Composition containing 5,10-methylene-(6R)-tetrahydrofolate disodium
A lyophilized composition of 5,10-methylene-(6R)-tetrahydrofolic acid with citrate and alkali metal sulfate addresses stability issues, achieving high stability and purity for pharmaceutical use, suitable for cancer treatment.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- MERCK PATENT GMBH
- Filing Date
- 2023-06-05
- Publication Date
- 2026-07-23
AI Technical Summary
Existing formulations of 5,10-methylene-(6R)-tetrahydrofolic acid (5,10-CH2-(6R)-THF) are unstable due to susceptibility to oxidation and chemical decomposition, particularly in aqueous solutions and amorphous forms, limiting their pharmaceutical applications.
A lyophilized composition comprising the disodium salt of 5,10-methylene-(6R)-tetrahydrofolic acid (5,10-CH2-(6R)-THF*Na2) combined with citrate and alkali metal sulfate, which provides stability equivalent to or better than formulations with reducing agents like L-(+)-ascorbic acid, without the need for antioxidants, and results in a high-content, stable lyophilized product.
The composition maintains high stability and purity, allowing for the preparation of solid-state pharmaceutical compositions with a high content of 5,10-CH2-(6R)-THF*Na2, suitable for pharmaceutical use, and can be administered intramuscularly or intravenously.
Smart Images
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