Causes of incomplete bioavailability
a- Route of administration
Generally parenteral administration produce higher bioavailability compared to oral or rectal administration.
Drug absorption is usually faster in areas that are rich in blood supply. For example IM administration results in faster drug absorption compared to subcutaneous administration because the skeletal muscles are supplied with more blood compared to subcutaneous tissues. Also, buccal absorption is very fast.
b- Factor related to the formulation.
Although it is not a general rule, the bioavailability of an oral solution is > oral suspension > capsule > tablet.
c- Factors related to the drug.
The physicochemical properties of the drug determine its solubility and dissolution rate which are major factors in determining the drug bioavailability.
The lipophilic/hydrophilic properties of the drug are very important in determining the ability of the drug to cross the biological membrane at the absorption site to reach the systemic circulation.
Stability of the drug at the site of administration is an important factor in determining the drug bioavailability.
d- Factors related to the patient.
Physiological factors such as gastric pH, gastric emptying rate, and gastric motility can significantly affect drug bioavailability.
Gastrointestinal diseases and aging usually affect the drug absorption process
Some drugs such as chemotherapeutic agents and phenytoin can decrease the absorption of other drugs after oral administration.
Bioavallability is a measure of the fraction of the administered dose that reaches the systemic circulation.
Absolute bioavailability is the fraction of the total dose that reaches the systemic circulation. It can have values between zero when the drug is not absorbed at all to 1 when all the administered dose reaches the systemic circulation. The absolute bioavailability can be expressed in terms of percentage (0% - 100%).
The relative bioavailability is the bioavailability of a drug product relative to the bioavailability of another drug product (reference standard preparation). The relative bioavailability can have any value above zero. It can be more than one when the product under investigation has bioavailability higher than that of the reference standard.