TABLE 4.
Pharmacokinetic parameters of jatrorrhizine.
Route of administration | Inclusion of drug components | Species | Dose | Pharmacokinetic parameters | References |
---|---|---|---|---|---|
Oral | Jiaotai Pills extracts | Rat (brain) | 300 mg/kg Rhizoma Coptidis extracts and 4.7 mg/kg cinnamon oil (equivalent to 15.52 mg/kg dose of jatrorrhizine) | Tmax = 2.17 ± 1.11 min | Zhang et al. (2018) |
T1/2 = 2.89 ± 1.76 h | |||||
AUC0-t = 16.96 ± 1.57 ng h−1·mL−1 | |||||
AUC0-∞ = 24.45 ± 1.73 ng h−1·mL−1 | |||||
Ke = 0.98 ± 1.79 h−1 | |||||
Cmax = 5.56 ± 2.40 ng/ml | |||||
Insomnic rat (brain) | Tmax = 2.13 ± 1.03 min | ||||
T1/2 = 6.35 ± 2.25 h | |||||
AUC0-t = 34.26 ± 7.03 ng h−1·mL−1 | |||||
AUC0-∞ = 43.53 ± 6.13 ng h−1·mL−1 | |||||
Ke = 0.21 ± 0.16 h−1 | |||||
Cmax = 8.74 ± 2.68 ng/ml | |||||
Oral | Jiaotai Pills extracts | Rat (plasma) | 300 mg/kg Rhizoma Coptidis extracts and 4.7 mg/kg cinnamon oil (equivalent to 15.52 mg/kg dose of jatrorrhizine) | Tmax = 5.25 ± 2.22 min | He et al. (2014a) |
T1/2 = 3.88 ± 1.46 h | |||||
AUC0-t = 10.36 ± 4.28 ng h−1·mL−1 | |||||
AUC0-∞ = 11.11 ± 4.63 ng h−1·mL−1 | |||||
Ke = 0.20 ± 0.08 h−1 | |||||
Cmax = 1.04 ± 0.67 ng/ml | |||||
Insomnic rat (plasma) | Tmax = 0.53 ± 0.30 min | ||||
T1/2 = 8.94 ± 15.99 h | |||||
AUC0-t = 9.47 ± 2.25 ng h−1·mL−1 | |||||
AUC0-∞ = 13.22 ± 4.69 ng h−1·mL−1 | |||||
Ke = 0.33 ± 0.20 h−1 | |||||
Cmax = 8.64 ± 2.17 ng/ml | |||||
i.v. | Jatrorrhizine | Rat (plasma) | 0.1 mg/kg | T1/2 = 8.5 ± 2.6 h | Shi et al. (2012) |
AUC0-t = 7.6 ± 2.9 μg h−1·L−1 | |||||
AUC0-∞ = 9.6 ± 3.6 μg h−1·L−1 | |||||
Vd = 188.9 ± 121.7 L/kg | |||||
CL = 11.6 ± 3.8 L/h/kg | |||||
MRT0-t = 5.7 ± 2.3 h | |||||
0.3 mg/kg | T1/2 = 10.6 ± 5.4 h | ||||
AUC0-t = 29.9 ± 13.1 μg h−1·L−1 | |||||
AUC0-∞ = 32.1 ± 13.4 μg h−1·L−1 | |||||
Vd = 149.9 ± 74.4 L/kg | |||||
CL = 10.6 ± 3.9 L/h/kg | |||||
MRT0-t = 8.3 ± 4.2 h | |||||
3 mg/kg | T1/2 = 8.9 ± 2.2 h | ||||
AUC0-t = 307.8 ± 85.9 μg h−1·L−1 | |||||
AUC0-∞ = 308.9 ± 85.7 μg h−1·L−1 | |||||
Vd = 137.0 ± 57.5 L/kg | |||||
CL = 10.3 ± 2.8 L/h/kg | |||||
MRT0-t = 8.8 ± 1.4 h | |||||
Oral | San-Huang decoction | Rabbit (plasma) | 7.67 ml/kg (equivalent to 7.13 mg/kg dose of jatrorrhizine) | Tmax = 0.50 ± 0 h | Liu et al. (2011) |
