Stable Nausea and Vomiting Injection via pH Control
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current compositions of 5-HT3 receptor antagonists and corticosteroids, such as ondansetron and dexamethasone, face challenges in forming stable injection solutions due to solubility issues at pH 6-7.5, leading to crystal precipitation and instability, which complicates their administration for preventing nausea and vomiting, especially in cases of chemotherapy and anesthesia recovery.
Innovation Solution
A pharmaceutical composition comprising a 5-HT3 receptor antagonist, a corticosteroid, and a pH modifier or buffering agent, adjusted to a pH range of 3.0-6.0, using organic acids like citric acid to maintain stability and prevent precipitation, allowing for a stable aqueous solution suitable for parenteral administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If a 5-HT3 receptor antagonist and a corticosteroid are mixed in an aqueous solution at pH 6-7.5, then the composition can be prepared, but crystal precipitation occurs and stability deteriorates
Solution Approach 1:
The patent changes the pH parameter from the conventional 6-7.5 range to an acidic range of 3.0-6.0. This parameter change prevents crystal precipitation and maintains the stability of both the 5-HT3 receptor antagonist and corticosteroid in the aqueous solution, resolving the contradiction between ease of preparation and compositional stability.
2Reliability
If separate injections are administered for 5-HT3 receptor antagonist and corticosteroid, then each drug can be administered effectively, but patient convenience deteriorates and compliance decreases
Solution Approach 1:
The patent merges two separate injections (5-HT3 receptor antagonist and corticosteroid) into a single mixed aqueous solution formulation. This combination allows both drugs to be administered simultaneously in one injection, improving patient convenience and compliance while maintaining the effectiveness of nausea and vomiting prevention through the synergistic action of both drugs.
3Reliability
If multiple injections are required for separate drug administration, then each drug can be optimized for its specific function, but the frequency of injections increases and cost increases
Solution Approach 1:
The patent combines multiple drugs into a single formulation, reducing the number of separate injections from two to one. This decreases injection frequency and preparation costs while maintaining therapeutic effectiveness through the coordinated action of the 5-HT3 receptor antagonist and corticosteroid in preventing nausea and vomiting.
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 prevents and treats nausea and vomiting, maintaining stability at room temperature without precipitation, enabling direct administration without dilution and reducing the frequency of injections, thus improving patient compliance and drug preparation costs.
Implementation Method 1
having a pH adjusted to 3.0-6.0, wherein the composition is an aqueous solution for parenteral administration
Implementation Method 2
the pH modifier is an organic acid and the buffering agent is an organic acid buffer
Data Source
AI summary
Provided is a composition for preventing nausea or vomiting, including a 5-HT3 receptor antagonist and a corticosteroid, and having a pH adjusted to 3.0-6.0. Provided also is a method for preparing a composition for preventing nausea or vomiting, including: mixing a 5-HT3 receptor antagonist with a corticosteroid; and adjusting pH of the mixture obtained from the preceding operation to 3.0-6.0.