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

Clinical Therapeutics

Volumn 33, Issue 12, 2011, Pages 2038-2053

  Lee, Donghwan ^a   Lim, Lay Ahyoung ^a   Jang, Seong Bok ^a   Lee, Yoon Jung ^a   Chung, Jae Yong ^a   Choi, Jong Rak ^a   Kim, Kiyoon ^b   Park, Jin Woo ^b   Yoon, Hosang ^b   Lee, Jaeyong ^b   Park, Min Soo ^a   Park, Kyungsoo ^a  

^a Yonsei University College of Medicine   (South Korea)

^b Pacificpharma Corporation   (South Korea)

Author keywords

Cilostazol; Circadian variation; Food effect; Multiple doses; Pharmacokinetics; Sustained release

Indexed keywords

3,4 DIHYDRO 6 [4 [1 (4 HYDROXYCYCLOHEXYL) 1H TETRAZOL 5 YL]BUTOXY] 2(1H) QUINOLINONE; CILOSTAZOL; DEHYDROCILOSTAZOL; DRUG METABOLITE; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; COMPARATIVE STUDY; COUGHING; CROSSOVER PROCEDURE; DIARRHEA; DIZZINESS; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG FEVER; DRUG FORMULATION; DRUG RELEASE; DRUG TOLERABILITY; EPIGASTRIC PAIN; FEMALE; FOLLOW UP; FOOD; FOOD DRUG INTERACTION; FOOD INTAKE; HEADACHE; HEART PALPITATION; HUMAN; IMMEDIATE DRUG RELEASE; KOREA; LIPID DIET; MALE; MAXIMUM PLASMA CONCENTRATION; NAUSEA; NORMAL HUMAN; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; SUSTAINED DRUG RELEASE; VOMITING;

ADMINISTRATION, ORAL; ADULT; AREA UNDER CURVE; ASIAN CONTINENTAL ANCESTRY GROUP; CARDIOVASCULAR AGENTS; CHEMISTRY, PHARMACEUTICAL; CROSS-OVER STUDIES; DELAYED-ACTION PREPARATIONS; FEMALE; FOOD-DRUG INTERACTIONS; HUMANS; MALE; METABOLIC CLEARANCE RATE; MIDDLE AGED; MODELS, BIOLOGICAL; REPUBLIC OF KOREA; TETRAZOLES; THERAPEUTIC EQUIVALENCY; YOUNG ADULT;

EID: 83455219371     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2011.10.024     Document Type: Article

References (31)

