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Controlled release preparation containing 5-methyltetrahydrofolate

A technology of methyltetrahydrofolate and methyltetrahydrofolate, applied in medical preparations containing active ingredients, pill delivery, organic active ingredients, etc., can solve problems affecting male fertility and improve treatment compliance Sex, improve curative effect, reduce the effect of taking times

Active Publication Date: 2019-06-28
SHENZHEN AUSA PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, stevioside is prohibited from being used in pharmaceutical preparations in many countries due to its influence on male fertility and other unsafe factors

Method used

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  • Controlled release preparation containing 5-methyltetrahydrofolate
  • Controlled release preparation containing 5-methyltetrahydrofolate
  • Controlled release preparation containing 5-methyltetrahydrofolate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Calcium 5-Methyltetrahydrofolate Controlled Release Tablets

[0039] Single-layer tablet core prescription:

[0040]

[0041] Tablet core preparation process:

[0042] Mix microcrystalline cellulose and (6S)-5-methyltetrahydrofolate calcium, pass through a 100-mesh sieve, add lactose and sodium chloride and mix evenly, make soft material with 60% ethanol, granulate with 18-mesh sieve, 40 Dry at -45°C, granulate with 18 mesh sieve, add magnesium stearate and mix evenly, test the intermediate product, and compress into tablets.

[0043] Coating Solution Prescription:

[0044]

[0045] Coating process:

[0046] Put the tablet cores in the coating pan for coating, the flow rate of the coating solution is 5-10ml / min, the temperature of the tablet bed is 40-45°C, the rotation speed of the coating pan is 8-15rpm, until the weight gain of the outer coating of the tablet cores reaches 3.5 %, continue heating for 0.5h, then dry the coated tablet in a drying o...

Embodiment 2

[0047] Example 2: Calcium 5-Methyltetrahydrofolate Controlled Release Tablets

[0048] Single-layer tablet core prescription:

[0049]

[0050] Preparation Process:

[0051] Mix microcrystalline cellulose and (6R,S)-5-methyltetrahydrofolate calcium, pass through a 100-mesh sieve, then add pregelatinized starch and magnesium chloride and mix evenly, add 10% povidone K30 soft material, 18 Granulate with a mesh sieve, dry at 40-45°C, granulate with a 18-mesh sieve, add magnesium stearate and mix evenly, test the intermediate product, and compress into tablets.

[0052] Coating Solution Prescription:

[0053]

[0054] Coating process: put the tablet core in the coating pot for coating, the flow rate of the coating solution is 5-10ml / min, the temperature of the tablet bed is 40-45°C, the speed of the coating pot is 8-15rpm, and the coating is carried out until the core is coated Continue heating for 0.5h until the weight gain reaches 4.0%, and then dry the coated tablet in...

Embodiment 3

[0055] Example 3: Calcium 5-methyltetrahydrofolate controlled-release tablets

[0056] Single-layer tablet core prescription:

[0057]

[0058] Preparation Process:

[0059] Mix microcrystalline cellulose and (6S) 5-methyltetrahydrofolate calcium, pass through a 100-mesh sieve, then add pregelatinized starch and magnesium chloride, mix evenly, add 10% povidone K30 soft material, and 18-mesh sieve Granules, dried at 40-45°C, granulated with 18 mesh sieve, added with magnesium stearate, mixed evenly, intermediate product inspection, compressed into tablets.

[0060] Coating Solution Prescription:

[0061]

[0062] Coating process:

[0063] Put the tablet cores in the coating pan for coating, the flow rate of the coating solution is 5-10ml / min, the temperature of the tablet bed is 40-45°C, the rotation speed of the coating pan is 8-15rpm, until the weight gain of the outer coating of the tablet cores reaches 5.0 %, continue heating for 0.5h, then dry the coated tablet i...

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Abstract

The invention relates to a controlled release preparation containing 5-methyltetrahydrofolate. The controlled release preparation comprises a 5-methyltetrahydrofolate osmotic pump tablet core and a polymeric semi-permeable membrane coating layer. The semi-permeable membrane coating layer accounts for 2-15% of the weight of the tablet core, and the 5-methyltetrahydrofolate osmotic pump tablet corecan be a single-layer tablet or a double-layer tablet. By means of the preparation, 5-methyltetrahydrofolate can be slowly and stably released for a long time, the dosing frequency is reduced, and themedication compliance of a patient is improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a controlled-release preparation containing 5-methyltetrahydrofolate. Background technique [0002] After oral administration, folic acid is absorbed through the small intestine, catalyzed by dihydrofolate reductase to form tetrahydrofolate, and then combined with various one-carbon units (including -CH 3 、-CH 2 , -CHO, etc.) into tetrahydrofolate coenzymes, transfer one-carbon units, and participate in many important reactions in the body, including homocysteine ​​(Hcy) metabolism: Hcy accepts the methyl group transferred by 5-methyltetrahydrofolate, Conversion to methionine (methionine cycle), which is the most important metabolic outlet for Hcy, and methylenetetrahydrofolate reductase (MTHFR) is the enzyme that reduces 5,10-methylenetetrahydrofolate to 5-methyltetrahydrofolate key enzymes. If the MTHFR C677T gene is mutated into MTHFR 677TT, the enzyme activity wi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/24A61K31/519A61P9/00A61P9/10
Inventor 徐希平陈亚宁陈平田敏卿张磊
Owner SHENZHEN AUSA PHARM CO LTD
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