Prodrugs

What are prodrugs? Not all active pharmaceutical ingredients are directly active. Some must first be converted to the active substance by an enzymatic or non-enzymatic conversion step in the body. These are the so-called . The term was introduced by Adrien Albert in 1958. It is estimated that up to 10% of all active ingredients … Prodrugs

Volume of Distribution

Definition and examples When a drug is administered, for example, a tablet is swallowed or an injection is injected into a vein, the active pharmaceutical ingredients subsequently spread throughout the body. This process is called distribution. Active ingredients distribute throughout the bloodstream, into tissues, and are eliminated through metabolism and excretion. Mathematically, the volume of … Volume of Distribution

Plasma Concentration

Definition Plasma concentration is the concentration of a pharmaceutical agent in blood plasma at a given time after administration. Plasma is the liquid portion of blood excluding its cellular components. Concentration is typically expressed in µg/ml. Plasma concentration-time curves If plasma levels are measured several times after administration, a plasma concentration-time curve can be constructed … Plasma Concentration

Bioavailability

Definition and properties When we take a tablet or capsule, it contains a defined amount of an active pharmaceutical ingredient. Usually, the full dose does not enter the bloodstream. Some active ingredients are not fully released from the dosage form (liberation), others are only partially absorbed from the intestine (absorption), and some are metabolized in … Bioavailability

Release (Liberation)

Definition After a drug is ingested, it passes through the esophagus into the stomach and into the small intestine. There, the active ingredient must first be released from the dosage form. This is the prerequisite for it to be absorbed into the bloodstream via the cells of the mucosa. The dosage form thus exerts a … Release (Liberation)