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Folic acid sustained-release composition, sustained-release preparation and application thereof

A technology of sustained-release composition and sustained-release preparation, applied in the field of folic acid sustained-release composition, which can solve the problems of ineffectiveness, increased burden on the kidneys, poor biotransformation ability of patients, etc.

Active Publication Date: 2021-01-01
北京斯利安药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the gene polymorphism of the folic acid conversion enzymes, the biotransformation of the enzymes is easily saturated, resulting in poor biotransformation ability in some patients. When a large dose is administered clinically, a large amount of unconverted folic acid enters the circulatory system and is excreted by the kidneys.
Excretion of such a large amount of folic acid through the kidneys will increase the burden on the kidneys and lead to damage to renal function, especially for those patients with renal function defects. A large amount of untransformed folic acid will also lead to physiological functions in the body. The obvious deficiency of 5-methyltetrahydrofolate, which may be one of the reasons why some patients are still ineffective in the prevention of neonatal neural tube defects despite the widespread clinical use of folic acid in the past 20 years (Apolline I et al. Neural Tube Defects, Folic Acid and Methyllation.Int J.Environ.2013,10:4352-4389), especially modern medical research shows that families with high incidence of neural tube defects in newborns, patients with high homocysteine, stroke patients, myocardial infarction patients, etc. is associated with folic acid low enzymatic activity
It is generally hoped to increase the intake of folic acid clinically, but the clinical effect is not ideal

Method used

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  • Folic acid sustained-release composition, sustained-release preparation and application thereof
  • Folic acid sustained-release composition, sustained-release preparation and application thereof
  • Folic acid sustained-release composition, sustained-release preparation and application thereof

Examples

Experimental program
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preparation example Construction

[0064] The different extended-release formulations of folic acid are prepared differently:

[0065] Matrix tablets of extended-release formulations of folic acid. The folic acid is taken, mixed evenly with the polymer material, the bleaching agent and the anti-adhesive agent, and the folic acid sustained-release matrix tablet is obtained through the powder direct tableting process or adding a binder for wet granulation and then tableting. The higher the viscosity of the polymer material, the slower the drug release. The variety and quantity of the bleaching agent affect the bleaching time of the preparation in the stomach. The invention controls the viscosity of the macromolecular material and the variety and quantity of the bleaching agent to control the release of the drug for more than 6 hours to achieve the slow release effect.

[0066] Preparation:

[0067] (1) Micronize the folic acid raw material drug to control the particle size D of the raw material drug 90 Contro...

Embodiment 1

[0094] Take 10g of folic acid, HPMC K150025.5g, 30g of sodium bicarbonate, and 4.5g of magnesium stearate, mix them evenly, control the hardness to 2.5-5.0kg, press them into folic acid tablets with a weight of 150mg, and obtain 5mg of folic acid per tablet. Use 900ml of 0.1mol / L HCl medium to avoid light, measure its dissolution rate, and measure its drifting time at the same time. The results are shown in Table 2.

[0095] Table 2

[0096]

[0097] Preparation:

[0098] (1) Micronize the folic acid raw material drug to control the particle size D of the raw material drug 90 ≤20μm, weigh each raw and auxiliary material according to the prescription amount.

[0099] (2) Add folic acid, HPMC K1500 and sodium bicarbonate into the high-speed mixing granulator in turn, stir at 120rpm, and cut at 1000rpm for 5min.

[0100] (3) Add magnesium stearate into the three-dimensional mixer, rotating speed: 13rpm, time 4min.

[0101] (4) Tablet pressing: shallow concave Punching sh...

Embodiment 2

[0103] Take 20g of folic acid, 245.5g of hydroxypropyl cellulose (HPC), 30g of sodium bicarbonate, and 4.5g of magnesium stearate, mix them evenly, control the hardness to 2.5-5.0kg, press them into folic acid tablets with a weight of 150mg, and obtain each tablet Contains folic acid 10mg. Use 900ml of 0.1mol / L HCl medium to avoid light, measure its dissolution rate, and measure its drifting time at the same time. The results are shown in Table 3.

[0104] table 3

[0105]

[0106] Preparation:

[0107] (1) Micronize the folic acid raw material drug to control the particle size D of the raw material drug 90 ≤20μm, weigh each raw and auxiliary material according to the prescription amount.

[0108] (2) Add folic acid, hydroxypropyl cellulose (HPC) and sodium bicarbonate into the V-shaped mixer in sequence, and stir at 50 rpm for 10 minutes.

[0109] (3) Add magnesium stearate into the three-dimensional mixer, rotating speed: 13rpm, time 4min.

[0110] (4) Use shallow co...

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Abstract

The invention relates to the field of medicines, and particularly relates to a folic acid sustained-release composition, a sustained-release preparation and application thereof. The invention providesthe folic acid sustained-release preparation, which adopts a gastric retention technology and can prolong the retention time of a folic acid preparation in the stomach to 6 hours or above. The sustained-release preparation has lower administration frequency than a common-release preparation, and the administration frequency is reduced from 2-3 times per day to once per day, so that the preparation has a faster 5-methyltetrahydrofolic acid level increase rate than a common folic acid common-release preparation unexpectedly, and the rat animal model shows that the dosage of the 5-methyltetrahydrofolic acid level of the same body can be reduced by about 50% compared with the common-release preparation. The sustained-release preparation can be used for patients who need to take folic acid fora long time, such as megaloblastic anemia caused by folic acid deficiency, hyperhomocysteinemia caused by folic acid deficiency, cerebral apoplexy prevention and myocardial infarction caused by hyperhomocysteinemia, depression and anxiety induced by folic acid deficiency and the like.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a folic acid sustained-release composition, a sustained-release preparation and applications thereof. Background technique [0002] Natural folic acid belongs to the low-molecular-weight B group water-soluble vitamins. After it was discovered, it was named: vitamin M, vitamin B 9 , R factor, etc., also known as pteroylglutamic acid, which cannot be synthesized and transformed by the human body, and almost participates in all biochemical metabolic processes of methylation in the body. It exists in many plants and animal tissues, mainly in the form of polyglutamate, and it must be hydrolyzed into monoglutamate by the glutamic acid carboxypeptidase II gene encoded by the glutamic acid carboxypeptidase Ⅱ gene before it can be absorbed by the small intestine Absorbed by villous epithelial cells. Due to insufficient intake of natural folic acid, compounds with pteridine structures (N-[4-[(2-a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K47/02A61K47/10A61K47/12A61K47/14A61K47/32A61K47/36A61K47/38A61K9/16A61K9/20A61K9/48A61P7/06A61P3/00A61P7/00A61P9/10A61P25/00A61P25/28
CPCA61K31/519A61K9/0002A61K47/38A61K47/32A61K47/36A61K47/02A61K47/10A61K47/14A61K47/12A61K9/2054A61K9/1652A61P7/06A61P25/00A61P3/00A61P7/00A61P9/10A61P25/28A61K9/0065
Inventor 蔡正军赵欢张颖然钟敏
Owner 北京斯利安药业有限公司
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