The pharmaceutical industry has shown significant interest in controlledrelease dosage forms due to their ability to improve pharmacological therapy by
providing prolonged and regulated drug administration. The pharmacokinetic
properties of a medicine are essential in establishing its efficacy and safety in a
therapeutic setting. Controlled-release dosage forms offer significant advantages, such
as reduced dosing frequency, improved patient compliance, and fewer adverse effects.
To maximize the use of these benefits, it is critical to understand the complex interplay
between formulation design, pharmacological properties, and controlled release
systems pharmacokinetics. This chapter examines the pharmacokinetic aspects of
controlled-release formulations, providing insight into their drug-release methods,
absorption, distribution, metabolism, and excretion. The chapter also delves into the
various elements that influence the rate of drug release from controlled-release dosage
forms. These aspects include mechanisms such as diffusion, dissolution, and erosion.
This study also investigates the impact of these mechanisms on medication absorption
in the gastrointestinal tract and their influence on the drug's pharmacokinetic
characteristics. Furthermore, the chapter emphasizes the importance of employing
modeling and simulation approaches to predict the behavior of pharmaceuticals
released from controlled-release formulations. Furthermore, the chapter undertakes an
endeavor to examine the impact of pharmacokinetic parameters on the dosing schedule,
therapeutic monitoring, and methods to enhance bioavailability. The chapter also
discusses the importance of tailored drug delivery methods for specific patients, as well
as the potential of personalized medicine. Understanding the pharmacokinetic
parameters of controlled-release formulations is critical for optimizing pharmaceutical
treatment. Gained knowledge can guide the development of innovative drug delivery
methods, enhance patient outcomes, and accelerate pharmaceutical sector
advancements
Keywords: Absorption, Distribution, Drug action, Excretion, Metabolism, Pharmacokinetic, Plasma drug concentration, Steady state.