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[2] [3] However, when a medication is administered via routes other than intravenous, its bioavailability is lower due to intestinal epithelium absorption and first-pass metabolism. Thereby, mathematically, bioavailability equals the ratio of comparing the area under the plasma drug concentration curve versus time (AUC) for the extravascular ...
Temperature may affect metabolic transformation, and bioenergetics. An example of this is the movement of the organism may change as well as rates of excretion. [15] If a contaminant is ionic, the change in pH that is influenced by a change in temperature may also influence the bioavailability [1]
Biological half-life (elimination half-life, pharmacological half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration (C max) to half of C max in the blood plasma.
For a response of 0.25a.u., Drug B is more potent, as it generates this response at a lower concentration. For a response of 0.75a.u., Drug A is more potent. a.u. refers to "arbitrary units". In pharmacology , potency or biological potency [ 1 ] is a measure of a drug's biological activity expressed in terms of the dose required to produce a ...
First-pass metabolism may occur in the liver (for propranolol, lidocaine, clomethiazole, and nitroglycerin) or in the gut (for benzylpenicillin and insulin). [4] The four primary systems that affect the first pass effect of a drug are the enzymes of the gastrointestinal lumen, [5] gastrointestinal wall enzymes, [6] [7] [8] bacterial enzymes [5] and hepatic enzymes.
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 ...
Formulation studies then consider such factors as particle size, polymorphism, pH, and solubility, as all of these can influence bioavailability and hence the activity of a drug. The drug must be combined with inactive ingredients by a method that ensures that the quantity of drug present is consistent in each dosage unit e.g. each tablet.
Factors such as poor compound solubility, gastric emptying time, intestinal transit time, chemical instability in the stomach, and inability to permeate the intestinal wall can all reduce the extent to which a drug is absorbed after oral administration. Absorption critically determines the compound's bioavailability.