Non-Micronized High-Load Pharmaceutical Formulation for Rapid Dissolution
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Solution Overview
Problem
Current pharmaceutical formulations of (4-chlorophenyl)[4-(4-pyridylmethyl)-phthalazin-1-yl] face challenges with solubility issues due to pH dependence, requiring immediate-release formulations for effective absorption, and traditional micronization methods are costly and problematic, leading to low patient compliance due to high dosing frequency.
Innovation Solution
Development of a non-micronized, high-load solid pharmaceutical formulation with a particle size distribution that ensures at least 70% of the drug is dissolved within 30 minutes at pH 3.0, using a formulation with a high percentage of the active ingredient and minimal excipients, allowing for efficient production and rapid release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If micronization is used to improve drug release, then dissolution rate is improved, but manufacturing complexity and cost increase
Solution Approach 1:
The patent changes the particle size parameter by defining specific ranges (d90: 50-300 μm, d50: 15-100 μm) that optimize dissolution without requiring full micronization. This parameter optimization resolves the contradiction by achieving adequate dissolution rates while avoiding the manufacturing complexity of traditional micronization processes.
2Speed
If micronization is used to improve drug release, then dissolution rate is improved, but manufacturing cost increases
Solution Approach 1:
The patent optimizes particle size parameters to achieve effective dissolution without the high costs associated with complete micronization. The specified ranges (d90: 50-300 μm, d50: 15-100 μm) represent a cost-effective compromise that maintains therapeutic efficacy while reducing manufacturing expenses.
3Reliability
If high dosing frequency is used to achieve therapeutic effect, then drug efficacy is maintained, but patient compliance decreases
Solution Approach 1:
The patent enables sustained therapeutic action by optimizing particle size for immediate release, allowing the drug to maintain effective concentrations over extended periods. This continuity of therapeutic effect reduces dosing frequency while maintaining efficacy, thereby improving patient compliance.
4Quantity of substance
If immediate-release formulation is used to improve absorption, then bioavailability is improved, but manufacturing precision requirements increase
Solution Approach 1:
The patent defines specific particle size ranges (d90: 50-300 μm, d50: 15-100 μm) that balance immediate-release performance with manufacturing feasibility. These parameter specifications enable effective absorption while maintaining reasonable manufacturing precision requirements.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The formulation achieves a reproducible immediate-release profile with high drug load, reducing dosing frequency and manufacturing complexities, enhancing patient compliance and stability while maintaining effective drug delivery.
Implementation Method 1
at least 70% of said (4-chlorophenyl)[4-(4-pyridylmethyl)-phthalazin-l- yl], or a pharmaceutical acceptable salt thereof, is dissolved from said solid pharmaceutical formulation within 30 minutes as determined by the USP 28 Paddle Method using 0.05 M KH2PCVHCI buffer adjusted to pH 3.0 at 37°C as the dissolution media
Data Source
AI summary
The invention relates to immediate-release and high-drug-load solid pharmaceutical formulations comprising non- micronized (4-chlorophenyl)[4-(4-pyridylmethyl)-phthalazin-1-yl] as well as pharmaceutically acceptable salts thereof.