Low-Solubility API Formulation With Room-Temperature Encapsulation
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Solution Overview
Problem
Existing pharmaceutical processing methods face challenges in producing sub-micron particles of low bioavailability drugs without thermal degradation, large particle size distribution, and difficulty in handling and scaling up, especially due to high temperatures and the use of organic solvents.
Innovation Solution
A method using a high-throughput installation at room or near room temperature with high voltage and nebulizing to encapsulate sub-micron particles of APIs within microparticles, ensuring controlled particle size and distribution, using a facility with an injection unit, drying unit, and collection unit to produce pharmaceutical formulations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If spray drying technique is used to prepare pharmaceutical powders, then dehydration and encapsulation can be achieved, but high temperatures can degrade thermally labile drugs and excipients, produce large particles with broad size distribution, and impair resolubilization
Solution Approach 1:
The patent changes the temperature parameter from high temperature (conventional spray drying) to room temperature or near room temperature (0-25°C), preventing thermal degradation of thermally labile drugs and excipients while maintaining particle formation capability
Solution Approach 2:
The patent replaces the thermal field (heat-based evaporation) with a combination of high voltage nebulization and controlled drying, substituting thermal energy with electrical and mechanical energy to achieve dehydration without thermal damage
2Ease of manufacture
If conventional spray drying is used, then encapsulation can be achieved, but high temperatures can cause explosion if organic or alcoholic solvents are used
Solution Approach 1:
The patent replaces thermal evaporation with high voltage nebulization and controlled drying mechanisms, eliminating the source of thermal energy that causes solvent vapor accumulation and explosion risk
Solution Approach 2:
The patent operates at room temperature with controlled atmosphere, preventing the formation of explosive solvent vapor mixtures by avoiding high temperature heating that would generate flammable vapor concentrations
3Manufacturing precision
If emulsion-based technologies are used to obtain sub-micron particles, then narrow size distribution and high retention of bioactive compound can be achieved, but undesirable materials (residual monomers or organic solvents) may be present in the final product
Solution Approach 1:
The patent removes and eliminates undesirable materials (residual monomers, organic solvents) from the final product through controlled drying and purification steps, extracting harmful substances while retaining the beneficial sub-micron particle characteristics
Solution Approach 2:
The patent uses temporary vehicle systems (emulsions, solvents) that are completely evaporated or decomposed during the drying process, leaving only the desired sub-micron particles without residual harmful materials
4Reliability
If sub-micron particles are produced, then solubility and bioavailability can be improved, but recovery and handling present several technical difficulties for industry
Solution Approach 1:
The patent nests sub-micron particles within larger carrier particles or uses them in concentrated formulations, making them easier to handle and recover while maintaining the solubility and bioavailability benefits of the sub-micron size
Solution Approach 2:
The patent creates composite particle systems combining sub-micron drug particles with carrier materials or matrix substances, improving handling properties while preserving the enhanced solubility and bioavailability characteristics of the sub-micron API
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 method achieves stable, non-agglomerated sub-micron particles with improved solubility and bioavailability, facilitating easier handling and reducing dosage, while maintaining the integrity of thermally labile drugs.
Implementation Method 1
a high throughput installation that works at room or near room temperature and that combines high voltage and nebulizing
Implementation Method 2
The spray drying technique has been widely used in the preparation of pharmaceutical powders, most often proposed as a dehydration process
Data Source
AI summary
The present invention relates to a pharmaceutical formulation comprising at least one active pharmaceutical ingredient (API) having low aqueous solubility or a pharmaceutically acceptable salt thereof in the form of particles of a size between 1 and 800 nm, wherein said particles are encapsulated within a large microparticle of a size between 1 and 100 μm formed by a matrix comprising at least an excipient. Therefore, the API is entrapped or encapsulated in the microparticles of excipients. This pharmaceutical formulation contains the pharmaceutical active ingredient having improved solubility and subsequently supra-bioavailability.