High-Concentration Opiranserin Composition for Stable Solubilization
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Solution Overview
Problem
Existing drugs with low solubility face challenges in achieving high bioavailability and require complex formulation methods that are not always effective.
Innovation Solution
A pharmaceutical composition comprising opiranserin or its pharmaceutically acceptable salt, combined with carriers like sodium benzoate, trisodium citrate, or sodium salicylate, and a solvent for injection, allowing for a high concentration of opiranserin to be prepared and stored in a small volume, facilitating quick and safe preparation of a bolus intravenous infusion.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional formulation methods are used to solubilize poorly soluble drugs, then some solubility improvement may be achieved, but the formulation becomes complex and the effect remains insignificant
Solution Approach 1:
The patent uses a composite formulation system combining opiranserin hydrochloride with specific carriers (sodium benzoate, trisodium citrate, or sodium salicylate) and co-solvents. This composite approach achieves high solubility (10 mg/mL) without requiring complex multi-component formulations, resolving the contradiction between solubility improvement and formulation simplicity
Solution Approach 2:
The patent changes the chemical parameters by selecting specific carriers (sodium benzoate, trisodium citrate, sodium salicylate) and co-solvents (glycerol, polyethylene glycol) to optimize solubility. By adjusting these chemical parameters, the formulation achieves high drug concentration while maintaining simplicity, addressing both solubility and complexity concerns
2Quantity of substance
If low concentration drug solutions are used, then the formulation is simple, but the administration volume becomes large and bioavailability is reduced
Solution Approach 1:
The patent changes the concentration parameter by developing a formulation that achieves 10 mg/mL (high concentration) through optimized carrier and co-solvent selection. This high concentration reduces the administration volume required to deliver the therapeutic dose, directly addressing the contradiction between concentration and volume
Solution Approach 2:
The patent applies local quality by concentrating the drug in a small volume through specific carrier-drug interactions. The formulation creates a localized high-concentration solution that maintains stability, allowing efficient drug delivery without requiring large administration volumes
3Quantity of substance
If high concentration drug solutions are prepared, then the administration volume is reduced, but the formulation stability becomes challenging to maintain
Solution Approach 1:
The patent uses a stable composite formulation combining opiranserin hydrochloride with specific carriers (sodium benzoate, trisodium citrate, or sodium salicylate) and co-solvents. This composite system maintains formulation stability at high concentrations (10 mg/mL) through synergistic interactions between components, resolving the contradiction between high concentration and stability
Solution Approach 2:
The patent introduces carriers (sodium benzoate, trisodium citrate, sodium salicylate) as intermediaries that mediate between the drug and the aqueous environment. These intermediaries stabilize the high-concentration formulation by preventing precipitation and maintaining solubility, addressing both concentration and stability requirements
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 enables the preparation of a high-concentration opiranserin solution that maintains stability and can be used conveniently in medical settings, ensuring accurate and efficient administration.
Implementation Method 1
a carrier selected from sodium benzoate, trisodium citrate, sodium salicylate and a mixture thereof
Data Source
Figure 1
AI summary
A pharmaceutical composition containing a high concentration of opiranserin is disclosed. More specifically, disclosed is a pharmaceutical composition comprising: opiranserin or a pharmaceutically acceptable salt thereof; a carrier selected from sodium benzoate, trisodium citrate, sodium salicylate and mixtures thereof; and a solvent for injection.