Biorelevant Dissolution Testing of Numerically Optimized Multiparticulate Drug Delivery Systems of Gliclazide

Elsayed, Ebtesam W; El-Ashmawy, Ahmed A.; Mursi, Nadia M.; Emara, Laila H.

doi:10.14227/dt300223p88

Cited by 1 publication

(1 citation statement)

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“…The optimized test incorporates the use of biorelevant fluid media in combination with the SIFC (stomach-to-intestine fluid changing) system ( 35 ). Biorelevant media are solutions designed to mimic specific regions of the GI tract such as gastric FaSSGF (Fasted State Simulated Gastric Fluid) and intestinal FaSSIF (Fasted State Simulated Intestinal Fluid) ( 57 , 58 ). The SIFC system is designed to simulate the dynamic changes in pH and composition of gastrointestinal fluid that occur as orally administered drugs transition from the stomach to the small intestine.…”

Section: Resultsmentioning

confidence: 99%

Designing an effective dissolution test for bilayer tablets tailored for optimal melatonin release in sleep disorder management

Bassetto,

Amadio,

Ciampanelli

et al. 2024

Front. Nutr.

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This project aims to investigate the release performance of bilayer tablet (BL-Tablet) designed with both fast and slow-release technology, targeting sleep disorders. The tablet incorporates Melatonin, extracts of Eschscholzia californica and Melissa officinalis. In order to validate the effectiveness of the extended-release profile, an advanced dissolution test was herein proposed. This new method utilizes biorelevant intestinal fluid media and incorporates a stomach-to-intestine fluid changing (SIFC) system. To demonstrate the advantages of employing this method for assessing the controlled release profile of active ingredients, the dissolution results were compared with those obtained using the conventional EU Pharmacopoeia approach. Furthermore, the comparative analysis was extended to include a monolayer tablet version (ML-Tablet) lacking the slow-release technology. Technological characterization and bioaccessibility studies, including intestinal permeability test, were conducted as well to assess the pharmacological performance and bioavailability of active ingredients. The dissolution data recovered revealed that the two dissolution methods did not exhibit any significant differences in the release of ML-Tablet’s. However, the dissolution profile of the BL-Tablet exhibited notable differences between the two methods particularly when assessing the behavior of the slow-release layer. In this scenario, both methods initially exhibited a similar release pattern within the first approximately 0.5 h, driven by the fast-release layer of the tablet. Following this, distinct gradual and sustained releases were observed, spanning 2.5 h for the EU Pharmacopoeia method and 8 h for the new SIFC-biorelevant dissolution method, respectively. Overall, the novel method demonstrated a substantial improvement compared to conventional EU Pharmacopoeia test in evaluating the performance of a controlled slow-release technology. Remarkably, the prolonged release technology did not have an adverse impact on melatonin intestinal absorption, and, consequently, maintaining its potential bioavailability of around 78%. Concluding, this research provides valuable insights into how the innovative dissolution test can assist formulators in developing controlled release formulations.

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Section: Resultsmentioning

confidence: 99%