European Patients’ Academy

on Therapeutic Innovation
http://www.eupati.eu

Fact Sheet: Bioavailability Examples

Example 1: Penicillin
Today, a certain type of penicillin is only available via IV injection. However, such IV
treatment must be administered at the hospital. To make it easier and possible to treat
patients while at home, a company has now developed a tablet containing penicillin. The
company would like to make the tablet available to patients. Before doing so, the regulatory
authorities request the company to compare the effect of the tablet with the commonly used
injection. They want to test bioavailability of the compound in the new formulation.

If you want to know the absolute bioavailability of an active substance you compare the
absorption from an oral medicine with that of an intravenous injection. Intravenous
bioavailability is used as a reference, as intravenous administration results in 100%
bioavailability. In contrast, when you take a tablet, only part of the active substance will be
absorbed and be available in the bloodstream. A mathematical equation exists to compare
the bioavailability of intravenous injection and of a tablet giving the absolute bioavailability.

Example 2: Asthma
Brian suffers from breathing problems when playing football. The doctor would like Brian to
be able to treat future asthma attacks himself, and considers giving Brian either tablets or an
asthma spray (via an inhaler), both containing the same active substance. But which
parameters do you think will affect the relative bioavailability?

What you have to consider is that Brian has trouble breathing, so he needs the active
substance to reach the target site in the body as fast as possible. The target site for asthma
medication is the lungs.1 Let’s forget everything about side effects and personal preferences
for receiving an injection versus taking a tablet (i.e. route of administration) for a minute and
focus only on bioavailability. We have already talked about absolute bioavailability when we
compared the AUC for intravenous injection versus a tablet. Now we want to compare two
formulations containing the same active substance, but administered via different routes: an
inhaler versus a tablet

The absolute bioavailability of inhalation relative to a tablet is 167%. You can therefore
conclude, that for this example more active substance from the inhalation spray reaches the
target site compared to the tablet. Most likely, this is due to a high degree of first pass

1
 European Patients’ Academy
on Therapeutic Innovation
http://www.eupati.eu

metabolism of the substance upon oral administration. Consequently, Brian should be

advised to use the inhaler. Another advantage of using the inhaler in this situation, where the
target site is the lungs, is that the inhaler will administer the active substance locally at the
site of action. Contrary, a tablet needs to be dissolved in the gastrointestinal tract before
uptake can take place. Uptake would result in the presence of the substance in the systemic
circulation; hence increase the risk of systemic side effects. When an active substance is
administered locally, the fraction of active substance that reaches systemic circulation is
minimized, and so is the risk of systemic side effects.

References
1
Labiris, N.R. and Dolovich, M.B. (2003). Pulmonary drug delivery. Part I: Physiological
factors affecting therapeutic effectiveness of aerosolized medications. British Journal of
Clinical Pharmacology, 56, 588–599. Retrieved 23 June, 2015, from
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1884307/pdf/bcp0056-0588.pdf