title: Ibuprofen lysinate, quicker and less variable: relative bioavailability compared to ibuprofen base in a pediatric suspension dosage form.
abstract: OBJECTIVE
  To assess and compare the bioavailability of ibuprofen enantiomers (R and S) of two different pediatric suspensions: the first one with ibuprofen lysinate (Algidrin® Pediátrico, FARDI S.A., Barcelona, Spain) and the second one with ibuprofen base (Dalsy®, Abbott Laboratories S.A., Madrid, Spain).
  
  
  METHODS
  A randomized, open-label, single-dose, balanced, crossover study under fasting conditions was performed at the CIM-Sant Pau. 24 healthy volunteers received a single dose of ibuprofen lysinate (AlgidrinÂ® PediÃ¡trico, FARDI S.A.) and ibuprofen base (Dalsy®, Abbott Laboratories S.A.) equivalent to 400 mg of ibuprofen. 18 blood samples were drawn and ibuprofen enantiomer plasma concentrations were determined using an enantioselective analytical method. An analysis of variance (ANOVA) model was used, and the 90% confidence intervals (CI) were calculated; further analyses were made regarding rate of absorption and variability.
  
  
  RESULTS
  The pharmacokinetic parameters (Algidrin® Pediátrico vs. Dalsy® (Mean±SD)) were: S-enantiomer: Cmax=22.39±5.33 vs. 19.97±3.19 μg/mL; AUC0t=74.83±16.69 vs. 74.64±14.80 μg×h/mL, and AUC0∞=77.46±19.33 vs. 76.98±17.13 μg×h/mL; and for R-enantiomer: Cmax=21.74±3.76 vs. 15.20±2.03 μg/mL; AUC0t=57.55±10.17 vs. 46.13±9.61 μg×h/mL, and AUC0∞ value was 58.49±10.57 vs. 47.03±10.02 μg×h/mL. The tmax (Median) for S-enantiomer (active) were: 0.5 vs. 1.33 hours (p=0.001) and for R-enantiomer: 0.5 vs. 1.0 hours (p=0.004). Ibuprofen pharmacokinetic values may vary under fed state and in pediatric population.
  
  
  CONCLUSIONS
  While S-ibuprofen shows a similar bioavailability for AUC0t, AUC0∞, and Cmax, R-ibuprofen shows suprabioavailability for the lysinate formulation. The rate of absorption of the ibuprofen lysinate suspension is quicker and less variable than that of the ibuprofen base reference suspension and it exhibits a shorter tmax, which is of particular interest for achieving a rapid and homogeneous analgesic and antipyretic effect.
authors.forename: Juan Manuel
authors.initials: JM
authors.lastname: Ferrero-Cafiero
authors.forename: Ignasi
authors.initials: I
authors.lastname: Gich
authors.forename: Montse
authors.initials: M
authors.lastname: Puntes
authors.forename: Joan
authors.initials: J
authors.lastname: Martínez
authors.forename: Maria R
authors.initials: MR
authors.lastname: Ballester
authors.forename: Jimena
authors.initials: J
authors.lastname: Coimbra
authors.forename: Yaira
authors.initials: Y
authors.lastname: Mathison
authors.forename: Maite
authors.initials: M
authors.lastname: Tarré
authors.forename: Xavier
authors.initials: X
authors.lastname: Font
authors.forename: Rosa M
authors.initials: RM
authors.lastname: Antonijoan
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000367:Age Factors; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D005215:Fasting / Q000097:blood; D005260:Female; D064368:Healthy Volunteers; D006801:Humans; D007052:Ibuprofen / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D007408:Intestinal Absorption; D007536:Isomerism; D008239:Lysine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D008875:Middle Aged; D019999:Pharmaceutical Solutions; D019518:Postprandial Period; D013810:Therapeutic Equivalency; D055815:Young Adult
chemical_list: D018712:Analgesics, Non-Narcotic; D019999:Pharmaceutical Solutions; D008239:Lysine; C016106:solufenum; D007052:Ibuprofen