ABSTRACT

The original controlled release pharmaceuticals were coated pills, and they date back over 1000 years to Greco-Roman antiquity. In the late 1940s and early 1950s, the first so-called sustained release products appeared as a major new class of pharmaceutical products in which product design was intended to modify and improve drug performance by increasing the duration of drug action and reducing the required frequency of dosing. Increasingly an objective of effector controlled delivery is not only to specifically maximize duration of action, but also to reduce toxicity and improve safety. Drug and drug product effectiveness may most meaningfully be assessed by determining how well the product relieves the disease or condition for which the drug is intended. The equilibrium aqueous solubility of a drug can mislead a pharmaceutical development scientist into thinking no problem exists where a major solubility problem may in fact exist.