Cyclodextrin Polymer Fractions as Multifunctional Tablet Excipients
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Solution Overview
Problem
Current pharmaceutical excipients fail to provide multifunctional properties such as good compressibility, solubilization, complexation, and disintegration of poorly hydrophilic active ingredients, necessitating the use of multiple excipients and complex formulations.
Innovation Solution
Separation and use of purified insoluble and soluble fractions of cyclodextrin polymers as sole excipients in tablets, allowing for modulation of properties like compression, dispersion, solubilization, and complexation, and controlled release of active ingredients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If multiple excipients are used to achieve multifunctional properties, then solubilization and complexation of poorly hydrophilic active ingredients are improved, but device complexity and formulation complexity increase
Solution Approach 1:
The patent applies universality by developing a single excipient (cyclodextrin polymer) that performs multiple functions simultaneously: it provides solubilization through inclusion complexes, complexation of active ingredients, disintegration upon water contact, and acceptable compressibility. This eliminates the need for multiple separate excipients and simplifies the formulation while maintaining all required functionalities.
Solution Approach 2:
The patent merges the functions of multiple traditional excipients (solubilizing agents, complexing agents, disintegrants, and compressibility modifiers) into a single substance: the cyclodextrin polymer. By combining these functionalities into one material, the formulation complexity is reduced while achieving the same or better overall performance.
2Ease of manufacture
If direct compression is used to simplify the manufacturing process, then manufacturing time and complexity are reduced, but compressibility requirements become more difficult to meet
Solution Approach 1:
The cyclodextrin polymer serves as a universal excipient that provides both disintegration functionality and acceptable compressibility, enabling direct compression manufacturing. This eliminates the need for separate disintegrant and compressibility modifier excipients, making direct compression feasible while maintaining all necessary tablet properties.
Solution Approach 2:
The patent utilizes the parameter change of the cyclodextrin polymer's solubility state: it maintains a dry, compressible powder form during manufacturing that can be directly compressed into tablets, then transforms into a water-soluble disintegrating structure upon contact with gastrointestinal fluids. This parameter change enables both direct compression and effective disintegration.
3Reliability
If cyclodextrin polymer is used to improve solubility and bioavailability, then therapeutic efficacy is enhanced, but the need for additional excipients increases formulation complexity
Solution Approach 1:
The cyclodextrin polymer is applied as a universal excipient that simultaneously provides solubilization through inclusion complexes (enhancing bioavailability), disintegration upon water contact, and acceptable compressibility for tablet formation. This multi-functionality eliminates the need for multiple separate excipients including solubilizing agents, disintegrants, and compressibility modifiers.
Solution Approach 2:
The patent extracts and utilizes the core functionality of multiple traditional excipients and consolidates them into the single cyclodextrin polymer material. By taking out the essential functions (solubilization, disintegration, compressibility) and combining them in one substance, the formulation is simplified while maintaining therapeutic efficacy.
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
Enables the production of tablets with improved bioavailability, solubility, and disintegration properties without the need for additional excipients, enhancing the therapeutic efficacy of poorly soluble active ingredients.
Implementation Method 1
Cyclodextrins in particular are known as excipients for their inclusion complex formation properties with hydrophobic molecules which improve the bioavailability of these molecules
Implementation Method 2
An insoluble fraction of a cyclodextrin polymer, a soluble fraction of a cyclodextrin polymer or a mixture of insoluble and soluble fractions of cyclodextrin polymers
Data Source
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AI summary
The present invention relates to the use of a water-insoluble fraction of a cyclodextrin polymer, of a water-soluble fraction of a cyclodextrin polymer or of a mixture of water-insoluble and water-soluble fractions of cyclodextrin polymers as an excipient in a tablet.