Antibody Solid Dosage Form Layering
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Solution Overview
Problem
Existing methods for preparing solid dosage forms of antibodies and functional fragments are hindered by instability and activity loss due to processing steps, excipient interactions, and unsuitable release profiles, particularly for sustained release in gastrointestinal treatments.
Innovation Solution
A method involving drug layering with an inert core unit coated using a polymeric binder and buffer in an aqueous solution or suspension, employing fluidized-bed spray coating to create a stable and controlled release formulation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional processing methods are used to prepare solid dosage forms of antibodies, then the dosage forms can be manufactured, but the stability and activity of the antibodies are compromised due to processing steps and excipient interactions
Solution Approach 1:
The patent changes the physical and chemical parameters of the processing method by using spray coating instead of traditional mixing, controlling temperature below 65°C, and using aqueous solutions with specific pH buffers. These parameter changes preserve antibody stability while enabling manufacturing.
Solution Approach 2:
The patent replaces mechanical mixing and high-shear processing with spray coating technology, which uses aerosolization and controlled deposition. This substitution eliminates mechanical stress on antibodies while achieving uniform distribution in the dosage form.
2Duration of action of moving object
If antibodies are incorporated into solid dosage forms using conventional methods, then the dosage forms can be produced, but the release profile is unsuitable for sustained release in gastrointestinal treatments
Solution Approach 1:
The patent incorporates sustained-release polymers and pH-buffering excipients into the coating formulation before the coating process. This preliminary action ensures that the coating matrix is pre-configured to provide sustained release and maintain pH stability throughout the gastrointestinal transit.
Solution Approach 2:
The patent uses composite coating formulations combining antibodies with sustained-release polymers (such as ethylcellulose, Eudragit RS/RL) and pH-buffering agents. This composite approach creates a matrix that simultaneously provides structural integrity, controlled release, and pH stability.
3Quantity of substance
If high loading of antibodies is achieved in solid dosage forms, then therapeutic efficacy is improved, but stability and activity are reduced due to concentration-dependent aggregation and degradation
Solution Approach 1:
The patent introduces pH-buffering excipients and stabilizing agents as intermediaries between the antibody molecules. These intermediaries maintain optimal pH conditions and prevent concentration-dependent aggregation, enabling high loading while preserving stability.
Solution Approach 2:
The patent creates an inert microenvironment within the coating matrix using pH buffers and protective excipients. This inert environment isolates the antibodies from destabilizing conditions, allowing high concentrations without degradation or aggregation.
4Ease of manufacture
If traditional coating methods are used to apply antibody-containing formulations, then coating can be achieved, but the antibodies are exposed to harmful factors such as high temperature and mechanical stress
Solution Approach 1:
The patent replaces traditional mechanical coating methods with spray coating technology. This substitution uses aerosolization and controlled deposition rather than mechanical mixing and spreading, eliminating shear stress and high-temperature exposure while achieving uniform coating.
Solution Approach 2:
The patent uses pneumatic spray coating technology to apply the antibody-containing formulation. The coating solution is atomized into fine droplets using compressed air and deposited onto the core particles, enabling coating at low temperatures without mechanical stress.
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 method ensures the stability and activity of antibodies during preparation, allows for optimal loading and controlled release, and achieves sustained release profiles over defined periods, enhancing therapeutic efficacy in gastrointestinal treatments.
Implementation Method 1
layering the inert core unit with the active agent coating liquid using spray coating, preferably fluidized-bed spray coating
Implementation Method 2
employing fluidized-bed spray coating to create a stable and controlled release formulation
Implementation Method 3
drying the wet drug layered inert core unit, simultaneously with step b), or after step b) has been completed, to give rise to a dried solid dosage form
Data Source
AI summary
The present invention relates to a method for preparing immediate and sustained release solid dosage forms, comprising antibodies and functional fragments thereof, by solution/suspension layering, optionally coated with a delayed release coating; the solid dosage forms prepared by the method; and the use of the solid dosage forms in the topical treatment in the gastrointestinal tract of a patient.