Botulinum Toxin pH-Neutralizing Mixing Device

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Solution Overview

Problem

Current Botulinum toxin pharmaceutical formulations either have short shelf-life or are painful upon administration due to acidic pH, leading to protein denaturation and increased antigenicity, which affects efficacy and patient comfort.

Innovation Solution

A device with multiple chambers storing an acidic Botulinum toxin solution and an acid-neutralizing solution, allowing mixing just before administration to adjust the pH to a neutral or alkaline range (6.5-7.4), minimizing pain and maintaining stability and shelf-life.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of stationary object

If Botulinum toxin is formulated as a liquid with low pH to maintain shelf-life stability, then shelf-life is improved, but pain upon administration increases

Engineering Contradiction:
Improveshelf-lifeVSAvoidpain upon administration
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The formulation is divided into two separate compartments: an acidic compartment containing Botulinum toxin at low pH for stability, and a neutralizing compartment containing base solution. The compartments remain separated during storage to maintain shelf-life, then mix upon activation to reduce pain upon administration.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The acid-neutralizing solution is prepared in advance and kept ready in a separate compartment. When needed, the barrier is broken to allow pre-prepared neutralizing solution to mix with the acidic toxin solution, converting it to a less painful formulation just before administration.

Inventive Principle:
Principle #10Preliminary action

2Duration of action of stationary object

If freeze- or flash-drying is used to stabilize Botulinum toxin at pH 7.4, then shelf-life is improved, but protein denaturation and antigenicity increase

Engineering Contradiction:
Improveshelf-lifeVSAvoidprotein stability
Core Design Contradiction:
Duration of action of stationary objectVSStability of the object's composition

Solution Approach 1:

The formulation maintains the toxin in liquid form at low pH where it is naturally stable, avoiding the phase changes and stress conditions of freeze- or flash-drying. The low pH parameter is maintained during storage, then adjusted after mixing with neutralizing solution to achieve both stability and reduced antigenicity.

Inventive Principle:
Principle #35Parameter changes

3Ease of manufacture

If acidic pH formulation is used to achieve room temperature stability, then ease of storage is improved, but pain upon injection increases

Engineering Contradiction:
Improvestorage convenienceVSAvoidinjection pain
Core Design Contradiction:
Ease of manufactureVSObject-affected harmful factors

Solution Approach 1:

The formulation transitions from a static acidic state (stable but painful) to a dynamic two-compartment system where the pH can change from acidic to neutral upon mixing. This dynamic approach allows the same formulation to provide both room-temperature stability during storage and reduced pain upon administration.

Inventive Principle:
Principle #15Dynamics

4Reliability

If sodium chloride is added to Botulinum toxin solution, then osmotic balance is improved, but protein denaturation increases during freeze-drying

Engineering Contradiction:
Improveosmotic balanceVSAvoidprotein stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The problematic sodium chloride is removed from the formulation. Instead, the invention uses the natural stability of Botulinum toxin at low pH in salt-free aqueous solution, eliminating the source of hypertonicity-induced denaturation while maintaining both osmotic balance and protein stability.

Inventive Principle:
Principle #2Taking out (Extraction)

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 solution results in a less painful, stable, and effective Botulinum toxin formulation with maintained potency, as evidenced by regional denervating assays, ensuring improved patient comfort and prolonged shelf-life without sacrificing stability.

Implementation Method 1

an acid-neutralizing solution, wherein the acid-neutralizing solution is present in an amount sufficient to raise the pH of the acidic solution of Botulinum toxin to about pH 6.5 to about pH 7.5 after mixing

Methodology Applied
Scientific EffectpH neutralization: Redox Reactions

Data Source

PatentUS8192979B2Compositions, methods and devices for preparing less painful Botulinum toxin formulations
Publication Date: 2012.06.05 REVANCE THERAPEUTICS INC

AI summary

Devices, methods and kits are disclosed for preparing and administering less-painful formulations of Botulinum toxin. The devices, methods and kits of the present invention are comprised of or use an acidic formulation of Botulinum toxin, or, in certain embodiments, a freeze- or flash-dried composition of Botulinum toxin, having a long shelf-life which is subsequently mixed with an acid-neutralizing solution and, optionally a sequestration agent prior to administration to a patient in need thereof. The pH-neutralized formulation of Botulinum toxin is pharmaceutically acceptable for administration to a patient and is significantly less painful than acidic formulations of Botulinum toxin or formulations of Botulinum toxin having unnecessary antigens.