Ready-to-Use Aqueous Ganciclovir Compositions at Lower Injection pH

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current lyophilized ganciclovir products are costly to manufacture, require aseptic reconstitution, and have a high pH that causes injection site reactions in some patients.

Innovation Solution

Development of stable, injectable, and ready-to-administer aqueous ganciclovir compositions with a ganciclovir base at 2.0 mg/ml, isotonic agents, and pH adjusters to achieve a pH of 5.5 to 8, which are terminally sterilized and free of particulate matter.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If lyophilized powder product is used, then ganciclovir can be provided as a stable formulation, but manufacturing cost increases and requires reconstitution

Engineering Contradiction:
Improveformulation stabilityVSAvoidmanufacturing cost
Core Design Contradiction:
Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The patent changes the physical state parameter from lyophilized powder to liquid formulation, and adjusts pH from 11 to 5.5-8.0, transforming the product into a ready-to-administer liquid that eliminates reconstitution steps while reducing manufacturing complexity and cost

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If lyophilized powder product is used, then ganciclovir can be provided as a stable formulation, but reconstitution requires aseptic technique which could lead to sterility compromise

Engineering Contradiction:
Improveformulation stabilityVSAvoidsterility reliability
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The patent performs sterility assurance during the final filling and sealing process rather than requiring aseptic technique at the point of use. The liquid formulation is filled into containers and sealed under controlled conditions, with terminal sterilization applied to the finished product, eliminating the need for healthcare providers to perform aseptic reconstitution

Inventive Principle:
Principle #10Preliminary action

3Quantity of substance

If ganciclovir sodium salt is used, then solubility is improved, but pH becomes 11 which causes injection site reactions

Engineering Contradiction:
ImprovesolubilityVSAvoidinjection site reactions
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent changes the pH parameter from 11 to 5.5-8.0 by using ganciclovir base instead of ganciclovir sodium salt and adding pH adjusters (hydrochloric acid or sulfuric acid), thereby maintaining adequate solubility while eliminating injection site reactions caused by high pH

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

The compositions provide stability, ease of administration, and reduced pH, minimizing manufacturing costs and patient discomfort, while maintaining solubility and sterility.

Implementation Method 1

a pH adjuster to adjust the pH of the composition from about 5.5 to about 8

Methodology Applied
Scientific EffectpH adjustment:

Implementation Method 2

either sodium chloride or dextrose as a tonicity agent at a concentration sufficient to make the composition isotonic

Methodology Applied
Scientific EffectTonicity regulation: Osmotic Pressure

Implementation Method 3

the composition is terminally sterilized

Methodology Applied
Scientific EffectTerminal sterilization:

Data Source

PatentUS20250319189A1Ganciclovir compositions and related methods
Publication Date: 2025.10.16 EXELA PHARMA SCIENCES LLC

AI summary

Gancyclovir formulations that are ready-to-use, substantially particulate free, and stable upon storage are disclosed. Methods of manufacture and administration of such compositions are also provided.