English
Español 
Português 
русский 
Français 
日本語 
Deutsch 
tiếng Việt 
Italiano 
Nederlands 
ภาษาไทย 
Polski 
한국어 
Svenska 
magyar 
Malay 
বাংলা ভাষার 
Dansk 
Suomi 
हिन्दी 
Pilipino 
Türkçe 
Gaeilge 
العربية 
Indonesia 
Norsk 
تمل 
český 
ελληνικά 
український 
Javanese 
فارسی 
தமிழ் 
తెలుగు 
नेपाली 
Burmese 
български 
ລາວ 
Latine 
Қазақша 
Euskal 
Azərbaycan 
Slovenský jazyk 
Македонски 
Lietuvos 
Eesti Keel 
Română 
Slovenski 
मराठी 
Srpski језик 
The present invention aims to provide a new drug or health food containing 5-methyltetrahydrofolic acid composition for improving sleep, where the sedative-hypnotic component of said composition can be taken for a long time, and the effect of said composition on improving sleep is clear and has no side effects.
The present invention confirms the sleep improving effect of 5-methyltetrahydrofolic acid through a mouse pentobarbital sleep model.
The inventors found that 5-methyltetrahydrofolate had no direct hypnotic effect, but could increase the number of sleeping mice under the pentobarbital sodium threshold and shorten the sleep latency, and the dose used was only 0.3 mg/kg to be effective, but 5-methyltetrahydrofolate alone had no significant effect on the length of sleep in mice, presumably it could improve the difficulty of falling asleep in patients, and had no significant effect on prolonging the sleep time.
Y-aminobutyric acid, a nationally approved new resource food, has the effect of being taken for a long time without side effects. Through the mouse pentobarbital sleep model, it was found that Y-aminobutyric acid could not increase the number of mice falling asleep at subthreshold doses of pentobarbital sodium, nor could it shorten the sleep latency, but it could improve the sleep duration of mice, suggesting that Y-aminobutyric acid could improve the sleep quality of patients.
The inventors found that y-aminobutyric acid in combination with 5-methyltetrahydrofolate had a significant sleep improving effect, both
The combination of y-aminobutyric acid and 5-methyltetrahydrofolate has a significant sleep improving effect, which can significantly increase the number of mice falling asleep at subthreshold doses of sodium pentobarbital and shorten the sleep latency of mice, and also increase the sleep duration of mice without direct sleep effects, suggesting that the combination can improve the sleep disorder of patients, improve the sleep quality, and has a very good safety profile without direct sedative-hypnotic effects on the nervous system.
A first object of the present invention is to provide a new use of a known compound, namely 5-methyltetrahydrofolic acid in the preparation of
The first object of the invention is to provide a new use of a known compound, namely 5-methyltetrahydrofolic acid, in the preparation of drugs for the prevention or treatment of insomnia.
A second object of the present invention is to provide a pharmaceutical composition with a definite sleep improving effect, which can be taken for a long period of time
said composition contains 5-methyltetrahydrofolic acid, Y-aminobutyric acid.
The 5-methyltetrahydrofolic acid described in the present invention comprises 5-methyl-(6S)-tetrahydrofolic acid, 5-methyl-(6R)-tetrahydrofolic
acid, 5-methyl-(6,S)-tetrahydrofolic acid, i.e. containing different spin isomers of 5-methyltetrahydrofolic acid, or a single chiral structure compound.
The pharmaceutically acceptable salts described in the present invention comprise the acidic groups of 5-methyltetrahydrofolate reacted with organic bases, inorganic bases
Exemplary salts include calcium, sodium, magnesium, glucosamine and arginine salts of 5-methyltetrahydrofolate.
The composition described herein contains an effective amount of 5-methyltetrahydrofolate and an effective amount of Y-aminobutyric acid, and said
compositions can be made into various formulations by adding one or more pharmaceutically acceptable excipients. When used for oral administration, they can be made into solid or liquid formulations, such as tablets, capsules, softgels, dispersible tablets, oral liquids, granules, chewable tablets, drops, etc.: when used for parenteral administration, they can be made into solutions, suspensions, powders for injection, such as aqueous injections, lyophilized powders, oil injections, etc.
The formulations of the compositions of the present invention can be produced by conventional methods in the existing pharmaceutical field, and when needed, can be added
Various pharmaceutically acceptable excipients can be added when needed. Said excipients include commonly used excipients, fillers, binders, disintegrants, surfactants, lubricants, etc.
The present invention provides a pharmaceutical or health food product in which the daily dose of 5-methyltetrahydrofolate is 0.0550 mg, preferably 515 mg, and the daily dose of 5-methyltetrahydrofolic acid is 0.0550 mg.
It should be understood that the dose of the medicine provided by the present invention is not a limitation of the present invention, but a preference for the present invention.
Y-aminobutyric acid as a new resource food in 2009 and 5-methyltetrahydrofolic acid as a nutritional additive to food in 2017, both of which are safe.
The safety of Y-aminobutyric acid, a new resource food in 2009, and 5-methyltetrahydrofolate, a nutritional food additive in 2017, have both been verified, and both can be taken for a long time.
The sleeping pills currently available in the market, which have significant effects, are all based on nerve cell receptors in the brain, especially the GABA receptors or the 5-GABA receptors.
GABA receptors or 5-hydroxytryptamine receptors as the target, with direct effects, long-term use will lead to loss of receptor function, changes in receptor expression, changes in receptor structure, thus further increasing the damage to the nervous system and brain function. The combination of 5-methyltetrahydrofolate and Y-aminobutyric acid has a more comprehensive and effective effect on sleep improvement, as it has no direct effect on the receptors (Y-aminobutyric acid cannot enter the brain directly because of the blood-brain barrier).
Magnafolate can be absorbed directly, no metabolism, suitable for all kinds of people including MTHFR gene mutation. While food folate and folic acid need to undergo several biochemical conversions in the body to become L-5-MTHF.
Online Service
