GLP-1 Peptide Tablet Spray-Drying With pH-Controlled Dissolution
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Solution Overview
Problem
Human GLP-1 peptides exhibit low bioavailability and require advance administration to ensure absorption, limiting their effectiveness in oral dosage forms.
Innovation Solution
A spray-drying process is employed to produce GLP-1 peptide tablets by adjusting the pH of the feed solution to be higher than the isoelectric point or within a specific range (about 5 to 10), resulting in enhanced dissolution rates and improved bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If GLP-1 peptides are administered orally in conventional dosage forms, then the drug can be taken conveniently, but the bioavailability remains low and absorption is delayed
Solution Approach 1:
The patent changes the pH parameter of the feed solution during spray-drying to be higher than the isoelectric point of the GLP-1 peptide (pH > 4.6). This parameter change modifies the peptide's charge state and interaction with the spray-drying environment, resulting in improved dissolution rate and bioavailability while maintaining oral administration convenience
Solution Approach 2:
The patent utilizes the spray-drying process to transition the GLP-1 peptide from a liquid feed solution phase through rapid drying to form a solid powder tablet. This phase transition process, combined with pH control, creates a formulation that enhances dissolution and absorption characteristics
2Reliability
If GLP-1 peptides are administered orally, then the drug can be absorbed, but the dissolution rate is slow and absorption is delayed
Solution Approach 1:
By adjusting the feed solution pH to be higher than the isoelectric point during spray-drying, the patent modifies the peptide's surface charge and interaction properties, which directly enhances the dissolution rate and reduces the time required for absorption
Solution Approach 2:
The patent performs preliminary pH adjustment and spray-drying processing before tablet formation, pre-conditioning the peptide to have improved dissolution characteristics that will manifest during subsequent absorption in the gastrointestinal tract
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
The process increases the dissolution rate of GLP-1 peptides, allowing for faster absorption and improved therapeutic efficacy by shortening the time between administration and meal intake.
Implementation Method 1
spray-drying a feed solution comprising the GLP-1 peptide and a feed solution solvent
Implementation Method 2
spray-drying a feed solution comprising the GLP-1 peptide and a feed solution solvent
Data Source
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AI summary
The present invention relates to a process for producing a tablet comprising a GLP-1 peptide wherein the GLP-1 peptide is obtained by spray-drying of a feed solution comprising the GLP-1 peptide and a feed solution solvent, wherein the pH of the feed solution is higher that the pI of the GLP-1 peptide or wherein the pH of the feed solution is in the range of about 5 to about 10. The invention also relates to the tablet obtained by said process and the use of said tablet in medicine.