Stable Cyclophosphamide Liquid Formulations via Moisture Control
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Solution Overview
Problem
Current formulations of cyclophosphamide are limited to solid forms due to its instability in aqueous solutions, lacking stable liquid formulations suitable for commercial use.
Innovation Solution
Development of stable liquid formulations of cyclophosphamide with a moisture content less than 2.0% by weight, achieved through a process involving the reduction of moisture content using suitable drying methods and adsorbents like molecular sieves.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If cyclophosphamide is formulated in aqueous solutions, then it is soluble and can be administered, but it degrades rapidly and loses stability
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by using non-aqueous solvents (ethanol, propylene glycol, polyethylene glycol) instead of water, and by controlling moisture content below 2.0%, thereby maintaining both solubility and stability of cyclophosphamide
Solution Approach 2:
The patent creates an inert environment by formulating cyclophosphamide in non-aqueous media and maintaining low moisture content, protecting the drug from hydrolytic degradation while preserving its solubility and administrability
2Stability of the object's composition
If solid formulations are used, then stability is maintained, but ease of administration and patient compliance are reduced
Solution Approach 1:
The patent transforms the physical state parameter from solid to liquid by developing stable liquid formulations with controlled moisture content and non-aqueous solvents, thereby improving ease of administration while maintaining stability through optimized composition
3Ease of operation
If moisture content is increased to improve solubility, then liquid formulation becomes more stable, but cyclophosphamide degradation accelerates
Solution Approach 1:
The patent optimizes the moisture content parameter to below 2.0% and selects specific non-aqueous solvents, achieving a balance where the liquid formulation remains stable without accelerating cyclophosphamide degradation
Solution Approach 2:
The patent uses composite solvent systems combining ethanol with propylene glycol or polyethylene glycol, creating a composite material that provides both solubility and stability while maintaining low moisture content
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 resulting stable liquid formulations of cyclophosphamide are suitable for parenteral administration, offering improved stability, safety, and ease of use, while reducing the risk of contamination and extending shelf life.
Implementation Method 1
The invention also relates to stable liquid formulations of cyclophosphamide prepared by a process comprising a step of reducing the moisture content from cyclophosphamide or liquid compositions of cyclophosphamide or both
Data Source
AI summary
The present invention relates to stable liquid pharmaceutical formulations of cyclophosphamide comprising cyclophosphamide and at least one pharmaceutically acceptable excipient wherein moisture content of the liquid formulation is less than about 2.0% by weight. The invention further relates to stable liquid formulations of cyclophosphamide prepared by a process comprising a step of reducing the moisture content from cyclophosphamide or liquid compositions of cyclophosphamide or both. The invention further relate to method of using such stable liquid formulations of cyclophosphamide for parenteral administration either as ready-to-use or ready-to-dilute for treating various cancer disorders.