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Background:

Pharmacokinetic parameters are usually determined by analysis of drug concentrations in plasma what could be misleading if drug distribution differs between blood and plasma. Therefore, in vitro blood partitioning represents an important DMPK property used for better interpretation and understanding of PK properties of tested compound.

Blood partitioning of the tested compound could be concentration- and time-dependent, involving both passive diffusion, protein binding and/or active transporters.
   Assay description

   Fresh blood source
mouse (CD1, Balb/c), rat (SD), human

   Compound concentration
500 ng/ml  (0.5% MeOH)

   Compound requirements
1-2 mg of dry matter

   Incubation details
1h at 37ºC
number of replicates: 3

   Assay controls
verapamil, chloroquine (Figure 1 and 2)

   Detection method
LC-MS/MS with internal standard

   Results
blood to plasma ratio

Assay details adjustable to client’s and/or project specific requests
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