JPH03120220A - Preparative drug and preparation thereof - Google Patents

Abstract

PURPOSE: To obtain an orally and percutaneously useful medicine comprising a solution of metal minute element, formed of a metal such as Fe or Zn and having a specific pH value and water, exhibiting antibacterial and treatment promoting action and capable of decreasing swelling at a low concentration. CONSTITUTION: This medicine comprises at least one constitutional metal trace element formed of at least one metal among Fe, Zn, Mn, Cr, Cu, Co, Mo, Sn, V, Ni and Se and contained in a physiological amount or an amount which is several times larger than the physiological amount and distilled water or deionized water and the solution is controlled to pH <=7, especially <=4 by addition of physiological acid such as hydrochloric acid, sulfuric acid, silicic acid, ascorbic acid or acetic acid. At least one trace element in the solution is contained, in an amount of maximally 1-2 in 100wt.% solution. The medicine is suitable as effective substance of sunscreen cream and for treatment of wound and burn of skin and subcutaneous cellular tissue and for supplementing lack of trace element in the case of oral administration.

Description

[Detailed description of the invention] (Industrial application field) The present invention relates to a drug preparation and a method for producing the same.

(Prior Art) It is known in principle to treat wound conditions with inorganic or mineral active substances, for example.

Zinc oxide is used for prevention and treatment of wounds, burns, etc.

In addition - inflammatory changes in the skin and subcutaneous tissue during boat fishing;
Furthermore, it is widely used to treat chronic wounds and ulcers. However, despite the widespread use of zinc oxide, the desired results are often unsatisfactory.

SUMMARY OF THE INVENTION The object of the present invention is to provide a pharmaceutical preparation and a method for producing the same, which guarantees high bioavailability not only for transdermal use but also for oral use.

In order to achieve the above object, a preparation according to the characterizing parts of claim 1 and a process for the production of said preparation according to the characterizing parts of claim 8 are carried out.

The specifically mentioned forms are the subject of dependent claims.

The preparations according to the invention, which are suitable for percutaneous use as well as for oral use (e.g. in place of trace element deficiencies), ensure in all cases a high bioavailability of the existing metal trace elements (trace substances). Therefore, the desired therapeutic effect can be obtained with a small amount of prescription.

Furthermore, the preparation according to the present invention, which is excellent in mucosal digestibility, exhibits the following pharmaceutical properties, especially in transdermal use.

Anti-inflammatory action Anti-coagulant action (particularly in fresh hematomas) Anti-bacterial and anti-viral action Promote granulation of the wound while reducing scar tissue This invention is based on the knowledge that there is a high need for other trace elements, especially metals, in highly active tissue areas (defensive processes and/or cell proliferation). According to the knowledge based on the literature, the tissue that is modified becomes less effective depending on the degree of injury, eg by reducing zinc.

On the other hand, in conventional treatment with zinc oxide ointments, the zinc does not dissolve and therefore does not act on the current wound, or only acts on a very limited and insufficient area of the wound. In contrast to conventional zinc ointments of this kind, the preparation according to the invention makes it possible to introduce zinc, iron or other essential, i.e. biologically necessary, trace elements into an acidic solution, which Therein, these trace elements are completely dissolved and are thereby able to function effectively.

At the same time, a pH value of clearly below 7, especially below 4, provides a biochemical environment suitable for protective activities suitable for living organisms.

Acids, especially also physiological acids, eg sulfuric acid.

Acids specific to the human body, such as hydrochloric acid, silicic acid, acetic acid and ascorbic acid, or the acids used therewith, or diluted solutions such as citric acid, have no pharmacological properties in nature, even if we ignore their definite antibacterial action. The trace amounts of metals in aqueous solution that characterize the invention, even if they do not show any reduction in action and especially also swelling, and in particular also, even if the metal or metal compound has only an extremely limited pharmaceutical action. The combination of elements and acids leads to completely unexpected and unexpected effects, i.e. on the basis of the cooperative effect of acids and metals.
The drug prepared according to the invention with essential metal trace elements present in the ions reduces swelling at very low concentrations and shows strong antibacterial and wound healing promoting effects.

