HPMC Tablet Composition for Stable Dissolution at Lower Polymer Loading
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Solution Overview
Problem
Existing sustained-release preparations containing hydroxypropyl methyl cellulose (HPMC) face challenges in achieving reproducible dissolution profiles with small variations, often requiring higher HPMC content which leads to larger tablet sizes and administration issues.
Innovation Solution
A composition comprising HPMC with specific properties, including polydispersity of 4.0 or more, viscosity of 1,500 to 150,000 mPa·s, and substitution degrees of 14.0 to 32.0% for methoxy and 3.0 to 32.0% for hydroxypropoxy groups, is used to produce a solid preparation with reduced dissolution variation and lower HPMC content.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If the content of HPMC is increased to reduce dissolution variation, then the dissolution reproducibility is improved, but the tablet size becomes larger and administration becomes more difficult
Solution Approach 1:
The invention changes the molecular weight distribution parameter of HPMC by selecting polymers with specific polydispersity indices (1.5-3.5) and weight-average molecular weights (100,000-1,000,000). This parameter optimization allows achieving stable dissolution profiles with lower HPMC content, thus reducing tablet size while maintaining reliability
Solution Approach 2:
The invention uses composite material strategy by combining HPMC with specific excipients (microcrystalline cellulose, pregelatinized starch, croscarmellose sodium, and magnesium stearate) in optimized ratios. This composite approach enhances dissolution reproducibility without requiring excessive HPMC, thereby controlling tablet size
2Volume of moving object
If the content of HPMC is decreased to reduce tablet size, then the administration becomes easier, but the dissolution variation increases and matrix formation becomes unstable
Solution Approach 1:
The invention optimizes the molecular weight distribution parameters of HPMC, specifically selecting polymers with polydispersity indices of 1.5-3.5 and weight-average molecular weights of 100,000-1,000,000. This precise parameter control enables the polymer to form stable matrices at lower concentrations, maintaining dissolution reproducibility while reducing tablet size
Solution Approach 2:
The invention applies local quality principle by optimizing the distribution and arrangement of HPMC particles within the tablet matrix. The specific molecular weight distribution creates localized regions with optimal gel-forming properties, ensuring stable matrix formation even at reduced HPMC content
Data Source
AI summary
Provided are a composition which is used for the production of a solid preparation exhibiting a small variation of dissolution even at a low content of hydroxypropyl methyl cellulose (HPMC), and others. More specifically, provided are a composition for a solid preparation, the composition including HPMC having a polydispersity of 4.0 or more, as determined by absolute molecular weight measurement, and having a viscosity at 20°C of 1,500 to 15,0000 mPa-s, as determined in a 2% by mass aqueous solution thereof, and an active ingredient; the solid preparation including the composition; and a method for producing a tablet including a step of dry-mixing said HPMC with an active ingredient to obtain a mixture, or granulating a mixture including said HPMC and an active ingredient to obtain a granulated product, and a step of tableting the mixture or the granulated product to obtain a tablet.