title: Multiple-Dose Study to Evaluate Pharmacokinetics, Pharmacodynamics, and Safety in Healthy Subjects: A Comparison of Controlled-Release Sarpogrelate and Immediate-Release Sarpogrelate.
abstract: OBJECTIVE
  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 Cmax in 1.25 h (vs. 1.00 h in IR sarpogrelate) and declined with a t1/2 of 3.59 h (vs. 1.12 h in IR sarpogrelate). The 90% CIs for the geometric mean ratio of AUCτ and Cmax,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.
authors.affiliation: Department of Health Sciences and Technology, Samsung Advanced Institute for Health Sciences and Technology (SAIHST), Sungkyunkwan University, Busan, Seoul, Republic of Korea.
authors.forename: Soo-Yun
authors.initials: SY
authors.lastname: Lee
authors.forename: Jung-Ryul
authors.initials: JR
authors.lastname: Kim
authors.forename: Jin Ah
authors.initials: JA
authors.lastname: Jung
authors.forename: Tae-Eun
authors.initials: TE
authors.lastname: Kim
authors.forename: Soo-Youn
authors.initials: SY
authors.lastname: Lee
authors.forename: Wooseong
authors.initials: W
authors.lastname: Huh
authors.forename: Jae-Won
authors.initials: JW
authors.lastname: Lee
authors.forename: Hun
authors.initials: H
authors.lastname: Jun
authors.forename: Jae-Wook
authors.initials: JW
authors.lastname: Ko
mesh_terms: D000328:Adult; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000493:pharmacokinetics; D005260:Female; D006801:Humans; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage / Q000009:adverse effects* / Q000493:pharmacokinetics* / Q000494:pharmacology; D013386:Succinates / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000494:pharmacology; D055815:Young Adult
chemical_list: D003692:Delayed-Action Preparations; D010975:Platelet Aggregation Inhibitors; D013386:Succinates; C064294:sarpogrelate