Advancing active pharmaceutical ingredients (APIs) through the drug product-development lifecycle is fraught with challenges. Development timelines are tight, so it’s crucial to determine early in the process if an API is a viable candidate for clinical testing. Given the increased complexity of most API molecules in development pipelines, it’s likely that these new compounds may have physicochemical or environmental constraints that require extra processing steps to produce a viable dosage form.
A key tool that has emerged to address these combined issues of tight timelines and complex molecules is precision powder micro-dosing in capsules. This development tool makes it possible to quickly get formulations to the clinic, saving time, money, and use of limited API, while avoiding premature termination of otherwise promising APIs.
This paper describes the use of precision micro-dosing to prepare API powder-in-capsule (PIC) dosage forms for oral or pulmonary administration. These PIC dosage forms reduce early-stage evaluation time (in Phase I and II) in part by reducing the need for formulation steps, such as excipient compatibility testing or tablet development. PIC studies have also proven a useful evaluation method for high-potency, low-dose applications where accurate micro-dosing is required. Case studies are presented.