1. Schror K. The pharmacology of cilostazol. Diabetes Obes Metab 2002, 4(Suppl 2):S14-S19.
2. Liu Y., Shakur Y., Yoshitake M., Kambayashi Ji J. Cilostazol (pletal): a dual inhibitor of cyclic nucleotide phosphodiesterase type 3 and adenosine uptake. Cardiovasc Drug Rev 2001, 19:369-386.
3. Robless P., Mikhailidis D.P., Stansby G.P. Cilostazol for the peripheral arterial disease. Cochrane Database Syst Rev 2008, (1). CD003748.
4. Dawson D.L., Cutler B.S., Meissner M.H., Strandness D.E. Cilostazol has beneficial effects in treatment of intermittent claudication: results from a multicenter, randomized, prospective, double-blind trial. Circulation 1998, 98:678-686.
5. Douglas J.S., Holmes D.R., Kereiakes D.J., et al. Coronary stent restenosis in patients treated with cilostazol. Circulation 2005, 112:2826-2832. Cilostazol for Restenosis Trial (CREST) Investigators.
6. Ge J., Han Y., Jiang H., et al. RACTS: a prospective randomized antiplatelet trial of cilostazol versus ticlopidine in patients undergoing coronary stenting: long-term clinical and angiographic outcome. J Cardiovasc Pharmacol 2005, 46:162-166. RACTS (Randomized Prospective Antiplatelet Trial of Cilostazol Versus Ticlopidine in Patients Undergoing Coronary Stenting) Trial Investigators.
7. Matsumoto M. Cilostazol in secondary prevention of stroke: impact of the Cilostazol Stroke Prevention Study. Atheroscler Suppl 2005, 6:33-40.
8. Kwon S.U., Cho Y.J., Koo J.S., et al. Cilostazol prevents the progression of the symptomatic intracranial arterial stenosis: the multicenter double-blind placebo-controlled trial of cilostazol in symptomatic intracranial arterial stenosis. Stroke 2005, 36:782-786.
9. Lee S.W., Park S.W., Yun S.C., et al. Triple antiplatelet therapy reduces ischemic events after drug-eluting stent implantation: Drug-Eluting stenting followed by Cilostazol treatment REduces Adverse Serious cardiac Events (DECREASE registry). Am Heart J 2010, 159:284-291. e1.
10. Declaration of Helsinki, Ethical Principles for Medical Research Involving Human Subjects, 2008 Accessed August 11, 2011. http://www.wma.net/en/30publications/10policies/b3/.
11. Korea good clinical practice (KGCP) guidelines [in Korean] Korea Food and Drug Administration (KFDA), Accessed August 11, 2011. http://clinicaltrials.kfda.go.kr/guide/laws/board_list.jsp?category_seq=12.
12. National Institute of Toxicological Research (NITR), Guideline on Food-Effect Bioavailability and Fed Bioequivalence Studies [in Korean] Accessed August 11, 2011. http://www.kfda.go.kr/index.kfda?mid=50&seq=2207&cmd=v.
13. Nirogi R.V., Kandikere V.N., Shukla M., et al. Simultaneous quantification of cilostazol and its primary metabolite 3,4-dehydrocilostazol in human plasma by rapid liquid chromatography/tandem mass spectrometry. Anal Bioanal Chem 2006, 384:780-790.
14. Tata P.N., Fu C.H., Browder N.J., et al. The quantitative determination of cilostazol and its four metabolites in human liver microsomal incubation mixtures by high-performance liquid chromatography. J Pharm Biomed Anal 1998, 18:441-451.
15. Bramer S.L., Tata P.N., Vengurlekar S.S., Brisson J.H. Method for the quantitative analysis of cilostazol and its metabolites in human plasma using LC/MS/MS. J Pharm Biomed Anal 2001, 26:637-650.
16. Guidance for industry, bioanalytical method validation, 2003 KFDA, Accessed August 11, 2011. http://betest.kfda.go.kr/data/docu/08_life.pdf.
17. Gabrielsson J., Weiner D. Pharmacokinetic and Pharmacodynamic Data Analysis: Concepts and Applications 2006, 161-180. Apotekarsocieteten, Stockholm, Sweden. 4th ed.
18. Guidance for Industry. Bioavailability and Bioequivalence Studies for Orally Administered Drug Products-General Considerations 2003, US Food and Drug Administration, US Department of Health and Human Services Office, Washington, DC.
19. Guidance document for bioequivalence studies 2008 [in English] Korea Food and Drug Administration (KFDA), Accessed August 27, 2011. http://betest.kfda.go.kr/country/GUIDANCE%20FOR%20INDUSTRY%20(KFDA_2005).pdf.
20. Bramer S.L., Forbes W.P. Relative bioavailability and effects of a high fat meal on single dose cilostazol pharmacokinetics. Clin Pharmacokinet 1999, 37(Suppl 2):13-23.
21. Suri A., Forbes W.P., Bramer S.L. Pharmacokinetics of multiple-dose oral cilostazol in middle-age and elderly men and women. J Clin Pharmacol 1998, 38:144-150.
22. Bramer S.L., Forbes W.P., Mallikaarjun S. Cilostazol pharmacokinetics after single and multiple oral doses in healthy males and patients with intermittent claudication resulting from peripheral arterial disease. Clin Pharmacokinet 1999, 37(Suppl 2):1-11.
23. Kolawole J.A., Chuhwak P.D., Okeniyi S.O. Chronopharmacokinetics of acetaminophen in healthy human volunteers. Eur J Drug Metab Pharmacokinet 2002, 27:199-202.
24. Baraldo M. The influence of circadian rhythms on the kinetics of drugs in humans. Expert Opin Drug Metab Toxicol 2008, 4:175-192.
25. Park K., Kim Y.S., Kwon K.I., et al. A randomized, open-label, two-period, crossover bioavailability study of two oral formulations of tacrolimus in healthy Korean adults. Clin Ther 2007, 29:154-162.
26. Umemiya N. Seasonal variations of physiological characteristics and thermal sensation under identical thermal conditions. J Physiol Anthropol 2006, 25:29-39.
27. Tsumura Y., Makonakwkeyoon L., Limtrakul P.N., et al. Seasonal variation in amount of unabsorbed dietary carbohydrate from the intestine after breakfast in young female Thai subjects: comparison with that of Japanese subjects. J Physiol Anthropol 2010, 29:141-147.
28. Nawaz M., Nawaz R. Pharmacokinetics and urinary excretion of sulphadimidine in sheep during summer and winter. Vet Rec 1983, 112:379-381.
29. Amirat Z., Brudieux R. Seasonal changes in the metabolic clearance rate of cortisol in the adult male sand rat (Psammomys obesus). Gen Comp Endocrinol 1984, 53:232-234.
30. Khammar F., Brudieux R. Seasonal changes in testicular contents of testosterone and androstenedione and in the metabolic clearance rate of testosterone in the sand rat (Psammomys obesus). J Reprod Fertil 1984, 71:235-241.
31. D'Hondt P., Maes M., Leysen J.E., et al. Seasonal variation in platelet [3H]paroxetine binding in healthy volunteers. Relationship to climatic variables. Neuropsychopharmacology 1996, 15:187-198.