JP3051413B2 - Substances that cross the blood-brain barrier - Google Patents

Description

Description: FIELD OF THE INVENTION The present invention relates to materials and methods for passing and transporting other materials through the blood-brain barrier. The invention relates in particular to substances and methods for overcoming the effects of alcoholism and overcoming baldness.

Conventional technology Most physiological functions are controlled by the brain,
Given the premise that the medium of control is electrical signaling as an incident to chemical activity in the brain,
It seems logical to conclude that the absence of chemicals required for its activity in the brain could lead to signal failure and, consequently, physiological disfunction. It can also be concluded that the presence of certain substances in the brain can chemically prevent proper generation of control signals.

Research that understands the mechanisms of such considerations, drug addiction, drunkenness, baldness and other illnesses, some brain-related illnesses, etc. has shown that many researchers have identified such diseases and chemicals in the brain. He has clearly refused to look for a relationship between usability and the utility. The medical literature contains a statement that suggests that there is a relationship between certain chemicals and disease compared to brain tissue of a person who died of a certain disease compared to brain tissue of a person who died of unrelated causes. I have. It states that lithium deficiency is associated with schizophrenia and neuropeptide deficiency is associated with Alzheimer's disease.

Research in that area, chemotherapy for brain cancer, and other research and procedures are hampered by difficulties in introducing chemicals into the brain because of what is commonly called the blood-brain barrier. Blood vessels in the brain are formed of denser cells than any other blood vessel in the body. That and the action of the astrocytes causes many substances to be difficult to introduce into the glia of the brain. In some cases, the only way for researchers to reach those substances was to form a hole in the subject's skull and inject the desired substance into the brain.

It is an object of the invention to provide vehicles and methods for transporting substances across the blood-brain barrier.

Another object is to provide certain substances that are suitable for studying and in some cases treating certain diseases. One of those diseases is loss of hair and another is loss of motor function as an incident to drunkenness.

SUMMARY OF THE INVENTION These and other objects and advantages of the invention, which will become apparent hereinafter, are materials that facilitate the rapid passage of blood-to-brain materials that cannot normally pass through the blood-brain barrier. It is achieved by providing a combination of such substances with other substances that can, for example, restore the function of blocked neurotransmitters (neurotransmitters) and promote the restoration of hair growth. The substance responsible for transporting other substances through the barrier is any one or a combination of any one of a number of finely divided, highly pure, concentrated sugars or amino sugars. .
The sugars are: mesoerythritol, xylitol,
D (+) galactose, D (+) lactose, D (+)
Xylose, dursit, myo-inositol, L (-)
Fructose, D (-) mannitol, sorbitol,
D (+) glucose, D (+) arabinose, D (-)
Arabinose, cellobiose, D (+) maltose, D
(+) Raffinose, L (+) rhamnose, D (+) melibiose, D (-) ribose, adunit, D (+)
Arabitol, L (-) arabitol, D (+) fucose, L (-) fucose, D (-) lyxose, L (+)
Lyxose, L (-) lyxose, D (+) glucosamine, D mannosamine and D galactosamine. As used herein, the term "pure" as applied to sugars has a crystal purity of 97-90.
Means 99% purity. The requirement for high purity is based both on the need for purity and the unknown nature of the impurities, some of which impair the effectiveness of sugars or amino acids. The requirement for micronization is mainly based on the desire for rapid action.

For the purpose of quickly restoring the motor function of a drunken subject, a certain amount of sugar is used from the list below.
Combined with species or more amino acids. The amino acids are: glutamine, lysine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glycine, histidine, leucine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine, valine and taurine. Amino acids are common foods, such as orange juice, clam chowder,
Although it can be found in soy soups, sheep's milk, and the like, it is preferred to add the amino acids in the form of pure crystals to make the results uniform and more predictable.

Amino acids are an essential component if the goal is to quickly restore motor function to those who have lost control of motor function as a result of excess ether in the body. For the purpose of introducing other substances into the brain through the blood-brain barrier, amino acids are desirable but obviously not essential. Thus, for example, ingestion of a quantity of one or more of the above sugars with beta-carotene or xanthophyll promotes hair growth, but the growth process is accelerated when amino acids from above are added. You.

Both the proportions of the test or therapeutic substances added and their combination in combination and the amount of the combination will depend on the nature and weight of the test subject. In humans, excessive amounts of any of the above sugars can cause nausea, fever sensation, flushing and tinnitus. If more than 5 grams of sugar is administered at one time, the adverse side effects described above can occur. There is no upper limit on the amount of amino acids that can be safely taken, except that excessive amounts of amino acids may have a detrimental effect on a subject with a given disease.

DESCRIPTION OF THE PREFERRED EMBODIMENTS Inclusion of amino acids is not essential except that it overcomes the effects of alcohol and achieves rapid recovery of motor function, but is useful for transporting other substances to the brain, and is therefore a preferred embodiment. Then join. Thus, preferred substances of the invention are those that have the ability to cross the blood-brain barrier and transport other substances through the barrier, and may comprise one or more of a number of pure sugars or amino sugars and a number of pure sugars. Includes combinations with one or more of the amino acids. The sugars are as follows: mesoerythritol, chylitol, D (+) galactose, D (+) lactose, D (+) xylose, dursit, myo-inositol, L (-) fructose, D
(-) Mannitol, sorbitol, D (+) glucose, D (+) arabinose, D (-) arabinose, cellobiose, D (+) maltose, D (+) raffinose, L (+) rhamnose, D (+) melibiose , D
(-) Ribose, adunit, D (+) arabitol,
L (-) arabitol, D (+) fucose, L (-) fucose, D (-) lyxose, L (+) lyxose and L (-) lyxose. As used herein, the term "pure" as applied to sugars refers to pulverized sugars having a purity of 97-100% crystalline. Amino sugars are D (+) glucosamine, D mannosamine and D galactosamine. From here onwards,
Amino sugars are included in the term "sugar".