In the form presented, the preparations according to the invention can best be adapted to the particular indication or application. Therefore, for example 1
The preparations according to the invention can be incorporated as pharmaceutically active components in ointments or creams, but can also be used directly in liquid form.

The metal trace elements (especially iron) in the preparation according to the invention also promote the formation of melanin, which is characteristic of the human body, by UV irradiation (natural solar rays or artificial UV irradiation), which promotes tanning of the skin due to UV irradiation. do. The preparations according to the invention are therefore also suitable as active ingredients in tanning creams.

In addition to the two primary transdermal uses listed above for treating wounds, burns, or other inflammatory changes in the skin and subcutaneous tissue, 1
The preparations according to the invention are also particularly suitable for oral use and in particular for compensating for trace element deficiencies or for replacing metallic trace elements in the human or animal body, in which case an excellent A high absorption rate is achieved due to the above-mentioned synergistic effect and the resulting good bioavailability.

EXAMPLES In practical administration, it is also possible to use the preparation according to the invention orally, for which purpose the preparation or solution contains major chlorides, but not in the blood (Serums
The concentration of minerals or trace elements in
The increase is many times stronger than what should be expected based on the concentration of the trace elements in the preparation or on the basis of the amount of the trace elements administered. This effect is clearly due to the administration of the preparation according to the invention.

It thus depends on the activation and exploitation of sequestered trace element deposits compatible with the human body by administering trace elements with a surplus of acid. Similar effects are established in the case of external use of the preparations according to the invention.

In the preparation according to the invention, water is also suitable, for example distilled water. Deionized water obtained by electrolysis is also used, especially for treating other artificial biological properties. The concentrations of the metal trace elements dissolved in water as salts or other water-soluble compounds and their mutual proportions correspond in particular to physiological quantities or concentrations, i.e. to the concentrations or quantities in natural serum or to multiples thereof. . The proportion of toxic metal salts or metal compounds in the relatively large quantity is present in the range of IQ solution photolimidarum and, like the proportions of the metal salts or metal compounds to each other, is determined approximately in terms of physiological amounts; In that case, it may exceed multiple times 1, for example 2 to 20 times. For example, 3 g of zinc chloride and 6 m
Very good results were obtained with a concentration of iron chloride of g.

Although in certain cases increasing the concentration can improve the action of the preparation, increasing the concentration of metal trace elements worsens the digestibility of the formulation.

As mentioned above, the main factor for the action of the preparations according to the invention is the pH value. Particularly good pharmaceutical action is p
A H value in the range of about 4.0 to 1.0 is obtained, in which case it is especially certain if the pH value is below 3.5. The pH value is adjusted by adding appropriate amounts of physiological acids (hydrochloric acid, sulfuric acid, silicic acid, acetic acid and/or ascorbic acid).

The preparation according to the invention, which is suitable for external or internal (internal) use, in particular for the treatment of inflammation, contains zinc and iron as trace metal elements in solution and, as a physiological acid, the pH value of the solution is approximately 2. , containing an amount of sulfuric acid such that it ranges from 0 to 3.0, in which case the proportion of zinc, iron and sulfuric acid is 1
About 5-30 ■g of zinc, about 10-5Qmg in the solution of a.
of iron and about 100-160 mg of sulfuric acid, when used in inflammation, detoxification of the sulfate takes place, i.e., toxic protein compounds present or occurring in the inflammation bind to the sulfate and are thereby neutralized. be done. For external use, this preparation forms, for example, the active ingredient of an ointment. This preparation can also be used as an active ingredient in preparations intended for oral administration.

In principle, various methods are suitable for producing the preparations according to the invention. Thus, for example, in particular the production of metals forming at least one essential metallic trace element of the group consisting of iron, zinc, manganese, chromium, copper, cobalt, molybdenum, tin, vanadium, nickel, selenium is particularly finely ground. In solid or powder form, it is introduced into the solution together with acid and water, the pH value of the solution being adjusted, for example, by the amount of water added and/or the amount of acid added.

Furthermore, the preparations according to the invention contain at least one water-soluble metal compound of essential metal trace elements, such as zinc chloride,
Iron chloride or chromium oxide can also be prepared by dissolving it in water with the addition of physiological acids, in which case the required pH value is adjusted by the amount of water and/or acid added.

