Structured Solid-Solution Framework for Rapid Drug Delivery
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Solution Overview
Problem
Current solid-solution dosage forms face challenges such as premature precipitation of drug particles and pore closing due to plasticization of excipients, leading to slow drug release rates, especially for sparingly soluble drugs.
Innovation Solution
Incorporating a substantial amount of amphiphilic polymer that self-assembles into micelles upon contact with physiological fluids, and creating a three-dimensional structural framework with precisely controlled inter-element spacing and composition, including an open pore network to enhance drug solubility and release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If a solid solution of sparingly-soluble drug in water-soluble excipient is used, then drug solubility is improved, but premature precipitation of drug particles occurs
Solution Approach 1:
The patent utilizes a porous matrix material to create a structured solid solution framework. The porous structure provides increased surface area and controlled release pathways, preventing premature precipitation while maintaining enhanced drug solubility. The matrix pores allow gradual dissolution and release of the drug-excipient complex.
Solution Approach 2:
The patent employs a composite structure combining the sparingly-soluble drug, water-soluble excipient, and porous matrix material. This composite approach creates a stable solid solution where the matrix supports the drug-excipient complex, preventing premature separation and precipitation while maintaining solubility enhancement.
2Productivity
If water-soluble excipient is used in solid solution, then drug release rate is enhanced, but pore closing due to plasticization occurs
Solution Approach 1:
The patent employs a porous matrix material that maintains its porous structure even when water-soluble excipient is present. The matrix pores remain open to allow fluid penetration and drug release, preventing the pore closing that would otherwise occur due to excipient plasticization. The porous structure provides stable pathways for drug dissolution and release.
3Ease of manufacture
If conventional solid dosage form is used, then manufacturing is simple, but drug delivery rate is slow for sparingly soluble drugs
Solution Approach 1:
The patent changes the physical state parameters of the drug by forming a solid solution within a porous matrix. This parameter change from conventional particulate dosage form to structured solid solution enhances the drug delivery rate while maintaining manufacturing feasibility through processes like direct compression or granulation of the pre-formed solid solution particles.
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 prevents premature precipitation and maintains an open pore network, allowing for rapid wetting and interdiffusion of fluids, thereby enhancing drug solubility and achieving faster and more efficient drug delivery.
Implementation Method 1
Incorporating a substantial amount of amphiphilic polymer that self-assembles into micelles upon contact with physiological fluids
Implementation Method 2
amphiphilic polymer that self-assembles into micelles upon contact with physiological fluids
Implementation Method 3
allowing for rapid wetting and interdiffusion of fluids
Implementation Method 4
rapid wetting and interdiffusion of fluids
Data Source
AI summary
By the ingestion of dosage forms containing sparingly water-soluble drug particles, it is not possible to deliver drug into the blood stream at high rates, because the drug dissolution rate, and the absorption rate, are limited by solubility. Herein, therefore, dosage forms comprising a slender, three-dimensional structural framework of sparingly-soluble drug dissolved in an excipient matrix comprising at least a water-soluble polymer carrier and an amphiphilic polymer are disclosed. Upon immersion in a physiological fluid, said fluid wets the structural framework, interdiffuses with it, and the amphiphilic polymer self-assembles as micelles, thereby enhancing drug solubility. Concomitantly, the framework erodes and rapidly releases drug molecules, thus enhancing drug concentration in the fluid and the drug delivery rate into the blood stream.