Determination of the metabolite
pharmacokinetic parameters (Cont'd)

4- Fraction of the parent drug dose converted to a particular metabolite, fm

After iv administration of the parent drug the metabolite AUC is dependent on the amount of metabolite formed and the total body clearance of the metabolite, CLT(m).

AUC(m) =

fm D

CLT (m)

The fraction fm can be determined after administration of the parent drug only if the metabolite total body clearance is known.

If CLT(m) is not known, it can be determined after administration of the preformed metabolite. The CLT(m) of the metabolite formed in vivo after administration of the parent drug is equal to the CLT(m) determined after administration of the preformed metabolite.

a- The CLT(m) can be determined after administration of the preformed metabolite as described before.

b- The metabolite AUC is calculated after administration of the parent drug.

c- Using the metabolite AUC, CLT(m) and the parent drug dose, fm can be calculated from the equation mentioned above.