JPS63313727A - External remedy - Google Patents

Abstract

PURPOSE:To obtain an external remedy containing an organic germanium compound having germanium sesquioxide at one end of fatty acid, having good absorbility from skin, free from dysphoria and convenient in treatment, storage, etc. CONSTITUTION:An organic germanium compound (e.g. bisbeta-ethylcarboxylic acid germanium sesquioxide, bisbeta-ethylcarboxylic amide germanium sesquioxide, etc.) having germanium sesquioxide group expressed by the formula at one end of fatty acid is contained as an active ingredient at an amount of 0.1-15.0wt.%. The active ingredient has advantages, e.g. being strong in bonding degree of oxygen, capable of activating metabolism of skin and having good permeability to skin and affinity compared with an inorganic germanium and a remedy containing the active ingredient has e.g. good absorbility from skin because of fluid and free from sense of oppression, pain, etc., because of having no contact with substance in stomach and capable of providing large effect by only applying cloth to an affected part.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an external therapeutic agent characterized by containing an organic germanium compound as an active ingredient.

[Prior art]

In order to treat and alleviate human skin diseases, athlete's foot, stiff shoulders, supplement II, neuralgia, arthritis, rheumatism, etc., germanium is made into a fluid or a solution, dissolved in a solvent, and absorbed into the body through the shoreline of the skin. It also works to promote the production of red blood cells. Therefore, it acts on cells in the living body, activates enzyme activity, and excretes cations of metabolic waste products in each cell as water and urine due to the strong binding power with oxygen, which is a characteristic of organic germanium compounds. is known to make it more effective.

That is, in human social activities, physical abnormalities occur due to mental stress due to overuse of the nervous system. At times like this, people used the wisdom of ancient people to take a bath in hot springs to relieve stress.

In addition, organic germanium compounds are used in the Chinese herbal medicine ginseng,
It is contained in large amounts in fruits such as goji berries, wisteria berries, rhombus berries, garlic, and aloe vera. Recently, Tohoku University School of Medicine and other institutions have announced that organic germanium has the ability to induce interferon in the body as a cancer treatment drug.

[Problem that the invention seeks to solve]

In the present invention, we focused on the remarkable effects of such organic germanium compounds in Chinese herbal medicine, and found that they are used for analgesic and anti-inflammatory effects, and are effective against skin diseases and athlete's foot.

That is, conventionally, germanium has an atomic number of 32;
It is an atom with 32 electrons, and 4 of these 32 electrons are active on the outside, and depending on the environment, these electrons can fly out. Transistors (amplification) and diodes (rectification) utilize this property in weak electric fields.
However, when one of these four electrons jumps out, it creates a positive ball of potential, which sucks in electrons from the surrounding area.

The present inventor discovered that the germanium contained in the Chinese herbal medicine exists as an organic compound, and there is a high possibility that this organic germanium compound causes charge transfer and organic free radicals of carboxylic acid and amide. We completed an external therapeutic agent containing an organic germanium compound having a germanium sesquioxide group at one end of the fatty acid for pain relief and treatment of skin diseases.

Therefore, an object of the present invention is to provide a novel external therapeutic agent containing an organic germanium compound as an active ingredient.

[Means for solving problems]

The gist of the present invention to achieve the above object is to use as an active ingredient an organic germanium compound having a germanium sesquioxide group shown below at one end of a fatty acid.

θ-cT--o-Cre - The organic germanium compound having a germanium sesquioxide group at one end of the fatty acid used in the present invention is bisβ-
Ethylcarboxylic acid germanium sesquioxide [I]
, or bisβ-ethylcarboxylic acid amide germanium sesquioxide [■].

