Compressible Sodium Caprate Form A Tabletting
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Solution Overview
Problem
Existing oral tablet formulations using sodium caprate as a permeability enhancer often face challenges with tableting properties, such as low tensile strength and high stickiness to tableting machinery, which affect the manufacturing efficiency and product quality.
Innovation Solution
The method involves mixing a macromolecule with Form A sodium caprate, characterized by specific XRPD and WAXS spectra, and then directly compressing the mixture into a tablet, eliminating the need for wet granulation, drying, or additional milling steps.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional sodium caprate is used as a permeability enhancer in oral tablets, then the therapeutic efficacy is improved, but the tablet tensile strength decreases and stickiness to tableting machinery increases
Solution Approach 1:
The patent applies parameter changes by modifying the crystal form of sodium caprate from conventional forms to Form A, characterized by specific XRPD patterns (peaks at 4.2°, 11.8°, and 24.6° 2θ) and WAXS patterns (peaks at 0.12 and 0.23 Å⁻¹). This crystal form transformation fundamentally changes the physical properties of sodium caprate, enabling it to maintain high tablet tensile strength (≥1.7 MPa) and low stickiness while preserving its permeability enhancer function at therapeutic concentrations
2Reliability
If conventional sodium caprate is used in oral tablets, then the permeability enhancement function is achieved, but the manufacturing efficiency decreases due to process complexity
Solution Approach 1:
The patent applies preliminary action by pre-establishing sodium caprate in its optimal crystal Form A through controlled crystallization processes (such as slow evaporation from aqueous solutions or precipitation from organic solvents). This preliminary formation of the correct crystal structure ensures that the material is ready for direct compression without requiring subsequent wet granulation, drying, or milling steps, thereby streamlining the manufacturing process
Solution Approach 2:
The patent extracts and eliminates unnecessary manufacturing steps (wet granulation, drying, milling) from the conventional tablet production process. By using sodium caprate Form A with its superior flow and compression properties, the process is reduced to simple mixing and direct compression, removing complex unit operations while maintaining product quality
3Reliability
If conventional sodium caprate is used in oral tablets, then the permeability enhancement is achieved, but the tablet physical integrity deteriorates
Solution Approach 1:
The patent applies parameter changes by transforming sodium caprate into Form A with specific crystallographic parameters (XRPD peaks at 4.2°, 11.8°, and 24.6° 2θ; WAXS peaks at 0.12 and 0.23 Å⁻¹). This crystal form modification fundamentally alters the material's mechanical properties, enabling it to contribute to tablet hardness and structural integrity while maintaining its biological function as a permeability enhancer
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 results in oral tablets with higher physical integrity, reduced stickiness to tableting equipment, and improved manufacturing efficiency, while maintaining the therapeutic efficacy of the active ingredients.
Implementation Method 1
Form A sodium caprate characterized by a X-Ray Powder Diffraction (XRPD) spectrum which includes a peak at 4° 2θ
Implementation Method 2
X-Ray Powder Diffraction (XRPD) spectrum which includes a peak at 4° 2θ
Implementation Method 3
wide-angle X-ray scattering (WAXS) spectrum which includes a peak at a region of 0.1 to 0.15 Å⁻¹
Implementation Method 4
wide-angle X-ray scattering (WAXS) spectrum
Implementation Method 5
small-angle X-ray scattering (SAXS) spectrum which includes a peak at a region of 0.1 to 0.15 Å⁻¹
Implementation Method 6
small-angle X-ray scattering (SAXS) spectrum
Data Source
AI summary
The present disclosure provides a method of making an oral tablet comprising mixing a macromolecule with sodium caprate to form a mixture, and compressing the mixture into a tablet, wherein the sodium caprate is Form A. The present disclosure also provides a tablet made by the process provided herein. Also provided is a composition comprising sodium caprate and a macromolecule.