Is once-daily mesalazine equivalent to the currently used twice-daily regimen? A study performed in 30 healthy volunteers.
A randomized, 2-way, crossover study was conducted in 30 volunteers to compare the pharmacokinetic profile of a new once-daily dosing regimen of mesalazine (1 x 4 g/d) with the current twice-daily dosage (2 x 2 g/d) used in many European countries. The 2 dosages were administrated orally for 8 days, separated by a 2-week washout. Plasma concentrations of mesalazine and N-acetyl-mesalazine were determined on days 1 and 8 by a validated high-performance liquid chromatography method and C(max), t(max), and AUCs calculated. The bioequivalence was obtained for a 90% confidence interval of the AUC(0-24h) ratio (test/reference) for mesalazine and N-acetyl-mesalazine on days 1 and 8, within the range of 0.80 to 1.25. The bioequivalence was demonstrated on day 1 for mesalazine and N-acetyl-mesalazine and on day 8 for mesalazine. As it is desirable to offer patients a preparation with a less frequent administration to enhance compliance, this once-daily regimen may be an attractive dosing option.
Gandia
Peggy
P
Laboratoire de Pharmacocinétique et Toxicologie Clinique, Institut Fédératif de Biologie, Hôpital Purpan, TSA 70034, 330 avenue de Grande Bretagne, 31059 Toulouse cedex 9, France.
Idier
Isabelle
I
Houin
Georges
G
D000118:Acetylglucosaminidase / Q000652:urine; D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001247:Asthenia / Q000139:chemically induced; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D005982:Glutathione Transferase / Q000652:urine; D006261:Headache / Q000139:chemically induced; D006801:Humans; D008297:Male; D019804:Mesalamine / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D008875:Middle Aged; D009325:Nausea / Q000139:chemically induced; D011507:Proteinuria / Q000139:chemically induced; D013608:Tablets, Enteric-Coated; D013810:Therapeutic Equivalency; D013997:Time Factors; D001613:beta 2-Microglobulin / Q000652:urine
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013608:Tablets, Enteric-Coated; D001613:beta 2-Microglobulin; D019804:Mesalamine; D005982:Glutathione Transferase; D000118:Acetylglucosaminidase