Targeting Colon Delivery with OralogiK™
BDD's patent protected OralogiK timed-release technology enables consistent pH-independent delivery of drugs targeted to the colon.
Exploiting the well documented transit times through the GI tract, OralogiK tablets can be designed to release the drug at a target time after dosing which will promote release in the colon.
OralogiK™ is a tablet-in-tablet technology in which an erodible barrier layer is compressed around a drug containing core tablet. The barrier layer erodes at a constant rate throughout the GI tract, unaffected by variables such as agitation and pH until the core tablet becomes exposed and the contents are released.
The erosion mechanism ensures that at the point of release, the barrier layer is no longer present and will not impede release from the core. This is important for facilitating complete release from the tablet core in the colonic environment where there is minimal agitation and only small pockets of fluid.
The OralogiK™ platform has been designed to work independently of GI tract variables such as agitation and pH which is critical for consistent performance in healthy and diseased populations. The diagram below shows how the GI tract varies between healthy individuals and IBD patients. Using a pH independent system ensures that the product performs as designed every time.
Redrawn after Hua S, Marks E, Schneider JJ, Keely S. Advances in oral nano-delivery systems for colon targeted drug delivery in inflammatory bowel disease: selective targeting to diseased versus healthy tissue. Nanomedicine. 2015 Jul;11(5):1117-32. doi: 10.1016/j.nano.2015.02.018. Epub 2015 Mar 14. PMID: 25784453.
Here the schematic shows how the OralogiK™ tablet travels throughout the GI tract.
The enteric coating ensures the erosion does not start until the tablet leaves the stomach, removing the variability of gastric emptying times.
Release in the colon can also be achieved using an uncoated tablet, simply by increasing the delay time of the erodible layer.
The erodible layer is designed to delay the release of the core tablet until it reaches the colon.
BDD have successfully demonstrated colon targeted delivery in a number of clinical studies with a range of different APIs. In each case, delivery to the colon was demonstrated using gamma scintigraphic imaging which allows visualisation of release and dispersion from the core tablet in the colon.
Clinical Evaluation 1 - Enteric Coating
Enteric coated tablets with a 5 hour OralogiK™ delay, for targeting ascending colon / transverse colon were tracked via scintigraphy. This study was performed in fasted healthy volunteers.
10/10 dosages released in the colon
5 released in the ascending colon
4 released in the transverse colon
1 in the descending colon
Clinical Evaluation 2 - 7 Hour Delay
Uncoated tablets with a 7 hour OralogiK™ delay, for targeting ascending colon / transverse colon were tracked via scintigraphy. This study was performed in fasted healthy volunteers.
10/11 dosages released in the colon
6 released in the ascending colon
3 released in the transverse colon
1 in the descending colon
1 in the terminal ileum
OralogiK™ provides a robust means of colon delivery of API. The timed release layer acts independently of the drug contained in the core, making it suitable for most APIs. Development and clinical demonstration of performance by gamma scintigraphic imaging can be achieved in less than 9 months.
Why Choose OralogiK™ for Colonic Delivery?
Consistent performance, independent of GI tract variables
Erosion during GI transit ensures unimpeded release on reaching the colon
When combined with enteric coating eliminates variability of gastric emptying
Independent of pH and agitation