Food effect on meal administration time of pharmacokinetic profile of cilostazol, a BCS class II drug

Abstract

1. Cilostazol (CLZ) is categorized as a biopharmaceutical classification system (BCS) class II drug. CLZ suspensions of jet-milled particles were orally administered to beagle dogs in fasted and fed states, for which food was given 0.5 h before the experiment.

2. The mean highest concentration of CLZ (C_max) and the area under the serum concentration–time curve (AUC_t) fed/fasted ratios were 2.90 and 2.85, respectively, indicating a large and variable food effect. Additionally, CLZ was administered to the same dogs at 2 and 4 h after food or 0.5 h before food. The serum concentrations of CLZ were similar when dosed 0.5 and 2 h after food; however, they were significantly lower when dosed 4 h after food but still greater compared with the fasted state.

3. Furthermore, the ratio of fed/fasted in AUC_t was better correlated than that in C_max. Additionally, the serum concentrations were similar to the fasted states when CLZ was dosed 0.5 h before food.

4. Therefore, the results of this study showed that the serum concentration–time profile of CLZ was significantly affected by the timing of food administration, and that a good correlation was observed between food administration time and the C_max and AUC_t fed/fasted ratios.

Keywords:

• Food effect
• food administration time
• cilostazol
• beagle dog
• BCS class II

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.