Abuse-Resistant Capsule Fill That Gels Under Heated Water Extraction
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Solution Overview
Problem
Existing capsule formulations of abuse-susceptible active pharmaceutical ingredients, such as opiates and opioids, are vulnerable to illicit extraction and injection, as users can solubilize the fill with a small amount of water, heat it, and filter it through a needle to achieve a high, despite viscosity challenges.
Innovation Solution
An immediate release capsule formulation comprising an abuse-susceptible active pharmaceutical ingredient, an ion exchange resin, and a surfactant, which upon mixing with water and heating, forms a turbid, bubbling mixture that increases viscosity and prevents injection through standard insulin syringes, using specific component combinations to deter parenteral abuse.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If the capsule fill is formulated to be soluble in water for oral administration, then the active pharmaceutical ingredient is readily absorbed in the gastrointestinal tract, but the formulation becomes vulnerable to illicit extraction and injection
Solution Approach 1:
The patent applies parameter changes by transforming the physical properties of the formulation through phase transitions. When heated with water, the formulation undergoes a phase change from a soluble state to a highly viscous gel state, making it unsuitable for injection while maintaining oral bioavailability at gastrointestinal temperatures
Solution Approach 2:
The patent uses composite materials by combining the active pharmaceutical ingredient with specific polymers (such as carbomers, xanthan gum, or guar gum) that exhibit temperature-dependent viscosity changes. This composite formulation provides both oral solubility and parenteral abuse deterrence through the gel-forming capability of the polymer matrix
2Object-affected harmful factors
If thickening agents are added to increase viscosity and prevent injection, then parenteral abuse is deterred, but the active pharmaceutical ingredient release and absorption in the gastrointestinal tract may be impaired
Solution Approach 1:
The patent applies dynamics by creating a formulation with temperature-dependent rheological properties. The viscosity of the formulation is low at gastrointestinal temperatures to facilitate rapid drug release and absorption, but becomes highly viscous at elevated temperatures to prevent injection
Solution Approach 2:
The patent utilizes phase transitions by incorporating polymers that undergo sol-gel transitions or significant viscosity changes at specific temperatures. The formulation remains in a soluble, low-viscosity state at body temperature for oral administration but transitions to a gel state when heated, preventing parenteral abuse
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 effectively deters intravenous injection by creating a viscous phase that is difficult to draw into needles, reducing the potential for illicit use and ensuring the active ingredient is not recoverable in significant quantities.
Implementation Method 1
a mixture of about 250 to about 1000 milligrams of the abuse resistant liquid with 5 milliliters of water at the mixture's boiling point forms a viscous phase
Implementation Method 2
a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 mL of an aqueous liquid
Data Source
AI summary
The present invention is directed to an immediate release and extended release capsule or capsule fill which mitigates the abuse of abuse-susceptible active pharmaceutical ingredients by direct intravenous injection. The fill comprises a parenteral abuse resistant liquid formulation which when mixed with water and heated, results in a turbid, viscous or bubbling mixture that is not injectable with a standard insulin syringe. The abuse-susceptible active pharmaceutical ingredient is selected from the group consisting of opiates, opioids, tranquillizers, stimulants and narcotics.