Definition
Biorelevant dissolution media are aqueous solutions or suspensions whose composition and physicochemical characteristics closely resemble human fluids found along the different portions of the gastrointestinal tract, developed to study the solubility and/or dissolution profile of orally administered drugs in a more physiologically relevant manner.
Main Text
Oral solid dosage forms are the most widely used dosage forms due to their ease of application and patient comfort. For these pharmaceutical dosage forms, the release, but more precisely, the dissolution characteristics are critical factors to ensure the in vivo performance of the pharmaceutical active ingredients: to be absorbed, drug must be dissolved under the physiological conditions that surround the absorption site at the gastrointestinal (GI) tract. Therefore, in vitro dissolution test has become a...
This is a preview of subscription content, log in via an institution to check access.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
References
Dressman J. Evolution of dissolution media over the last twenty years. Dissolution Technol. 2014;21:6–10.
USP42. <1092> the dissolution procedure: developments and validation. United States Pharmacop. 2019.
Amidon GL, Lennernäs H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res. 1995;12:413–20.
Kleberg K, Jacobsen J, Müllertz A. Characterising the behaviour of poorly water soluble drugs in the intestine: application of biorelevant media for solubility, dissolution and transport studies. J Pharm Pharmacol. 2010;62:1656–68.
Galia E, Nicolaides E, Hörter D, Löbenberg R, Reppas C, Dressman JB. Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs. Pharm Res. 1998;15:698–705.
Jantratid E, Janssen N, Reppas C, Dressman J. Dissolution media simulating conditions in the proximal human gastrointestinal tract: an update. Pharm Res. 2008;25:1663–76.
Vertzoni M, Dressman J, Butler J, Hempenstall J, Reppas C. Simulation of fasting gastric conditions and its importance for the in vivo dissolution of lipophilic compounds. Eur J Pharm Biopharm. 2005;60:413–7.
Vertzoni M, Diakidou A, Chatzilias M, Söderlind E, Abrahamsson B, Dressman JB, Reppas C. Biorelevant media to simulate fluids in the ascending colon of humans and their usefulness in predicting intracolonic drug solubility. Pharm Res. 2010;27:2187–96.
Dressman JB, Vertzoni M, Goumas K, Reppas C. Estimating drug solubility in the gastrointestinal tract. Adv Drug Deliv Rev. 2007;59:591–602.
Otsuka K, Shono Y, Dressman J. Coupling biorelevant dissolution methods with physiologically based pharmacokinetic modelling to forecast in-vivo performance of solid oral dosage forms. J Pharm Pharmacol. 2013;65:937–52.
Aulton M, Taylor KMG. Aulton’s pharmaceutics. 5th ed. Elsevier; 2017.
D’Arcy DM, Persoons T. Understanding the potential for dissolution simulation to explore the effects of medium viscosity on particulate dissolution. AAPS PharmSciTech. 2019;20:1–13.
Pentafragka C, Vertzoni M, Dressman J, Symillides M, Goumas K, Reppas C. Characteristics of contents in the upper gastrointestinal lumen after a standard high-calorie high-fat meal and implications for the in vitro drug product performance testing conditions. Eur J Pharm Sci. 2020;155:105535.
Braun RJ, Parrott EL. Influence of viscosity and solubilization on dissolution rate. J Pharm Sci. 1972;61:175–8.
Finholt P, Solvang S. Dissolution kinetics of drugs in human gastric juice—the role of surface tension. J Pharm Sci. 1968;57:1322–6.
Dressman JB, Amidon GL, Reppas C, Shah VP. Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms. Pharm Res. 1998;15:11–22.
Efentakis M, Dressman JB. Gastric juice as a dissolution medium: surface tension and pH. Eur J Drug Metab Pharmacokinet. 1998;23:97–102.
Galia E, Horton J, Dressman JB. Albendazole generics - a comparative in vitro study. Pharm Res. 1999;16:1871–5.
Vertzoni M, Pastelli E, Psachoulias D, Kalantzi L, Reppas C. Estimation of intragastric solubility of drugs: in what medium? Pharm Res. 2007;24:909–17.
Fuchs A, Leigh M, Kloefer B, Dressman JB. Advances in the design of fasted state simulating intestinal fluids: FaSSIF-V3. Eur J Pharm Biopharm. 2015;94:229–40.
Markopoulos C, Andreas CJ, Vertzoni M, Dressman J, Reppas C. In-vitro simulation of luminal conditions for evaluation of performance of oral drug products: choosing the appropriate test media. Eur J Pharm Biopharm. 2015;93:173–82.
McPherson S, Perrier J, Dunn C, Khadra I, Davidson S, Ainousah B, Wilson CG, Halbert G. Small scale design of experiment investigation of equilibrium solubility in simulated fasted and fed intestinal fluid. Eur J Pharm Biopharm. 2020;150:14–23.
Klumpp L, Leigh M, Dressman J. Dissolution behavior of various drugs in different FaSSIF versions. Eur J Pharm Sci. 2020;142:105138.
Marques MRC, Loebenberg R, Almukainzi M. Simulated biological fluids with possible application in dissolution testing. Dissolution Technol. 2011;18:15–28.
Klein S. Advancements in dissolution testing of Oral and non-oral formulations. AAPS PharmSciTech. 2019;20:266.
Hens B, Al-Gousous J, Wang K, et al. Summary of the in vivo predictive dissolution (iPD) - Oral drug delivery (ODD) conference 2018. Dissolution Technol. 2018;25:50–3.
Author information
Authors and Affiliations
Corresponding author
Editor information
Editors and Affiliations
Section Editor information
Rights and permissions
Copyright information
© 2022 Springer Nature Switzerland AG
About this entry
Cite this entry
Ruiz, M.E., Talevi, A. (2022). Biorelevant Dissolution Media. In: Talevi, A. (eds) The ADME Encyclopedia. Springer, Cham. https://doi.org/10.1007/978-3-030-84860-6_43
Download citation
DOI: https://doi.org/10.1007/978-3-030-84860-6_43
Published:
Publisher Name: Springer, Cham
Print ISBN: 978-3-030-84859-0
Online ISBN: 978-3-030-84860-6
eBook Packages: Biomedical and Life SciencesReference Module Biomedical and Life Sciences