Multiple-Dose Study to Evaluate Pharmacokinetics, Pharmacodynamics, and Safety in Healthy Subjects: A Comparison of Controlled-Release Sarpogrelate and Immediate-Release Sarpogrelate

Aims: To compare the pharmacokinetics, pharmacodynamics, and safety of sarpogrelate between controlled-release (CR) and immediate-release (IR) formulations after multiple-dose administration. Methods: This study was a randomized, open-label, 2-period, 2-treatment, crossover study in healthy subjects...

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Vydáno v:Pharmacology Ročník 96; číslo 1-2; s. 68 - 75
Hlavní autoři: Lee, Soo-Yun, Kim, Jung-Ryul, Jung, Jin Ah, Kim, Tae-Eun, Lee, Soo-Youn, Huh, Wooseong, Lee, Jae-Won, Jun, Hun, Ko, Jae-Wook
Médium: Journal Article
Jazyk:angličtina
Vydáno: Basel, Switzerland S. Karger AG 01.08.2015
Témata:
Adult
Comparative analysis
Comparative studies
Controlled release technology
Delayed-Action Preparations - administration & dosage
Delayed-Action Preparations - pharmacokinetics
Dosage and administration
Dose-response relationship (Biochemistry)
Drug therapy
Female
Health
Humans
Kinetics
Male
Original Paper
Patient safety
Pharmacokinetics
Pharmacology
Platelet Aggregation - drug effects
Platelet Aggregation Inhibitors - administration & dosage
Platelet Aggregation Inhibitors - adverse effects
Platelet Aggregation Inhibitors - pharmacokinetics
Platelet Aggregation Inhibitors - pharmacology
Serotonin agents
Succinates - administration & dosage
Succinates - adverse effects
Succinates - pharmacokinetics
Succinates - pharmacology
Young Adult
South Korea
Multiple dose
Pharmacokinetics
Formulation
Collagen
Sarpogrelate
Controlled release
ISSN:0031-7012, 1423-0313, 1423-0313
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Shrnutí:Aims: To compare the pharmacokinetics, pharmacodynamics, and safety of sarpogrelate between controlled-release (CR) and immediate-release (IR) formulations after multiple-dose administration. Methods: This study was a randomized, open-label, 2-period, 2-treatment, crossover study in healthy subjects. All subjects received CR sarpogrelate 300 mg once daily and IR sarpogrelate 100 mg three times daily by random order each for 3 days with a 7-day washout period. Serial blood sampling was performed over 24 h. Pharmacokinetic parameters were determined by noncompartmental methods. Platelet aggregation to collagen, measured by light transmission aggregometry, was reported as maximal platelet aggregation. Results: Thirty-two subjects completed the study. CR sarpogrelate increased rapidly, reaching C max in 1.25 h (vs. 1.00 h in IR sarpogrelate) and declined with a t 1/2 of 3.59 h (vs. 1.12 h in IR sarpogrelate). The 90% CIs for the geometric mean ratio of AUC τ and C max,ss between IR and CR formulations were 1.18 to 1.40 and 0.99 to 1.29, respectively. The degree of inhibition of platelet aggregation was similar between two formulations. Conclusions: CR sarpogrelate showed slightly higher systemic exposure and similar peak concentration compared with IR sarpogrelate. The profiles of pharmacodynamics and safety were comparable between two formulations.
Bibliografie:SourceType-Scholarly Journals-1
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ISSN:0031-7012
1423-0313
1423-0313
DOI:10.1159/000430889