Bioavailability is the percentage of unchanged administered drugs reaching systemic circulation and becoming available at the site of action. On the other hand, by definition, bioequivalence (BE) indicates that when two drug products are administered to the same patient under similar conditions, will result in similar drug concentrations in the plasma and tissues. Bioequivalence services conduct BE studies for the approval of generic drug products. Thus, bioavailability and bioequivalence testing (BABE studies) are crucial components of the drug development process.
Determining the bioavailability of drugs is a necessary step in the drug discovery flowchart. Some benefits of bioavailability studies are as follows:
- Bioavailability aid in food effect studies
- It can estimate inter and intra assay variability
- It can determine the linearity of bioavailability parameters over the proposed clinical range
- Can evaluate absolute systemic bioavailability of dosages
- Bioavailability can evaluate physicochemical changes in the drug product and effects on pharmacokinetic properties.
Researchers can assess the bioavailability of drug products through direct and indirect methods. They can evaluate bioavailability by determining active drug concentration in the blood, evaluating pharmacological effects, or through cumulative urinary excretion. For drugs that are not absorbed in the bloodstream, researchers can determine the rate and extent of active ingredients present at the site of action to assess the bioavailability of the drug product.
Bioavailability depends on absorption in the gastrointestinal tract. Drugs with lower bioavailability can be poorly absorbed in the GI tract. This poor absorption will result in lower blood concentration of the active ingredient. Hence, the availability of active ingredients in the blood is a marker of active moiety present in the site of action. Let us dive deep into how researchers assess the bioavailability of drug products.
Methods for determining the bioavailability of drugs
As mentioned earlier, there are both direct and indirect ways of determining the bioavailability of drug products. The indirect method includes pharmacokinetic analysis, whereas the direct method uses pharmacodynamic methods. Let us study both these methods in detail.
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Pharmacokinetic methods or indirect methods
- Plasma drug concentration
This approach assumes that the drug plasma concentration and drug concentration at the site of action are directly related. Once a drug is administered to a patient, blood samples are withdrawn to determine the bioavailability of the drug product. It employs pharmacokinetic parameters such as Tmax, Cmax, and AUC. The plasma drug concentration method is the most widely used method for assessing bioavailability.
- Urinary drug excretion
This method studies the amount of excreted drugs through the urine. It is based on the relationship between the amount of drug excreted and the plasma drug level-time curve showing when the drug was completely eliminated from the body. As the drug concentration in the plasma reaches zero, the maximum amount of drug is excreted through the urine.
Pharmacodynamic methods or direct methods
- Acute pharmacological response
Researchers use acute pharmacological responses during inaccuracy in measuring plasma or urine drug concentration. For instance, the plasma drug concentration of topical corticosteroids may not accurately reflect the bioavailability of the drug product. Here, researchers can employ acute pharmacological response to assess bioavailability.
- Therapeutic response
This method administers a drug product and observes the clinical response to the administered drug. However, the primary disadvantage of this method is that the observed response may not quantitatively assess the bioavailability of the drug product.
