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. Author manuscript; available in PMC: 2020 Jul 1.
Published in final edited form as: Mol Pharm. 2019 May 30;16(7):3024–3039. doi: 10.1021/acs.molpharmaceut.9b00263

Table 2.

Pharmacokinetic Parameters of IV- or SC-Delivered FAF–Rapa Analyzed Using Compartmental Analysis and Noncompartmental Analysis (Mean ± SD)

route of administration
parameter (unit) IV SC IV SC
preferred model one compartment three compartments noncompartment
AUC (μM·hr) 141 ± 16 92 ± 19 207 ± 33 109 ± 14
AUMC (μM·hr2) - - 2207 ± 344 2214 ± 328
F (%) 100 65.5 ± 13.2 100 52.7 ± 6.7
CL (mL/h) 0.15 ± 0.01 0.15a 0.10 ± 0.01 0.09 ± 0.01
CL/F (mL/h) 0.15 ± 0.01 0.23 ± 0.04 0.10 ± 0.01 0.18 ± 0.03
Vd (mL) 1.46 ± 0.2 1.46a 0.88 ± 0.1 0.85 ± 0.1
Cmax (μM) 13.4 ± 2.4 3.3 ± 0.1 11.7 ± 2.9 4.4 ± 0.7
Tmax (hr) 0.0 12.4 ± 0.7 0.0 12.0
MRT (hr) - - 10.7 ± 0.3 20.3 ± 1.1
MAT (hr) - - - 9.6 ± 1.1
Tl/2,absorption (hr) - 4.2 ± 0.4 - -
Tl/2,elimination (hr) 6.9 ± 0.5 6.9a 6.2 ± 0.4 6.4 ± 0.7
kabsorption (hr−1) - 0.16b - -
kelimination (hr−1) 0.10 ± 0.01 0.10a 0.11 ± 0.01 0.11 ± 0.01
kdegradation (hr−1) - 0.09 ± 0.05 - -
a

Compartmental values from IV analysis were adopted to estimate other SC parameters.

b

To fit the observed time to peak concentration, the assumption was required that kabsorption = kinjection siteinterstitial = kinterstitial fluidsystemic circulation.