LU500641B1

LU500641B1 - A pharmaceutical composition for treating depression

Info

Publication number: LU500641B1
Application number: LU500641A
Authority: LU
Inventors: Jian Li; Chenxi Li; Shan Xiong; Peter ping LEE
Original assignee: Zibo Weikexun Pharmaceutical Tech Co Ltd
Priority date: 2021-09-09
Filing date: 2021-09-09
Publication date: 2022-03-09

Abstract

The invention belongs to the field of pharmaceutical technology, specifically involves a pharmaceutical composition for treating depression, which consists of methylfolate and arginine. The invention has no obvious side effects, which not only solves the problem of patients' arginine deficiency, but also awakens the activity of autologous NO synthesis. Compared with the antidepressant effect of using methylfolate alone, the antidepressant effect is enhanced and the range of indications is expanded.

Description

A PHARMACEUTICAL COMPOSITION FOR TREATING DEPRESSION LU500641

TECHNICAL FIELD

[0001] The invention belongs to the field of pharmaceutical technology and specifically involves a pharmaceutical composition for treating depression

BACKGROUND TECHNOLOGY

[0002] Folic acid is an important B-group vitamin and a transmitter of carbon unit in biochemical reactions in the body. It is closely related to many important biochemical processes, directly affecting the synthesis of nucleic acids and amino acid metabolism, and playing an extremely important role in cell division, proliferation and tissue growth. The lack of folic acid can not only cause human megaloblastic anemia, but also affect neural tube defects, tumors, and cardiovascular diseases. Folic acid carries the carbon unit in the human body to form active forms such as 5-methyltetrahydrofolic acid and methylenetetrahydrofolate, among which 5- methyltetrahydrofolate is the main form of active folic acid in the human body. Folic acid will have physiological function after changing into methylfolate.

[0003] Arginine is a semi-essential amino acid and a direct precursor for NO synthesis. It is a necessary bioactive substance to maintain the normal function of nervous system and blood circulation. Arginine will become more deficient with age.

[0004] Methylfolate is a medicinal vitamin approved by FDA for assisting in the treatment of refractory depression. The main principle of clinical use is that some patients with depression is unable to convert folic acid in food into active folic acid (Methylfolate). Methylfolate can achieve the therapeutic effect on depression according to the release of antidepressant neurotransmitters, dopamine, norepinephrine (NE), and serotonin (5-HT) substances through brain tissue.

[0005] Arginine is the direct precursor for the synthesis of NO, and NO synthase can be active only when combined with auxiliary factors. Methylfolate is the main auxiliary factor of synthase. The arginine-NO channel that synthesizes NO to ensure the normal work of arginine-NO pathway depends on the participation of arginine and methylfolate.

[0006] Restoration and improvement of arginine-NO pathway is helpful for the improvement of depression and normal brain thinking. Numerous studies have shown that disrupting this pathway can cause brain dysfunction, resulting in neurological disorders such as depression.

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THE CONTENT OF THE INVENTION LU500641

[0007] The purpose of the invention is to provide a pharmaceutical composition for the treatment of depression, which is safe, basically without side effects and expands the applicability.

[0008] The pharmaceutical composition for the treatment of depression as described in the invention consists of methylfolate and arginine.

[0009] The mass ratio of methylfolate to arginine as described was 7.5:200-600.

[0010] The invention can be made into various pharmaceutically acceptable preparations.

[0011] Preparation method: After mixing the raw materials, bulk, pill, tablet or capsule preparations are prepared based on conventional methods.

[0012] Usage and dosage: The quality of each capsule is 210-620mg. One capsule is taken after dinner for 30 days as a course of treatment. The usage and dosage of other dosage forms are the same as capsules.

[0013] The present invention is a composition of methylfolate and arginine. Since arginine is the precursor of NO, coupled with L-metylfolate coenzyme factor, the coenzyme factor makes the autologous NO synthase become active to form a complete arginine-NO channel, which can improve, restore the cerebral blood circulation and maintain the normal function of the brain, thus achieving the anti-depression effect.

[0014] Metylfolate itself can enhance the release of brain antidepressant transmitters, thus achieving the anti-depression effect. The combination of metylfolate and arginine can enhance and expand the antidepressant superposition effect.

[0015] Efficacy judgment:

[0016] Healing: All the disease has disappeared.

[0017] Improvement: the disease has improved significantly.

[0018] Invalid: no significant improvement.

[0019] Treatment results: clinical observation of 156 patients. 31 cases were cured, accounting for

19.9%, 81 cases improved, accounting for 51.9%, 44 cases were ineffective, accounting for 28.2%, and the total effective rate was 71.8%.

[0020] Compared with the existing technologies, the present invention has the following beneficial effects:

[0021] Methylfolate and arginine are substances needed by human body, and long-term clinical trials have shown that they have no significant side effects when using within the recommended dosage 2 range. LU500641

[0022] Methylfolate is only a coenzyme factor for the synthesis of NO, and the antidepressant effect channel of using methylfolate alone is relatively simple. By adding the precursor arginine of NO synthesis, the invention further meets the needs of NO synthesis (due to the lack of arginine in the patient or caused by age and illness). A complete arginine-NO channel is formed, more effectively ensuring the function of the NO pathway and achieving a more effective anti-depression effect.

[0023] Compared with the existing technology, the invention can meet the maximum synthesis of NO by adding arginine and increasing synthetic substances. Sufficient NO can ensure the normal work of the brain and achieve antidepressant effect.

[0024] Compared with the existing technology, the invention not only solves the problem of patients’ lack of arginine, but also awakens the activity of autologous NO synthesis. Compared with the antidepressant effect of methylfolate alone, the indications are greatly expanded, the antidepressant effect is enhanced, and the range of indications is expanded.

SPECIFIC IMPLEMENTATION MODE

[0025] The invention is further described below in combination with the embodiments.

[0026] Example 1

[0027] After mixing 7.5 mg of methylfolate and 200 mg of arginine, capsules are prepared according to conventional methods.

[0028] Example 2

[0029] After mixing 7.5 mg of methylfolate and 400 mg of arginine, dispersions are prepared according to conventional methods.

[0030] Example 3

[0031] After mixing 7.5 mg of methylfolate and 600 mg of arginine, pellets are prepared according to conventional methods.

[0032] Example 4

[0033] After mixing 7.5 mg of methylfolate and 200 mg of arginine, tablets are prepared according to conventional methods.

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Claims

CLAIMS LU500641

1. The feature of the pharmaceutical composition for treating depression is that it consists of methylfolate and arginine.

2. According to the pharmaceutical composition of treating depression of claim 1, its feature is that the mass ratio of the methylfolate and arginine is 7.5:200-600.

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