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Stable pharmaceutical composition of (6S)-5-methyl-calcium tetrahydrofolate

A technology of calcium tetrahydrofolate and its composition, which is applied in the field of medicine and can solve problems such as the inability to fundamentally avoid the harm of JK12A

Inactive Publication Date: 2015-04-08
LIANYUNGANG JINKANG HEXIN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] 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-calcium tetrahydrofolate
  • Stable pharmaceutical composition of (6S)-5-methyl-calcium tetrahydrofolate
  • Stable pharmaceutical composition of (6S)-5-methyl-calcium tetrahydrofolate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] Example 1 - Direct Compression:

[0088] The composition of the prescription is as follows: 80mg / tablet

[0089]

[0090] The preparation method is as follows:

[0091] 1. Pass (6S)-5-methyl-tetrahydrofolate calcium, lactose T80, microcrystalline cellulose PH112, hypromellose, and croscarmellose sodium through a 60-mesh sieve respectively; stearic acid Magnesium through 80 mesh sieve;

[0092] 2. Mix the above-mentioned raw and auxiliary materials except magnesium stearate by doubling dilution method, so that the mixing is uniform;

[0093] 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.

[0094] 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%.

[0095] 5.15% Opadry solution is used for film coating,...

Embodiment 2

[0096] Example 2 - Direct Compression:

[0097] The composition of the prescription is as follows: 80mg / tablet

[0098]

[0099] Preparation:

[0100] 1. Pass (6S)-5-methyl-tetrahydrofolate calcium, vitamin C, pregelatinized starch PC-10, microcrystalline cellulose PH112, and sodium carboxymethyl starch through a 60-mesh sieve; pass magnesium stearate 80 mesh sieve;

[0101] 2. Mix the above-mentioned raw and auxiliary materials except magnesium stearate by doubling dilution method, so that the mixing is uniform;

[0102] 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.

[0103] 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%.

[0104] 5.15% Opadry solution is used for film coating, and the tablet bed temper...

Embodiment 3

[0105] Embodiment 3-direct compression method

[0106] The composition of the prescription is as follows: 80mg / tablet

[0107]

[0108]

[0109] Preparation method: with reference to Example 1 and Example 2.

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Abstract

The invention discloses a stable pharmaceutical composition, which contains (6S)-5-methyl-calcium tetrahydrofolate crystal and / or pharmaceutically acceptable reducing substances, and pharmaceutically acceptable auxiliary materials. Specifically, the reducing substances can protect (6S)-5-methyl-tetrahydrofolic acid and its salt from being oxidized, and can be selected from vitamin C and its salt, isovitamin C and its salt, mercaptoethanol, cysteine, mercaptoethyl sulfonic acid, dithiothreitol, reduced glutathione, and lipoic acid. The stable pharmaceutical composition provided by the invention has good stability during processing and storage, the drug risk caused by degradation can be avoided, and at the same time fast and reliable release of (6S)-5-methyl-tetrahydrofolic acid in the composition can be ensured.

Description

technical field [0001] 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 [0002] (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 taking folic acid alone. [0003] 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, 4(4), 187-191). And the preparation product not only needs its preparation process to ensure product quality, but also needs satisfactory stability during storage. Therefore, from a formulation point of view, formulation or incorporation of 5-methyltetrahydrofolate...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K31/567A61K31/566A61K31/565A61K31/585A61K47/22A61K47/20A61K47/26A61K47/18A61P15/18
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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