An Introduction to Biorelevant Media

Up to 90% of new drugs in development have poor solubility.

1/3 of development costs are spent in the pre-clinical phase so early decisions should be informed and rational.

This is why it's vital to test your drug in media which simulate fluids actually found in the gut.

Biorelevant Media contain bile salts and lecithin to replicate fluids from different regions of the gut.

They also represent both 'fasted' and 'fed' states.

And even simulate fluids of different animal species.

They can help you determine biorelevant solubility: how much drug product dissolves in the gut.

Also biorelevant dissolution: how much time it takes to dissolve.

More predictive results will help you make better decisions for the successful development of your drug product.

“Media that follow more closely the composition of fluids in the stomach and intestinal tract and are designed to represent the fed and fasted state in the stomach and small intestine... may be very useful in modeling in vivo dissolution behavior of immediate-release (IR) dosage forms.”

USP 1092 The Dissolution Procedure: Development and Validation

This is how Unilever recommends using Biorelevant Media to investigate 'Food Effects':

“Data from dissolution in FaSSIF and FeSSIF are especially valuable to plan the time of administration, e.g. whether to dose with or without a meal… in order to properly design and guide nutrition intervention trials and to enhance the success rate of an investigational product or dietary supplement, a good understanding of the formulation’s in vitro performance is crucial, as the release profiles will greatly affect the timings of clinical measurements.”

Glube, N., Moos, L. von & Duchateau, G. Capsule shell material impacts the in vitro disintegration and dissolution behaviour of a green tea extract. Results Pharma Sci. 3, 1–6 (2013)

Pfizer/Bayer Pharma describe how biorelevant dissolution testing can help predict 'Food Effects':

“The present study demonstrated that it is possible with in vitro dissolution tests to detect dosage form dependent food effects using biorelevant dissolution media. It was also shown that a reasonably accurate estimation of the physiological solubility, as can be found in biorelevant dissolution media, is necessary for obtaining physiologically relevant and therefore predictive dissolution rates.”

Andreas, C. J. et al. Can dosage form-dependent food effects be predicted using biorelevant dissolution tests? Case example extended release nifedipine. Eur. J. Pharm. Biopharm. 105, 193–202 (2016)

GSK explains how Biorelevant Media can help predict in vivo solubility:

“Measured particle size, pH versus solubility data and solubility in biorelevant media (SGF, FaSSIF and FeSSIF) gave an accurate prediction of how the solubility of the API varies as the pH and level of surfactants varies in the gastro-intestinal tract in the fasted and fed state.”

Bloomer, J. C. et al. Identification and characterisation of a salt form of Danirixin with reduced pharmacokinetic variability in patient populations. Eur. J. Pharm. Biopharm. 117, 224–231 (2017)