13首届北方药学研究生论坛曾苏ADME在药物研发中作用从成药性评价到新药转化研究.ppt

LLC-PK1/BCRP细胞 +抑制剂 3. CNS BBB P450 UGT Initially, CYP1A2, CYP2B6, and CYP3A should be evaluated in vitro Drug is not an inducer of CYP3A4 then it can be concluded that the test drug is also not an inducer of CYP2C8, CYP2C9, or CYP2C19 Overcoming a Limited Absorption Window Stomach Small Intestine Colon 2 to 4 hours 1 to 6 hours 8 to 18 hours High Capacity Transporter Increased bioavailability Greater dose proportionality Lower inter-patient variability Reduced dosing frequency (sustained release) Modify the drug for recognition by high capacity transporters located throughout the inte