Table 3: In vivo bioavailability of selected oxazolidinones.
Compd.
~ MIC (g/mL) − serum
~ MIC (g/mL) + serum
Dilution factora
~ Compd in serum (g/mL)
Bioavailabilityb
1g
1.1
3.3
1 : 20
22
low
1i
3.3
3.3
0
0
none
1o
0.37
3.3
0
0
none
2b
3.3
3.3
0
0
none
2j
1.1
1.1
0
0
none
2k
1.1
1.1
0
0
none
2l
1.1
0.37
1 : 10
11
low
3a
0.37
1.1
0
0
none
PH-27
1.1
0.37
1 : 80
88
medium
LZD
0.37
0.37
1 : 320
118.4
high
INH
0.014
0.041
1 : 320
4.48
high
aDilution factor represents the last dilution step of the serum samples in which drug activity was still observed in the bioassay. (Drug levels in mouse serum are estimated by multiplying the dilution factor by the MIC value of the drug in absence of serum).
bRating of bioavailability: low: activity of drug can be seen in 1 or 2 wells of the bioassay; medium: activity of drug can be seen in 3 or 4 wells of the bioassay; high: activity of drug can be seen in 5 or 6 wells.