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Following oral administration, A-58632 readily appeared in plasma where very high concentrations were detected. As dose increased, both Cmax and AUCinf increased almost dose proportionally: dose ratio was 1:10, Cmax ratio was 1:6.97, and AUC ratio was 1:8.72. Cmax at the nominal dose of 30 and 300 mg/kg was 2,563 and 17,867 ng/mL, which corresponds to a total concentration of 5.87 and 40.9 ¦ÌM. A-58632 was 88.4 and 88% bound at 1 and 10 ¦Ìg/mL concentrations. Using these data the free plasma concentration (Cmax) was calculated as approximately 0.68 and 4.91 ¦ÌM at nominal dose of 30 and 300 mg/kg. ¼Ó´Ö²¿·Ö²»¶®£¬boundºÍfreeÔÚÕâÀïÊDZíʾʲôÒâ˼£¿£¿ ![]() ![]() |
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