Oral Adsorbent Tablet Maintaining Activated Carbon Structure
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Solution Overview
Problem
Existing oral adsorbent formulations, such as Kremezin, result in residue in the oral cavity and require large volumes of water for administration, which is discomforting for patients, especially those with kidney disease, due to their insolubility and large capsule or granule sizes.
Innovation Solution
A tablet-formed pharmaceutical composition comprising 65% or more spherical activated carbon with specific excipients like pullulan, polyvinyl alcohol, and gelatin, which form a thin film, maintaining the spherical form and structure of the activated carbon, thus reducing volume and improving ingestion feel.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If spherical activated carbon is administered as fine granules or capsules, then the adsorbent function is achieved, but the volume increases and requires large quantity of water for administration
Solution Approach 1:
The patent combines spherical activated carbon particles with excipients (binders, disintegrants, lubricants) to form a compressed tablet structure. This merging of the active ingredient with auxiliary materials creates a compact unit that maintains the adsorbent function while significantly reducing the administered volume compared to loose granules or capsules.
Solution Approach 2:
The patent applies a coating film to the tablet surface to prevent residue in the oral cavity. This thin film layer modifies the surface properties of the tablet, allowing it to be administered without requiring large quantities of water while preventing the activated carbon from adhering to the oral mucosa.
2Volume of moving object
If spherical activated carbon is compressed into tablets using conventional methods, then the volume is reduced, but the spherical form and pore structure are destroyed
Solution Approach 1:
The patent employs specific compression parameters (pressure, duration, temperature) that are optimized to maintain the spherical form and pore structure of the activated carbon. By carefully controlling these physical parameters during tablet formation, the invention achieves volume reduction while preserving the critical structural characteristics needed for adsorbent function.
Solution Approach 2:
The patent creates a composite tablet structure where spherical activated carbon particles are embedded within a matrix of excipients. This composite approach allows the rigid spherical carbon particles to be held in place by the surrounding material, preventing deformation during compression while still achieving compact tablet formation.
3Ease of operation
If fine granules are administered to avoid residue in oral cavity, then the ingestion feel is improved, but large quantity of water is required for administration
Solution Approach 1:
The patent applies a coating film to the tablet surface that prevents residue formation in the oral cavity. This film modifies the surface properties to reduce adhesion to oral mucosa, providing the comfort of fine granules while maintaining the compact tablet form that requires minimal water for administration.
Solution Approach 2:
The patent optimizes the physical and chemical parameters of the tablet surface (surface energy, hydrophobicity, roughness) through coating and compression conditions to achieve low residue formation. These parameter changes allow the tablet to exhibit fine granule-like properties in terms of oral comfort while maintaining tablet integrity for low-water administration.
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 composition achieves reduced volume and improved ingestion comfort by maintaining the spherical form and structure of the activated carbon, ensuring effective adsorption without residue and minimizing water intake, enhancing patient experience.
Implementation Method 1
the excipient for tablet formulation forms a thin film when 0.5 mL of a water solution or water dispersions of the excipient for tablet formulation of 1 % by weight is put on a flat surface made of fluorine resin and heat-dried
Implementation Method 2
a spherical activated carbon as an active ingredient for adsorbing toxic substances
Data Source
Figure 1
Figure 2(A)~2(F)
Figure 3(A)~5(B)
AI summary
The object of the present invention is to provide an adsorbent for oral administration, which can: obviate sandy texture of granules-formed adsorbent for oral administration, reduce the volume administered compared to encapsulated adsorbent for oral administration, and be easy to take. The object of the present invention is solved by a tablet-formed pharmaceutical composition consisting of 65 % or more by weight of particulate substance as an active ingredient and one or more additives, characterized in that: (a) the particulate substance does not exhibit water solubility and swelling property in water, has a distortion rate of 2 % or less when subjected to a pressure of 2 MPa, and has a fracture strength of 5 MPa or more, (b) the tablet-formed pharmaceutical composition comprises one or more particle-formulating additives wherein the amount of the particle-formulating additives is 1 % or more by weight in total with respect to the weight of the tablet-formed pharmaceutical composition, and a thin layer of the particle-formulating additive can be formed when 0.5 mL of solution or dispersion liquid of the particle-formulating additive of 1 % by weight is dropped on a plane surface of fluorine resin and heat-dried.