Abstract:

AIM: To study human bioequivalence between atorvastatin tablets and original preparation Lipitor. METHODS: Sixty-four healthy subjects participated in the fasting test and 64 healthy subjects participated in the postprandial test. Both were designed using a randomized two-way crossover study. They were orally administered with 10 mg of the test preparation or reference preparation. The plasma concentration of atorvastatin and its two active metaboliteswere determined by LC-MS/MS. By means of WinNonlin 7.0 software, pharmacokinetic parameters were calculated.RESULTS:The pharmacokinetic parameters for atorvastatin of the two preparations under fasting condition were as follow: C _max of test and reference preparations were （4.31±2.24）, （4.64±2.73） ng/mL, T _max were （0.58±0.36）, （0.58±0.35） h，t _1/2 were （9.10±2.67）, （9.16±3.13） h，AUC _0-t were （23.79±10.73）,（21.93±9.29） ng·h·mL ^-1，AUC _0-∞ were （24.87±10.88）, （23.04±9.29） ng·h·mL ^-1. The pharmacokinetic parameters for atorvastatin of the two preparations under fed condition were as follow: C _max of test and reference preparations were（2.41±1.37）,（2.39±1.21） ng/mL，Tmax were （2.38±1.43）,（2.15±1.54） h，t _1/2 were （10.86±8.77）,（9.59±2.81） h，AUC0-t were （19.03±9.26）, （19.25±9.20） ng·h·mL ^-1，AUC _0-∞ were （20.25±9.30）, （20.39±9.27） ng·h·mL ^-1. CONCLUSION: The atorvastatin calcium test formulation and the reference formulation were both bioequivalent in both fasting and postprandial conditions.

Key words: atorvastatin, ortho-hydroxy atorvastatin, para-hydroxy atorvastatin, bioequivalence