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Method for preparing L-sodium folinate or DL-sodium folinate

A technology of sodium leucovorin and sodium folinate, which is applied in the field of medicine, can solve the difficulties in quality control and preparation research of sodium leucovorin or sodium folinate, and does not prepare sodium folinate or sodium folinate solid , Oxidation, cyclization, hydrolysis and other problems are prone to occur, achieving the effect of low equipment requirements, avoiding side effects, and easy operation

Active Publication Date: 2011-06-22
天津康鸿医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This preparation method has the following disadvantages: on the one hand, the raw material used is folinic acid, which is unstable in aqueous solution compared with folinate, and is prone to reactions such as oxidation, cyclization, and hydrolysis; on the other hand, the prepared The product obtained is a sodium folinate solution, which brings difficulties to the quality control and formulation research of sodium levofolinate or sodium folinate
In the prior art, there is no method for preparing sodium levofolinate or sodium folinate

Method used

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  • Method for preparing L-sodium folinate or DL-sodium folinate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Dissolve 50g of calcium levofolinate in 5000mL of water, and the solution is treated with gel-type sodium-type cation exchange resin 001×7 (Nankai University Chemical Plant), to exchange cations, collect the exchange solution, wash 1200mL with water, and mix the solution with the exchange solution Combine, adjust the pH value to 10.0-11.0, concentrate under reduced pressure at 50°C to 500mL, ethanol precipitate with absolute ethanol, the final concentration of ethanol is 85%, filter the resulting precipitate, and dry under vacuum to obtain sodium levofolinate or mixed Sodium folinate solid.

Embodiment 2

[0046] Dissolve 60g of magnesium levofolinate in 2000mL of 10% ethanol, treat the solution with macroporous sodium-type cation exchange resin D001SS (Nankai University Chemical Factory), exchange cations, collect the exchange liquid, and then elute with 10% ethanol in 1000mL, and combine the elution solution and exchange solution, and adjust the pH value of the solution to 9.0-10.0, concentrate under reduced pressure at 40°C to 120mL, distill off ethanol, precipitate with isopropanol, the final concentration of isopropanol is 65%, and filter out the resulting precipitate and drying to obtain a solid sodium levofolinate.

Embodiment 3

[0048] Dissolve 10 g of leucovorin in 1000 mL of water, and the solution is treated with sodium-type cation-exchange chromatography cellulose SE-Cellulose (Beijing Hengye Zhongyuan Chemical Co., Ltd.) to exchange cations, collect the exchange liquid, and then elute with 300 mL of water, and combine The eluate and the exchange solution were adjusted to a pH value of 8.5-9.5, concentrated under reduced pressure at 60°C to 30 mL, and lyophilized in vacuo to obtain a solid of vortex sodium folinate.

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Abstract

The invention relates to a preparation method of L-sodium folinate or DL-sodium folinate. The preparation method comprises the following steps of: exchanging positive ions with a sodium ion-exchange material by taking an alkaline-earth metal salt of L-folinate or DL-folinate as a raw material to obtain L-sodium folinate or DL-sodium folinate; and concentrating the solution of the obtained L-sodium folinate or DL-sodium folinate, depositing in alcohol, drying under reduced pressure or performing freeze drying to obtain a L-sodium folinate or DL-sodium folinate solid. The preparation method hasthe advantages of mild and controllable condition, easiness and convenience in operating, and low requirement on equipment condition, and is beneficial to the industrialized production; moreover, an obtained active pharmaceutical ingredient solid is beneficial to quality researches before preparation, and provides foundations for the development of novel preparation formulations or the optimization of the conventional formulations.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular, the invention relates to a method for preparing sodium levofolinate or sodium folinate. Background technique [0002] Folinic acid (5-formyl-5,6,7,8-tetrahydrofolate) is a folic acid derivative, its pharmacological activity is similar to folic acid, it is often used as an antidote for the overdose of anti-folate metabolites, and it can also be used in giant Treatment of erythroblastic anemia and leukopenia. [0003] There are two configurations of R and S on the 6-position carbon atom of folinic acid, and it has been used as a mixture of diastereomers. Studies have shown that the two isomers have different effects on enzymes in vivo. Among them, the compound with the configuration of the 6th carbon atom as the S configuration (left-handed) shows good efficacy, while the configuration of the 6th carbon atom is S configuration (left-handed). Compounds with the R configuration (dex...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D475/04
Inventor 侯文彬邹美香李袆亮孙歆慧单淇李鹏旺石玉张彩霞周渭渭吴疆任晓文
Owner 天津康鸿医药科技发展有限公司