From the Research
Sermorelin has extremely poor oral bioavailability, effectively zero percent, which means it cannot be taken by mouth as a viable treatment option. This GHRH analogue is a peptide hormone that would be rapidly degraded by digestive enzymes in the gastrointestinal tract and would not be absorbed intact into the bloodstream 1. Due to this limitation, sermorelin must be administered via injection, typically subcutaneously, to achieve therapeutic effects. The standard administration method is through subcutaneous injections, usually given daily, often at bedtime to mimic natural growth hormone release patterns.
Some key points to consider:
- The poor oral bioavailability of sermorelin is common among peptide medications because their large molecular size and chemical structure make them unsuitable for passing through the intestinal wall intact 2.
- Additionally, the acidic environment of the stomach would denature and break down the peptide before it could be absorbed 1.
- Various technologies have been explored to overcome the problems associated with the oral delivery of macromolecules, but with limited success 1, 2.
- The use of polymeric particulate systems to improve the oral absorption of peptide drugs has been investigated, but the development of a satisfactory oral formulation remains a challenge 2.
- Recent advances in drug discovery have led to the development of design and testing strategies and formulation options to optimize oral bioavailability, but these are not applicable to sermorelin due to its peptide nature 3.
Overall, the oral bioavailability of sermorelin is effectively zero percent, and it must be administered via injection to achieve therapeutic effects.