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Stable pharmaceutical composition of (6s)‐5‐methyl‐tetrahydrofolate calcium salt

By adding reducing substances such as vitamin C to the drug, 5-methyltetrahydrofolate calcium is protected from oxidation, solving its stability and safety problems, and achieving higher drug stability and lower JK12A content. Reduced risk of venous thrombosis.

Active Publication Date: 2021-04-20
LIANYUNGANG JINKANG HEXIN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] Although the above technology slows down the oxidation process of 5‐methyltetrahydrofolate, it cannot fundamentally avoid the harm of JK12A

Method used

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  • Stable pharmaceutical composition of (6s)‐5‐methyl‐tetrahydrofolate calcium salt
  • Stable pharmaceutical composition of (6s)‐5‐methyl‐tetrahydrofolate calcium salt
  • Stable pharmaceutical composition of (6s)‐5‐methyl‐tetrahydrofolate calcium salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Example 1 - direct compression tablet:

[0089] The composition of the prescription is as follows: 80mg / tablet

[0090]

[0091] The preparation method is as follows:

[0092] 1. Pass (6S)‐5‐methyl‐tetrahydrofolate calcium, lactose T80, microcrystalline cellulose PH112, hypromellose, and croscarmellose sodium through a 60-mesh sieve; stearic acid Magnesium through 80 mesh sieve;

[0093] 2. Mix the above-mentioned raw and auxiliary materials except magnesium stearate by doubling dilution method, so that the mixing is uniform;

[0094] 3. Add the prescribed amount of magnesium stearate to the mixture obtained in the above 2 to make the mixture uniform and avoid excessive lubrication.

[0095] 4. The theoretical tablet weight is 80 mg / tablet, and the tablet weight difference is controlled to be no more than 10%, the disintegration time limit is less than 15 minutes, and the friability is less than 1.0%.

[0096] 5.15% Opadry solution is used for film coating, the t...

Embodiment 2

[0097] Example 2 - Direct Compression:

[0098] The composition of the prescription is as follows: 80mg / tablet

[0099]

[0100] Preparation:

[0101] 1. Pass (6S)‐5‐methyl‐tetrahydrofolate calcium, vitamin C, pregelatinized starch PC‐10, microcrystalline cellulose PH112, and carboxymethyl starch sodium through a 60-mesh sieve; magnesium stearate 80 mesh sieve;

[0102] 2. Mix the above-mentioned raw and auxiliary materials except magnesium stearate by doubling dilution method, so that the mixing is uniform;

[0103] 3. Add the prescribed amount of magnesium stearate to the mixture obtained in the above 2 to make the mixture uniform and avoid excessive lubrication.

[0104] 4. The theoretical tablet weight is 80 mg / tablet, and the tablet weight difference is controlled to be no more than 10%, the disintegration time limit is less than 15 minutes, and the friability is less than 1.0%.

[0105] 5.15% Opadry solution is used for film coating, and the tablet bed temperature...

Embodiment 3

[0106] Embodiment 3-direct compression method

[0107] The composition of the prescription is as follows: 80mg / tablet

[0108]

[0109]

[0110] Preparation method: with reference to Example 1 and Example 2.

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PUM

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Abstract

The invention discloses a stable pharmaceutical composition, comprising (6S)-5-methyl-tetrahydrofolate calcium salt crystals and / or pharmaceutically acceptable reducing substances, and pharmaceutically acceptable auxiliary materials; wherein the Reducing substances capable of protecting (6S)‐5‐methyl‐tetrahydrofolate and its salts from oxidation, selected from vitamin C and its salts, isovitamin C and its salts, mercaptoethanol, cysteine, mercaptoethyl Sulfonic acid, dithiothreitol, reduced glutathione, lipoic acid. The stable pharmaceutical composition of the present invention has good stability during processing and storage, avoids the risk of medication due to degradation, and at the same time ensures the rapid and reliable release of (6S)-5-methyl-tetrahydrofolate in the composition.

Description

[0001] This application is a divisional application of a Chinese invention patent with an application date of 2014.09.04, an application number of 201410449805.4, and an invention name of a stable pharmaceutical composition of (6S)-5-methyl-tetrahydrofolate calcium salt. technical field [0002] The invention belongs to the field of medicine, in particular, the invention relates to a stable pharmaceutical composition of C-type (6S)-5-methyl-tetrahydrofolate calcium salt. Background technique [0003] (6S)‐5‐methyl‐tetrahydrofolate is the natural active form of folic acid, which can directly cross the blood-brain barrier without any metabolism in the body. What's more, taking (6S)‐5‐methyl‐tetrahydrofolate avoids the significant risk of vitamin B12 deficiency masking from folic acid alone. [0004] It is well known that 5‐methyltetrahydrofolate products are very unstable and easily degraded, especially highly sensitive to oxygen and moisture (A.L. Fitzhugh, Pteridines, 1993, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61K31/519A61K31/567A61K31/566A61K31/565A61P15/18A61P3/02A61K47/22A61K47/20A61K47/26A61K47/18A61K31/585
CPCA61K31/519A61K31/565A61K31/566A61K31/567A61K31/585A61K45/06A61K47/183A61K47/20A61K47/22A61K47/26A61K2300/00
Inventor 成永之成志
Owner LIANYUNGANG JINKANG HEXIN PHARMA CO LTD
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