Absorption from the gastrointestinal tract of the peptide hormone Calcitonin

Preliminary studies demonstrate absorption from the gastrointestinal tract of the peptide hormone Calcitonin by use of Egalet^® controlled release technology.
The 3K burst Egalet^® technology has been tested for oral administration of the synthetic salmon calcitonin peptide in a pilot study in humans, and absorption of calcitonin indicative for future oral administration of pharmaceutically active dosages has been demonstrated by blood tests. A new study will be set up to confirm the data.

The 3K Egalet^® technology is a 3-component time-release model (consisting of coat, matrix and a lag built into the matrix) resulting in release of the active substance with a predetermined burst. In the present case, the peptide burst was predetermined with respect to duration from administration to release in order to reach the ileoceacal junction where absorption was believed to take place.

To verify where the burst actually took place in the subjects, a scintigraphic image was obtained identifying radio-labelled lactose incorporated into the matrix whereby the position in the intestines upon release could be identified in the eight volunteers. In the subjects where the release took place close to the ileoceacal junction, a rise in plasma concentrations of calcitonin was observed, and in two subjects where the release took place in the jejunum or upper ileum, no increase in plasma concentration was observed.
Accordingly, the present study demonstrates that the 3K Egalet^® technology will be useful for the delivery of peptides which is only absorbed if presented to the right segments of the intestines. In addition to the Egalet^® technology used in the present study, the release target can be further improved by use of a pH sensitive matrix in the system and the absorption increased by incorporation into the formulation of enhancers.