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

T_max: the time of maximum plasma concentration; T_1/2: the elimination half-life; AUC: area under the concentration-time curve; C_max: maximum plasma concentration; K_e: eliminate rate constant; V_d: apparent volume of distribution; CL: clearance; MRT: mean residence time; VRT: the variance of residence time.