Pharmaceutical preparations of short-chain amino acid sequences, known as peptides, that are specifically designed for systemic therapeutic action and are administered via the oral route. These formulations utilize specialized delivery technologies to overcome the significant biological challenges of enzymatic degradation in the gastrointestinal tract and poor absorption across the intestinal epithelium. Developing effective oral delivery remains a major frontier in peptide therapeutics for improved patient compliance.
Origin
This term is a pharmaceutical and medicinal chemistry construct, combining the biochemical nature of “Peptide” drugs with the common, non-invasive route of administration, “Oral Formulation.” It addresses the long-standing clinical challenge of making traditionally injectable biologic medications available as convenient oral medications.
Mechanism
The mechanism involves various strategies to protect the peptide, such as encapsulating the peptide within protective matrices, using permeation enhancers to temporarily and safely loosen tight junctions between intestinal cells, or employing specialized protease inhibitors to shield the peptide from digestive enzymes. The ultimate goal is to deliver the intact, bioactive peptide across the intestinal barrier into the systemic circulation in a predictable and bioavailable manner.
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