For example, trichlorogermanium ethyl cyanide, which is obtained by reacting trichlorogermanium with acrylonitrile, is hydrolyzed with acid to form trichlorodermanium ethyl cyanide, which is then reacted with thionyl chloride to produce trichlorogermanium ethyl cyanide. germanium propionic acid chloride, which is hydrolyzed with water to obtain bisβ-ethylcarboxylic acid germanium sesquioxide [
I] was obtained, and when trichlorodermanium ethylcarboxylic acid chloride was treated with aqueous ammonia, bisβ-
Ethylcarboxylic acid amide germanium sesquioxide (II) can be obtained.

This can be expressed as a chemical reaction formula as follows.

crLHdb+04-・QHCN-1→bi1Cte・
CH-CH-CN(JaCr==CH-CH,0)θH
−5ρCf, →(L(7eCH,CH,Qt>(J, 1
Lin Shu 0- to a-(:, #, anti-zQoo@Bisβ-ethylcarboxylic acid and bisβ-ethylcarboxylic acid amide germanium sesquioxide [IN are both water-soluble white crystalline compounds obtained in this way. It is a powder that polymerizes when heated.It decomposes when the temperature is further increased, making it impossible to measure the melting point.

When these are dissolved in water, the oxygen in germanium sesquioxide is hydroxylated, hydrogen causes charge transfer, and is activated. Therefore, such organic germanium compounds have various characteristics when fluidized with water.

However, inorganic germanium is a solid metal piece, which poses a problem. Further, since the solid metal pieces are used as a tape as a base material and are attached to an adhesive or the like, various inconveniences occur.

b) There is a feeling of pressure because the solid object is brought into contact with the skin, and at the same time, the edges of the solid object dig into the skin due to the pressure, causing pain.

Since it is fixed with a tape-like adhesive, it is easy to peel off because the solid part has no adhesive properties.

c) Since it is solid, it is inconvenient to attach it to narrow areas.

The present invention solves the conventional problem by applying fluidized germanium instead of the conventional method using solid germanium.

Therefore, the present invention provides an external therapeutic agent characterized in that the organic germanium compound mixed together with a base fluid is applied to the skin.

When this organic germanium compound is blended into a base fluid, it can be prepared into an appropriate dosage form, and its blending amount is preferably 0.1 to 15.0% by weight of the entire product.

Examples of the dosage form include a spray-like product sealed in a sealed container equipped with a spraying means, a cream-like or liquid-like product blended into an ointment base, and a poultice.

[Action of the invention]

The present invention uses an organogermanium compound having germanium sesquioxide groups in 1 ml of fatty acid. This organic germanium compound is bis-l'l-β-ethylcarboxylic acid germanium sesquioxide,
Or bisβ-ethylcarboxylic acid amide germanium sesquioxide is preferred.

The organic germanium compound has the following advantages over inorganic germanium.

b) Compared to inorganic germanium, organic germanium compounds have a stronger degree of oxygen bonding.

Mouth) Activates skin metabolism.

c) It has good skin permeability and affinity.

2) Solid inorganic germanium is expected to have a therapeutic effect by stimulating the autonomic nerves. In other words, the effect is due to physical action, whereas the effect of organic germanium compounds is caused by chemical action. In other words, the effect of strong bonding force with oxygen is used. Therein lies its chemical properties. Therefore, it has skin activation permeability, affinity, bactericidal and absorption properties.

〔Effect of the invention〕

Since the external therapeutic agent of the present invention is a fluid, it is easily absorbed through the skin, and since it does not come into contact with foreign substances, there is no discomfort, and there is no feeling of pressure, pain, or discomfort due to sticky substances. It is sufficient to apply it to the affected area, and in addition to being highly efficient and easy to carry, it is convenient to carry and handle, and is also good for storage.

Hereinafter, as examples of the present invention, various forms of the external therapeutic agent of the present invention will be shown together with their compositions (% by weight), and the results of their use will be shown.

