Vol. 7, Issue 2, Part J (2025)

Developing a formulation to achieve the preferred target release to match the kinetics is expected to be the mainly important part of biopharmaceutics1. Innovators have a challenge to maintain the desired concentration of the drug plasma within the targeted therapeutic window to be effective as classified by the biopharmaceutical needs. Thus, the need for variety of delivery strategies and dosage forms has risen over the years. Models of pharmacodynamics and pharmacokinetics are defined to provide an understanding of the involved dynamics of time-course for the concentration of drug and planned target release which are adopted for finalizing the formulation development objectives. Out of several factors, few are closely related to the pharmacokinetics which were accomplishing the input flux of drug and reaching to the desired concentration time profile. A detailed consideration of these two parameters and studying the properties of drug is important to strategize the formulation development. Formulating a controlled release dosage form to achieve the desired input flux of drug is planned to be the biggest test. Also, developing pulsatile delivery formulations is considered as the still bigger challenge. For designing a successful controlled release delivery system the target is to achieve satisfactory input drug flux which is considered to be the greatest challenge. Some of the controlled release delivery dosage forms or systems even face a bigger design challenges, like the pulsatile drug delivery systems. The physiological processes ideally manage the drug disposition the body, but several pharmacokinetic parameters are still considered for evaluating drugs which could be considered as candidates for developing the controlled release delivery systems. Along with the drug potency, other pharmacokinetic parameters like systemic clearance, volume of distribution, and elimination rate constant or half-life can provide useful information in designing of the delivery systems. Half-life is considered to be an important link and hence could be considered in the design between systemic clearance and volume of distribution and controlled release delivery systems. Half-life is a good indicator how quickly systemic clearance can be intentionally modulated in either upward or downward direction.