FACTORS THAT AFFECT

ABSORPTION AND BIOAVAILABILITY

Seven factors affect Absorption and Bioavailability, namely:

1. Forms and solubility – Drugs given in aqueous solution are more rapidly
absorbed than those in oily solution because they mix more readily with the
aqueous phase at the absorptive site. The rate at which the drug dissolves may be
limiting factor if the drug is solid. Local conditions at the site of absorption, like
pH, can alter solubility. This is especially true in the gastrointestinal tract e.g.,
aspirin is relatively insoluble in acidic gastric contents.

2. Concentration – More concentrated solutions of a drug are more extensively

absorbed.

3. Route of administration – Parenterals (especially intravenous injections) are

more actively absorbed than orally administered drugs.

4. Blood circulation at the site of absorption – Vasoconstrictors decrease blood

flow. Shock and some diseases decrease the rate of absorption while local
application of heat and massage increase blood flow and enhance absorption.

5. Surface area available for absorption – Drugs are rapidly absorbed at sites
where epithelial membranes have large surface areas; e.g., drugs are rapidly
absorbed in the pulmonary alveolar epithelium, the intestinal mucosa and, in
cases of extensive application, the skin. Absorption in the stomach is not as rapid
or extensive.

6. Presence of food and other drugs.

7. Changes in liver metabolism caused by dysfunction and inadequate blood

supply