Linzagolix Oral Solid Formulation for Rapid, Stable Dissolution
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Solution Overview
Problem
Existing oral solid preparations containing Linzagolix or its pharmacologically acceptable salts do not maintain rapid dissolution properties when the content varies over a wide range, and they lack adequate storage stability.
Innovation Solution
An oral solid preparation comprising Linzagolix or its pharmacologically acceptable salt, crystalline cellulose, low-substituted hydroxypropyl cellulose, and one or more disintegrants such as carmellose sodium, carmellose calcium, or croscarmellose sodium, with specific ratios and formulations to ensure rapid dissolution and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If the content of Linzagolix in the oral solid preparation is increased to achieve higher therapeutic efficacy, then the therapeutic effectiveness is improved, but the dissolution property deteriorates and rapid dissolution cannot be satisfied
Solution Approach 1:
The patent changes the physical and chemical parameters of the formulation by introducing specific disintegrants (carmellose sodium, carmellose calcium, or croscarmellose sodium) and controlling the total amount of cellulose and disintegrant components within specific ranges (20-40% by mass). This parameter optimization allows the formulation to maintain rapid dissolution even at high Linzagolix content (50-65% by mass), resolving the contradiction between high drug content and fast dissolution rate.
2Adaptability or versatility
If the content of Linzagolix in the oral solid preparation is varied over a wide range to accommodate different dosage requirements, then the adaptability is improved, but the dissolution property deteriorates
Solution Approach 1:
The patent creates a universal formulation formula that can accommodate wide content ranges of Linzagolix (from low to high dosage requirements) while maintaining consistent rapid dissolution properties. The specific combination of disintegrants and cellulose derivatives serves multiple functions: binding, disintegration, and dissolution control, making the formulation adaptable to different therapeutic needs without sacrificing dissolution performance.
3Volume of moving object
If the content of Linzagolix in the oral solid preparation is increased to achieve miniaturization, then the dosage form size is reduced, but the dissolution property deteriorates
Solution Approach 1:
The patent optimizes formulation parameters including the total amount of disintegrant and cellulose components (20-40% by mass) and the specific types of disintegrants used. This allows miniaturization of the dosage form while maintaining rapid dissolution through enhanced disintegrant activity and controlled release characteristics, enabling small tablet sizes with high Linzagolix content that still dissolve quickly.
Data Source
AI summary
An object of the present invention is to provide an oral solid preparation having a rapid dissolution property even when the content of Linzagolix or a pharmacologically acceptable salt thereof in the oral solid preparation varies over a wide range.The present invention relates to an oral solid preparation comprising Linzagolix or a pharmacologically acceptable salt thereof; crystalline cellulose; low-substituted hydroxypropyl cellulose; and one or more disintegrants selected from the group consisting of carmellose sodium, carmellose calcium and croscarmellose sodium, and the like.