In addition to essential metallic trace elements, the preparation according to the invention also contains essential non-metallic trace elements, in particular from the group consisting of silicon, iodine and fluorine, which non-metallic trace elements are present in the preparation in physiological amounts or below. Contains several times the amount.

A preferred method for producing the preparation according to the invention will now be explained on the basis of a diagram showing a simplified cross-section of equipment for the production of preparations by electrolysis.

In the figure, (1) is a container made of an electrically nonconductive material such as glass or resin. This container (1)
An essentially neutral, aqueous initial solution containing chloride and/or sulfate dissolved in water is introduced into the solution. Into this initial solution (2) a pair of electrodes (3L (4) are placed, both electrodes (3L (4)) located in the container and placed at a predetermined distance from each other. 3) and (4) are connected to the same power source (not shown), electrode (3) acts as a cathode and electrode 1 (4) as an anode. Between the pair of electrodes are two membranes or diaphragms (5), ( 6) are arranged, and these membranes (5) and (6) cover the container (1).
) has three areas: the area of the electrode (3) or the area with the cathode (7), the area with the electrode (4) or the area with the anode (8), and the areas (8) and (7). It is divided into areas (9) between the two areas. The membranes (5) and (6) are made of a suitable material, such as ceramic, textile, felt or fur material, and have a suitable thickness, and are connected to the electrode (3) and ( 4) First solution (2) by
Furthermore, the membranes (5) and (6) have a concentration of acidic moieties (H+) obtained by ionization or electrolysis in the region of zone (7) and by electrolysis in the region of zone (8). Basic moiety (O
simultaneously ensuring the concentration of H-) and the intermediate area (9)
Precipitation is prevented by separating both zones (7) and (8) by . In the illustrated installation, which allows a reproducible working method, the electrode (3) forming the cathode is made of at least one metal or an alloy of such metals suitable for the formation of essential metallic trace elements. . By electrolysis, at least one metal forming the electrode (3) or an alloy forming the electrode (3) is melted in the zone (7), so that
The concentration of essential metal trace elements in the acidic solution in that area increases. It is self-evident that one area (7) can also be provided with a plurality of electrodes (3) of different or identical metals and/or different or identical alloys.

A plurality of electrodes (4) can likewise be used in the area (8). Furthermore, in addition to the electrode (3), one zone (7) can also be provided with another neutral electrode which, unlike the electrode (3) or a plurality of similar electrodes (3), does not dissolve in the solution.

In order to be able to adjust the desired concentration of the metal trace element or metal trace elements in the zone (7), at least the electrode or electrodes (3) present there are installed on a movable support and, if necessary, the electrodes allows the immersion depth to be adjusted.

Instead of membranes (5) and (6), it is also possible to use membranes formed as at least one tube, in particular such membranes made of water-permeable fired porcelain. In that case, the electrodes used are arranged inside the at least one membrane in such a way that the arrangement causes the acid part or the alkali part from the electrolysis to be concentrated inside the tubular membrane.

[Brief explanation of drawings]

The figure is a cross-sectional view schematically showing an adaptation for manufacturing the preparation according to the invention. In the figure, 1: container, 2: solution, 3.4: electrode, 5.6: membrane, 7.8.9: area 158-

Claims (20)

