TABLE 3.
Primary pharmacodynamics parameters and mathematical quality of respective nonlinear regressions obtained from the dose-response relationships of the different animal modelsa
| Bacterial pathogen | Model | M:C ratio | Meropenem formb | Emax (mean Δlog10 CFU/g at 24 h ± SEM) | BD (mean mg/kg/day ± SEM) | N (mean Hill's slope ± SEM) | PDP with multicollinearity | P value (CFA) | T>MIC for BD (%) |
|---|---|---|---|---|---|---|---|---|---|
| P. aeruginosa GRP-0019 | Mouse thigh | 1:0 | iMer | NSc | NS | 0.769 ± 0.287 | All | NAd | NA |
| gMer-B | NS | NS | 0.673 ± 0.242 | All | |||||
| gMer-C | NS | NS | 0.645 ± 0.252 | All | |||||
| P. aeruginosa GRP-0019 | Mouse thigh | 1:0 | iMer | 6.358 ± 0.202 | 105.50 ± 8.07 | 2.079 ± 0.297 | None | 0.3220 | 67.9 |
| gMer-A | 6.028 ± 0.160 | 121.20 ± 7.36 | 2.948 ± 0.463 | None | 76.3 | ||||
| P. aeruginosa GRP-0019 | Mouse thigh | 1:1 | iMer | 5.929 ± 0.267 | 33.26 ± 2.53 | 3.025 ± 0.713 | None | 0.4150 | 19.5 |
| gMer-A | 6.480 ± 0.267 | 37.65 ± 2.34 | 2.243 ± 0.351 | None | 21.3 | ||||
| P. aeruginosa GRP-0019 | Mouse thigh | 1:3 | iMer | 6.935 ± 0.196 | 44.57 ± 2.32 | 1.861 ± 0.199 | None | 0.2310 | 23.8 |
| gMer-A | 7.019 ± 0.236 | 47.12 ± 2.55 | 1.520 ± 0.158 | None | 24.7 | ||||
| P. aeruginosa GRP-0049 | Mouse thigh | 1:1 | iMer | 6.836 ± 0.532 | 85.74 ± 5.17 | 1.303 ± 0.166 | Emax, BD | NA | NA |
| gMer-A | 6.465 ± 0.187 | 62.62 ± 2.31 | 1.857 ± 0.154 | None | 18.7 | ||||
| P. aeruginosa GRP-0049 | Mouse thigh | 1:3 | iMer | 5.827 ± 0.164 | 60.60 ± 3.03 | 3.290 ± 0.472 | None | 0.9863 | 18.2 |
| gMer-A | 5.797 ± 0.151 | 59.65 ± 2.79 | 3.529 ± 0.480 | None | 18.0 | ||||
| P. aeruginosa GRP-0049 | Mouse thigh | 1:5 | iMer | 5.812 ± 0.187 | 54.66 ± 3.22 | 3.102 ± 0.502 | None | 0.9661 | 16.8 |
| gMer-A | 5.904 ± 0.177 | 54.47 ± 2.98 | 3.225 ± 0.493 | None | 16.8 | ||||
| P. aeruginosa GRP-0019 | Mouse brain | 1:0 | iMer | 6.482 ± 0.212 | 66.25 ± 7.19 | 1.444 ± 0.236 | None | 0.0020 | 31.5 |
| gMer-B | 6.931 ± 0.295 | 58.88 ± 7.56 | 1.167 ± 0.235 | None | 28.7 | ||||
| gMer-C | 5.900 ± 0.104 | 44.29 ± 3.35 | 3.140 ± 0.415 | None | 23.7 | ||||
| P. aeruginosa GRP-0019 | Mouse brain | 1:0 | iMer | 6.427 ± 0.520 | 41.07 ± 4.07 | 0.689 ± 0.179 | All | NA | NA |
| gMer-A | 5.916 ± 0.318 | 44.03 ± 5.15 | 1.115 ± 0.279 | Emax, BD | NA | ||||
| P. aeruginosa GRP-0019 | Mouse brain | 1:1 | iMer | 7.164 ± 0.207 | 50.21 ± 2.81 | 0.846 ± 0.105 | None | NA | 25.7 |
| gMer-A | 6.605 ± 0.167 | 60.73 ± 4.37 | 1.279 ± 0.173 | Emax, N | NA | ||||
