Food does not affect the pharmacokinetics of solifenacin, a new muscarinic receptor antagonist: results of a randomized crossover trial.

AIM

To determine the effect of food ingestion on the pharmacokinetic profile of solifenacin succinate (YM905; Vesicare, a new bladder selective muscarinic receptor antagonist for the treatment of overactive bladder, a chronic disease usually caused by involuntary detrusor muscle contractions during bladder filling.

METHODS

A randomized, two-period, crossover study in two groups of 12 healthy men (aged 18-45 years, body weight 60-100 kg, body mass index < or =30). A single 10-mg dose of solifenacin was administered to the first group in the fasting state during period 1 and in the fed state during period 2, and to the second group in the fed state during period 1 and in the fasting state during period 2 (10 mg is two times the suggested starting dose). There was a 14-day washout between treatment periods. Parameters obtained included C(max), AUC(last), and AUC(0-inf), as well as t(1/2), t(max), and t(lag).

RESULTS

One subject withdrew during the first period for personal reasons. No statistically or clinically significant pharmacokinetic differences occurred between subjects in the fed and fasting states. All geometric mean ratios were close to 1 (C(max), 1.033; AUC(last), 1.068; AUC(0-inf), 1.040). The 90% confidence intervals (CIs) fell in the predefined no-food-effect boundaries of 0.8-1.25 (C(max), 0.953-1.120; AUC(last), 0.990-1.153; AUC(0-inf), 0.976-1.109). The mean difference in t(1/2) was -3.8 h (90% CI 7.6-0.0). There were no significant differences between the fed and fasting states with regard to t(max) and t(lag) (P > 0.05).

CONCLUSIONS

The pharmacokinetics of oral solifenacin was not affected by food ingestion, suggesting that this drug may be administered with or without food. The results observed in this investigation are consistent with those of previous studies of solifenacin.