Table 1.
Pharmacokinetic parameters of nirmatrelvir in the blood and brain after nirmatrelvir (15 mg/kg, i.v.) administration compared with those after nirmatrelvir (15 mg/kg, i.v.) and nirmatrelvir (15 mg/kg, i.v.) + Scutellaria formula NRICM101 (3 g/kg, p.o. for five days) (n = 6), nirmatrelvir (15 mg/kg, i.v.) + Scutellaria formula JGF (0.3 g/kg, p.o. for five days) (n = 6), and nirmatrelvir (15 mg/kg, i.v.) + Scutellaria formula ZYF (3 g/kg, p.o. for five days) (n = 6) administration in male rats.
| Parameter | nirmatrelvir (15 mg/kg, i.v.) |
nirmatrelvir (15 mg/kg, i.v.) + NRICM101 (3 g/kg, p.o. for five days) |
nirmatrelvir (15 mg/kg, i.v.) + JGF (0.3 g/kg, p.o. for five days) |
nirmatrelvir (15 mg/kg, i.v.) + ZYF (3 g/kg, p.o. for five days) |
||||
|---|---|---|---|---|---|---|---|---|
| blood | brain | blood | brain | blood | brain | blood | brain | |
| AUClast (min μg/mL) | 798.3 ± 58.56 | 187.2 ± 23.46 | 1297 ± 91.80a | 207.7 ± 32.38 | 1543 ± 153.0a | 171.7 ± 45.41 | 1467 ± 61.83a | 111.6 ± 6.50 |
| Cmax (μg/mL) | 27.39 ± 4.03 | 2.60 ± 0.36 | 57.90 ± 9.14 | 2.32 ± 0.32 | 53.38 ± 9.59 | 1.95 ± 0.43 | 60.74 ± 7.52 | 1.30 ± 0.21 |
| t1/2, α (min) | 16 ± 3 | – | 12 ± 2 | – | 13 ± 2 | – | 14 ± 3 | – |
| t1/2, β (min) | 47 ± 7 | – | 38 ± 4 | – | 62 ± 23 | – | 47 ± 15 | – |
| t1/2 (min) | 23 ± 4 | 55 ± 5 | 17 ± 2 | 71 ± 4 | 23 ± 5 | 76 ± 9 | 18 ± 3 | 83 ± 6 |
| Tmax (min) | – | 20 ± 0 | – | 36 ± 3 | – | 27 ± 6 | – | 30 ± 4 |
| CL (mL/min/kg) | 2.64 ± 2.38 | – | 11.98 ± 1.04a | – | 10.25 ± 0.91a | – | 10.33 ± 0.44a | – |
| MRT (min) | 42 ± 6 | 79 ± 7 | 34 ± 3 | 96 ± 3 | 42 ± 9 | 98 ± 10 | 30 ± 3 | 107 ± 11 |
| AUCtissue/AUCblood | – | 0.24 ± 0.02 | – | 0.17 ± 0.01b | – | 0.13 ± 0.02b | – | 0.08 ± 0.002b |
| AUCherb/AUCnirmatrelvir | – | – | 1.62 ± 0.12 | 1.1 ± 0.17 | 1.93 ± 0.19 | 0.92 ± 0.24 | 1.84 ± 0.15 | 0.60 ± 0.03 |
The data are expressed as the means ± S.E.M.s (n = 6). NRICM101, JGF and ZYF represent the herbal formulas Scutellaria formula JGF, Scutellaria formula JGF and Scutellaria formula ZYF, respectively. The AUCbrain/AUCblood represents the maternal blood-to-tissue transfer ratio. AUCherb/AUCnirmatrelvir represents nirmatrelvir (15 mg/kg, i.v.) administered alone compared with nirmatrelvir (15 mg/kg, i.v.) plus three Scutellaria formula group ratios. a: p < 0.05 compared with blood in the nirmatrelvir (15 mg/kg, i.v.) group, as determined by one-way ANOVA with Tukey's HSD post hoc test. b: p < 0.05 compared with brain tissue in the nirmatrelvir (15 mg/kg, i.v.) group, as determined by one-way ANOVA with Tukey's HSD post hoc test.