Pharmacokinetic Comparison of Sustained- and Immediate-Release Oral Formulations of Cilostazol in Healthy Korean Subjects: A Randomized, Open-Label, 3-Part, Sequential, 2-Period, Crossover, Single-Dose, Food-Effect, and Multiple-Dose Study

Lee, Donghwan; Lim, Lay Ahyoung; Jang, Si‐Hyong; Lee, Yoon Jung; Chung, Jae Yong; Choi, Jong Rak; Kim, Kiyoon; Park, Jin Woo; Yoon, Hosang; Lee, Jae Yong; Park, Min Soo; Park, Kyungsoo

doi:10.1016/j.clinthera.2011.10.024

Cited by 16 publications

(27 citation statements)

References 24 publications

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“…[8,9] Cilostazol was reported to exhibit diurnal variation, which is characterized by the peak concentration that is higher after the morning dose than after the evening dose. [8,10] and the trough concentration that is higher before the morning dose than before the evening dose. [8][9][10] The pharmacodynamics (PD) of cilostazol in Korean populations has been assessed by the inhibition of platelet aggregation, [11,12] which is based on Light Transmittance Aggregometry (LTA).…”

Section: Introductionmentioning

confidence: 89%

“…[8,10] and the trough concentration that is higher before the morning dose than before the evening dose. [8][9][10] The pharmacodynamics (PD) of cilostazol in Korean populations has been assessed by the inhibition of platelet aggregation, [11,12] which is based on Light Transmittance Aggregometry (LTA). Although LTA has been considered to be the gold standard assay for the assessment of platelet functions, it has problems such that the technique is affected by pre-analytical and procedural conditions and highly skillful and experienced laboratory staff is needed.…”

Section: Introductionmentioning

confidence: 89%

“…[10] Note, however, that, in the cited work, only PK was reported as PD was not the main objective of the study.…”

Section: Study Design and Datamentioning

confidence: 99%

“…[9] The half-life of cilostazol is governed by "flip-flop" kinetics with the absorption rate constant slower than the elimination rate constant. [9,10] Cilostazol is extensively bound primarily to albumin. [9] Food significantly increases the bioavailability of cilostazol [10] but age and gender have no effect on cilostazol PK.…”

Section: Introductionmentioning

confidence: 99%

“…[9,10] Cilostazol is extensively bound primarily to albumin. [9] Food significantly increases the bioavailability of cilostazol [10] but age and gender have no effect on cilostazol PK. [8,9] Cilostazol was reported to exhibit diurnal variation, which is characterized by the peak concentration that is higher after the morning dose than after the evening dose.…”

Section: Introductionmentioning

confidence: 99%

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Population pharmacodynamics of cilostazol in healthy Korean subjects

Jung

Chae

Park

2018

Transl Clin Pharmacol

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Section: Introductionmentioning

confidence: 89%

Section: Introductionmentioning

confidence: 89%

“…[10] Note, however, that, in the cited work, only PK was reported as PD was not the main objective of the study.…”

Section: Study Design and Datamentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Population pharmacodynamics of cilostazol in healthy Korean subjects

Jung

Chae

Park

2018

Transl Clin Pharmacol

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Pharmacokinetic and Safety Comparison of Fixed‐Dose Combination of Cilostazol/Rosuvastatin (200 + 20 mg) Versus Concurrent Administration of the Separate Components in Healthy Adults

Kim,

Hong,

Jung

et al. 2024

Clinical Pharm in Drug Dev

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The combined cilostazol and rosuvastatin therapy is frequently used for coronary artery disease treatment. This open‐label, 3 × 3 crossover clinical trial evaluated the pharmacokinetics and safety of a fixed‐dose combination (FDC) of cilostazol/rosuvastatin (200 + 20 mg) versus a concurrent administration of the separate components (SCs) under both fasted and fed conditions. Among 48 enrolled healthy adults, 38 completed the study. Participants were administered a single oral dose of cilostazol/rosuvastatin (200 + 20 mg), either as an FDC or SCs in a fasted state, or FDC in a fed state, in each period of the trial. Blood samples were taken up to 48 hours after dosing, and plasma concentrations were analyzed using validated liquid chromatography‐tandem mass spectrometry. The geometric mean ratios of FDC to SCs for area under the plasma concentration‐time curve from time zero to the last quantifiable concentration (AUClast) and maximum plasma concentration (Cmax) were 0.94/1.05 and 1.06/1.15 for cilostazol and rosuvastatin, respectively (AUClast/Cmax). Compared with that during fasting, fed‐state administration increased the AUClast and Cmax for cilostazol by approximately 72% and 160% and decreased these parameters for rosuvastatin by approximately 39% and 43%, respectively. To conclude, the FDC is bioequivalent to the SCs, with notable differences in pharmacokinetics when administered in a fed state. No significant safety differences were observed between the treatments.

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