The amino acids are: glutamine, lysine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glycine, histidine, leucine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine, valine and taurine.
Arginine, tryptophan, tyrosine are presently preferred. It is even more preferred that the substance of the invention is taken orally, for example, in a liquid such as water or orange juice.

Overcoming drunkenness The above-described compositions are preferred for the purpose of overcoming drunkenness. The minimum effective amount of a fast acting substance will depend on the subject's weight. For a 100 pound (45 kg) individual, the minimum amount of high purity sugar is about 1.2 grams and the minimum amount of amino acids is about 400 milligrams. 200 pounds (91k
For g) individuals, the minimum amount is about 2.0-2.5 grams of high purity sugar and about 480 milligrams of amino acids. One is to restore motor function and the other is to metabolize alcohol. Rapid recovery of motor function requires high purity sugar. To promote the reasonably rapid metabolism of alcohols only requires a sugar purity of 90% or higher. If a minimal amount of "pure" sugar is included, a mixture of sugars is also permitted. The combination of high-purity sugars and amino acids, when taken in liquid or liquid form, restores motor function in less than 1 minute, usually within 30 seconds after oral ingestion. Reduces the amount of blood alcohol in a normal 200 lb. individual consuming 6 ounces (17 grams) of 80 proof alcohol and orally ingesting the substance of the invention in liquid form to less than 0.05% within 30 minutes. Relatively rapid detoxification is due to the inclusion of some amino acids.

Hair Growth Certain substances have proven to be useful in delaying hair loss. There are a number of proprietary products on the market that claim to provide some good results both in reducing hair loss and in restoring hair. They are applied externally and are thought to act as neuroreceptors on the surface of hair follicle cells. The substances of the invention are beta-carotene and / or xanthophylls, which can act as neurotransmitters that, when introduced into the glia, signal and act on the sac. The tests demonstrate that beta carotene and / or xanthophyll promote hair growth when taken with one or more of the high purity sugars described above. Hair growth in the area of the head was previously bald. In one study, beta-carotene 30 mg was added to orange juice 25.
Ingestion daily with 2500 mg of fructose in 0 cc for 45 days stopped the hair loss at the user's hairline and led to the growth of new hair in the area of the top.
A subject whose natural hair color is black and turned gray,
At the end of the 45-day test, he had virtually only black skull and hair.

The test is based on the amounts of base substance, sugar and amino acid described above,
It shows that beta carotene and other substances are effective to transport in about half an hour. It is not known whether it is due to the sugar remaining in the blood for that period or to producing effects in the brain that last for that period.
However, beta-carotene does not need to be taken with the base substance for its action, but can be taken at the point where it is eventually removed. There appears to be no critical dose of beta-carotene. Beta-carotene is considered to be the preferred minimum at this time, since it is consumed and its recommended daily amount is 5000 IU. No increase in hair recovery was observed with beta-carotene levels greater than 50,000 IU. Therefore, at this time, 50,000 IU is considered to be the upper limit at which increasing it further does not produce any additional benefit at the expense of additional cost. Beta-carotene and xanthophyll are equally effective.

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI A61P 9/00 A61P 9/00 17/14 17/14 25/32 25/32 43/00 43/00 (58) Fields surveyed (Int. Cl. ⁷ , DB name) A61K 31/198 A61K 31/401 A61K 31/405 A61K 31/70 A61K 47/26 A61P 9/00 A61P 17/14 A61P 25/32 A61P 43/00 CA (STN) MEDLINE (STN )

Claims (5)

(57) [Claims] (1) One or more concentrated sugars selected from the group consisting of: mesoerythritol, xylitol, D (+) galactose, D (+) lactose, D
(+) Xylose, dursit, myo-inositol, L
(-) Fructose, D (-) mannitol, sorbitol, D (+) glucose, D (+) arabinose, D
(-) Arabinose, cellobiose, D (+) maltose, D (+) raffinose, L (+) rhamnose, D
(+) Melibiose, D (-) ribose, adnit,
D (+) arabitol, L (-) arabitol, D
(+) Fucose, L (-) fucose, D (-) lyxose, L (+) lyxose, L (-) lyxose, D
(+) Glucosamine, D-mannosamine and D-galactosamine; and (2) one or more amino acids selected from the group consisting of: glutamine, lysine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glycine, histidine, leucine A composition for crossing the blood-brain barrier by ingesting a substance containing methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine, valine and taurine. 2. The composition of claim 1, further comprising sugar, typically in the range of 1.2-2.5 grams, and amino acids, typically in the range of 400-480 milligrams, wherein the minimum amounts of sugar and amino acids are associated with changes in patient weight. A composition according to claim 1 for use in overcoming drunkenness. 3. The composition according to claim 1, which is further used for delaying hair loss, comprising at least one of beta-carotene and xanthophyll. 4. The method according to claim 1, wherein said beta-carotene is administered in a daily dose, at a point spaced from ingestion of said composition.
4. The composition according to claim 3, which can be taken in 00IU. 5. The composition according to claim 1, wherein the sugar component serves as a means for transporting the amino acid component through the blood-brain barrier, and a combination thereof enhances the function of a neurotransmitter in the brain.