Development of New Excipients

Excipient Innovation Through Precompetitive Research

“…Typically, a novel excipient generally takes 6-7 years to develop, 3-4 years to be incorporated into an approved drug product, and an additional years to have a pharmacopeial compendial monograph issued. The whole process takes on average ~ 12 years (13). The true cost of this process is hard to specify, as the development of novel excipients and novel APIs are often tied together.…”

“…Also, makers of generic drugs are disincentivized to use novel excipients because drug products that contain novel excipients are ineligible for the ANDA pathway (5). Overall, drug makers often avoid using novel excipients to minimize regulatory risk; the consequence of avoiding the use of novel excipients could result in developing suboptimal products, or even discontinuation of drug development programs (11,13).…”

“…With biologics in mind, we suggest that precompetitive excipient research could have the biggest impact if directed towards mechanistic studies of the functions of excipients in biologics. Excipient selection is often ad hoc, based more on the experience of the formulator and prior usage in foods, cosmetics and other drugs (13,22) than on fundamental understanding of the underlying mechanisms of the function of an excipient. Mechanistic understandings of excipient-API interactions and excipient-excipient interactions may guide the development of novel excipients as well as the selection of recognized excipients.…”

In Silico Investigation of First-Pass Effect on Selected Small Molecule Excipients and Structural Dynamics of P-glycoprotein

“…According to Kolter and Guth, 3 drug delivery systems often require highly functional excipients to achieve the targeted product properties. There are 3 types of excipients based on development approaches: (a) modified excipients (existing physical or purity has been changed)—examples include Kollidon VA 64 Fine, Polyplasdone Ultra, and Tween 80 HP; (b) coprocessed excipients (excipients are formulated to yield new combination)—examples include Aquarius, Ludiflash (Mannitol–Polyvinylacetate–Crospovidone), and StarCap 1500; and (c) novel excipients (chemical entities newly discovered)—examples include Captisol, Kollicoat IR, and Soluplus.…”