Ready-to-Use Ascorbic Acid Composition Stabilization
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Solution Overview
Problem
Current pharmaceutical formulations of ascorbic acid for parenteral administration, such as scurvy treatment, require dilution before use, leading to potential dosing errors and contamination risks, and are challenging to stabilize in aqueous solutions due to oxidation, necessitating refrigerated storage and complex handling procedures.
Innovation Solution
Development of ready-to-use pharmaceutical compositions of ascorbic acid that are pre-mixed and stable at room temperature for extended periods, eliminating the need for dilution and allowing direct administration, incorporating stabilizing agents like sodium metabisulfite and edetate disodium to maintain efficacy and safety.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If ascorbic acid is formulated in aqueous solution for parenteral administration, then it can be administered directly to patients, but it undergoes oxidation and degradation leading to quality and color changes
Solution Approach 1:
The patent introduces stabilizing agents as intermediary substances that mediate between ascorbic acid and the aqueous environment. Specifically, it uses metal chelating agents (such as edetate disodium) and antioxidant agents (such as sodium metabisulfite) that act as intermediaries to prevent oxidation and degradation of ascorbic acid while maintaining its stability in the aqueous formulation for direct parenteral administration
Solution Approach 2:
The patent creates a composite pharmaceutical composition by combining ascorbic acid with multiple stabilizing agents, chelating agents, and antioxidant agents in a single aqueous formulation. This composite approach allows the formulation to maintain both direct administrability and chemical stability through the synergistic effects of multiple components working together to protect ascorbic acid from degradation
2Ease of operation
If ascorbic acid is stored in aqueous solution, then it can be ready for immediate use, but it requires refrigerated storage to prevent oxidation
Solution Approach 1:
The patent employs stabilizing agents as intermediaries that enable the formulation to be stored at room temperature while maintaining stability. The metal chelating agents and antioxidant agents act as protective intermediaries that prevent oxidation reactions, thereby eliminating the need for refrigeration while preserving immediate use readiness
Solution Approach 2:
The patent changes the chemical parameters of the formulation by adding specific stabilizing agents, chelating agents, and antioxidant agents. These parameter changes in composition allow the aqueous solution to be stored at elevated temperatures (room temperature) without undergoing oxidation or degradation, thus removing the refrigeration requirement while maintaining readiness for use
3Quantity of substance
If ascorbic acid is provided in high concentration for scurvy treatment, then it can treat the condition effectively, but it requires dilution before use increasing complexity
Solution Approach 1:
The patent performs the stabilizing action in advance by pre-formulating the ascorbic acid solution with stabilizing agents, chelating agents, and antioxidant agents before administration. This preliminary stabilization allows the high-concentration formulation to be used directly without requiring dilution, thereby maintaining treatment efficacy while eliminating the complexity of dilution procedures
Solution Approach 2:
The patent uses stabilizing agents as intermediaries that enable high-concentration ascorbic acid to be stored and administered directly. The chelating and antioxidant agents act as protective intermediaries that prevent degradation at high concentrations, allowing the formulation to skip the dilution step while maintaining both efficacy and safety
4Stability of the object's composition
If ascorbic acid is formulated requiring dilution, then it can be stabilized, but it increases risk of dosing errors and contamination
Solution Approach 1:
The patent performs all necessary stabilization actions in advance during the formulation process by incorporating stabilizing agents, chelating agents, and antioxidant agents before the product reaches the patient. This preliminary stabilization ensures the formulation remains stable without requiring subsequent dilution, thereby eliminating the risks of dosing errors and contamination associated with dilution procedures
Solution Approach 2:
The patent employs stabilizing agents as intermediaries that protect ascorbic acid from degradation throughout storage and administration. The chelating and antioxidant agents act as protective intermediaries that maintain formulation stability without requiring dilution, thereby improving reliability by eliminating dosing errors and contamination risks associated with the dilution process
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 ready-to-use compositions provide a stable, safe, and convenient form of ascorbic acid for scurvy treatment, reducing waste and contamination risks while maintaining therapeutic effectiveness and stability at room temperature for several months, thus improving patient care and healthcare efficiency.
Implementation Method 1
ascorbic acid is easily oxidized in aqueous solution. The degradation processes of ascorbic acid are very complex, such processes containing several oxidation/reduction and intermolecular rearrangement reactions
Data Source
AI summary
The invention described here provides ready-to-use (RTU) pharmaceutical compositions in single unit dose packaging, such compositions including ascorbic acid compound(s), such as sodium ascorbate, and one or more pharmaceutically acceptable excipients (e.g., a carrier and optionally other agents, such as a tonicity agent, a chelator, or both). The compositions provided by the invention are stable when stored at 20° C. to 25° C.±2° C. for at least about 3 months. Compositions provided by the invention comprise an osmolality of between about 270 mOsm/kg to about 340 mOsm/kg and do not require dilution or further manipulation prior to use. In certain aspects, the invention comprises methods of using such compositions in the treatment of diseases, conditions, or symptoms related to vitamin C deficiency, such as, in specific embodiments, scurvy.