Self-Regulated Opioid Release via pH-Dependent Solubility
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Solution Overview
Problem
Current opioid analgesics face challenges in preventing abuse and addiction, as they can be easily tampered with to administer excessive doses, leading to misuse and diversion, and existing deterrent methods have not been effective in reducing abuse potential.
Innovation Solution
An abuse-deterrent pharmaceutical composition is developed, incorporating an acid soluble salt of a pharmaceutically active ingredient and a buffering ingredient, which retards the release of the active ingredient when ingested in excess doses, using a pH modifying and pH dependent solubility feature to prevent rapid absorption and euphoric effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If opioid analgesics are made available in standard dosage forms, then therapeutic pain relief is achieved, but abuse potential and addiction risk increase
Solution Approach 1:
The patent applies parameter changes by utilizing pH-dependent solubility characteristics of the opioid salt form. The active ingredient is formulated as a salt that exhibits high solubility at low pH (stomach conditions) but low solubility at high pH (intestinal conditions), thereby controlling release based on physiological pH parameters
Solution Approach 2:
The patent introduces an intermediary mechanism in the form of a pH-sensitive release system. The gastrointestinal pH environment acts as an intermediary that automatically regulates drug release - acidic stomach pH permits release while basic intestinal pH prevents release, creating a self-regulating system
2Reliability
If excessive doses are administered to overcome tolerance, then pain relief may be achieved, but euphoric effects and addiction risk increase
Solution Approach 1:
The patent implements preliminary anti-action by pre-formulating the opioid as a salt with restricted solubility characteristics that prevent rapid absorption. The formulation is designed in advance to resist the harmful effect of rapid drug delivery that causes euphoria, even when large doses are administered
3Object-affected harmful factors
If the drug is made less soluble to prevent abuse, then abuse potential is reduced, but therapeutic delivery at standard doses is compromised
Solution Approach 1:
The patent applies local quality by creating different solubility characteristics in different gastrointestinal locations. The drug formulation has high solubility in the acidic local environment of the stomach (enabling therapeutic delivery) but low solubility in the basic local environment of the intestine (preventing abuse)
Solution Approach 2:
The patent utilizes parameter changes by exploiting the pH parameter variation along the gastrointestinal tract. The salt form of the opioid is specifically selected to exhibit solubility that changes with pH, being soluble at stomach pH (1-3) but insoluble at intestinal pH (6-8)
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 composition effectively reduces the euphoric effect of excessive opioid ingestion, acting as a deterrent to abuse while ensuring therapeutic delivery of the drug at standard doses, thereby minimizing physical and psychological dependency.
Implementation Method 1
using a pH modifying and pH dependent solubility feature to prevent rapid absorption
Implementation Method 2
incorporating an acid soluble salt of a pharmaceutically active ingredient and a buffering ingredient, which retards the release of the active ingredient when ingested in excess doses
Data Source
AI summary
An abuse deterrent pharmaceutical composition including an acid soluble salt of a pharmaceutically active ingredient and a buffering ingredient; wherein the acid soluble salt of the pharmaceutically active ingredient and the buffering ingredient retard release of the pharmaceutically active ingredient when the composition is ingested in excess of an intended dosage.