Lyophilized TAT-NR2B9c Formulation for Stroke Treatment

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Solution Overview

Problem

Current treatments for stroke and ischemic conditions often require immediate diagnosis to administer medication, but existing formulations are not stable enough for prehospital use, limiting their availability at the scene of an incident.

Innovation Solution

A lyophilized formulation of TAT-NR2B9c, combined with histidine and trehalose, which is stable at room temperature and can be reconstituted with an aqueous solution, allowing for administration before reaching a medical facility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current stroke treatment formulations are used, then immediate diagnosis and administration is required, but the formulations are not stable enough for prehospital use

Engineering Contradiction:
Improveformulation stabilityVSAvoidadministration accessibility
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent changes the physical and chemical parameters of the TAT-NR2B9c formulation by adjusting pH to 6-7 and adding specific excipients (histidine and trehalose), transforming it from an unstable liquid formulation to a stable lyophilized solid formulation that can be stored at room temperature without refrigeration

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent utilizes lyophilization (freeze-drying) to transition the formulation from liquid phase to solid phase, creating a stable lyophilized cake that can be stored at room temperature and then reconstituted with aqueous solution immediately before administration, enabling prehospital use

Inventive Principle:
Principle #36Phase transitions

2Stability of the object's composition

If lyophilized formulation is prepared, then room temperature stability is achieved, but reconstitution process is required

Engineering Contradiction:
Improveroom temperature stabilityVSAvoidformulation preparation steps
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The formulation is prepared in advance as a lyophilized cake with all necessary excipients (histidine buffer and trehalose) already incorporated, so that upon arrival at the medical facility, only simple reconstitution with aqueous solution is needed, eliminating the need for complex preparation steps

Inventive Principle:
Principle #10Preliminary action

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 formulation maintains stability and potency, enabling effective treatment of stroke and ischemic conditions even in emergency settings without the need for immediate diagnosis, reducing infarction size and functional deficits.

Implementation Method 1

A lyophilized formulation of TAT-NR2B9c, combined with histidine and trehalose, which is stable at room temperature

Methodology Applied
Scientific EffectFreeze-drying: Freeze Drying

Implementation Method 2

reconstituted with an aqueous solution, allowing for administration before reaching a medical facility

Methodology Applied
Scientific EffectReconstitution:

Data Source

PatentEP2925338B8Lyophilized formulation of tat-NR2b9c
Publication Date: 2019.05.22 NONO INC

AI summary

The present invention provides lyophilized formulations of active agents, particularly of TAT-NR2B9c. TAT-NR2B9c has shown promise for treating stroke, aneurysm, subarachnoid hemorrhage and other neurological or neurotraumatic conditions. Such formulations are stable at room temperature thus facilitating maintenance of supplies of such a formulation in ambulances for administration at the scene of illness or accident or in transit to a hospital.