دورية أكاديمية
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
| العنوان: | 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 |
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| المساهمون: | Donghwan Lee, Lay Ahyoung Lim, Seong Bok Jang, Yoon Jung Lee, Jae Yong Chung, Jong Rak Choi, Kiyoon Kim, Jin Woo Park, Hosang Yoon, Jaeyong Lee, Min Soo Park, Kyungsoo Park, Park, Kyung Soo, Park, Min Soo, Lee, Dong Hwan, Lim, Lay Ahyoung, Chung, Jae Yong, Choi, Jong Rak |
| سنة النشر: | 2011 |
| مصطلحات موضوعية: | Administration, Oral, Adult, Area Under Curve, Asian Continental Ancestry Group, Cardiovascular Agents/administration & dosage, Cardiovascular Agents/adverse effects, Cardiovascular Agents/blood, Cardiovascular Agents/pharmacokinetics, 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/administration & dosage, Tetrazoles/adverse effects, Tetrazoles/blood, Tetrazoles/pharmacokinetics, Therapeutic Equivalency, Young Adult, cilostazol, circadian variation |
| الوصف: | BACKGROUND: A sustained-release (SR) formulation of cilostazol was recently developed in Korea and was expected to yield a lower C(max) and a similar AUC to the immediate-release (IR) formulation. OBJECTIVE: The goal of the present study was to compare the pharmacokinetic profiles of a newly developed SR formulation and an IR formulation of cilostazol after single- and multiple-dose administration and to evaluate the influence of food in healthy Korean subjects. This study was developed as part of a product development project at the request of the Korean regulatory agency. METHODS: This was a randomized, 3-part, sequential, open-label, 2-period crossover study. Each part consisted of different subjects between the ages of 19 and 55 years. In part 1, each subject received a single dose of SR (200 mg 횞 1 tablet, once daily) and IR (100 mg 횞 2 tablets, BID) formulations of cilostazol orally 7 days apart in a fasted state. In part 2, each subject received a single dose of the SR (200 mg 횞 1 tablet, once daily) formulation of cilostazol 7 days apart in a fasted and a fed state. In part 3, each subject received multiple doses of the 2 formulations for 8 consecutive days 21 days apart. Blood samples were taken for 72 hours after the dose. Cilostazol pharmacokinetics were determined for both the parent drug and its metabolites (OPC-13015 and OPC-13213). Adverse events were evaluated through interviews and physical examinations. RESULTS: Among the 92 enrolled subjects (66 men, 26 women; part 1, n = 26; part 2, n = 26; part 3, n = 40), 87 completed the study. In part 1, all the primary pharmacokinetic parameters satisfied the criterion for assumed bioequivalence both in cilostazol and its metabolites, yielding 90% CI ratios of 0.9624 to 1.2323, 0.8873 to 1.1208, and 0.8919 to 1.1283 for C(max) and 0.8370 to 1.0134, 0.8204 to 0.9807, and 0.8134 to 0.9699 for AUC(0-last) of cilostazol, OPC-13015, and OPC-13213, respectively. In part 2, food intake increased C(max) and AUC significantly (P < 0.0001), yielding geometric ... |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | 2038~2053 |
| اللغة: | unknown |
| تدمد: | 0149-2918 1879-114X |
| العلاقة: | CLINICAL THERAPEUTICS; J00614; OAK-2011-02111; https://ir.ymlib.yonsei.ac.kr/handle/22282913/94637Test; http://www.sciencedirect.com/science/article/pii/S0149291811007132Test; T201104120; CLINICAL THERAPEUTICS, Vol.33(12) : 2038-2053, 2011 |
| DOI: | 10.1016/j.clinthera.2011.10.024 |
| الإتاحة: | https://doi.org/10.1016/j.clinthera.2011.10.024Test https://ir.ymlib.yonsei.ac.kr/handle/22282913/94637Test http://www.sciencedirect.com/science/article/pii/S0149291811007132Test |
| حقوق: | CC BY-NC-ND 2.0 KR ; https://creativecommons.org/licenses/by-nc-nd/2.0/krTest/ ; not free |
| رقم الانضمام: | edsbas.F63F578F |
| قاعدة البيانات: | BASE |
| تدمد: | 01492918 1879114X |
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| DOI: | 10.1016/j.clinthera.2011.10.024 |