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Gastrointestinal spread of oral prolonged-release mesalazine microgranules (Pentasa) dosed as either tablets or
I R Wilding1, C J Kenyon, G Hooper
1Pharmaceutical Profiles Ltd, Faraday Building, Highfields Science Park, Nottingham, UK. iwilding@pharmprofiles.co.uk
Background:
There is increasing interest in using higher dosages of mesalazine for the treatment of inflammatory bowel disease; however, with current mesalazine products this involves the use of 8-16 tablets per day.
Aim:
To evaluate the disposition, dispersion and movements of Pentasa prolonged-release microgranules following single dosing of either tablets (2 x 500 mg) or a new 1 g sachet (unit dose, microgranules in a foil bag).
Methods:
A randomized crossover study in eight healthy volunteers was undertaken. Both formulations were radiolabelled by neutron activation and dosed in the fasted state. Location of the preparations in the bowel was assessed over 24 h by scintigraphy.
Results:
Dissolution testing at pH 7.5 showed comparable in vitro mesalazine release properties for the tablet and sachet preparations. In vivo disposition of the microgranules administered as either tablets or sachet was comparable in terms of gastric emptying, small intestinal transit and colon arrival.
Conclusions:
Pentasa sachets 1 g unit dose offers the same release of mesalazine as Pentasa 500 mg tablets. Drug release occurs throughout the gastrointestinal tract from stomach to colon, with the advantage of fewer oral doses and ease of swallowing.
Insights
A new 1 g Pentasa sachet provides mesalazine release comparable to tablets. This formulation offers convenient dosing and ease of swallowing for inflammatory bowel disease treatment.
Area of Science:
- Gastroenterology
- Pharmacokinetics
- Drug Delivery Systems
Background:
- Higher mesalazine dosages are of interest for inflammatory bowel disease (IBD).
- Current mesalazine products require 8-16 tablets daily for higher doses.
- This necessitates exploring more convenient mesalazine formulations.
Purpose of the Study:
- To evaluate the disposition, dispersion, and gastrointestinal transit of Pentasa prolonged-release microgranules.
- To compare a new 1 g sachet (unit dose) with standard 500 mg tablets.
- To assess mesalazine release profiles in healthy volunteers.
Main Methods:
- Randomized crossover study in eight healthy volunteers.
- Both tablet and sachet formulations were radiolabeled and administered in a fasted state.
- Scintigraphy was used to assess drug location in the gastrointestinal tract over 24 hours.
Main Results:
- In vitro dissolution testing at pH 7.5 showed comparable mesalazine release for both formulations.
- In vivo studies demonstrated similar gastric emptying, small intestinal transit, and colonic arrival for both tablets and sachets.
- The disposition and movement of mesalazine microgranules were consistent between the two dosage forms.
Conclusions:
- The Pentasa 1 g sachet offers equivalent mesalazine release to Pentasa 500 mg tablets.
- Mesalazine release occurs throughout the gastrointestinal tract, from the stomach to the colon.
- The sachet formulation provides the advantage of fewer daily doses and improved ease of swallowing for patients.