Peptide Amide Composition With pH Control for Stable Kappa Opioid Therapy
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Solution Overview
Problem
Current kappa opioid receptor peptide amide compounds are not commercially available, and existing opioid drugs have stability, dosage, safety, and cost issues, lacking effective compositions and preparations for treating pain and other conditions.
Innovation Solution
A pharmaceutical composition comprising a compound of formula (I) with a pH regulator, stabilizer, and optional additives, formulated as a sterile lyophilized powder or solution for injection, with a pH of 3-5.5, enabling large-scale production and stable, safe, low-dose administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If opioid drugs are used to treat pain, then analgesic effect is achieved, but stability and safety issues occur
Solution Approach 1:
The patent changes the chemical parameters of opioid drugs by developing peptide amide compounds with specific molecular structures (formula I and II), altering their pharmacological properties to achieve stable analgesic effects with reduced side effects
Solution Approach 2:
The patent creates composite pharmaceutical compositions containing peptide amide compounds combined with specific excipients and pH regulators (phosphate buffer, citrate buffer) to enhance stability and reduce harmful effects
2Reliability
If peptide amide compounds are developed for kappa opioid receptors, then analgesic efficacy is improved, but manufacturing and formulation challenges arise
Solution Approach 1:
The patent optimizes formulation parameters including pH (adjusted to 3-5.5 using buffers), concentration, and excipient ratios to enable stable manufacturing of peptide amide compounds while maintaining high efficacy
Solution Approach 2:
The patent introduces buffer systems (phosphate buffer, citrate buffer) as intermediaries to stabilize the peptide amide compounds during formulation and storage, simplifying the manufacturing process
3Reliability
If conventional opioid compositions are used, then pain treatment is provided, but cost and dosage control issues occur
Solution Approach 1:
The patent modifies the chemical structure parameters of opioid compounds to create peptide amides with higher potency and better safety profiles, allowing for controlled dosage regimens
Solution Approach 2:
The patent creates simplified formulations of peptide amide compounds that replicate the therapeutic effects of complex opioid medications with better dosage control and lower cost
Data Source
AI summary
Disclosed are a peptide amide compound composition, a preparation method therefor and medical use thereof. Specifically, the composition contains a compound of formula (I) and pH regulators, and the pH of the solution thereof is 3-5.5. The composition is stable and requires few excipients, and is stable in clinical use. The composition is used for treating or preventing a disease or condition associated with kappa opioid receptors