The ColoPulse Technology
The ColoPulse technology offers a pH-controlled pulsatile release system. The delivery system allows for the pulsatile (fast and transient) release of a substance in response to a pH change around 7.0 (ileum). It combines a pH-sensitive polymer with a swellable agent to result in an irreversible disruption of the coating once the pH threshold has been reached. The result, fast disintegration of the coating and release of the therapeutic molecule in the ileo-colonic region.
Delivering APIs in the ileum and ascending colon
In patients with colon-related diseases to offer reliable and specific release
Creating new opportunities to extend the life cycle management of drug products
Colon-specific delivery may be achieved by a wide variety of controlled release technologies. These include programmed-release technologies (time-based erosion) or triggered-release technologies (luminal pH, bacterial enzymes or pressure). Most of these technologies show suboptimal release kinetics. The most reliable systems use a triggering mechanism related to the location of the product in the GI tract. Several studies have shown that both healthy subjects and subjects suffering from IBD show a pH drop (from 7.6 to 6.1) around the ileocecal junction, which separates the small intestine from the colon. Therefore, the intraluminal pH profile is considered to provide a reliable trigger for colon-specific delivery. Conventional pH-triggered colon-specific delivery systems, however, suffer from an incomplete release of the core substance because the pH threshold is often hardly exceeded and the time of exposure to pH values over 7.0 is often too short (
The ColoPulse technology overcomes this issue by incorporating a swelling agent in the pH-sensitive coating. This unique combination triggers the irreversible disintegration process when the pH threshold is reached, even when the threshold is only exceeded slightly and for a short amount of time. The core substance is released in a pulsatile fashion, resulting in reliable and complete delivery at the site of action. In addition, the ColoPulse technology allows to efficiently release a high concentration of a substance in the ileum or ascending colon, which can be beneficial for local treatment or can favour absorption.
Colonova is developing new formulations in collaboration with the University of Groningen (RUG) department of Pharmaceutical Technology and Biopharmacy of prof. dr H.W. Frijlink. A list of those formulations are available for licensing.