Bendamustine Liquid Composition for Small-Volume IV Solubility

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Solution Overview

Problem

Current bendamustine formulations face solubility limitations at lower volumes, leading to potential drug precipitation and side effects during small volume infusions, necessitating large volumes and long infusion times, which are uncomfortable for patients and increase the risk of extravasation.

Innovation Solution

A liquid composition containing bendamustine, polyethylene glycol, and propylene glycol as solubilizers, administered in volumes of 325 ml or less over 30 minutes or less, maintaining solubility and avoiding precipitation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If bendamustine is administered in smaller infusion volumes to improve patient comfort and reduce extravasation risk, then patient comfort and safety are improved, but solubility limitations cause drug precipitation and side effects

Engineering Contradiction:
Improvepatient comfortVSAvoiddrug solubility
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent changes the chemical parameters of the formulation by introducing polyethylene glycol and propylene glycol as co-solvents, which alter the solubility characteristics of bendamustine. This allows the drug to remain soluble at higher concentrations in smaller volumes, resolving the contradiction between reduced infusion volume and maintained solubility.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite solvent system combining polyethylene glycol, propylene glycol, and aqueous buffers. This composite material provides enhanced solubility capacity compared to单一 solvents, enabling concentration of bendamustine in smaller volumes without precipitation, thus improving patient comfort while maintaining drug stability.

Inventive Principle:
Principle #40Composite materials

2Reliability

If large infusion volumes are used to maintain drug solubility, then drug precipitation is avoided, but patient discomfort and infusion time increase

Engineering Contradiction:
Improvedrug solubilityVSAvoidinfusion time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

By modifying the solvent composition parameters to include polyethylene glycol and propylene glycol, the patent increases the solubility capacity of the formulation. This allows administration of therapeutic doses in smaller volumes over shorter times, reducing infusion time while preventing drug precipitation through enhanced solubility properties.

Inventive Principle:
Principle #35Parameter changes

3Volume of stationary object

If bendamustine concentration is increased to reduce infusion volume, then infusion volume is reduced, but solubility is exceeded and precipitation occurs

Engineering Contradiction:
Improveinfusion volumeVSAvoiddrug stability
Core Design Contradiction:
Volume of stationary objectVSReliability

Solution Approach 1:

The patent changes the physical-chemical parameters of the formulation system by incorporating polyethylene glycol and propylene glycol, which fundamentally alter the solubility envelope of bendamustine. This enables concentration of the drug at levels that reduce infusion volume to practical ranges while maintaining stability and preventing precipitation through the extended solubility provided by the glycol-based solvent system.

Inventive Principle:
Principle #35Parameter changes

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

Enables administration of bendamustine in smaller volumes and shorter times, reducing patient discomfort and side effects while maintaining drug solubility, thus improving patient experience and safety.

Implementation Method 1

a solubilizer comprising polyethylene glycol and propylene glycol

Methodology Applied
Scientific EffectSolubilization: Solvation

Data Source

PatentUS20260000767A1Formulations of bendamustine
Publication Date: 2026.01.01 EAGLE PHARMACEUTICALS INC

AI summary

Methods of treatment using bendamustine formulations designed for small volume intravenous administration are disclosed. The methods conveniently allow shorter administration time without the active ingredient coming out of solution as compared to presently available formulations.