Pharmaceutical Formulation Using Fine MCC for Drug Dissolution
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Solution Overview
Problem
Existing pharmaceutical compositions containing NEP inhibitors and Angiotensin II Receptor Blockers (ARBs) face issues with hygroscopicity, leading to poor dissolution and release of active ingredients due to moisture absorption, resulting in ineffective disintegration and reduced bioavailability.
Innovation Solution
Incorporating microcrystalline cellulose with a particle size of 95 µm or less, along with other excipients, to enhance the stability and disintegration of the pharmaceutical preparation, ensuring effective release of active components.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If microcrystalline cellulose with larger particle size is used, then manufacturing is easier, but disintegration and dissolution of active ingredients are poor
Solution Approach 1:
The patent applies parameter changes by specifying a particular particle size range (95 µm or less) for microcrystalline cellulose to optimize both manufacturability and disintegration performance. This quantitative parameter adjustment resolves the contradiction between ease of manufacture and disintegration effectiveness.
2Reliability
If active ingredients are combined, then treatment effect is improved, but hygroscopicity increases leading to poor dissolution
Solution Approach 1:
The patent uses microcrystalline cellulose with controlled particle size as an intermediary excipient that mediates between the combined active ingredients and moisture. This intermediary prevents excessive hygroscopicity while maintaining the synergistic treatment effect of the drug combination.
3Reliability
If particle size of microcrystalline cellulose is reduced, then disintegration is improved, but manufacturing complexity increases
Solution Approach 1:
The patent resolves the contradiction by establishing a specific particle size threshold (95 µm or less) that balances disintegration performance with manufacturing feasibility. This quantified parameter provides clear manufacturing guidance while achieving reliable disintegration.
Data Source
AI summary
The invention discloses a pharmaceutical preparation and use thereof. The preparation includes a first active component, a second active component and pharmaceutically acceptable excipients, wherein the first active component is at least one selected from the group consisting of a neutral endopeptidase inhibitor and a precursor, an active metabolite, a stereoisomer, a pharmaceutically acceptable salt, a prodrug and a solvate thereof. The second active component is at least one selected from the group consisting of a compound represented by the following formula (I) or a precursor, an active metabolite, a stereoisomer, a pharmaceutically acceptable salt, a prodrug and a solvate thereof. The pharmaceutically acceptable excipients include one or more disintegrants and/or one or more fillers. The preparation can ameliorate the problem that conventional excipients cannot effectively dissolve out the active ingredients.