[Preparation of organic germanium compound]

(1) Add a hydrochloric acid solution to ethylene cyanide trichlorogermanium obtained by adding 60 g of bis β-ethyl carboxylic acid germanium sesquioxide dermanium chloro7olm 180 #j and reacting with heating in a nitrogen stream. The mixture is heated to form trichlorogermanium ethylcarboxylic acid, which is taken out and reacted with 120 g of thionyl chloride being added dropwise to form trichlorogermanium ethylcarboxylic acid chloride. Water is added to the product obtained by distilling it under reduced pressure and hydrolyzed to obtain bisβ-ethylcarboxylic acid germanium sesquioxide. If this is washed with water until the reaction of chlorine disappears, a white powder is obtained. Yield is approximately 60g.

Calculated value of this as Ca H+ o 07 G e 2 C: 21.17 0: 33.25H:
2.94 Ge: 42, 64 experimental value C: 21,
00 0:32,91H: 3.00 Ge
:42,41(I[]]bisβ-ethylcarboxylic acid amide germanium sesquioxide To 130 g of trichlorodermanium ethylcarboxylic acid chloride prepared by the method described above, 220 g of ammonia water was added.
cc is added and hydrolyzed to precipitate bisβ-ethylcarboxylic acid amide germanium sesquioxide. This is washed with cold water until no chloro reaction is present and dried. Yield is approximately 60g.

This is Cs Hl 20 s N 2 G e 2
Calculated value as C: 21,18 H: 3.53
N: 8.23 0: 23.53 Ge: 42
．． 70 Experimental value C: 21,20 H: 3,6O-11
= N: 8.30 0: 23.63 Ge:
42.50 Example-1 Hydrophilic ointment White petrolatum 23.0% Stearyl alcohol 22.0 Propylene glycol 12.0 Sodium lauryl sulfate 1
2.0 Ethyl paraoxybenzoate 0.025〃
〃 Propyl 0.015n-)lihendecanoin 10.0 Bisβ-ethylcarboxylic acid germanium sesquioxide 10.0 Fragrance 0.5 Purified water
10.5 Example-2 Hap ointment polyethylene glycol 4000 45.0% //
// 400 45.0n-) Lysocaine 5.0=19- Bisβ-ethylcarboxylic acid amide germanium sesquioxide 5.0 Example-3 Medicinal liquid (07-nimaldione type) Stearic acid
1.5% heptyl alcohol 1
．． 5 Vaseline 4.0 Liquid paraffin 8.0 Polyoxyethylene (10
Mol) Monooleate 2.0 Triethanolamine 1. On-heptadecanoic acid
4.0 Bisβ-ethylcarboxylic acid amide germanium sesquioxide 3.0 Fragrance
0.5 Purified water 7
6.0 Example-4 Aerosol composition (spray) Gelatin
20.0 boric acid
1.0 ethanol 57.0
Menthol 1. On-Pentadecatuin 3.0 Bisβ-ethylcarboxylic acid germanium sesquioxide 13.0 Fragrance 0.5 Purified water
5.0 Propellant Near 0 12/70 11 40/60 The above topical therapeutic agents of Examples 1 to 4 were given to 30 people with diseases who come to hot springs at diseased areas (stiff shoulders, neuralgia, dermatitis affected areas). used for. The results of this improvement were classified into 10% effective, effective (+), slightly effective (±), and ineffective (-), and the results are shown in the table below.

Claims (1)

[Scope of Claims] 1) An external therapeutic agent characterized by containing as an active ingredient an organic germanium compound having a germanium sesquioxide group shown below at one end of a fatty acid. ▲There are mathematical formulas, chemical formulas, tables, etc.▼ 2) The organic germanium compound is characterized by being bis-β-ethylcarboxylic acid germanium sesquioxide [I] or bis-β-ethylcarboxylic acid amide germanium sesquioxide [II] Claim 1
External therapeutic agents as described in Section. 3) The blending amount of the organic germanium compound is 0.1 to 15.
The external therapeutic agent according to claim 1 or 2, characterized in that the content is 0% by weight.