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COMPARABLE PHARMACOKINETICS OF TWO DELAYED RELEASE FORMULATIONS OF ORAL MESALAMINE
WJ Sandborn1, G Balan, B Kuzmak, SB Hanauer
1Mayo Clinic, Rochester, MN, United States
Purpose: Both Asacol® and Lialda™ are delayed release mesalamine preparations for topical action in the colon with a pH dependent coating that controls mesalamine release at pH => 7. Lialda also contains lipophilic and hydrophilic excipients. According to US labeling, Asacol is dosed TID and Lialda is dosed QD for mildly to moderately active UC. The purpose of this study is to evaluate the pharmacokinetic (PK) parameters from 2.4 g/d of oral mesalamine administered as Lialda QD, Asacol QD, and Asacol TID.
METHODS: 37 healthy volunteers completed a randomized, open-label, parallel group, steady state PK study. All doses were taken within 30 minutes of a meal/snack, and subjects were dosed for 7 consecutive days. Plasma samples were obtained once daily up to Day 7 and for 48hrs after the first dose on day 7. Urine was collected over 8hr intervals for 24hrs after the first dose on day 7. Plasma and urine samples were analyzed for 5-ASA & N-Ac-5-ASA using a validated LC/MS assay.
RESULTS: 5-ASA plasma PK parameters and profile of all 3 treatment arms are shown:
The plasma PK parameters for 5-ASA & N-Ac-5-ASA were comparable across all treatment arms. The total (5-ASA & N-Ac-5-ASA) urinary excretion was 21.3%, 20.2%, and 17.9% for Lialda QD, Asacol QD, and Asacol TID, respectively.
CONCLUSION: Overall, Asacol and Lialda dosed QD exhibited a similar PK profile in healthy volunteers. These results suggest no apparent differences in the release profile of Lialda or Asacol given once daily. Clinical significance is unknown.
This research was funded by Procter & Gamble Pharmaceuticals
