Introduction to Pharmacology by Mannfred A. Hollinger

By Mannfred A. Hollinger

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In addition to surface area, other important factors include drug solubility (drugs must dissolve before absorption), particle size, contact time with the absorption surface, membrane integrity, and hydrogen ion concentration (pH). Materials that are insoluble or only slightly soluble in both polar and nonpolar media are pharmacologically inert. For example, barium sulfate is a highly toxic material if absorbed into the body. However, because of its poor solubility in the GI tract, it can be swallowed and used as a contrast medium for radiography in this region without toxicological hazard.

However, it should be appreciated that bioavailability refers ultimately to plasma concentration per se. 4 Comparative bioavailability of three oral forms of a drug. Reference is serum level of the drug administered in its intravenous (IV) form. Source: Pharmacia and Upjohn, Pharmacokinetics Applied to the Treatment of Asthma. Reprinted with permission. © 1997, 2003 Taylor & Francis 34 Pharmacokinetics equivalence, which deals with comparable efficacy and safety (issues to be addressed in subsequent chapters).

The processes of distribution can be considered in terms of compartments. Absorption of a drug into the theoretical central or main compartment may be followed by distribution into one or more peripheral compartments, or the drug may undergo excretion or metabolism from the central compartment. While compartmental analysis of drug distribution can be informative, it is beyond the scope of this book. For more details on the effect of multicompartmental distribution of a drug on pharmacokinetics, see references in the Bibliography.

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