Table 2 Main PK parameters of SHR8554 in plasma after a single intravenous pump infusion of 1 mg SHR8554 and combined administration with Itraconazole in healthy subjects.

From: Exploring Pharmacokinetic interactions between SHR8554, a µ-opioid receptor biased agonist, and Itraconazole in healthy Chinese subjects

Parameters (unit)

Groups

Monotherapy

Combination therapy

Cmax (ng/mL)

16.69 ± 3.48 (20.9)

16.58 ± 8.79 (53.0)

Tmax* (h)

0.16 (0.0828, 0.1678)

0.22 (0.1636, 0.7489)

AUC0–t (ng∙h/mL)

18.10 ± 3.60 (19.9)

19.58 ± 3.51 (17.9)

AUC0−∞ (ng∙h/mL)

18.37 ± 3.61 (19.7)

19.91 ± 3.59 (18.0)

AUC0 − 4 h (ng∙h/mL)

11.42 ± 2.19 (19.2)

10.97 ± 2.25 (20.5)

AUC0 − 6 h (ng∙h/mL)

13.23 ± 2.56 (19.4)

12.96 ± 2.45 (18.9)

AUC0–12 h (ng∙h/mL)

15.59 ± 3.05 (19.6)

15.92 ± 2.89 (18.1)

AUC0–24 h (ng∙h/mL)

17.26 ± 3.40 (19.7)

18.34 ± 3.26 (17.8)

T1/2z (h)

9.28 ± 3.13 (33.7)

8.81 ± 2.06 (23.4)

Vz (L)

751.35 ± 315.01 (41.9)

653.26 ± 185.56 (28.4)

CLz (L/h)

56.41 ± 11.00 (19.5)

51.77 ± 9.27 (17.9)

λz (/h)

0.09 ± 0.04 (46.7)

0.08 ± 0.02 (26.0)

MRT0–t (h)

5.10 ± 0.95 (18.6)

6.23 ± 1.43 (23.0)

MRT0−∞(h)

5.95 ± 1.50 (25.2)

7.08 ± 1.96 (27.7)

AUC_%Extrap(%)

1.51 ± 0.98 (65.0)

1.63 ± 1.00 (61.5)

  1. *Median (minimum, maximum) was used for Tmax and other parameters were described as Mean ± SD(%CV). Cmax, peak concentration; Tmax, peak time; λz, terminal elimination rate constant; T1/2, terminal elimination half-life; AUC0 − t, area under the curve from 0 to the last detectable time; AUC0−∞, area under the curve from 0 to infinite time; CLz, apparent clearance rate; Vz, apparent distribution volume; MRT0 − t , mean residence time from time 0 to the last detectable time; MRT0−∞, mean residence time from time 0 to infinite time; AUC%Extrap, the extrapolated percentage of AUC0−∞.
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