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  • Define drug product performance and biopharmaceutics.

  • Describe how biopharmaceutics affects drug product performance.

  • Define pharmacokinetics and describe how pharmacokinetics is related to pharmacodynamics and drug toxicity.

  • Define the term clinical pharmacokinetics and explain how clinical pharmacokinetics may be used to develop dosage regimens for drugs in patients.

  • Define pharmacokinetic model and list the assumptions that are used in developing a pharmacokinetic model.

  • Explain how the prescribing information or approved labeling for a drug helps the practitioner to recommend an appropriate dosage regimen for a patient.


Drugs are substances intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease. Drugs are given in a variety of dosage forms or drug products such as solids (tablets, capsules), semisolids (ointments, creams), liquids, suspensions, emulsions, etc, for systemic or local therapeutic activity. Drug products can be considered to be drug delivery systems that release and deliver drug to the site of action such that they produce the desired therapeutic effect. In addition, drug products are designed specifically to meet the patient’s needs including palatability, convenience, and safety.

Drug product performance is defined as the release of the drug substance from the drug product either for local drug action or for drug absorption into the plasma for systemic therapeutic activity. Advances in pharmaceutical technology and manufacturing have focused on developing quality drug products that are safer, more effective, and more convenient for the patient.


Biopharmaceutics examines the interrelationship of the physical/chemical properties of the drug, the dosage form (drug product) in which the drug is given, and the route of administration on the rate and extent of systemic drug absorption. The importance of the drug substance and the drug formulation on absorption, and in vivo distribution of the drug to the site of action, is described as a sequence of events that precede elicitation of a drug’s therapeutic effect. A general scheme describing this dynamic relationship is illustrated in Fig. 1-1.


Scheme demonstrating the dynamic relationship between the drug, the drug product, and the pharmacologic effect.

First, the drug in its dosage form is taken by the patient by an oral, intravenous, subcutaneous, transdermal, etc, route of administration. Next, the drug is released from the dosage form in a predictable and characterizable manner. Then, some fraction of the drug is absorbed from the site of administration into either the surrounding tissue for local action or into the body (as with oral dosage forms), or both. Finally, the drug reaches the site of action. A pharmacodynamic response results when the drug concentration at the site of action reaches or exceeds the minimum effective concentration (MEC). The suggested dosing regimen, including starting dose, maintenance dose, dosage form, and dosing interval, is determined ...

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