Drug Metabolism in Drug Design and Development Basic Concepts and Practice

TABLE 18.A2 Estimated pharmacokinetic parameters used to calculate radiation absorbed from selected tissues in male Long–Evansrats following a single oral dose of

x

mg/kg dose of radiolabeled test article.

Tissue

AUC

0–

t

(m

g-eq h/g)

AUC

0–

1

(m

g-eq h/g)

C

max

(m

g-eq/g)

Tmax(H)

Half-life

(H)

xy

corr

Coefficient

(terminal phase)

Dose

exposure(m

Ci H)

Radiation

absorbed dose

(mRad or mrem)

a

Adrenal glandBileBloodBoneBone marrowCecumCecum contentsCerebellumCerebrumCerebrospinal fluidDiaphragmEpididymisEsophageal contentsEsophageal mucosaEsophagusExorbital lacrimal glandEyeEye (lens)Fat (abdominal)Fat (brown)xy

correlation; this coefficient predicts the goodness-of-fit for the concentration–time line (theoretical versus observed).

Note

: When AUC

0–

1

is not calculated, AUC

0–

is used to calculate the absorbed dose.t

aCalculated for a 100-

mCi dose of radiolabeled test article in humans.

600