A Phase Ⅰb Study of Remimazolam Tosylate in Healthy Volunteers
- Registration Number
- NCT03444480
- Lead Sponsor
- Jiangsu HengRui Medicine Co., Ltd.
- Brief Summary
The purpose of this study is to evaluate the Pharmacokinetics/Pharmacodynamics and safety of Remimazolam Tosylate in healthy volunteers after loading/maintenance dose regimen.
- Detailed Description
1. Study the Pharmacokinetics/Pharmacodynamics of Remimazolam Tosylate in healthy volunteers after loading/maintenance dose regimen.
2. Study the reversal effect and time required of Flumazepine on Rimazolam'effect.
3. Study the Safety of Remimazolam Tosylate in healthy volunteers after loading/maintenance dose regimen.
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 8
Inclusion Criteria
- Aged ≥18 and ≤55 years.
- Weight range 50 to 100 kg and body mass index (BMI) 18 to 26 kg/m2.
- Willing and able to comply with the requirements of the protocol.
- Provide written informed consent to participate in the study.
Exclusion Criteria
- Abnormal results of physical or laboratory examination with clinical significance
- With a history of laboratory results that show the presence of hepatitis B surface antigen (HBs Ag), hepatitis C antibody (HCV Ab), or human immunodeficiency virus (HIV).
- With evidence of uncontrolled renal, hepatic, central nervous system, respiratory, cardiovascular, or metabolic dysfunction, in the opinion of the investigator or medical monitor.
- Subject with clinically significant abnormalities in baseline 12-lead electrocardiogram (ECG) or vital signs（SBP <90 mmHg or >140 mmHg，DBP <50 mmHg or >90 mmHg；Hr <50 bpm or >100 bpm；SpO2 <95%）.
- Has a known sensitivity to benzodiazepines, flumazenil, or anesthetic agents, or a medical condition such that these agents are contraindicated.
- Receipt of other medication within 14 days of the first study day.
- Blood donation greater than 200 ml or participation in a clinical study of an unlicensed drug in the previous 3 months.
- History of smoking or alcohol abuse within 6 months of screening.
- History of grapefruit juice or any other foods affect the activity of cytochrome P450 3A4（CYP3A4） within 7 days of screening.
- Pregnant,lactating.
- Mallampati score ≥3.
- Patients who in the opinion of the investigator may not be able to comply with the requirements of the study are not eligible
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description Remimazolam Tosylate 1 Remimazolam Tosylate IV bolus of Remimazolam Tosylate with a loading dose of 0.4mg/kg body weight over 1 minute followed by a maintenance dose of 1.5mg/kg/h over 2 hours.1 h 55 min after dosing start， 0.5 mg Flumazenil is administered Remimazolam Tosylate 2 Remimazolam Tosylate IV bolus of Remimazolam Tosylate with a loading dose of 0.4mg/kg body weight over 1 minute followed by a maintenance dose of 1.5mg/kg/h over 2 hours.1 h 55 min after dosing start time,0.5ml placebo is administered
- Primary Outcome Measures
Name Time Method Area under the plasma concentration versus time curve (AUC) of Remimazolam in human plasma. From prior to study drug injection until 4 hours post-dose Peak Plasma Concentration (Cmax) of M01 in human plasma. From prior to study drug injection until 4 hours post-dose M01 is the main metabolite of Remimazolam
Area under the plasma concentration versus time curve (AUC) of M01 in human plasma. From prior to study drug injection until 4 hours post-dose M01 is the main metabolite of Remimazolam
Peak Plasma Concentration (Cmax) of Remimazolam in human plasma. From prior to study drug injection until 4 hours post-dose
- Secondary Outcome Measures
Name Time Method Safety by measurement of Adverse Events. From start of study drug injection to patient discharge (approx. 2 days)
Trial Locations
- Locations (1)
Peking Union Medical College Hospital
🇨🇳Beijing, Beijing, China