Fumaric Acid Crystal Form for Coronavirus Drug Dissolution
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Solution Overview
Problem
Current pharmaceutical compositions for treating coronavirus-induced diseases, particularly those caused by 2019-nCoV, lack effective treatment methods that meet clinical needs due to inadequate dissolution rates and stability.
Innovation Solution
A crystal form of a specific compound and fumaric acid with a defined X-ray powder diffraction pattern and specific particle size range, combined with physiologically acceptable excipients, is used to create a pharmaceutical composition that enhances dissolution rates and stability, suitable for oral preparations and industrial-scale production.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional pharmaceutical compositions are used for treating coronavirus-induced diseases, then the treatment can be administered, but the dissolution rate is insufficient and stability is inadequate
Solution Approach 1:
The patent applies parameter changes by controlling the particle size of the active ingredient within specific ranges (D50: 10-30 μm, D90: 20-60 μm) and defining precise X-ray powder diffraction pattern characteristics. These parameter optimizations enhance the dissolution rate and stability of the pharmaceutical composition, directly resolving the technical contradiction between adequate dissolution performance and effective treatment efficacy.
2Reliability
If the particle size is reduced to improve dissolution rate, then dissolution rate increases, but manufacturing precision requirements increase
Solution Approach 1:
The patent specifies precise particle size parameters (D50: 10-30 μm, D90: 20-60 μm) that balance dissolution rate improvement with manufacturability. These defined ranges provide clear manufacturing targets that achieve enhanced dissolution performance while remaining practical for industrial production, resolving the contradiction between dissolution rate and manufacturing precision.
3Reliability
If crystal form with specific X-ray diffraction pattern is used, then stability and dissolution rate improve, but characterization complexity increases
Solution Approach 1:
The patent defines specific X-ray powder diffraction pattern characteristics (peak positions at 2θ: 10.94°, 19.06°, 23.50°, 24.66° with Cu-Kα radiation) as identification criteria for the crystal form. These defined parameters enable reliable stability and dissolution rate improvement while providing clear, objective criteria for crystal form characterization and verification.
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 higher dissolution rates, improved stability, and acceptable friability, ensuring reliable quality and clinical application value, with no significant sticking or picking phenomena during tablet preparation.
Implementation Method 1
the crystal form of the present disclosure within the specific particle size (e.g., D50 and/or D90) range can enable the pharmaceutical composition containing the crystal form to have a higher dissolution rate and a higher dissolution
Implementation Method 2
a crystal form comprising a compound of Formula (I) and fumaric acid, characterized in that an X-ray powder diffraction pattern of the crystal form obtained by using Cu-Kα radiation includes at least three peaks selected from a group consisting of 10.94°±0.2° 2θ, 19.06°±0.2° 2θ, 23.50°±0.2° 2θ, and 24.66°±0.2° 2θ
Data Source
AI summary
The present disclosure provides a crystal form comprising a compound of Formula (I) and fumaric acid, wherein the crystal form satisfies at least one of the following conditions: (1) a particle size D90 of the active pharmaceutical ingredient ranges from about 5 μm to about 60 μm; and (2) a particle size D50 of the active pharmaceutical ingredient does not exceed about 30 μm; a pharmaceutical composition containing the crystal form, and a method for treating coronavirus-induced diseases by using the crystal form. The crystal form of the present disclosure enables the pharmaceutical composition containing the crystal form to have advantages such as a higher dissolution rate, a higher dissolution, and the like.