Particulate Oral Pharmaceutical Composition Without Surfactants
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Solution Overview
Problem
Current pharmaceutical formulations for drugs with narrow therapeutic ranges face challenges in dose adjustment, ingestibility, and bioavailability, particularly for patients with swallowing difficulties, and often require surfactants that complicate production and regulatory compliance.
Innovation Solution
A particulate oral pharmaceutical composition is developed by incorporating active ingredients into a hydrophobic liquid, which is then dispersed in a solution containing a water-soluble polymer and excipient, and shaped into granules or powders without using surfactants, allowing for easy dose adjustment and high ingestibility.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If conventional formulations are ground, decapsulated, and manually dispensed for dose adjustment, then dose flexibility is improved, but productivity decreases and occupational safety risks increase
Solution Approach 1:
The invention divides the formulation into discrete granules of uniform size and weight, allowing precise dosing by simple counting or weighing without manual manipulation. This segmentation enables both dose flexibility and maintained productivity, as granules can be dispensed automatically while still allowing easy dose adjustment.
2Reliability
If surfactants are added to improve dissolution properties of poorly water-soluble drugs, then bioavailability is improved, but formulation complexity and regulatory compliance difficulty increase
Solution Approach 1:
The invention extracts and eliminates surfactants from the formulation entirely, achieving dissolution enhancement through alternative means (particle size reduction, crystal structure modification, or use of co-solvents in the granulation process). This removal simplifies the formulation and reduces regulatory complexity while maintaining improved bioavailability.
Solution Approach 2:
The invention changes physical parameters such as particle size, surface area, and crystal structure of the drug substance to enhance dissolution without adding surfactants. By modifying these parameters during granulation, the formulation achieves better bioavailability while remaining simpler and easier to regulate.
3Reliability
If large amounts of excipient are used to improve dissolution properties, then dissolution is enhanced, but formulation size increases making frequent dosing necessary
Solution Approach 1:
The invention applies dissolution enhancement locally at the particle level rather than requiring bulk excipient additions. By modifying the surface properties and internal structure of individual granules, effective dissolution is achieved with minimal excipient, keeping the formulation compact and reducing dosing frequency.
4Measurement precision
If manual dispensing and shaping operations are performed for individualized dosing, then dose accuracy is improved, but exposure to pharmacologically active components increases
Solution Approach 1:
The invention enables the dispensing system to serve itself by using pre-formed granules with uniform properties that can be automatically counted or weighed with high precision. This self-service approach eliminates the need for manual handling and shaping operations, maintaining dose accuracy while protecting operators from exposure to active pharmaceutical ingredients.
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
This approach simplifies the formulation process, enhances bioavailability, and improves medication adherence for drugs with narrow therapeutic ranges, while avoiding the use of surfactants that can complicate production and regulatory compliance.
Implementation Method 1
adding dropwise, spraying or discharging the aqueous solution of the oral pharmaceutical composition in a cooling medium or in the air for shaping
Implementation Method 2
incorporating an active ingredient into a hydrophobic liquid, which is then dispersed in a solution containing a water-soluble polymer and excipient
Data Source
AI summary
Provided is an oral pharmaceutical composition characterized by containing a medicinal ingredient (A), a hydrophobic liquid (B), a water-soluble macromolecular substance (C), and an excipient (D), but not containing a surfactant, wherein: the medicinal ingredient (A) is included in the hydrophobic liquid (B); and the hydrophobic liquid (B) is dispersed in a composition including the water-soluble macromolecular substance (C) and the excipient (D). The oral pharmaceutical composition: allows easy dose-adjustment; has excellent dosability and safety; is biologically equivalent to a standard formulation having established profiles regarding efficacy, safety, etc.; and can be easily produced.