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Preparations of leucovorin and its carbonates

A technology of leucovorin and folinic acid, which is applied to medical preparations containing active ingredients, pharmaceutical formulas, blood diseases, etc., can solve the problems of high manufacturing cost, complicated process, and low pharmaceutical efficiency, and achieve easy industrial production and effective results High, simple and effective method

Inactive Publication Date: 2003-11-19
杭州新望族科技有限公司 +1
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  • Summary
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  • Description
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  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the above two preparation methods are relatively complex in process, difficult to ensure industrial production, and the manufacturing cost is high, and the efficiency of pharmacy is low.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0012] Example 1: Take DEAE cellulose with a suitable particle size and put it on the column (5cm×120cm), rinse it with EDTA-2Na buffer solution of pH 8.5; dissolve 30g (6RS)-calcium folinate in 200ml hot water, and after cooling Put on the column, wash with the EDTA-2Na buffer solution of pH8.5, detect with the HPLC of the protein silica gel column, collect the solution when the (6S)-folinate content is greater than 80%, adjust the pH7.0, add ethanol to separate out ( 6S)-calcium folinate, and then recrystallized with water for 1 to 3 times to obtain more than 99% (6S)-calcium folinate.

example 2

[0013] Example 2: Take a magnesium silicate adsorbent with a suitable particle size and put it on the column (5cm×120cm), rinse it with an ammonium salt buffer solution with a pH of 8.5 to 9.0; take 30g (6RS)-calcium folinate and dissolve it in 200ml hot water , put it on the column after cooling, rinse with ammonium salt buffer solution with pH 9.0, detect with HPLC on protein silica gel column, collect the solution when the content of (6S)-leucovorin is greater than 80%, adjust the pH to 7.0, and add ethanol to precipitate (6S)-calcium folinate is obtained, and then recrystallized with water for 1 to 3 times to obtain more than 99% (6S)-calcium folinate.

example 3

[0014] Example 3, take an alkaline alumina adsorbent with a suitable particle size and put it on the column (5cm×120cm), rinse it with an aqueous solution; get 30g (6RS)-calcium folinate and dissolve it in 200ml hot water, put it on the column after cooling, and wash it with an aqueous solution Rinse, use protein silica gel column for HPLC detection, collect the solution when the content of (6S)-leucovorin is greater than 80%, adjust the pH to 7.0, add ethanol to precipitate (6S)-calcium folinate, and then recrystallize with water for 1~ Get more than 99% (6S)-leucovorin calcium for 3 times.

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PUM

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Abstract

A process for preparing levo-folinic acid and its calcium salt includes such steps as dissolving (6RS)-folinic acid and its calcium salt, chromatography with the adsorption column of neutral or alkaline adsorbent, eluting, collecting solution, regulating pH to 7.0, adding alcohol to educe out (6S)-folinic acid and its calcium salt, and recrystallizing in water 1-3 times. Its advantages are high purity (99% or more), high output and low cost.

Description

technical field [0001] The invention relates to a preparation method of (6S)-folinic acid and its calcium salt, especially a direct preparation method of (6S)-folinic acid calcium, which is mainly used as a detoxification antagonist of anti-anemia and tumor drugs. Background technique [0002] In the Chinese Patent Gazette, there are two invention patents about the preparation method of calcium levofolinate, the patent numbers are 88102709.X and 89109727.9 respectively. Other related technologies also have similar disclosures in foreign technical magazines. However, all the current technical publications can be summarized into two preparation routes of (6S)-calcium folinate, and route <1> is an intermediate resolution method: (6S) can be obtained by resolution of (6RS)-tetrahydrofolate -Tetrahydrofolate, through cyclization to obtain (6R)-5,10-methylenetetrahydrofolate, or directly resolve from (6RS)-5,10-methylenetetrahydrofolate to obtain (6R)-5 , 10-Methylenetetra...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P7/06A61P35/00A61P39/02C07D475/06
Inventor 姚培元黄羿
Owner 杭州新望族科技有限公司
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