Table 5.
Pharmacokinetic parameters of WV, SVMPs and SVSPs following intramuscular injection in G3.
| Blood Absorption | |||
|---|---|---|---|
| Parameter | WV | SVMP | SVSP |
| Administration route | I.M. | I.M. | I.M. |
| Dose (mg) | 9.65 (±0.17) | 2.47 (±0.44) | 3.53 (±0.06) |
| tz (h) | 8.90 (±5.37) | 9.00 (±5.20) | 9.00 (±5.20) |
| ʎz (1/h) | 0.03 (±0.03) | 0.05 c | 0.07 (±0.08) |
| t1/2 (h) | 37.96 (±34.52) | 14.50 c | 32.16 (±37.26) |
| tmax (h) | 2.40 (±0.79) | 5.5 (±5.68) | 2.67 (±0.58) |
| Cmax (ng/mL) | 31.57 (±17.30) | 1.42 (±0.78) | 17.25 (±11.55) |
| CL/F (l/h) | 14.19 (±11.39) | 91.53 c | 18.13 (±18.10) |
| AUC 0-t (ng × h/mL) | 156.45 (±53.29) | 6.61 (±2.50) | 69.23 (±15.50) |
| AUC 0-∞ (ng × h/mL) | 1006.90 (±823.01) | 26.43 c | 390.17 (±393.58) |
| AUMC (ng × h2/mL) | 76,644.93 (±96,707.77) | 624.10 c | 29,250.31 (±39,833.31) |
| MRT (h) | 55.36 (±50.80) | 23.61 c | 47.79 (±53.88) |
| Vss (l) | 496.26 (±90.33) | 2161.29 c | 379.04 (±112.4) |
| Vz/F (l) | 493.32 (±83.19) | 1914.45 c | 354.86 (±135.38) |
| F0-t | 0.30 (±0.03) | 0.07 (±0.03) | 0.08 (±0.02) |
| F0-∞ | 1.94 (±1.56) | 0.28 c | 0.46 (±0.46) |
| Lymphatic Absorption | |||
| Venom in lymph (mg) | 0.187 (±0.08) | 0.01 (±0.006) | 0.05 (±0.02) |
| F(lymph) 0-t | 0.02 (±0.01) | 0.004 (±0.003) | 0.01 (±0.01) |
| Total Absorption | |||
| F total 0-t | 0.32 (±0.11) | 0.074 (±0.03) | 0.10 (±0.02) |
tz, time of last analytically quantifiable concentration; ʎz, terminal rate constant; t1/2 terminal half-life; tmax, time to reach maximal concentration; Cmax, maximum concentration; CL/F, apparent total plasma or serum clearance of drug after extravascular administration; AUC 0-t,area under the concentration-time curve from zero up to a definite time; AUC 0-∞, area under the concentration-time curve from zero to infinite; AUMC, area under the first moment of the concentration-time; MRT, mean residence time; Vss, apparent volume of distribution at equilibrium determined after intravenous administration; Vz/F, apparent volume of distribution during terminal phase after extravascular administration; F0-t, fraction of the administered dose systemically available between time zero and a definite time; F0-∞, fraction of the administered dose systemically available between time zero and infinity. The PK parameters were calculated from the data from the three sheep that make up each group.