Selection of Excipients Based on the Biopharmaceutics Classification System of Drugs

Abstract

Active agents have been considered the main ingredients of any therapeutic product since the early ages of formulation technology. However, the importance of the inactive ingredients has been realized during the last three decades. With the development and manufacturing of more intelligent and multifunction excipients, new ways became available for formulation technologists to increase the beneficial effects of drugs on human body. Many modern active agents have internal characteristics that significantly decrease their potential and theoretical bioavailability; however, today we have the widest variety of inactive ingredients that we can utilize in order to change these properties. The careful and educated selection of excipients might significantly influence the effect of the drugs, including hastening or delaying their onset of action, increasing their bioavailability by changing their physicochemical characteristics, and increasing their stability. In this chapter, we focus primarily on the factors determining and influencing bioavailability as well as the selection of excipients for formulating new dosage forms with enhanced therapeutic efficacy, based on the physicochemical properties of drugs. We will provide some examples from the scientific literature to demonstrate the achievements in this multidisciplinary area.

Pharmaceutical nanococrystal synthesis: a novel grinding approach

“…4,5 According to the biopharmaceutical classification system (BCS), adopted by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) as the basis for granting API biowaivers, 6,7 drugs included in class II present high permeability but low aqueous solubility, which impacts their oral bioavailability. [8][9][10] Many researchers have proven that by inducing structural modifications in the API solid forms, it is possible to increase the aqueous solubility and dissolution rate of drugs while maintaining their biological activity. [11][12][13][14] Among the referred structural modifications, cocrystal formation has emerged in the past two decades as an attractive way to modify the desired physicochemical properties since they allow crystalline structure modifications without making and/or breaking covalent bonds.…”