Folic acid preparation and preparation method thereof

A technology of folic acid and preparations, which is applied in the direction of pill delivery, pharmaceutical formulations, and medical preparations of non-active ingredients. It can solve the problems of poor solubility, folic acid sensitivity to oxygen and temperature, and folic acid instability, so as to achieve high safety and improve Absorption speed and bioavailability, effects of improving water solubility and stability

Active Publication Date: 2021-04-09
CHINESE MEDICINES GUANGZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] For traditional folic acid preparations, in order to achieve a better molding effect, it is often necessary to add ingredients such as binders to the formula, which is complex and costly
[0008] Folic acid has poor solubility and belongs to BCS Ⅱ drugs. Dissolution is the rate-limiting step of its absorption in vivo, which leads to low bioavailability and large differences in absorption.
Folic acid is extremely unstable under acidic conditions, and it is easily degraded in gastric juice after oral administration of ordinary tablets, which affects bioavailability
In addition, the dosage of folic acid in folic acid preparations is relatively small, and the commonly used specification is 0.4mg / tablet, accounting for less than 1% of the weight of the entire preparation. In traditional production operations, the uniformity of folic acid content is also a difficult problem in this technical field
Folic acid is sensitive to oxygen and temperature, and has poor stability. Usually, antioxidants need to be added to folic acid preparations to ensure its stability
[0009] At present, domestic folic acid commercially available folic acid preparations are ordinary tablets, which have many defects such as low bioavailability, slow absorption, low oral compliance and adverse reactions in the gastrointestinal tract.

Method used

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  • Folic acid preparation and preparation method thereof
  • Folic acid preparation and preparation method thereof
  • Folic acid preparation and preparation method thereof

Examples

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preparation example Construction

[0039] The embodiment of the present invention relates to the preparation method of the above-mentioned folic acid preparation, and the preparation method includes the following steps: taking the components, mixing and molding.

[0040] In one example, the forming method is freeze-vacuum drying. The formula is prepared into a solution by freeze-drying, which is more accurate than the traditional oral solid preparation method, and the dosage is accurate without considering the problem of dosage uniformity. The orally disintegrating tablets prepared by freeze-drying do not need water to be taken, there is no obvious gritty feeling in the mouth, and they disintegrate rapidly in the oral cavity within 5 seconds, which has obvious therapeutic advantages for patients who are not suitable for oral administration. over-effect.

[0041] In one example, the freeze-vacuum drying process includes: placing the mixed mixture at -40°C to -60°C for 2h to 4h, sublimation with a vacuum of 10Pa...

Embodiment 1

[0060] The formula composition of folic acid freeze-dried orally disintegrating tablets is shown in the following table:

[0061] Table 2

[0062]

[0063]

[0064] The preparation method of folic acid freeze-dried orally disintegrating tablet comprises the following steps:

[0065] (1) Mixing: Add the hydroxypropyl folic acid-β-cyclodextrin inclusion complex, lactose, polyethylene glycol 15-hydroxystearate, sucralose, and sweet orange flavor in 500ml of purified water in sequence , stirring and dissolving to obtain a clear liquid medicine;

[0066] (2) Injection molding: accurately inject the liquid medicine into the mold by 0.5ml / tablet;

[0067] (3) Freeze-drying process: cool down the shelf of the freeze-dryer to -40°C, place the mold filled with the liquid medicine in the freeze-dryer, and keep it warm for 3 hours; cool down the water-catching condenser of the freeze-dryer to below -40°C, Turn on the vacuum pump to evacuate, and sublimation begins at a vacuum deg...

Embodiment 2

[0071] The formula composition of folic acid freeze-dried orally disintegrating tablets is shown in the following table:

[0072] table 3

[0073]

[0074]

[0075] The preparation method of folic acid freeze-dried orally disintegrating tablet comprises the following steps:

[0076] (1) Mixing: add folic acid hydroxypropyl-β-cyclodextrin inclusion compound, mannitol, Tween 80, cyclamate, and lemon flavor in 500ml of purified water in sequence, stir and dissolve to obtain a clear medicinal solution ;

[0077] (2) Injection molding: accurately inject the liquid medicine into the mold by 0.5ml / tablet;

[0078] (3) Freeze-drying process: cool down the shelf of the freeze-dryer to -50°C, place the mold filled with the liquid medicine in the freeze-dryer, and keep it warm for 2 hours; cool down the water-catching condenser of the freeze-dryer to below -40°C, Turn on the vacuum pump to evacuate, and sublimation begins at a vacuum degree of 20Pa; raise the temperature of the ...

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PUM

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Abstract

The invention provides a folic acid preparation. The folic acid preparation comprises the following components in parts by mass of 10-30 parts of a folic acid inclusion compound, 50-80 parts of an excipient, 6-30 parts of a stabilizer and 1-10 parts of a flavoring agent, wherein the sum of the mass parts of the components is 100 parts. Compared with the prior art, the folic acid preparation has the following beneficial effects that the folic acid preparation selects the folic acid inclusion compound, and after folic acid is included by an inclusion agent, the water solubility and the stability of folic acid are remarkably improved, so that the absorption speed and the bioavailability can be remarkably improved. Moreover, the folic acid preparation formula disclosed by the invention does not contain an antioxidant and an organic reagent, does not need to consider the toxicity of auxiliary materials excessively, and is high in safety.

Description

technical field [0001] The invention relates to the technical field of medicines, and relates to a folic acid preparation and a preparation method thereof. Background technique [0002] Folic acid is a water-soluble B vitamin composed of residues of pteridine, p-aminobenzoic acid and glutamic acid, and is an essential substance for the growth and reproduction of body cells. Folic acid via dihydrofolate reductase and vitamin B 12 The role of the formation of tetrahydrofolate (THFA), THFA and a variety of one-carbon units (including CH 3 、CH 2 , CHO, etc.) combined into tetrahydrofolate coenzymes, transfer one-carbon units, participate in many important reactions in the body and the synthesis of nucleic acids and amino acids. Under the action of serine transhydroxylase, THFA forms N5,10 methylenyl tetrahydrofolate, which can promote uracil nucleotides (dUMP) to form thymine nucleotides (dTMP), and thymine nucleotides can participate in cell metabolism DNA synthesis, promot...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/519A61K47/69A61K47/40A61K47/10A61K47/32A61K47/26A61K47/18A61P3/02
CPCA61K31/519A61K47/6951A61K9/0056A61K9/2018A61K9/2031A61K9/2013A61K9/2027A61K9/205A61K9/2095A61P3/02
Inventor 黄宏轩姚青樊化平
Owner CHINESE MEDICINES GUANGZHOU
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