The stability of a drug directly affects the dose a patient receives. The dose received depends on the way the compound is metabolised or accumulated in the body. This metabolism is a key determinant of drug bioavailability. A drug that is rapidly metabolised may require multiple daily dosing or continuous infusion to maintain a concentration in the bloodstream or target organ that is sufficient to elicit a therapeutic effect. However, a slowly metabolised drug may remain in the body for long periods, potentially causing toxic build-up. Hepatocytes may provide a model more representative of the in vivo drug stability situation. Hepatocytes contain a cell membrane and do not require additional co-factors.
Hepatocytes contain enzymes for both phase I (oxidation, reduction and/or hydrolysis of test compound) and phase II (conjugation of test compounds or metabolites) metabolism. Browse the LGC Standards hepatocyte offering here. |