A Simple Method for Assessing Free Brain/Free Plasma Ratios Using an In Vitro Model of the Blood Brain Barrier
Figure 2
Free brain and plasma concentrations - time profile of three commercial compounds.
Sulpiride (A), Risperidone (B), Clozapine (C) and 3 proprietary compounds (D, E and F) determined by brain microdialysis and compared with free brain concentrations obtained by multiplying the free plasma concentration from the microdialysis experiment with Cu,b/Cu,p ratios obtained in vitro using the in vitro BBB model. Free plasma concentration at earlier time point than 1 hour were used together with in vitro Cu,br/Cu,pl ratio at 1 h and microdialysis plasma concentration data at 2 hours and beyond were multiplied by the in vitro steady state ratio to simulate the microdialysis profile. Values for drugs are defined in Table 2 and values for proprietary compounds in Table 3.