A method of preparing for a L-5-methyl hydrogen folic acid microcarbon

A technology of methyltetrahydrofolate and shellac, which is applied in microcapsules, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Capsule preparation method, no L-5-methyltetrahydrofolate microcapsules, no general industrialization and other problems, to achieve the effects of improving bioavailability, improving content stability, and low production cost

Active Publication Date: 2021-07-30
FERGUSON WUHAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In foreign countries, there are many reports about L-5-MTHF, but because of its poor stability, sensitivity to oxygen and other defects, it has not been widely industrialized in production
[0005] Through literature search, there is no report about L-5-methyltetrahydrofolate microcapsules and its preparation method in the literature at home and abroad, and there is no L-5-methyltetrahydrofolate microcapsules on the market at home and abroad.

Method used

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  • A method of preparing for a L-5-methyl hydrogen folic acid microcarbon
  • A method of preparing for a L-5-methyl hydrogen folic acid microcarbon
  • A method of preparing for a L-5-methyl hydrogen folic acid microcarbon

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Experimental program
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Embodiment 1

[0029] 1) Under the protection of nitrogen, dissolve 30g of L-5-methyltetrahydrofolate and 20g of ornithine in 200ml of water, stir and react at 15°C for 10min, dissolve 15g of shellac in anhydrous methanol, and make a weight concentration of 2% shellac solution, then slowly add the above-mentioned reacted solution into the shellac solution dropwise, stir while adding, filter the precipitated solid and wash with water to obtain a yellow solid powder;

[0030] 2) 14g zein and 7g ethylcellulose are dissolved with 70% ethanol to make a mixed solution with a weight concentration of 1.5%, then add 6g starch, 6g dextrin, 1g silicon dioxide and stir in the mixed solution Evenly, mix the yellow solid powder obtained in step 1) with 1 g of ascorbic acid, disperse it with a small amount of water and add it to the mixed solution, stir it evenly, and then spray dry it. The material temperature is controlled at 60 ° C, the feed rate is 3 mL / min, and the drying time is After 60 minutes, L-5...

Embodiment 2

[0035] 1) Under the protection of nitrogen, dissolve 30g of L-5-methyltetrahydrofolate and 30g of ornithine in 300ml of water, stir and react at 10°C for 30min, dissolve 10g of shellac in anhydrous methanol, and make a weight concentration of 1% shellac solution, then slowly add the above-mentioned reacted solution into the shellac solution dropwise, stir while adding, filter the precipitated solid and wash with water to obtain a yellow solid powder;

[0036] 2) 10g zein and 10g ethylcellulose are dissolved with 50% ethanol to make a mixed solution with a weight concentration of 5%, then add 3g starch, 3g dextrin, 2g silicon dioxide to the mixed solution and stir Evenly, mix the yellow solid powder obtained in step 1) with 2g of tert-butylhydroquinone, disperse it with a small amount of water and add it to the mixed solution, stir it evenly and then spray dry it. Control the material temperature at 50°C and feed rate at 1mL / min, the drying time is 100min, and L-5-methyltetrah...

Embodiment 3

[0041] 1) Under the protection of nitrogen, dissolve 30g of L-5-methyltetrahydrofolate and 10g of ornithine in 100ml of water, stir and react at 20°C for 10min, dissolve 20g of shellac in anhydrous methanol, and make a weight concentration of 5% shellac solution, and then slowly drop the above-mentioned reacted solution into the shellac solution, stir while adding, and wash the precipitated solid with water after filtering to obtain a yellow solid powder;

[0042] 2) 20g zein and 5g ethylcellulose are dissolved with 90% ethanol to make a mixed solution with a weight concentration of 0.5%, then add 10g starch, 3g dextrin, 0.5g silicon dioxide and Stir evenly, mix the yellow solid powder obtained in step 1) with 1.5g ascorbic acid, disperse it with a small amount of water and add it to the mixed solution, stir it evenly, and spray dry it. The time is 10min, and the L-5-methyltetrahydrofolate microcapsules are obtained after discharging.

[0043] Wherein, the weight proportion o...

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Abstract

The invention discloses a preparation method of L-5-methyltetrahydrofolate microcapsules. In the method, an aqueous solution of L-5-methyltetrahydrofolate is added to a methanol solution of shellac, causing phase separation and precipitation, thereby Wrap L-5-Methyltetrahydrofolate in shellac to form the first layer of microcapsules, and then use film-forming materials zein and ethyl cellulose to film-wrap the first layer of microcapsules to form L‑5‑Methyltetrahydrofolate microcapsules with two layers of encapsulation can greatly improve the stability of L‑5‑Methyltetrahydrofolate.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method of L-5-methyltetrahydrofolate microcapsules. Background technique [0002] Folic acid, also known as vitamin B9, is a water-soluble vitamin. 0.4 mg of folic acid is used to prevent fetal neural tube defects. Mothers-to-be who take 0.4 mg of folic acid during pregnancy can reduce the rate of fetal neural tube defects by 85%; 5 mg of folic acid can be used to treat anemia in women, and can promote the maturation of young cells in the bone marrow. Humans such as lack of folic acid can cause megaloblastic anemia and leukopenia, especially important for pregnant women. [0003] The biologically active form of folic acid in the body is tetrahydrofolate (THF). THF is the coenzyme in the one-carbon unit transferase system in the body. It is produced by folic acid in the presence of vitamin C and NADH+ under the action of folate reductase to dih...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/519A61K47/18A61K47/46A61K47/42A61K47/38A61K47/36A61P3/02A61P7/00A61P7/06A61P25/00
CPCA61K9/5036A61K9/5042A61K9/5052A61K31/519A61K47/183A61K47/46A61P3/02A61P7/00A61P7/06A61P25/00
Inventor 刘欣张琨邱洁章秀梅孙晓菲
Owner FERGUSON WUHAN BIOTECH
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