A Phase Ⅰa Study of Remimazolam Tosylate in Healthy Volunteers

Study Overview
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Brief Summary
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The purpose of this study is to evaluate and compare the Pharmacokinetics/Pharmacodynamics and safety of Remimazolam Tosylate with midazolam in healthy volunteers

Official Title
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A Placebo- and Midazolam-Controlled, Phase Ia, Single Ascending-Dose Study Evaluating the Safety, Pharmacokinetics, and Pharmacodynamics of Remimazolam Tosylate

Conditions
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Healthy

Intervention / Treatment
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* Drug: Remimazolam Tosylate
* Drug: Midazolam


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Healthy males or females Weight range 50 to 100 kg inclusive Body mass index (BMI) 18 to 26 kg/m2 Exclusion Criteria: Has a known sensitivity to benzodiazepines, flumazenil, or anesthetic agents, or a medical condition such that these agents are contraindicated With evidence of uncontrolled renal, hepatic, central nervous system, respiratory, cardiovascular, or metabolic dysfunction, in the opinion of the investigator or medical monitor Has known or suspected history of alcoholism or drug abuse or misuse within 6 months of Screening or evidence of tolerance or physical dependence before dosing with study drug 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) Pregnant,lactating Mallampati score ≥3

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 55 Years

Sexes Eligible for Study
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All

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Treatment
Allocation: Randomized
Intervention Model: Parallel Assignment
Masking: Double


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: 1.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.01 mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Experimental: 2.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.02 mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Experimental: 3.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.05 mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Experimental: 4.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.075 mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Experimental: 5.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.1 mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Experimental: 6.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.15 mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Experimental: 7.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.2 mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Experimental: 8.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.25 mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Experimental: 9.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.3mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Experimental: 10.Remimazolam Tosylate<br>Single IV bolus of Remimazolam Tosylate over 1 minute at 0.35 mg/kg body weight | Drug: Remimazolam Tosylate<br> <br> |
| Active Comparator: 11.Midazolam<br>Single IV bolus of Midazolam over 1 minute at 0.075 mg/kg body weight | Drug: Midazolam<br> <br> |

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| To study the Pharmacokinetics of Remimazolam Tosylate by assessment of drug concentration through blood sample analysis |  | Pre-dose to 8 hours post-dosee | 
| Bispectral index (BIS) and Modified Observer's Assessment of Alertness/Sedation(MOAA/S) score assessments |  | Pre-dose to 2 hours post-dose | 
| Adverse event；Vital sign；Physical examination；Laboratory examination；ECG；The nervous system function test |  | Pre-dose to 24 hours post-dose | 

 Terms related to the study
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Keywords Provided by Centre Hospitalier Valida
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Remimazolam Tosylate, Phase Ⅰ study, Health