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Theoretical and computational basis for drug bioavailability determinations using pharmacological data. I. General considerations and procedures

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Abstract

The use of data deriving from monitoring the time variation of the intensity of pharmacological effect(s) following dosing can often present an advantageous alternative to the more conventional approach of using chemical or radiological assay of blood and/or urine level data for bioavailability evaluations of drug products: bioavailability studies can be performed with drugs where no assay exists. A relatively simplified discussion of the general theoretical principles on which the use of pharmacological data is based and a stepwise description of the approach for its routine application in bioavailability studies are presented. Approaches for computing rates and extents of drug bioavailability vs. time profiles on analog and digital computers are qualitatively described and quantitatively presented in a subsequent report. The concept of preabsorption (gastrointestinal bioavailability) is introduced and biophasic availability of drugs to local sites of action is discussed.

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Research supported by Food and Drug Administration Contract No. 223-73-3026, Alcon Laboratories, Fort Worth, Texas, and the Purdue Biomedical Engineering Center.

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Smolen, V.F. Theoretical and computational basis for drug bioavailability determinations using pharmacological data. I. General considerations and procedures. Journal of Pharmacokinetics and Biopharmaceutics 4, 337–353 (1976). https://doi.org/10.1007/BF01063123

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