Dissolution of mesalazine modified release tablets under standard and bio-relevant test conditions

Abstract

The study demonstrates that besides the investigation of the pH dependency of drug release, the characterisation of the mechanical robustness of the dosage forms is an essential factor determining the dissolution characteristics of such pH-dependent targeted modified release tablets. The susceptibility of 800 mg mesalazine MR tablets towards mechanical stress may be one reason for undesired drug delivery in vivo.

In Vitro Methodologies for Evaluating Colon-Targeted Pharmaceutical Products and Industry Perspectives for Their Applications

“…Stress parameters, namely pressure and velocity, are controlled by inflating/deflating the inner balloon and rotating/resting the horizontal axis (such that the sphere rotates between exposition to air/media), respectively. Dissolution of mesalazine locally acting colon-targeting products in this apparatus was found to be influenced by the stress conditions and was different from the results obtained from the pharmacopeial USP II apparatus [100].…”

Rheological and textural analysis as tools for investigation of drug-polymer and polymer–polymer interactions on the example of low-acyl gellan gum and mesalazine

“…Therefore, mesalazine seems to be an ideal candidate for attempts to develop formulations that would not only release the drug at the colonic area but also maximize the time of the release. 43 To the best of our knowledge, there is no data concerning systems containing a combination of gellan gum and mesalazine, although they appear to be beneficial in terms of potential applications in colorectal diseases, combining both the features of modified and sustained release formulations. Therefore, this study is focused on the drug which is currently in use and plays an important role in this particular condition.…”

Comparison of the stability and pharmacokinetics in dogs of modified ciclosporin capsules stored at −20°C and room temperature

“…Additionally, some capsules were observed to fracture along the seam of the vessel (the capsules being two symmetrical halves fused together), and this possible weak point may have artificially decreased the force required to fracture the capsules. A recent model for tablet dissolution parameters involving simulated gastrointestinal transit has been published and may offer a better way to measure capsule integrity in vitro for future studies …”