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Stable medicine composition of 5-methyltetrahydrofolic acid or salt thereof

A technology of methyltetrahydrofolate and composition, which is applied in the direction of drug combination and metabolic diseases, and can solve problems such as content decline, poor stability, and easy discoloration

Inactive Publication Date: 2014-05-07
广东岭南制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to overcome the disadvantages of 5-methyltetrahydrofolate or its salts, such as poor stability, easy discoloration, obvious decrease in content, increased degradation products, and large toxic and side effects, and provide a preparation containing 5-methyltetrahydrofolate. stable composition

Method used

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  • Stable medicine composition of 5-methyltetrahydrofolic acid or salt thereof
  • Stable medicine composition of 5-methyltetrahydrofolic acid or salt thereof
  • Stable medicine composition of 5-methyltetrahydrofolic acid or salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Embodiment 1: the preparation of 5-methyltetrahydrofolate for injection (1000 bottle amount)

[0092]

[0093] Process: Take about 1.5L of water for injection, add mannitol, arginine and calcium 5-methyltetrahydrofolate, stir to dissolve, adjust the pH value to about 7.5 with 1mol sodium hydroxide solution, add water for injection to 2L, and dissolve the solution Sterile filtration is carried out under sterile conditions, the solution is divided into 2ml, and freeze-dried. Each bottle contains 50mg of 5-methyltetrahydrofolate.

Embodiment 2

[0094] Embodiment 2: the preparation of 5-methyltetrahydrofolate for injection (1000 bottle amount)

[0095]

[0096] Process: Take about 1.5L of water for injection, add mannitol, isoleucine, arginine and calcium 5-methyltetrahydrofolate, stir to dissolve, adjust the pH value to about 7.5 with 1mol sodium hydroxide solution, add water for injection to 2L, the solution was sterilized and filtered under aseptic conditions, the solution was divided into 2ml, and freeze-dried. Each bottle contains 50mg of 5-methyltetrahydrofolate.

Embodiment 3

[0097] Embodiment 3: Preparation of 5-methyltetrahydrofolate aqueous injection preparation (1000 bottles)

[0098]

[0099] Process: Process: Take about 1.5L of water for injection, add sodium chloride, methionine and calcium 5-methyltetrahydrofolate, stir to dissolve, adjust the pH value to about 7.5 with 1mol sodium hydroxide solution, add water for injection to 2L, and The solution is sterilized and filtered under aseptic conditions, and the solution is divided into 2ml. Each bottle contains 50mg of 5-methyltetrahydrofolate.

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Abstract

The invention relates to a stable medicine composition of 5-methyltetrahydrofolic acid or salt thereof. Specifically, the composition contains (a) 5-methyltetrahydrofolic acid or salt thereof, (b) amino acid or salt thereof, and (c) optional physiologically-acceptable accessories. The composition provided by the invention has good pharmaceutical properties.

Description

technical field [0001] The present invention relates to a stable pharmaceutical composition such as a pharmaceutical preparation made of 5-methyltetrahydrofolate or its salt, and specifically relates to a preparation prepared by adding specific pharmaceutical excipients to 5-methyltetrahydrofolate or its salt. The auxiliary material is one or more of amino acids or their salts. This preparation can be used in the rescue of folic acid antagonists such as high dose methotrexate. technical background [0002] 5-Methyltetrahydrofolate and its salts can be represented by following structural formula I: [0003] [0004] Wherein X1 and X2 are each independently selected from H, alkali metals or alkaline earth metals, for example X1 and X2 may each independently be selected from H, Na, Ca, Mg or Ba. For example, the calcium salt of the compound of formula I, i.e. calcium 5-methyltetrahydrofolate, has the structure of the following formula Ia: [0005] [0006] Preparations...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61P3/02
Inventor 徐文凯王荣陈良强
Owner 广东岭南制药有限公司
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