Abstract: There is a wide inter-individual response to statin therapy including rosuvastatin calcium
(RC), and it has been hypothesized that genetic differences may contribute to these variations.
In fact, several studies have shown that pharmacokinetic (PK) parameters for RC are affected
by race. The aim of this study is to demonstrate the interchangeability between two generic
RC 20 mg film-coated tablets under fasting conditions among Mediterranean Arabs and to compare
the pharmacokinetic results with Asian and Caucasian subjects from other studies. A single oral
RC 20 mg dose, randomized, open-label, two-way crossover design study was conducted in 30
healthy Mediterranean Arab volunteers. Blood samples were collected prior to dosing and over a 72-h
period. Concentrations in plasma were quantified using a validated liquid chromatography tandem
mass spectrometry method. Twenty-six volunteers completed the study. Statistical comparison
of the main PK parameters showed no significant difference between the generic and branded
products. The point estimates (ratios of geometric mean %) were 107.73 (96.57–120.17), 103.61
(94.03–114.16), and 104.23 (94.84–114.54) for peak plasma concentration (Cmax), Area Under the Curve
(AUC)0!last, and AUC0!¥, respectively. The 90% confidence intervals were within the pre-defined
limits of 80%–125% as specified by the Food and Drug Administration and European Medicines
Agency for bioequivalence studies. Both formulations were well-tolerated and no serious adverse
events were reported. The PK results (AUC0!last and Cmax) were close to those of the Caucasian
subjects. This study showed that the test and reference products met the regulatory criteria for
bioequivalence following a 20 mg oral dose of RC under fasting conditions. Both formulations also
showed comparable safety results. The PK results of the test and reference in the study subjects
fall within the acceptable interval of 80%–125% and they were very close to the results among
Caucasians. These PK results may be useful in order to determine the suitable RC dose among Arab
Mediterranean patients.

Title

Sci Pharm

Publisher

MDPI

Publisher Country

Switzerland

Indexing

Thomson Reuters

Impact Factor

1.07

Publication Type

Both (Printed and Online)

Volume

84

Year

2016

Pages

536-546