ABSTRACT
Objective:
To compare the antibacterial activity of domestic and branded
tigecycline with
in vitro pharmacokinetics (PK)/pharmacodynamics (PD) model.
Methods:
The
in vitro PK automatic simulation system PASS400 was used to simulate different doses of
tigecycline administration regimen (100 mg, 1
time/d; 50 mg, 12 h/d; 100 mg, 12 h/d), and to observe domestic and imported
tigecycline time sterilization curve and related pharmacodynamic
parameters of the
drug against the standard
strain of
Escherichia coli (ATCC25922),
carbapenem-resistant
Klebsiella pneumoniae (ATCC BAA-1706) and the clinical
strain of
Acinetobacter baumannii (AB-16703). The GraphPad Prism 7 statistical
software was used to analyze the data.
Results:
Under the condition of simulating different doses of PK, domestic and original
tigecycline had
similar antibacterial effects, but both showed weak antibacterial effects. The
time sterilization curves of the two were almost overlapped, and the maximum
sterilization amount was less than 2 log. Within 24 h, the
bacteria all recovered to the
growth plateau. In the comparison of PD
parameters, the original and domestic
tigecycline (100 mg, 1
time/12 h) had the maximum bactericidal doses of (-1.101±0.147) lg CFU/mL and (-1.105±0.208) lg CFU/mL for
Escherichia coli ATCC25922; the maximum bactericidal capacity for
Klebsiella pneumoniae ATCC BAA-1706 was (-1.999±0.187) lg CFU/mL and (-1.865±0.066) lg CFU/mL; the maximum bactericidal capacity for
Acinetobacter baumannii AB-16703 was (-0.240±0.209) lg CFU/mL and (-0.230±0.187) lg CFU/mL. Under different
dosage regimens, the maximum
sterilization amount against the three
bacteria, the
time required for the
bacteria to regenerate to the initial amount, the 24 h bacterial reduction, and the difference between the area of the
sterilization and recovery
growth curve and the blank control curve were all not statistical significant between the two
drugs ( P>0.05).
Conclusion:
Tigecycline cannot show good antibacterial activity under the conditions of simulating
human drug metabolism in vitro. The original branded
tigecycline and domestic
tigecycline have
similar in vitro PK/PD effects.