The objective of this study was to compare the pharmacokinetic profiles of the test product, 300 mg trazodone hydrochloride (HCl) extended-release caplets (containing Contramid®), when administered as a single dose, and the reference product, 100 mg trazodone HCl immediate-release tablets (Apotex Corp), when administered three times daily. For this purpose the rate and extent of absorption of trazodone and formation of m-chlorophenylpiperazine (mCPP) after administration of the two formulations, were compared under fasting conditions.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
26
Dosage form: Extended-release caplets containing 300 mg trazodone HCl Dose: 300 mg trazodone HCl extended-release caplets (one caplet) at 23:30 on Day 1 of the test product treatment period following a fasting period of at least 4 hours.
Dosage form: Immediate-release tablets containing 100 mg trazodone HCl Dose: 100 mg trazodone HCl immediate-release tablets (one tablet per dosing time) at 23:30 on Day 1, at 07:30 and 15:30 on Day 2 of the reference product treatment period.
Bioequivalence Based Cmax
Cmax = Maximum plasma concentration. Measured in nanogram per milliliter (ng/mL).
Time frame: 68 hours
Bioequivalence Based on AUC(0-tlast)
AUC(0-tlast) = Area under the plasma concentration curve (AUC) vs (versus) time data pairs, where tlast is the time of the last quantifiable concentration. Measured in nanogram x hours per milliliter (ng\*h/mL).
Time frame: 68 hours
Bioequivalence Based on AUC(0-∞)
AUC(0-∞) = Area under the plasma concentration curve vs time data pairs, with extrapolation to infinity (∞). Measured in nanogram x hours per milliliter (ng\*h/mL).
Time frame: 68 hours
Area Under the Plasma Concentration vs. Time Data Pairs, for the First 24 Hours [AUC(0-24)]
Time frame: 24 hours
Time to Maximum Plasma Concentration (Tmax)
Time frame: 68 hours
Apparent Terminal Elimination Rate Constant (λz)
The elimination rate constant of trazodone (Lamda z). It is the ratio of clearance to volume of distribution and is expressed in units of 1/hour. This constant is used in half-life calculations.
Time frame: 68 hours
Apparent Terminal Half-life (t½.z)
The elimination half-life (T½z) of trazodone in plasma (time it takes for the concentration of trazodone to fall to half), expressed in hours.
Time frame: 68 hours
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.