RESEARCH ARTICLES
Influence of First-Pass Effect on Availability of Drugs on Oral Administration

https://doi.org/10.1002/jps.2600600909Get rights and content

Abstract

Currently used pharmacokinetic models assume that drug administered both intravenously and orally initially enters the same vascular pool. However, literature data suggest that although a drug is completely absorbed, the area under the plasma level—time curve after oral administration may be considerably less than the corresponding area following intravenous therapy. This has been explained on the basis of a “first-pass” effect in the liver. Simple equations have been derived, allowing prediction of the extent of this first-pass effect for a particular drug. Plasma level data for propranolol in man have been used to indicate the utility of these equations. The significance of these calculations to the design of clinical studies with new drugs intended for oral use is discussed.

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