HU209652B - Process for producing plant extract for treating diseases of the renal system - Google Patents

Abstract

The present invention relates to a method for producing a herbal extract against kidney and bladder disorders, comprising: 25-35% of angelic root, 15-25% of field horsetail, 15-25% of gold litter, 15-25% of lean root containing dried ground powder. optionally extracting known excipient (s), (a) extracting by cooking in a manner known per se, or b) soaking in water at 40-70 ° C for 1 to 4 hours, compressing the liquid from the pulp obtained and / or centrifuged, if desired, the residue is again soaked in water and re-extruded and / or centrifuged, and the resulting liquor is concentrated and, if desired, an adsorbent is added to the effluent and vapor, which is washed with a solvent at the end of the concentration, and the resulting solution is combined to remove the solvent. residual concentration. EN 209 652 A Scope of description: 6 pages

Description

The present invention relates to a novel process for the preparation of herbal extracts for the treatment of renal and bladder disorders, 25-35% by weight of angelica root, 15-25% by weight of horsetail, 15-25% by weight of golden willow, 15-25% by weight of leeches and containing herbal mixtures.

Herbs containing medicinal and aromatic substances have been playing an increasingly important role in medicine in recent decades.

There are many arguments for the medicinal use of herbs. It is a very important fact that herbs that are known and used today (hundreds of herbs) have been in use for centuries, so it is also clear that they have no harmful effects and / or side effects on the human body.

Recently, the so-called aromatherapy, which focuses on the use of aromatic and essential oil constituents of various herbs (G. Rácz, A. Laza, E. Coiciu: Medicinal and essential oil plants, Ceres Publishing House, Bucharest, 1972) has recently come to the fore.

There is currently a wide variety of herbal remedies available from various herbs, and of course, the literature also suggests a variety of mixtures for the treatment of various diseases.

It is still a much debated question which of the various herbal blends used to cure various diseases or even to maintain health are the most suitable to achieve the desired effect. In the current state of science, this debate cannot be resolved because, while some plants can identify the molecule responsible for the effect (eg Digital, Claviceps, Papaver, Catharantus, Vinca), in the vast majority of plants, despite the isolation of many constituents and their structure it was possible to find the molecule that is clearly responsible for the effect, so that the theory is likely that the synergistic effect of synergistic, possibly complex, organic molecules (alkaloids, glycosides, terpenes, flavonides, anthraquinone derivatives, etc.) would seem to be suitable (synergistic). ) (H. Wagner, Drogen und ihre Inhalttsstoffe, Pharmazeutische Biologie, 1979, G. Fischer Verlag, Stuttgart, New York; F. Deutschmann et al., Droganalyse I: Morphologie und Anatomie Pharmazeutische Biologie, 1979, G. Fischer Verlag). , Stuttgart, New York).

The synergistic effect or effects of a system of molecules made up of many herbs that are theoretically suited to exert a number of effects, and this depends on the proportion of the ingredients, is essentially inconceivable based on our present knowledge.

The various formulations used in a particular field of action are said to have a common principal effect, but differ in their degree of effect and in other, generally advantageous, side effects, and each generally has some positive effect over the others.

However, it seems clear that herbal products based on herbal products contain the highest proportion of the active ingredients of the herbal medicinal product in the form of formulations or applications to be used.

Kidney and bladder tea mixtures are described in numerous works and patents, of which the following are mentioned.

From the book "Healing plants" of Rápóti-Romváry we mention the following compositions:

Thistle I (5 units by weight), goldenrod (5 tsp.), Rose hips (10 tsp.), Igloo root (5 tsp.), Goose pimple (5 tsp.), Bearberry leaf (5 tsp.), Chives (5 tsp.), Tarragon root (5 tsp.), Horsetail (5 tsp.), Birch leaf (5 tsp.), Lentil root (6 tsp.), Parsley root (5 tsp.), Juniper (10 tsp.).

