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.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
64
succesfule screened subject, take single dose of 15mg Tolvaptan tablet with no feeding.
succesfule screened subject, take single dose of 30mg Tolvaptan tablet with no feeding.
succesfule screened subject, take single dose of 60mg Tolvaptan tablet with no feeding.
single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
peak concentration (Cmax)
Time frame: 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
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
peak concentration (Cmax)
Time frame: 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.
single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
time to peak (Tmax)
Time frame: 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
Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
area under the drug-time curve (AUC0-t and AUC0-∞)
Time frame: 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
single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
elimination half-life (t1/2)
Time frame: 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
single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
apparent clearance (CL/F)
Time frame: 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
single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
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succesfule screened subject, take single dose of 120mg Tolvaptan tablet with no feeding.
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.
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.
apparent volume of distribution (Vd/F)
Time frame: 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
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
time to peak (Tmax)
Time frame: 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
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
area under the drug-time curve (AUC0-t and AUC0-∞)
Time frame: 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
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
elimination half-life (t1/2)
Time frame: 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
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
apparent clearance (CL/F)
Time frame: 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
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
apparent volume of distribution (Vd/F)
Time frame: 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