IN VITRO PREDICTION OF DRUG RELEASE PROFILE OF RIFAMPICIN IN CROHN’S DISEASE AND CHOLESTASIS DISEASE CONDITIONS USING BIOPHARMACEUTICAL TOOLS AND BIORELEVANT MEDIA
DOI:
https://doi.org/10.22159/ijap.2026v18i3.57188Keywords:
Rifampicin, Crohn's disease, Cholestasis, Biorelevant media, In vitro release, Bioavailability, Altered gastric motilityAbstract
Objective: Altered gastrointestinal physiology in Crohn’s disease and cholestasis may affect the intraluminal environment and impact the dissolution of orally administered drugs. Rifampicin exhibits pH and bile salt–dependent solubility, making it susceptible to variations in gastrointestinal conditions. The present research investigates in vitro dissolution behaviour of rifampicin in biorelevant media that simulate both healthy and disease-specific gastrointestinal environments.
Methods: Biorelevant dissolution medium that mimic the fasted-state intestinal conditions for healthy people, Crohn’s disease, and cholestasis were created by modifying pH, bile salt concentration, and the levels of mucin and inflammatory cytokines based on reported physiological values. Rifampicin fast-dissolving tablets (100 mg) were tested using United States Pharmacopeia (USP) Apparatus II (900 mL, 37 °C ± 0.5 °C) and spectrophotometric analysis. Dissolution profiles were analyzed descriptively.
Results: Rifampicin demonstrated slower drug release in Crohn’s disease–simulated medium (FaSSIF-CD) compared with FaSSIF-NA ( healthy condition). Drug release at 60 minutes exceeded 90% in FaSSIF control, whereas in FaSSIF-CD, it was limited to approximately 58–62% (p < 0.05). Conversely, dissolution in the cholestasis medium exhibited no significant divergence from the FaSSIF-NA under the evaluated conditions. The data demonstrate significant diversity in dissolution behaviour among media that simulate both healthy and disease-altered gastrointestinal environments.
Conclusion: These findings support the idea that physiological characteristics of the gastrointestinal environment may affect how rifampicin dissolves, as well as highlight the importance of media composition in predicting oral bioavailability in pathological states. Additional research with adequate clinical data is needed to go deeper into these findings and examine the molecular impacts on specific components.
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