This is a phase 1 randomized, double blind, crossover study examining the pharmacokinetic profile of two different doses of minoxidil sublingual tablets in healthy adult volunteers. The main objective is to determine the pharmacokinetics of minoxidil following sublingual administration of a single dose in adult male and female healthy volunteers. The secondary objective is to evaluate the safety of minoxidil following sublingual administration of a single dose in adult male and female healthy volunteers. A total of 12 participants (6 male and 6 female) will be recruited for study participation. The duration of study participation is up to 43 days including screening and safety follow up. A single dose of study medication (strength A or strength B) will be administered on Day 1 to all study participants and PK samples will be taken periodically over a 12-hr period. After at least 7-day washout period the other dose of study medication (strength B or strength A, respectively) will be administered to all participants and PK samples will be taken periodically over a 12-hr period.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
TRIPLE
Enrollment
12
One single dose of Strength A sublingual minoxidil
One single dose of Strength B sublingual minoxidil
Dr Rodney Sinclair Pty Ltd
East Melbourne, Victoria, Australia
Area under the concentration-time profile (AUClast, AUCinf) of sublingual minoxidil
The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). AUClast measures the total minoxidil exposure in the body up to the last measurable time point, while AUCinf estimates total minoxidil exposure from the time it's taken until it completely leaves the body.
Time frame: At Day 1 and Day 8
Maximum observed concentration (Cmax) of sublingual minoxidil
The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). Cmax is the highest concentration of minoxidil in the blood after it's taken.
Time frame: At Day 1 and Day 8
Time of maximum observed concentration (Tmax) of sublingual minoxidil
The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). Tmax measures the time it takes for minoxidil to reach its highest concentration in the blood after it's taken.
Time frame: At Day 1 and Day 8
Terminal rate constant (λz) of sublingual minoxidil
The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). The terminal rate constant measures the speed at which the concentration of minoxidil decreases in the blood during the last stage of elimination.
Time frame: At Day 1 and Day 8
Terminal half-life (T½) of sublingual minoxidil
The primary endpoints will be the area under the concentration-time curve from time zero to the last measurable concentration (AUClast), the area under the concentration-time curve from time zero to infinity (AUCinf), maximum concentration (Cmax), time to maximum concentration (Tmax), half-life (T1/2), and the terminal rate constant (λz). The terminal half-life measures the time it takes for the concentration of minoxidil in the blood to decrease by half during the last stage of elimination.
Time frame: At Day 1 and Day 8
Type of adverse events
The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.
Time frame: At Day 1, Day 8, and Day 15
Incidence of Adverse Events
The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.
Time frame: At Day 1, Day 8, and Day 15
Relationship of adverse events to study drug
The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.
Time frame: At Day 1, Day 8, and Day 15
Severity of adverse events
The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.
Time frame: At Day 1, Day 8, and Day 15
Change from baseline in clinical safety monitoring parameters
The safety profile of sublingual minoxidil will be evaluated by analyzing the type, incidence, relationship to study drug and severity of adverse events for each dose of sublingual minoxidil. It will also be evaluated through the change from baseline in clinical safety monitoring parameters, including clinical laboratory tests, vital signs, and ECG.
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Time frame: At Day 1, Day 8, and Day 15