Buprenorphine and Compound-1 Combination for Opioid Dependency
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Solution Overview
Problem
Current treatments for chronic pain and mood disorders, particularly depression, often lead to opioid dependency and undesirable side effects, and there is a need for effective management of treatment-resistant depression and pain while minimizing opioid abuse risks.
Innovation Solution
A composition comprising pharmaceutically effective amounts of buprenorphine and Compound-1, or its pharmaceutically acceptable salt, in specific molar ratios, administered to treat opioid receptor-mediated diseases or disorders, including depression and pain, with a controlled release formulation and potential combination with additional antidepressant agents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If full μ-opioid agonists are used to treat depression and pain, then antidepressant effects and analgesia are achieved, but opioid dependency and addictive qualities increase
Solution Approach 1:
The patent combines a μ-opioid antagonist ( Compound-1) with a μ-opioid agonist (buprenorphine) into a single pharmaceutical composition. This merging allows the agonist to provide antidepressant and analgesic effects while the antagonist simultaneously blocks overactivation of μ-opioid receptors, preventing dependency and abuse potential
Solution Approach 2:
The μ-opioid antagonist acts as an intermediary that modulates the interaction between the μ-opioid agonist and its receptors. By selectively blocking certain receptor interactions while allowing others, the antagonist mediates between the therapeutic effects needed and the harmful effects to be avoided
2Reliability
If μ-opioid agonists are used to treat depression, then mood-altering effects are produced, but undesirable side effects such as sedation, respiratory depression, and constipation increase
Solution Approach 1:
The patent merges the μ-opioid agonist buprenorphine with the μ-opioid antagonist Compound-1 in specific dosage ratios. This combination allows maintenance of mood-altering therapeutic effects while the antagonist component simultaneously reduces harmful side effects by blocking excessive receptor activation
Solution Approach 2:
The patent changes the pharmacological parameters by using a partial agonist (buprenorphine) instead of a full agonist, and by adjusting the dosage ratio between agonist and antagonist components. This parameter change allows achieving therapeutic effects at lower doses with reduced side effect profile
3Ease of operation
If buprenorphine is used at low doses to enable opioid-addicted individuals to discontinue misuse, then withdrawal symptoms are prevented, but additive potential and respiratory depression remain
Solution Approach 1:
The patent combines buprenorphine with a μ-opioid antagonist in a fixed-ratio formulation. This merging allows the buprenorphine to provide withdrawal prevention at low doses while the antagonist simultaneously blocks additive effects and reduces respiratory depression by limiting overactivation of μ-opioid receptors
Data Source
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AI summary
The invention relates a composition comprising an opioid agonist and Compound- 1 : Compound- 1.