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Clinical Trial
. 2021 Nov;38(11):5484-5500.
doi: 10.1007/s12325-021-01914-4. Epub 2021 Sep 24.

Sedation Effects Produced by a Ciprofol Initial Infusion or Bolus Dose Followed by Continuous Maintenance Infusion in Healthy Subjects: A Phase 1 Trial

Chao Hu #  1 , Xiaofeng Ou #  2 , Yi Teng  3 , Shiqing Shu  1 , Ying Wang  1 , Xiaohong Zhu  1 , Yan Kang  4 , Jia Miao  5
Affiliations
Clinical Trial

Sedation Effects Produced by a Ciprofol Initial Infusion or Bolus Dose Followed by Continuous Maintenance Infusion in Healthy Subjects: A Phase 1 Trial

Chao Hu et al. Adv Ther. 2021 Nov.

Abstract

Introduction: The effects of continuous infusions of ciprofol on its pharmacodynamic and pharmacokinetic properties and safety profiles in healthy Chinese subjects were evaluated.

Methods: In this open-label, randomized, two-way cross-over study, subjects received initial doses of continuous ciprofol/propofol as an infusion for 30 min in part 1 (n = 8) and a bolus dose in part 2 (n = 8) followed by maintenance infusions for a total of 4 h in part 1 and 12 h in part 2. Each subject participated in both parts with a washout time of at least 40 h.

Results: The safety and tolerability parameters of ciprofol were similar to those of propofol, and all treatment-emergent adverse events were mild. The incidences of injection pain and respiratory depression in subjects given ciprofol were lower than those receiving propofol. The pharmacokinetic parameters Cmax, tmax, t1/2, λz and MRT for ciprofol and propofol were similar, while CL, Vd and Vss were statistically significantly different. Pharmacodynamic parameters including the Richmond Agitation Sedation Scale and bispectral index profiles of ciprofol were similar to those of propofol.

Conclusion: Ciprofol has potential for clinical application for continuous intravenous infusion to maintain sedation for 12 h with the same safety, tolerability and efficacy as propofol.

Keywords: Ciprofol; Pharmacodynamics; Pharmacokinetics; Propofol; Safety; Sedation.

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Figures

Fig. 1
Fig. 1
Flowchart of the trial
Fig. 2
Fig. 2
Changes of the A, B mean heart rate (HR) C, D mean systolic blood pressure (SBP) and E, F mean saturation of blood oxygen (SpO2) with different time points in eight subjects injected with ciprofol and propofol
Fig. 3
Fig. 3
Change in plasma concentrations of ciprofol and propofol in subjects in the part 1 and part 2 studies. A, B Part 1 study; C, D part 2 study
Fig. 4
Fig. 4
BIS-time profiles and BIS-RASS profiles of ciprofol and propofol in subjects in the part 1 and part 2 studies. A, C, E Part 1 study; B, D, F part 2 study
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