| P. aeruginosa GRP-0019 | Mouse brain | 1:3 | iMer | 6.537 ± 0.168 | 81.94 ± 6.86 | 2.057 ± 0.245 | None | <0.0001 | 41.5 |
| gMer-A | 7.279 ± 0.167 | 120.20 ± 5.80 | 1.709 ± 0.125 | None | 75.8 | ||||
| P. aeruginosa GRP-0049 | Mouse brain | 1:1 | iMer | 5.874 ± 0.2373 | 121.6 ± 10.7 | 3.676 ± 0.827 | None | NAe | NA |
| gMer-A | 6.311 ± 0.3355 | 96.11 ± 9.67 | 2.164 ± 0.4129 | None | 25.0 | ||||
| P. aeruginosa GRP-0049 | Mouse brain | 1:3 | iMer | 6.498 ± 0.113 | 87.64 ± 3.92 | 1.797 ± 0.126 | None | 0.0002 | 23.5 |
| gMer-A | 6.498 ± 0.363 | 136.80 ± 13.3 | 1.599 ± 0.246 | None | 32.4 | ||||
| K. pneumoniae GRP-0107 | Mouse lung | 1:0 | iMer | NS | NS | 0.722 ± 0.288 | All | NA | NA |
| gMer-A | NS | NS | 0.784 ± 0.259 | All | NA | ||||
| K. pneumoniae GRP-0107 | Mouse lung | 1:0 | iMer | 5.577 ± 0.310 | 13.91 ± 2.46 | 0.843 ± 0.166 | None | 0.1265 (iMer vs gMer-B)f | 92.9 |
| gMer-B | 5.764 ± 0.526 | 26.69 ± 6.10 | 0.771 ± 0.182 | Emax, BD | NA | ||||
| gMer-C | 5.906 ± 0.913 | NS | 0.614 ± 0.195 | All | NA | ||||
| K. pneumoniae GRP-0107 | Mouse lung | 1:3 | iMer | 5.916 ± 0.614 | 5.37 ± 1.25 | 0.875 ± 0.386 | Emax, N | NA | NA |
| gMer-A | 6.774 ± 0.955 | 9.89 ± 1.37 | 0.780 ± 0.237 | All | NA | ||||
| K. pneumoniae GRP-0107 | Mouse lung | 1:5 | iMer | 5.137 ± 0.260 | 9.05 ± 1.04 | 1.719 ± 0.453 | None | NA | 85.0 |
| gMer-A | NS | NS | 0.395 ± 0.152 | All | NA | ||||
| P. aeruginosa GRP-0019 | Guinea pig soleus | 1:0 | iMer | 6.485 ± 0.094 | 11.53 ± 0.40 | 3.331 ± 0.351 | None | <0.0001 | NDg |
| gMer-A | 6.642 ± 0.345 | 21.60 ± 2.55 | 1.444 ± 0.274 | None | ND | ||||
| P. aeruginosa GRP-0019 | Guinea pig soleus | 1:0 | iMer | 6.463 ± 0.184 | 10.99 ± 1.10 | 1.438 ± 0.257 | None | <0.0001f | ND |
| gMer-B | 6.349 ± 0.162 | 11.75 ± 0.99 | 1.503 ± 0.239 | None | ND | ||||
| gMer-C | 7.238 ± 0.466 | 25.12 ± 2.84 | 1.082 ± 0.197 | Emax | ND |
The ranges of the adjR2 and Sy|x were 0.7 to 0.988 and 0.222 to 0.624, respectively (data not shown).
gMer-A, generic product Vitalis; gMer-B, generic product Procaps; gMer-C, generic product Farmioni.
NS, not significant.
NA, not applicable. Statistical comparison of this regression was not possible due to serious multicollinearity of the PDP in one or both products.
*, in this instance in which this parameter was not applicable, violation of normality and homoscedasticity assumptions (iMer) prevented statistical comparison.
In this experiment, a formal statistical comparison was indicated because only one product had multicollinearity and it was mild (highest VIF, <7.0).
ND, not done.