A Phase Ⅰb Study of Remimazolam Tosylate in Healthy Volunteers

Hengrui Medicine

Status and phase: Completed; Phase 1

Conditions: Anesthesia

Treatments: Drug: Remimazolam Tosylate

Study type: Interventional

Funder types: Industry

Identifiers

NCT03444480

RMZL-PIb

Details and patient eligibility

About

The purpose of this study is to evaluate the Pharmacokinetics/Pharmacodynamics and safety of Remimazolam Tosylate in healthy volunteers after loading/maintenance dose regimen.

Full 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.

Enrollment: 8 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: Double Blind

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8 participants in 2 patient groups

Remimazolam Tosylate 1

Experimental group

Description:

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

Treatment:

Drug: Remimazolam Tosylate

Remimazolam Tosylate 2

Experimental group

Description:

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

Treatment:

Drug: Remimazolam Tosylate