PHARMACOKINETICS OF BACAMPICILLIN AND BACMECILLINAM IN PLASMA AND PERIPHERAL LYMPH
- T Bergan
- A Engeset
- W Olszewski
- R Solberg
The pharmacokinetics of tablets containing equimolar amounts of bacampicillin and bacmecillinam totalling 500 mg were studied in healthy volunteers. Bacampicillin and bacmecillinam are prodrugs which hydrolyse completely upon absorption to give ampicillin and mecillinam respectively. The concentrations of ampicillin and mecillinam were determined in serum, peripheral lymph and urine. Both substances were found to invade lymph more slowly than serum and also to remain in the former somewhat longer. There were also longer lag time values for lymph than for serum, lasting 0. 7 hours for both compounds after the first dose and 0.5 hours after the 7th dose. The elimination half-life was around one hour for both antibiotics and sites, the individual values usually longer for lymph than for serum. After 7 doses, the levels were of the same order as after one dose. The peak concentrations in lymph were approximately half of those in serum and appeared somewhat later than in serum. The mean (± SD) curve peaks in lymph for ampicillin were 2.3 ± 0.7 and 2.1 ± 0.4 µg/ml after the first and 7th doses. The corresponding values for mecillinam were 1.6 ± 0.6 and 1.5 ± 0.2 µg/ml. For ampicillin, the areas under the serum curves were 40- 50 percent higher than under the lymph curves, whereas the areas were smaller, although similar, for mecillinam in both types of specimens. The ratio of ampicillin to mecillinam was close to the optimal for antibacterial in vitro synergistic activity in serum, lymph, and urine. Penetration into the lymph was satisfactory. This is significant, since lymph levels reflect concentrations obtainable in unmanipulated tissues, which may become infected. Consequently, the design of the fixed combination of equimolecular quantities bacampicillin and bacmecillinam seems suitable from a pharmacokinetic point of view.
How to Cite:
Bergan, T. & Engeset, A. & Olszewski, W. & Solberg, R., (1979) “PHARMACOKINETICS OF BACAMPICILLIN AND BACMECILLINAM IN PLASMA AND PERIPHERAL LYMPH”, Lymphology 12(2), p.85-94.