Table 4.
Parametera | ROP | 1.03P20k-R26 | 0.99P30k-R | 0.98P40k-R |
---|---|---|---|---|
AUC0–∞ (g · h/L) | 0.160 ± 0.010 | 2.10 ± 0.46 | 5.50 ± 0.74 | 10.4 ± 0.8b |
MRT0–∞ (hours) | 1.08 ± 0.04 | 58.4 ± 8.7 | 89.2 ± 1.3 | 131 ± 6b |
t1/2 (hours)c | 0.577 ± 0.082 | 35.1 ± 15.7 | 66.8 ± 9.0 | 89.2 ± 4.4d |
ka (×10−2)e | 394 | 2.78 | 2.87 | 2.09 |
Cmax (mg/L) | 118 ± 13 | 43.7 ± 4.5 | 86.8 ± 17.1 | 99.4 ± 9.4f |
Tmax (hours) | 0.444 ± 0.192 | 18.7 ± 4.6 | 24.0 ± 0.0 | 30.0 ± 0.0 |
F (%) | 94.1 | 68.9 | 75.4 | 43.9 |
CL/F (L/h per kg) | 0.328 ± 0.020 | 0.025 ± 0.005 | 0.009 ± 0.001 | 0.005 ± 0.001 |
Notes: Calculated by noncompartmental moment analysis assuming first-order elimination;
P < 0.01, compared with 0.99P30k-R;
calculated from the elimination rate constant (λZ) using the formula t1/2 = 0.693/λZ;
P < 0.05, compared with 0.99P30k-R;
estimated as the reciprocal of MAT (MAT = MRTsc – MRTiv);
P > 0.05, compared with 0.99P30k-R.
Abbreviations: AUC, area under the curve; CL, systemic clearance; Cmax, maximal concentration; F, absolute bioavailability; ka, absorption rate constant; mPEG, methoxy-polyethylene glycol; MRT, mean residence time; MRTiv, MRT intravenous; MRTsc, MRT subcutaneous; P, mPEG; R, ROP; ROP, radix ophiopogonis polysaccharide; SD, standard deviation; t1/2, half-life; Tmax, time to maximal concentration.