This is an open-label, randomized, two treatment, two sequences, two periods crossover study, using a crossover 2x2 design, where each subject will be randomly assigned to reference or test formulation, in order to evaluate if both formulations are bioequivalent.
The objective of this study is to confirm if two formulations of rosuvastatin calcium 20 mg tablets are bioequivalent. Test formulation is rosuvastatin calcium 20 mg tablets - manufactured by Laboratorios Phoenix S.A.I.C.F/Argentina for GlaxoSmithKline Brazil Ltda., administration of one single-dose tablet. Reference formulation is rosuvastatin calcium 20 mg tablets (Crestor® 20 mg - AstraZeneca do Brasil Ltda.), administration of one single-dose tablet. Sixty-four healthy volunteers, of both genders, with age ranging from 18 and 50 years old, will receive test or reference formulation under fasting conditions, according to the randomization list. In each period, after administration of medication, blood samples are collected at the following times: 0:00 (prior to administration), 0:30, 1:00, 1:30, 2:00, 2:20, 2:40: 3:00, 3:20, 3:40, 4:00, 4:20, 4:40, 5:00, 5:30, 6:00, 7:00, 8:00, 10:00, 12:00, 24:00, 36:00, 48:00 and 72:00 hours. The comparative bioavailability of formulations is evaluated based on relevant pharmacokinetic parameters for statistical comparison. Such parameters are obtained directly from the determination of the drug active principle plasmatic concentration, based on the application of a non-compartmental pattern for the evaluation of these concentrations after the drug oral administration.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
60
Reference formulation is rosuvastatin calcium tablets, 20mg, currently commercialized by AstraZeneca do Brasil Ltda., under the trademark Crestor®
Test formulation is rosuvastatin calcium tablets, 20 mg, produced by Laboratorios Phoenix S.A.I.C.F/Argentina for GlaxoSmithKline Brasil Ltda.
GSK Investigational Site
Bragança Paulista, São Paulo, Brazil
Area Under the Curve 0-t (AUC)
Drug concentration area under the curve versus time, calculated by trapezoidal methods of time 0 to time t, where t is the time related to the last drug concentration, experimentally determined above the Quantification Limit (QL).
Time frame: Collections points from time 0 to 72 hours after the drug administration, evaluated in two periods.
Area Under the Curve 0-infinite (AUC)
Drug concentration area under the curve versus time, (time 0) infinite-extrapolated, where AUC\[0-infinite\] = AUC\[0-t\] + Ct/k, where Ct is the last drug concentration, experimentally determined (above the quantification limit) in that k is the terminal phase clearance constant.
Time frame: Collections points from time 0 to 72 hours after the drug administration, evaluated in two periods.
Half Life (T1/2)
Half life is calculated as ln(2) / k
Time frame: Collections points from time 0 to 72 hours after the drug administration, evaluated in two periods.
Maximum concentration (Cmax)
Maximum concentration reached after drug administration
Time frame: Collections points from time 0 to 72 hours after the drug administration, evaluated in two periods.
Time to Cmax (Tmax)
Time to obtain the maximum concentration
Time frame: Collections points from time 0 to 72 hours after the drug administration, evaluated in two periods.
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