Health Subjects
Conditions
Brief summary
Tolvaptan oral administraction phase I PK clinical trial. Two groups of healthy male subjects. One group receives single dose of Tolvaptan. The other group receives multi dose of Tolvaptan.
Interventions
DRUGsinge dose 15mg
succesfule screened subject, take single dose of 15mg Tolvaptan tablet with no feeding.
DRUGsingle dose 30mg
succesfule screened subject, take single dose of 30mg Tolvaptan tablet with no feeding.
DRUGsingle dose 60mg
succesfule screened subject, take single dose of 60mg Tolvaptan tablet with no feeding.
DRUGsingle dose 120mg
succesfule screened subject, take single dose of 120mg Tolvaptan tablet with no feeding.
DRUGmulti dose 30mg
radomize 24 healthy adult male to 2 groups, 12 subjects each. One group take 30mg Tolvaptan. First day, with no feeding, take single 30mg dose, then start from day 3rd, take medication for 7 days. 8 days treatment in total.
DRUGmulti dose 60mg
radomize 24 healthy adult male to 2 groups, 12 subjects each. One group take 60mg Tolvaptan. First day, with no feeding, take single 60mg dose, then start from day 3rd, take medication for 7 days. 8 days treatment in total.
Sponsors
Chinese Academy of Medical Sciences, Fuwai Hospital
Otsuka Beijing Research Institute
Study design
Allocation
NON_RANDOMIZED
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 40 Years
Healthy volunteers
Yes
Inclusion criteria
1. Healthy male volunteers. 2. Aged 18 to 40 years old. 3. Weight no less than 50kg and within the range of standard weight (body mass index between 19 and 24). 4. Auxiliary examinations: blood routine and coagulation, urine routine, blood biochemistry (total protein, albumin, blood glucose, total bilirubin, AST (GOT), ALT (GPT), ALP, γ-GTP, LDH, CK (CPK), total cholesterol, triglycerides, urea nitrogen, creatinine, uric acid, Na, K, Cl, Mg, Ca, P), hepatitis B surface antigen, hepatitis C antibody, HIV antibody, syphilis antibody, 12-lead electrocardiogram, 24-hour ambulatory electrocardiogram (Holter) examination, all items are normal. 5. Signed the informed consent form.
Exclusion criteria
1. The patient has a history of heart, liver, kidney, digestive tract, metabolic, respiratory, blood, mental, nervous system and other disorders, and the doctor's judgment is not suitable. 2. Hepatitis B virus, syphilis, hepatitis C virus, HIV infection. 3. Patients with a history of clinically significant arrhythmias of various types, including rapid and slow types, such as atrioventricular block, sinus arrest, and supraventricular tachycardia, were assessed by the investigators. 4. He has a history of postural hypotension (blood pressure drop ≥20/10mmHg when he changes from lying position to standing position, accompanied by dizziness and other symptoms), standing dizziness, collapse, fainting, and vertigo. 5. Quiet for more than 3 minutes, sitting pulse below 55 beats/min or more than 90 beats/min. 6. Quiet for more than 3 minutes, sitting systolic blood pressure is lower than 100mmHg or higher than 140mmHg; Diastolic depression of 60mmHg or higher than 90mmHg. 7. Various voiding disorders (frequent urination, or difficulty urinating, etc.). 8. Have a family history of genetic diseases (including a history of genetically predisposed arrhythmias in relatives). 9. A history, allergy or propensity to be allergic to drugs or any other substance. 10. Smokers, alcoholics, or other drug addicts. 11. Physical examination had clinically significant positive findings. 12. People who have donated blood or been sampled as a subject within the last 3 months. 13. People who have taken prophylactic or therapeutic drugs in the last 2 weeks. 14. Otherwise, the clinical trial physician or the clinical trial physician determines that the safety of the trial is affected.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107 | Day 1 pre-dose and post-dose 0.5 hour, 1 ,2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours | area under the drug-time curve (AUC0-t and AUC0-∞) |
| single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107 | Day 1 pre-dose and post-dose 0.5hour, 1 ,2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours | peak concentration (Cmax) |
| multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103 | Day 1 & Day 9 at pre-dose, post-dose 0.5hr, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 (2nd and 10th day) and 48 (day 3rd and 11th). For other dosing day ( day 4 to 8) to collect at pre-dose( 24hr after last dose) point. | peak concentration (Cmax) |
Outcome results
None listed