SHEN26 Oral Composition for Dissolution and Bioavailability
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Solution Overview
Problem
Current treatments for the novel coronavirus lack drugs with good safety, stability, and bioavailability, and existing vaccines have inconvenient storage requirements.
Innovation Solution
A pharmaceutical composition comprising compound SHEN26 and pharmaceutically acceptable excipients, including diluents, disintegrants, binders, and lubricants, formulated into solid oral dosage forms to enhance dissolution, release rate, and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If Remdesivir is used as the only approved novel coronavirus drug, then RdRp inhibition activity is achieved, but safety is compromised and bioavailability is insufficient
Solution Approach 1:
The patent modifies the chemical structure of nucleoside analogues by changing key parameters such as introducing specific substituents at defined positions (e.g., fluorine at 2'-position, methoxy groups at 5'-position) to optimize both safety profile and bioavailability. The compound SHEN26 exemplifies this with its specific molecular structure designed to improve absorption and reduce toxicity compared to Remdesivir.
Solution Approach 2:
The patent employs composite formulation strategies combining multiple excipients with specific functions (disintegrants, binders, lubricants) to create a pharmaceutical composition that enhances bioavailability. The formulation includes microcrystalline cellulose as diluent, croscarmellose sodium as disintegrant, hydroxypropyl cellulose as binder, and magnesium stearate as lubricant, working synergistically to improve drug delivery and absorption.
2Reliability
If vaccines are stored at low temperatures, then vaccine efficacy is maintained, but storage convenience deteriorates
Solution Approach 1:
The patent provides a new antiviral drug composition that eliminates the need for complex cold chain storage infrastructure. Unlike vaccines requiring strict low-temperature storage, the pharmaceutical composition can be stored under常规 conditions, effectively replacing the need for specialized cold storage facilities and enabling wider distribution and use.
3Productivity
If compound SHEN26 is formulated with specific excipients, then dissolution and release rate are improved, but formulation complexity increases
Solution Approach 1:
The patent divides the formulation into distinct functional components, each serving a specific purpose: microcrystalline cellulose as diluent, croscarmellose sodium as disintegrant, hydroxypropyl cellulose as binder, and magnesium stearate as lubricant. This segmentation allows each excipient to be optimized independently while working together to enhance dissolution and release rate of SHEN26.
Solution Approach 2:
The patent optimizes formulation parameters including the ratios of different excipients, particle size of SHEN26, and processing conditions to achieve optimal dissolution and release characteristics. By carefully controlling these parameters, the patent achieves high productivity without excessive formulation complexity.
Data Source
AI summary
A pharmaceutical composition of a nucleoside-derived compound, a preparation method therefor, and use thereof are provided. The pharmaceutical composition includes a compound SHEN26 and a pharmaceutically acceptable excipient. The pharmaceutically acceptable excipient includes at least one selected from a diluent, a disintegrant, an adhesive, a lubricant, and a glidant. The pharmaceutical composition has the advantages of a high dissolution rate, good compatibility of raw and auxiliary materials, good stability, high bioavailability, and the like.