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In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. [1]By definition, when a medication is administered intravenously, its bioavailability is 100%.
Absolute bioavailability refers to the bioavailability of a drug when administered via an extravascular dosage form (i.e. oral tablet, suppository, subcutaneous, etc.) compared with the bioavailability of the same drug administered intravenously (IV). This is done by comparing the AUC of the non-intravenous dosage form with the AUC for the drug ...
At a practical level, a drug's bioavailability can be defined as the proportion of the drug that reaches the systemic circulation. From this perspective the intravenous administration of a drug provides the greatest possible bioavailability, and this method is considered to yield a bioavailability of 1 (or 100%).
The bioavailability of those products is limited by their solvation rate. A correlation between the in vivo bioavailability and the in vitro solvation can be found. Class III – low permeability, high solubility . Example: cimetidine; The absorption is limited by the permeation rate but the drug is solvated very fast.
Oral bioavailability of many vulnerable drugs appears to be increased in patients with compromised liver function. Bioavailability is also increased if another drug competing for first-pass metabolism enzymes is given concurrently (e.g., propranolol and chlorpromazine).
Lipinski's rule of five, also known as Pfizer's rule of five or simply the rule of five (RO5), is a rule of thumb to evaluate druglikeness or determine if a chemical compound with a certain pharmacological or biological activity has chemical properties and physical properties that would likely make it an orally active drug in humans.
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Drug permeability, together with drug aqueous solubility are the two parameters that define the fate of the active ingredient after oral administration and ultimately define its bioavailability. [1] When drug permeability is empirically measured in vitro, it is generally called apparent permeability (P app) as its absolute value varies ...