title: Pharmacokinetics of sugammadex 16 mg/kg in healthy Chinese volunteers.
abstract: OBJECTIVE
  Elimination of sugammadex occurs predominantly via the kidneys, with the majority of the drug excreted unchanged in the urine. To date, most studies with sugammadex have been performed in non-Asian populations. The objectives of this open-label study were to determine the pharmacokinetics (PK) and safety of single-dose sugammadex (16 mg/kg) in healthy Chinese adult volunteers.
  
  
  METHODS
  12 Chinese subjects (6 male; 6 female) received intravenous sugammadex (16 mg/kg) as a 10-second bolus infusion. Blood samples were collected pre-sugammadex and at regular intervals up to 24 hours post-sugammadex for PK assessment. Safety was assessed via AEs, vital signs, electrocardiogram, and laboratory parameters.
  
  
  RESULTS
  Following sugammadex 16 mg/kg infusion, peak sugammadex concentration was 197 μg/mL, clearance was 99.7 mL/min, and apparent volume of distribution at equilibrium was 10.5 L. Plasma sugammadex concentrations showed a polyexponential decline over time, with an overall geometric mean (CV%) terminal half-life of 145 minutes (17.9%) (139 minutes (17.7%) for males; 152 minutes (18.6%) for females). No influence of gender on the PK of sugammadex was observed. Three subjects experienced an adverse events (AE) (dysgeusia of mild intensity), which was considered possibly or probably related to sugammadex. There were no clinically significant changes in vital signs, electrocardiography or laboratory parameters.
  
  
  CONCLUSIONS
  PK of sugammadex (16 mg/kg) was characterized in healthy Chinese subjects. Overall between-subject variability on clearance and apparent volume of distribution was ~ 10%. Sugammadex was generally well tolerated.
authors.forename: Pieter-Jan
authors.initials: PJ
authors.lastname: de Kam
authors.forename: Jie
authors.initials: J
authors.lastname: Hou
authors.forename: Zaiqi
authors.initials: Z
authors.lastname: Wang
authors.forename: Wen Hong
authors.initials: WH
authors.lastname: Lin
authors.forename: Michiel
authors.initials: M
authors.lastname: van den Heuvel
mesh_terms: D019540:Area Under Curve; D044466:Asian People; D002681:China; D016903:Drug Monitoring; D005260:Female; D006207:Half-Life; D064368:Healthy Volunteers; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D008657:Metabolic Clearance Rate; D009465:Neuromuscular Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D018570:Risk Assessment; D000077122:Sugammadex; D055815:Young Adult; D047408:gamma-Cyclodextrins / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*
chemical_list: D009465:Neuromuscular Agents; D047408:gamma-Cyclodextrins; D000077122:Sugammadex