[Claims] (1) is formed of at least one metal from the group consisting of iron, zinc, manganese, chromium, copper, cobalt, molybdenum, tin, vanadium, nickel, and selenium, and is contained in the solution described below in a physiological amount or slightly twice that amount. A prepared drug, characterized in that it consists of a solution of at least one essential metal trace element containing water, the pH of which is clearly below 7, in particular below 4. (2) The prepared drug according to claim 1, in which the pH value of the solution is determined by the addition of at least one physiological acid from the group consisting of hydrochloric acid, sulfuric acid, silicic acid, ascorbic acid, acetic acid. A prepared drug characterized in that it is adjusted. (3) In the prepared drug according to claim 1 or 2, the pH value of the solution is about 4.0 and about 1.0.
A prepared drug characterized in that it is in the range between. (4) A prepared medicament according to any one of claims 1 to 3, in which at least one trace element in the solution contains at most 1 to 100% by weight of the solution. 2 percent by weight. (5) A prepared drug according to any one of claims 1 to 4, characterized in that the water is distilled water or deionized water. (6), in a prepared medicament according to any one of claims 1 to 5, wherein the additional moiety in the at least one essentially non-metallic trace element is silicon, iodine and fluorine; A pharmaceutical preparation characterized in that it is in a physiological amount or several times that amount taken from the group consisting of: (7) In the prepared drug according to any one of claims 1 to 6, the solution has a pH of
containing zinc and iron as the metal trace elements and sulfuric acid as the physiological acid, with zinc, iron and sulfuric acid in the following proportions: A prepared drug characterized in that it contains about 5 to 30 mg of zinc, about 10 to 50 mg of iron, and about 100 to 160 mg of sulfuric acid. (8) A method for producing a mineral preparation, in which at least one mineral is formed of a metal from the group consisting of iron, zinc, manganese, chromium, copper, cobalt, molybdenum, tin, vanadium, nickel, and selenium. It is characterized by dissolving in water a physiological amount of essential mineral trace elements or slightly twice that amount, and the pH value of the solution being clearly adjusted to a value of 7 or less, particularly 4 or less. A method for producing a preparation. (9) In the manufacturing method according to claim 8, at least one essential metal trace element is present in the solution in which the proportion of said trace element in the solution is at most 1 to 100% by weight. A process for producing a preparation, characterized in that it is dissolved in water in an amount such that it amounts to 2% by weight. (10) In the manufacturing method according to claim 8 or 9, the pH value of the solution is about 4.0 and about 1.0.
A method for producing a preparation, characterized in that the preparation is adjusted to a value between 0. (11) In the manufacturing method according to any one of claims 8 to 10, at least one selected from the group consisting of hydrochloric acid, sulfuric acid, acetic acid, silicic acid, and ascorbic acid.
1. A method for producing a pH adjusting agent, which comprises adjusting the pH value using an additive of physiological acids. (12) In the manufacturing method according to any one of claims 8 to 11, the solution is set so as to improve the action of the current action on the drug and to ionize it. A method for producing a characterized preparation. (13) In the manufacturing method according to any one of claims 8 to 12, from iron, zinc, manganese, chromium, copper, cobalt, molybdenum, tin, vanadium, nickel, and selenium. at least one pure metal of the group consisting of at least one pure metal, especially in finely divided or powdered form, is introduced into a solution together with an acid and water, and the pH value of the solution is adjusted, in particular by the amount of water added. Method for manufacturing preparation. (14) In the manufacturing method according to any one of claims 8 to 12, from iron, zinc, manganese, chromium, copper, cobalt, molybdenum, tin, vanadium, nickel, and selenium. A method for producing a preparation, characterized in that the solution is made using at least one water-soluble metal compound of a metal of the group consisting of physiological acids and water. (15) A method for producing a preparation according to claim 14, wherein the water-soluble metal compound is zinc chloride, iron chloride or chromium oxide. (16) In the manufacturing method according to claim 14 or 15, the proportion of water, the physiological acid and the metal compound is such that at least one A method for producing a preparation, characterized in that the proportion of essential metal trace elements and/or the pH value of the solution is adjusted. (17), in the manufacturing method according to any one of claims 8 to 13, in which chloride and/or sulfate (e.g. MgCl
An approximately neutral initial aqueous solution containing (CoCl) is used which is electrolyzed using at least one cathode and at least one anode such that the acid fraction formed therein is concentrated at the anode. and at least one electrode made of at least one metal from the group consisting of iron, zinc, manganese, chromium, copper, cobalt, molybdenum, tin, vanadium, nickel, and selenium or an alloy of such metals as an anode. A method for producing a preparation used, characterized in that the metal or its alloy is dissolved by a portion of the acid produced by electrolysis. (18) A method for producing a preparation according to claim 17, characterized in that at least one membrane placed between the cathode and the anode is used. (19) A method for producing a preparation according to claim 18, characterized in that a tubular membrane, particularly a membrane made of fired ceramics that permeates water, is used. (20) A method for producing a preparation according to claim 19, characterized in that the acid or alkali portion generated by electrolysis is concentrated inside the tubular membrane.