Technology

The pH triggered ColoPulse technology is an innovative coating for oral administration characterized by the incorporation of a swell-able material in the coating matrix that results in a fast and site-specific coating disintegration. This coating was invented and developed by Dr. Reinout Schellekens and prof. Dr. Erik Frijlink at the Groningen Research Institute of Pharmacy (GRIP), department Hospital and Clinical Pharmacy at the University Medical Centre Groningen (UMCG).

    1. check-mark-1Pulsatile release: Delivering APIs in the ileum and ascending colon.
    1. check-mark-1Clinically proven: In patients with colon-related diseases to offer reliable and specific release.
    1. check-mark-1Patented technology: Creating new opportunities to extend the life cycle management of drug products.

ColoPulse Drug Delivery Technology

The coating was developed to target the ileo-colonic region in humans and therefore, it was designed to improve the release efficiency of drugs treating colon-related diseases. The ColoPulse technology is an example of a pH-responsive system which in several human studies was shown to deliver a drug site-specific into the ileocolonic region. The ColoPulse system consists of a coating that dissolves at pH > 7.0, enabling drug release in the ileocolonic region. The release from the ColoPulse system is faster and more pulsatile than from other pH responsive systems because a special disintegrant is incorporated in the coating.

One of the first clinical studies with the ColoPulse coating in both healthy volunteers and CD patients confirmed that ColoPulse tablets perform comparably well. The study also showed that food and time of food intake had no influence on bio-availability. This study also showed that the ColoPulse coating is safe to use in humans. Previously, a clinical trial using a dual label isotope strategy demonstrated that release from a ColoPulse tablet in vivo is not related to transit times but occurs in the ileo-colonic region after pH 7.0 is reached.

A second group of studies showed the safety and efficacy of a new peppermint oil soft capsule formulation with ColoPulse. In a phase I study, it was shown that the results obtained from in vitro dissolution tests agree with the pharmacokinetic profiles in healthy volunteers and also confirmed the safety of the ColoPulse technology. A follow-up phase II clinical study using the same peppermint oil formulation was used to study the efficacy and safety in patients with Irritable Bowel Syndrome (IBS).Even though the study showed that peppermint oil was efficiently released in the ileo-colonic region, the study found no benefits of a targeted ileo-colonic release for peppermint oil for the treatment of IBS.

Altogether, the results confirmed that ColoPulse-coated tablets and capsules allow to target the ileo-colonic region and that is safe to use in humans. Based on the scientific findings, Colotech Pharma proposes to apply the ColoPulse technology to drugs that have already been proven effective in IBD treatment but for which the current formulations on the market have suboptimal release in the colonic region.

 

Colotech Pharma products

Colotech Pharma is developing new formulations in collaboration with the Pharmaceutical Technology and Bio pharmacy department of the University of Groningen (RUG).

Our technology has been used successfully to formulate several types of molecules of different sizes, from small ones (mesalamine, budesonide, peppermint oil or aspirin) to biologics such as infliximab (Remicade®).

Several formulations are available for licensing.