Dual Capsule Peptide Delivery via Segmentation and Nesting
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Solution Overview
Problem
Oral administration of peptide pharmaceuticals is challenging due to degradation by proteolytic enzymes in the digestive system, leading to low bioavailability, and existing solutions are complex, costly, and unstable during storage.
Innovation Solution
A single dosage form comprising two capsules, where an inner enteric or non-enteric capsule containing a peptide agent and an absorption enhancer is enclosed within an outer enteric capsule filled with an organic acid, ensuring spatial separation and controlled release in the intestines to protect the peptide from degradation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If the peptide agent is intermixed with pH lowering agents (organic acids) in the same compartment, then the peptide is protected against stomach proteases, but the peptide stability deteriorates due to constant contact with acids during storage
Solution Approach 1:
The invention divides the dosage form into two separate compartments: an inner water-soluble capsule containing the peptide agent and an outer enteric capsule containing the organic acid. This segmentation prevents contact between the peptide and acid during storage while ensuring both are released together in the intestine to protect the peptide from stomach proteases.
Solution Approach 2:
The inner water-soluble capsule is nested within the outer enteric capsule. The inner capsule dissolves first in the intestine, releasing the peptide, while the outer enteric capsule provides continued acid protection. This nested structure ensures sequential release that maintains peptide stability while providing protease protection.
2Stability of the object's composition
If complex manufacturing processes (spray fluid bed, layered tablets with coating) are used to protect peptide stability, then peptide protection is improved, but manufacturing cost and equipment complexity increase
Solution Approach 1:
The invention uses two simple, separately manufactured capsules instead of complex coated tablets or spray-fluidized beds. Each capsule can be produced using standard capsule-filling equipment, avoiding the need for specialized coating or layering machinery while achieving the same protective function.
Solution Approach 2:
The invention employs conventional, readily available capsule forms rather than expensive specialized delivery systems. The simple capsule structure can be manufactured with basic equipment, making the process cost-effective and avoiding investment in complex manufacturing infrastructure.
3Ease of manufacture
If the peptide is subjected to mechanical stress during tablet manufacturing, then the dosage form is compacted, but peptide stability deteriorates
Solution Approach 1:
The invention uses flexible, water-soluble capsule shells that can be easily filled with peptide powder without subjecting the peptide to compressive forces. The capsule structure provides containment without mechanical stress, preserving peptide integrity while achieving a compact, portable dosage form.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
This approach enhances bioavailability by minimizing peptide degradation and simplifies the manufacturing process, avoiding the need for expensive equipment and reducing mechanical stress, resulting in higher and more stable peptide delivery compared to existing methods.
Implementation Method 1
an outer enteric capsule which surrounds the inner capsule and comprises an enteric capsule coating
Implementation Method 2
comprises at least one organic acid; lowering the local intestinal pH substantially below the pH optima for proteases
Implementation Method 3
comprises at least one absorption enhancer effective to promote bioavailability of said active agent
Data Source
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AI summary
Present invention refers to a pharmaceutical single dosage form for oral delivery consisting of two capsules, an outer enteric capsule, and an inner capsule, wherein said inner capsule comprises at least one physiologically active peptide agent and at least one absorption enhancer, and wherein said outer capsule contains inner capsule and an organic acid.