T1/2 = 18.12 ± 4.74 h | |||||
AUC0-∞ = 1,099.54 ± 292.67 h ng/ml | |||||
Cmax = 71.30 ± 7.72 ng/ml | |||||
Oral | Coptis–evodia powder (6:1, g/g) | Rat (plasma) | 1.086 g/kg (equivalent to 14.4 mg/kg dose of jatrorrhizine) | Tmax = 90 ± 0 min | Deng et al. (2008) |
T1/2 = 325.3 ± 8.0 min | |||||
AUC0-∞ = 43,576.9 ± 4,767.8 ng min/ml | |||||
Cmax = 219.9 ± 12.8 ng/ml | |||||
Oral | Coptis Root extract | Rat (plasma) | 800 mg/kg | Tmax = 0.67 ± 0.23 h | Zhao et al. (2018) |
T1/2 = 8.6 ± 2.61 h | |||||
AUC0-t = 7.5 ± 0.87 ng h/mL | |||||
AUC0-∞ = 8.6 ± 0.80 ng h/mL | |||||
Cmax = 3.12 ± 0.84 ng/ml | |||||
Shuanghua Baihe tables powder | 3.13 g/kg | Tmax = 4.2 ± 0.53 h | |||
T1/2 = 11.1 ± 2.06 h | |||||
AUC0-t = 7.7 ± 2.02 ng h/mL | |||||
AUC0-∞ = 11.8 ± 3.06 ng h/mL | |||||
Cmax = 1.53 ± 0.20 ng/ml | |||||
Oral | Coptidis Rhizoma extract | Rat (plasma) | 0.0650 g/200 g | Cmax = 33.35 ± 5.82 μg/L | Sun et al. (2018) |
AUC0-tn = 96.58 ± 21.69 ug/L h | |||||
MRT0-tn = 6.14 ± 0.30 h | |||||
VRT0-tn = 15.45 ± 1.26 h2 | |||||
JinQi Jiangtang tablets | 0.4536 g/200 g | Cmax = 11.35 ± 2.48 μg/L | |||
AUC0-tn = 279.70 ± 83.40 ug/L h | |||||
MRT0-tn = 5.08 ± 0.42 h | |||||
VRT0-tn = 24.55 ± 5.42 h2 | |||||
Oral | Coptidis Rhizoma powder | Rat (plasma) | 1.08 g/kg | Tmax = 0.75 ± 0.11 h | Yan et al. (2012) |
T1/2 = 7.1 ± 6.4 h | |||||
AUC0-t = 123.1 ± 31.1 μg/L·h | |||||
AUC0-∞ = 128.9 ± 37.4 μg/L·h | |||||
MRT0-t = 3.5 ± 0.8 h | |||||
MRT0-∞ = 4.9 ± 3.8 h | |||||
Cmax = 82.09 ± 17.44 μg/L | |||||
Zoujinwan | Rhizoma coptidis powder 1.08 g/kg and Evodia rutaecarpa powder 0.18 g/kg | Tmax = 1.50 ± 0.89 h | |||
T1/2 = 8.0 ± 3.7 h | |||||
AUC0-t = 107.9 ± 50.8 μg/L·h | |||||
AUC0-∞ = 113.8 ± 48.1 μg/L·h | |||||
MRT0-t = 4.3 ± 0.9 h | |||||
MRT0-∞ = 5.9 ± 3.0 h | |||||
Cmax = 39.63 ± 13.35 μg/L |
Tmax: the time of maximum plasma concentration; T1/2: the elimination half-life; AUC: area under the concentration-time curve; Cmax: maximum plasma concentration; Ke: eliminate rate constant; Vd: apparent volume of distribution; CL: clearance; MRT: mean residence time; VRT: the variance of residence time.