Extemporaneously prepared controlled release formulations for accelerating the early phase development of drug candidates

Abstract

Extemporaneous drug preparations, which are compounded by a pharmacist at a clinical site, are commonly used in early clinical studies to evaluate the performance of drug candidates. However, the types of formulations compounded have been limited to relatively simple preparations such as solutions, suspensions and active ingredients filled into capsules. This article describes the preparation of advanced formulations, specifically extemporaneously prepared matrix tablets and osmotic capsules, which can be used to evaluate the feasibility of controlled release for exploratory new drug candidates or new formulations of existing drugs with a differentiated medical advantage. Extemporaneously prepared dosage forms enable the rapid assessment (i.e. reduced cycle time) of new formulation ideas with minimal quantity of the active pharmaceutical ingredient needed to demonstrate proof-of-concept.