? (2) ???????????[?????????????ILS???1???????????S???2????±??Τ?????????????in vivo?? ??4 ???????????[???????????????? (3) ??`????????BALB/c-nu/nu??????????????η????6?????^?i??????3???????????1??????m?i????2?????LD50??1/2????29.6mg/kg????g????}??????????????????4???????????1??????m?i????1??????????[???????????????????????in vivo?? 2. ????C?? ????????????????????????????`????λ??Υ????`???????????νY????Ф???????????????????????N??????N?????????????e?壩??????????Τ????????????????`????λ????????????????x?????N???Υ?????N?ˉ仯?????????Υ?????N??DNA??Y????? ???Τ褦????a????????????????νU·??DNA??Y????????νY????DNA???}?u???躦??????????[??????????????????? ????????a????????????????DNA??η???????????Y?ωc???ηN???????????¤??????????_?J???????? 10)?? ?a???a???α? ??4 ???????????[???????????? ???? ?[?? ???????λ?? ??????U· ???ILS????? ????????S????? ????? Lewis??? ?????? ?B?A5??? ????? ??53 2.2??78/35?? ?1??ILS????increased life span??:???????=??(?????????????????????????????????????)/??????????????????????100 ?2??????????S??=???ILS???r?ξt?????/ILS30???r?ξt????? ????????v????????????? ????????? ?????????JAN?? Nedaplatin ??????? cis-Diammineglycolatoplatinum ??????? C2H8N2O3Pt ???????? 303.17 ?????????? ????? ???????????νY????η??????? ????????????????????Ω`??95?????????????`???????????????? ??? ?N?¤?????????k????仯??餤????????_???????J???????? ????S???? 0.006??pH7????????????/???n??? ??? ??????????10mg??1? ??????????50mg??1? ??????????100mg??1? ??????????????????? ????????? ??????????? 1) β????Τ?????????Y????????????????ξ???r??????????B??1992????199201728?? 2) ??????????????????????1992,19(6),863??199200724?? 3) ??????????????????????1992,19(6),871??199200723?? 4) ??????Ф????????????????1992,19(6),879??199200728?? 5) ????F?Ф????????????????1992,19(4),483??199200265?? 6) Akaza,H.et al.??Cancer Chemother.Pharmacol.,1992,31,187??199201900?? 7) ??????????????????????1992,19(5),695??199200340?? 8) ????????????????????????1992,19(6),885??199200727?? 9) Fukuda,M.et al.??Cancer Chemother.Pharmacol.,1990,26,393??199001803?? 10) С?????????????Y?????????????η??????????v????????1993????199302374?? ????????? ??????????d???????Y??????????????????????????? ?c??x?u?a??????? ??a????` ??541-0045 ?????????????????3???1??8?? ??0120-956-734 FAX 06-6202-1541 ?u?????I????????????????????? ?u?????? ?c??x?u?a??????? ??541-0045 ?????????????????3???1??8?? |
2楼2012-09-13 12:27:00