A Single-center, Open-label, Randomized, Two-stage, Two-way Crossover Study to Evaluate the Differences in Pharmadynamics, Pharmacokinetics, and Safety Between Ciprofol and Propofol at Different Doses in Healthy Subjects

Haisco Pharmaceutical Group Co., Ltd.1 site in 1 country18 target enrollmentMay 26, 2020

ConditionsAnesthesia

InterventionsCiprofol Propofol

Overview

Phase: Phase 1
Intervention: Ciprofol
Conditions: Anesthesia
Sponsor: Haisco Pharmaceutical Group Co., Ltd.
Enrollment: 18
Locations: 1
Primary Endpoint: Safety by measurement of Adverse Events
Status: Completed
Last Updated: 5 years ago

Overview Investigators Eligibility Criteria Arms & Interventions Outcomes Sites Similar Trials

Overview

Brief Summary

This is a single-center, open-label, randomized, two-stage, two-way crossover Phase I study in healthy male subjects.The main objective is to evaluate the differences in pharmadynamics (PD), pharmacokinetics (PK), and safety between ciprofol injectable emulsion and propofol injectable emulsion at different doses in healthy subjects.

Registry

clinicaltrials.gov

Start Date

May 26, 2020

End Date

September 18, 2020

Last Updated

5 years ago

Study Type

Interventional

Study Design

Crossover

Sex

Male

Investigators

Sponsor

Haisco Pharmaceutical Group Co., Ltd.

Responsible Party

Sponsor

Eligibility Criteria

Inclusion Criteria

•Healthy adult males, aged 18-45 years (inclusive);
•Body weight ≥ 50 kg, body mass index (BMI) between 18-26 kg/m\^2 (inclusive);
•Blood pressure between 90-140/50-90 mmHg (inclusive); heart rate between 60-100 bpm (inclusive); body temperature between 35.4-37.5°C (inclusive); respiratory rate between 12-20 breaths per min (inclusive); SpO2 when inhaling ≥ 92%;
•Normal results of physical examination, laboratory tests (routine blood, routine urine, blood biochemistry (including hepatic function, renal function, blood glucose, and electrolytes such as Na, K, and Mg), and blood coagulation), 12-lead ECG, and abdominal ultrasonography, or abnormalities considered by the investigators to be clinically insignificant; no significant potential difficult airway (modified Mallampati score Class I-II);
•No previous history of primary diseases in major organs, such as liver, kidneys, digestive tract, blood, and metabolic diseases; no history of malignant hyperthermia and other hereditary disorders; no history of mental/neurological disorders; no history of epilepsy; no contraindications for deep sedation/general anesthesia; no clinically significant history of anesthesia accidents;
•Subjects must understand the procedures and methods of this study, and be willing to signing the informed consent form and to complete the trial in strict accordance with clinical trial protocol;

Exclusion Criteria

•Patients with known allergies to ciprofol injectable emulsion, excipient in propofol injectable emulsion (soybean oil, glycerin, triglyceride, egg lecithin, sodium oleate, and sodium hydroxide); history of drug allergies (including other anesthetics), allergic diseases, or hyperactive immune response;
•Patients receiving any of the following drugs or therapies prior to screening/administration:
•History of drug abuse within 3 months prior to screening, or positive result in urine drug screening during baseline period;
•Participated in other drug/medical device trials within 3 month prior to screening;
•Serious infection, trauma, or major surgery within 4 weeks prior to screening.
•Acute disease with clinical significance (determined by the investigators) within 2 weeks prior to screening, including GI diseases or infections (such as respiratory tract or CNS infections);
•Patients who received propofol, other sedatives/anesthetics, and/or opioid analgesics within 1 week prior to administration;
•Patients who received prescription drugs, Chinese herbal medicines, over-the-counter drugs, or food supplements (such as vitamins and calcium supplements) other than contraceptives, paracetamol, oral non-steroidal anti-inflammatory drugs, and topical over-the-counter preparations, within 2 weeks prior to administration; those who received UGT or CYP2B6 inhibitors within 7 days prior to administration (refer to Attachment 6 for prohibited drugs); patients can only be enrolled when the principal investigator (PI) and the sponsor agree that the medication has no effect on the safety and PK/PD results of the trial;
•Patients with history or evidence of any of the following diseases prior to screening/administration:
•History of cardiovascular diseases, such as postural hypotension, severe arrhythmia, heart failure, Adams-Stokes syndrome, unstable angina, myocardial infarction within 6 months before screening, tachycardia/bradycardia requiring medications, third-degree atrioventricular block, or QTcF interval ≥ 450 ms (per Fridericia's correction formula);

Arms & Interventions

Ciprofol

First-stage: 0.4mg/kg, 0.6 mg/kg, 0.8 mg/kg Second-stage: 0.4mg/kg, 0.6 mg/kg, 0.8 mg/kg

Intervention: Ciprofol

Propofol

First-stage: 2.0mg/kg, 3.0 mg/kg, 4.0 mg/kg Second-stage: 2.0mg/kg, 3.0 mg/kg, 4.0 mg/kg

Intervention: Propofol

Outcomes

Primary Outcomes

Safety by measurement of Adverse Events

Time Frame: First dose of study drug on day 1

Bispectral index （BIS）

Time Frame: From first dose of study drug until fully alert on day 1

Modified observer's assessment of alertness/sedation（MOAA/S）

Time Frame: From first dose of study drug until fully alert on day 1

Observe the change of modified observer's assessment of alert /sedation during the whole trial

Secondary Outcomes

volume of distribution (Vz)(First dose of study drug on day 1)
Terminal half-life (t1/2)(First dose of study drug on day 1)
time to peak concentration (Tmax)(First dose of study drug on day 1)
clearance (CL)(First dose of study drug on day 1)
mean residence time (MRT)(First dose of study drug on day 1)
Peak concentration (Cmax)(First dose of study drug on day 1)
Area under the plasma concentration versus time curve (AUC)(First dose of study drug on day 1)