Excipient pharmacokinetics and profiling.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Pharmacokinetics

Background:

• Novel pharmaceutical excipients are new chemical entities requiring extensive safety evaluations, leading to high costs and long development times.
• Current development processes for new excipients and drug delivery systems are hampered by the expense and risk associated with safety studies.

Purpose of the Study:

• To explore the application of predictive methods, commonly used for drug candidates, to assess pharmacokinetic and ADME properties of novel excipients.
• To demonstrate how established tools like the Rule-of-Five and Biopharmaceutics Classification System can guide the development of new excipients and delivery systems.

Main Methods:

• Review of pharmacokinetic properties of currently used pharmaceutical excipients.
• Application of simple predictive methods based on physicochemical properties, such as the Rule-of-Five and Biopharmaceutics Classification System.
• Adaptation of drug-centric prediction models for excipient development objectives.

Main Results:

• Physicochemical-based prediction methods can be adapted to estimate pharmacokinetic and ADME properties of novel excipients.
• The objectives for excipients differ from drugs, focusing on reduced bioavailability and enhanced elimination rather than maximized absorption.

Conclusions:

• Simple predictive methods offer a valuable approach for the early assessment of novel excipients and drug delivery systems.
• This strategy can significantly streamline the development process, reducing costs and timelines for new pharmaceutical innovations.