Key result
Once-daily sustained-release cilostazol matches steady-state exposure of twice-daily immediate-release formulation.
Why the study?
A new extended-release formulation of cilostazol was recently developed, necessitating comparison of its pharmacokinetic characteristics with the immediate-release formulation.
Does cilostazol 200 mg sustained-release once daily provide comparable pharmacokinetics to cilostazol 100 mg immediate-release twice daily in healthy male volunteers?
RCT (n=30)
Open-label
randomized
Does cilostazol 200 mg sustained-release once daily provide comparable pharmacokinetics to cilostazol 100 mg immediate-release twice daily in healthy male volunteers?
Cilostazol 200 mg sustained-release once daily provides comparable systemic exposure to cilostazol 100 mg immediate-release twice daily at steady state.
Answers are grounded in this paper and cite their sources.
Supports once-daily cilostazol for adherence; leaves open clinical outcome equivalence versus twice-daily dosing.
BACKGROUND: A new extended-release form of cilostazol has recently been developed. This study was conducted to compare the pharmacokinetic characteristics of sustained-release (SR) and immediate-release (IR) formulations of cilostazol after multiple oral doses in healthy male Korean volunteers. METHODS: This was an open-label, randomized, multiple-dose, crossover study conducted in 30 healthy Korean subjects. In each treatment period, subjects received oral doses of 200 mg SR formulation every 24 hours or 100 mg IR formulation every 12 hours for 5 consecutive days in a fed state, with a washout period of 9 days. The plasma concentrations of cilostazol and its metabolites were determined using a validated liquid chromatography-tandem mass spectrometry method. The area under the plasma concentration-time curve within a dosing interval (AUC T ), the measured peak plasma concentration at steady state (C max,ss), and the time to reach C max,ss (t max,ss) were analyzed using a noncompartmental method. RESULTS: A total of 24 healthy male subjects completed the study. The mean (standard deviation [SD]) AUC T (96-120 hours) values for SR and IR were 27,378.0 (10,301.6) ng·h/mL and 27,860.3 (7,152.3) ng·h/mL, respectively. The mean (SD) C max,ss values were 2,741.4 (836.0) ng/mL and 2,051.0 (433.2) ng/mL, respectively. The median t max,ss values were 8.0 hours and 4.0 hours, respectively. The geometric mean ratios (90% confidence intervals) of the SR to IR formulations were 0.937 (0.863-1.017), 0.960 (0.883-1.043), and 0.935 (0.859-1.017) for AUC T and 0.644 (0.590-0.703), 0.586 (0.536-0.642), and 0.636 (0.577-0.702) for dose-normalized C max,ss of cilostazol, OPC-13015 (3,4-dehydro-cilostazol), and OPC-13213 (4'-trans-hydroxyl-cilostazol), respectively. All formulations were well tolerated. CONCLUSION: At steady state, the AUC T of cilostazol SR 200 mg is comparable to that of cilostazol IR 100 mg twice a day in healthy male Korean subjects. Both formulations are well tolerated.
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Kim et al. (2015) conducted an RCT in Healthy volunteers (n=30). Sustained-release cilostazol vs. Immediate-release cilostazol 100 mg every 12 hours was evaluated on Area under the plasma concentration-time curve within a dosing interval (AUC T) (Geometric mean ratio 0.937, 95% CI 0.863-1.017). Sustained-release cilostazol 200 mg once daily demonstrated comparable steady-state AUC to immediate-release 100 mg twice daily (geometric mean ratio 0.937; 90% CI 0.863-1.017).
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