Nasal Powder Flowability via Crystalline Cellulose and Calcium Phosphate
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Solution Overview
Problem
Conventional crystalline cellulose used as a carrier for nasal drug administration has poor flowability, which hinders efficient automated capsule filling and nasal device spray efficiency, leading to inconsistent drug delivery and reduced therapeutic effectiveness.
Innovation Solution
Combining crystalline cellulose with tribasic calcium phosphate and starch to enhance flowability, specifically using a first crystalline cellulose with high bulk density and specific surface area, and a second crystalline cellulose or starch with lower bulk density and surface area, to create a nasal preparation that improves powder flowability without affecting drug absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If crystalline cellulose is used as a carrier for nasal drug administration, then drug absorption through nasal mucosa is improved, but flowability is poor which hinders automated capsule filling and spray efficiency
Solution Approach 1:
The patent combines crystalline cellulose with tribasic calcium phosphate and starch to create a composite powder formulation. This composite material integrates the drug absorption properties of crystalline cellulose with the flowability enhancement provided by tribasic calcium phosphate and starch, resolving the contradiction between reliable drug absorption and productive automated filling.
Solution Approach 2:
The patent modifies the physical and chemical parameters of the powder formulation by adjusting the particle size distribution, bulk density, and compositional ratios of the crystalline cellulose, tribasic calcium phosphate, and starch. These parameter changes optimize both the flowability for automated processing and the drug absorption characteristics.
2Reliability
If crystalline cellulose is used as a carrier, then drug retention in nasal cavity is improved, but flowability is poor leading to inconsistent drug delivery
Solution Approach 1:
The composite formulation combines crystalline cellulose (for drug retention) with tribasic calcium phosphate and starch (for improved flowability). This composite approach maintains the beneficial drug retention properties while achieving consistent drug delivery through enhanced flow characteristics.
Solution Approach 2:
The patent creates a heterogeneous powder mixture where different components serve localized functions: crystalline cellulose particles provide drug retention at the nasal cavity site, while tribasic calcium phosphate and starch particles provide flowability throughout the formulation. The local quality of each component addresses specific requirements.
3Reliability
If conventional crystalline cellulose is used, then nasal administration is effective, but spray efficiency in nasal devices is reduced
Solution Approach 1:
The patent formulates a composite powder containing crystalline cellulose, tribasic calcium phosphate, and starch that optimizes spray efficiency in nasal devices. The combination improves powder flow and aerosolization characteristics while maintaining the nasal administration effectiveness provided by crystalline cellulose.
Solution Approach 2:
The patent adjusts particle size distribution and compositional parameters to optimize spray efficiency. The composite formulation with controlled particle characteristics enables better powder flow into the spray device and more efficient aerosol generation, while preserving drug absorption properties.
Data Source
AI summary
Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties, and physiologically active substance.