ADME

Model In-vitro model for metabolic stability
Test System Human Liver Microsomes, S9, Hepatocytes 
Species Rodent & Non-rodent (as per request)
Quantitation method   HPLC-UV or LC/MS/MS
Positive control Suitable substrate 
Deliverables Parent compound loss, in-vitro half life
Model In-vitro model for matrix stability
Test System Plasma, serum, blood, CSF, Tissue, aqueous buffers 
Quantitation method   HPLC-UV or LC/MS/MS
Deliverables Parent compound loss, in-vitro half life
Model In-vitro model for cytochrome P450 Inhibition 
Test System Human Liver Microsomes or recombinant enzymes
Quantitation method   HPLC-UV or LC/MS/MS or Fluorescence reader 
Positive control Suitable substrate 
End Point Metabolite formation
Deliverables Percent inhibition, IC50 determination
Model In-vitro model for drug-drug or herb-drug interaction 
Test System Human Liver Microsomes or recombinant enzymes
Method Co-incubation of herb-drug or drug-drug with CYP enzymes
Quantitation method   HPLC-UV or LC/MS/MS or Fluorescence reader 
End Point Metabolite formation
Deliverables Percent inhibition, IC50 determination, Drug interaction potential
Model In-vitro model for CYP450 Reaction Phenotyping 
Test System Human Liver Microsomes or recombinant enzymes
Quantitation method   HPLC-UV or LC/MS/MS or Fluorescence reader 
Method Selective inhibitor for CYP450 – to determine cytochrome P450 involved in metabolism
End Point Metabolite formation
Model In-vitro model for CYP450 Induction 
Test System Human Hepatocytes, Cell line (LS180)
Quantitation method   LC/MS/MS & RT-PCR
Positive Control Suitable Substrate
Method Determination of enzyme activity and m-RNA levels
End Point Metabolite formation
Model In-vitro model for Plasma Protein Binding 
Test System Plasma, serum, whole blood, purified proteins (Albumin, AGP)
Species Rodent and non-rodent (as per request)
Quantitation method   LC/MS/MS or HPLC-UV 
Method Rapid equilibrium dialysis (RED), Ultrafiltration
Deliverables Percent protein binding
Model In-vitro model for metabolite ID/profiling 
Test System Human Liver Microsomes, S9, Hepatocytes
Species Rodent and non-rodent (as per request)
Quantitation method   LC/MS/MS or HPLC-UV 
Deliverables Metabolite identification/profiling based of m/z found, mass difference from parent compound, possible addition or deletion 
Model In-vitro model for determination of Blood to plasma ratio 
Test System Whole Blood & Plasma
Species Rodent and non-rodent (as per request)
Quantitation method   LC/MS/MS or HPLC-UV 
Deliverables Blood to plasma ratio 
Model In-vitro model for permeability & Efflux (Caco-2 & MDCK) 
Test System Caco-2, MDCK cell lines
Method Unidirectional or bidirectional
Quantitation method   LC/MS/MS or HPLC-UV 
Deliverables Permeability Coefficient, Efflux ratio 
Model In-vitro model for Dermal Absorption/penetration 
Test System Rat Skin, Human skin, artificial membranes
Quantitation method   LC/MS/MS or HPLC-UV 
Deliverables Permeability Coefficient (Kp), Flux