Characterization Requirements for New Excipients

Novel excipients can play a major role in innovation processes, but physicochemical properties, performance and safety must be adequately demonstrated. Characterization requirements for novel excipients are discussed and illustrated with two examples, polyethyleneglycol-polyvinyl caprolactam polyvinyl acetate grafted copolymer (Soluplus®) and methyl methalcrylate and diethylaminoethyl methacrylate copolymer dispersion (Kollicoat® Smartseal 30 D).

Introduction: 

With the recent advancements in pharmaceutical technology, drug formulations have evolved from traditional medicinal products into drug delivery systems. This progress was brought forward with the use of new technologies in the pharmaceutical industry as well as by the introduction of new or novel excipients.

ICH Guideline M4Q defines an excipient to be novel if it is used for the first time in a drug product of if it is used a new route of administration. Regulatory filings should include full details of manufacture, characterization and controls, with cross references to supporting safety data (nonclinical and/or clinical) according to the drug substance format. But excipients as such are not approved or rejected by health authorities. They are reviewed only in the context of a drug product application. This puts a significant regulatory burden on the excipient user, particularly in Europe, due to the lack of an excipient master file system.

Novel excipients require a thorough characterization with focus on three aspects:

• Functionality: Performance in the drug product e.g. drug delivery properties.
• Physiochemistry: Chemical assessment including physicochemical properties, impurities and stability.
• Safety: Toxicological assessment very similar to new active ingredients.

The development of a novel excipient requires a strong commitment of the manufacturer.

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