Lidocaine Heparin Buffer pH Control
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Solution Overview
Problem
Existing compositions for treating urinary bladder symptoms such as interstitial cystitis and overactive bladder face challenges in maintaining the bioavailability of local anesthetics like lidocaine due to precipitation when mixed with heparin and a buffer, particularly at pH levels above 7.0, which reduces their efficacy.
Innovation Solution
A method involving the preparation of a composition by dissolving heparin and lidocaine in solid form in water and then adding a buffer like sodium bicarbonate to achieve a pH between 6.7 and 8.3, specifically 7.4, to prevent precipitation and maintain bioavailability, ensuring stability and efficacy for instillation into the urinary bladder.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If lidocaine is mixed with heparin and buffer at pH above 7.0, then the composition achieves effective pH for treating urinary bladder conditions, but lidocaine precipitates and loses bioavailability
Solution Approach 1:
The patent applies preliminary action by adjusting the pH of the buffer solution before mixing with lidocaine and heparin. The buffer is pre-adjusted to a specific pH range (6.8-7.2) to prevent lidocaine precipitation during the mixing process, ensuring the final composition maintains lidocaine bioavailability while achieving therapeutic effectiveness.
Solution Approach 2:
The patent applies parameter changes by precisely controlling the pH parameter of the buffer solution within a narrow range (6.8-7.2). This parameter optimization prevents lidocaine precipitation while maintaining the composition's therapeutic efficacy for treating urinary bladder conditions, resolving the contradiction between stability and effectiveness.
2Stability of the object's composition
If the composition is prepared with solid heparin and lidocaine dissolved in water followed by buffer addition, then precipitation is prevented and bioavailability is maintained, but the manufacturing process becomes more complex
Solution Approach 1:
The patent applies segmentation by dividing the composition preparation into distinct sequential steps: first dissolving solid heparin and lidocaine in water to form a base solution, then separately preparing and adding the buffer solution. This segmented approach allows precise control of each component's dissolution and mixing conditions, preventing precipitation while maintaining a manageable manufacturing process.
Solution Approach 2:
The patent applies preliminary action by pre-dissolving heparin and lidocaine in water before buffer addition, and pre-adjusting the buffer pH beforehand. These preliminary preparations ensure that when components are combined, lidocaine remains stable and bioavailable, simplifying the overall manufacturing by preventing precipitation issues during mixing.
3Duration of action of moving object
If buffer is added to achieve optimal pH for treatment, then the composition becomes effective for prolonged relief, but lidocaine precipitation occurs reducing bioavailability
Solution Approach 1:
The patent applies parameter changes by optimizing the buffer pH to a specific range (6.8-7.2) that simultaneously achieves prolonged symptom relief duration and maintains lidocaine bioavailability. This precise parameter control ensures that the therapeutic duration is extended without sacrificing the quantity of active lidocaine available for treatment.
Solution Approach 2:
The patent applies preliminary action by pre-adjusting the buffer pH before mixing with the lidocaine-heparin solution. This preliminary pH adjustment ensures that when the buffer is added to extend the duration of action, lidocaine precipitation is prevented, maintaining both prolonged relief and adequate bioavailability.
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 method maintains the stability and bioavailability of lidocaine, resulting in a composition that effectively treats lower urinary tract conditions without precipitation, providing prolonged relief and improved efficacy compared to previous methods.
Implementation Method 1
adding a buffer like sodium bicarbonate to achieve a pH between 6.7 and 8.3, specifically 7.4, to prevent precipitation and maintain bioavailability
Implementation Method 2
The method maintains the stability and bioavailability of lidocaine, resulting in a composition that effectively treats lower urinary tract conditions without precipitation
Data Source
AI summary
An improved method for preparing a composition including a heparinoid, a local anesthetic, and a buffer for treatment of a lower urinary tract disease or condition can comprise: (i) providing a heparinoid in solid form or liquid form; (ii) providing a local anesthetic in solid form or liquid form; (iii) adding a liquid buffer to the heparinoid in solid form or liquid form; (Iv) adding the local anesthetic to the mixture of the liquid buffer and the heparinoid; and (v) if necessary, adjusting the pH of the mixture of the liquid buffer, the local anesthetic, and the heparinoid so that a pH is achieved of from about 6.8 to about 8.3 is achieved without precipitation of the local anesthetic.