II. Yarrow (10 tsp.), bearberry leaf (10 tsp.), elderberry (10 tsp.), nettle leaf (10 tsp.), calendula (10 tsp.), peppermint leaf (10 tsp.), horsetail (10 tsp.), elderflower (10 teas.), Linden flowers (10 teas.), Juniper (10 teas.), Rose hips (10 teas.).

There are five more recipes in the book, with a variety of herbs that are similar to the above.

Hungarian Patent No. 196,130, for the preparation of preventive or soluble kidney stones (kidney sand), starts from the following mixture (preferred version): 0.15 te. nettle leaves, 0.50 te. lemongrass, 0.20 te. juniper, 0.25 te. burdock root, 0.50 te. elderflower, 0.30 te. horseradish, 0.50 te. burdock, 0.30 te. coriander seed, 0.75 te. mustard seed, 0.30 te. lestyángyökér.

It is clear from the above that many herbal preparations for kidney and bladder disorders with different compositions are known, and it is likely that each has some positive additional effects over the others (while, of course, they have other, also called positive) effects.

Specifically, each of the works mentioned in the above sources considers it necessary to boil the drug mixture for a period of time (usually at least 20 minutes).

A common feature of herbal, volatile, and aromatic substances is that they are generally heat-, light- and oxygen-sensitive and hydrolyze when heated in aqueous solution. For centuries, it has been observed that boiling or boiling the plants can produce aqueous solutions which are curative. Only one or two of the very decomposing plants, such as rose hips, are subjected to gentler heat treatment, however, as shown above, boiling extraction is used in the field of tea mixtures for kidney and bladder disorders. One reason for this is that, by boiling, the more soluble components can be dissolved, and on the other hand, the solution is sterilized. Significant loss of active substance was previously not significant2

EN 209 652 Gel with regard to low availability of starting materials.

Currently, commercially available herb-based products are manufactured on an industrial scale, reaching the required production capacity by simply enlarging and expanding conventional methods. Due to the size increase, the large amount of starting material will remain relatively longer in the active ingredient under non-mild conditions.

We have investigated the question of the proportion of useful materials in the final product which is present in the manufacturing processes used.

In the generally used extraction at 100 ° C (for 15-20 minutes, with about 25-27% dry matter recovery) about 50% alkaloids, about 55% glycosides, about flavonides . 60%, anthraquinones ca. 65% of the terpene, ca. 50% can be analyzed in the aqueous solution and only 10-15% of the aromatics were found.

For commercial formulations, it is essential to concentrate the resulting solution, usually by vacuum evaporation (atmospheric evaporation is even more disadvantageous). According to our measurements, the amount of organic matter belonging to the group listed above is further reduced by 10-30%, while the aroma substances are completely eliminated.

It is an object of the present invention to provide an herbal extract containing a proportion of components which, in addition to its action against renal and bladder disorders, has beneficial physiological effects, and requires a large amount of available starting materials. , which yields significantly better yields of the active aroma.

The inventive herbal composition of the present invention required lengthy experimentation to find a mixture of commercially available, relatively inexpensive formulations having a potent composition or further derivative of the composition having adequate activity against kidney and bladder disorders, do not burden the kidneys or the liver itself.

Another very important aspect of the process according to the invention is the new method of preparing the herbal extract.

A method has been developed during lengthy laboratory and field experiments which avoids boiling that is commonly used in the preparation of such herbal extracts, and provides significantly better yields of active ingredients, volatiles and aromas (100-300% yield increase :) .

A reference example to illustrate the advantages of the process of the invention is also provided herein (see Example 3).

Among the analytical results supporting the increase in yield, the following are highlighted:

Yield: 60-65 ° C 60-65 ° C 80-100 ° C Adsorbent: Yes no no Example number: 1. Second Third Essential oil (mg / ml): 0.5, 0.3 0 Flavones (mg / ml): 2.3 2.3 1.4.

The present invention therefore relates to a process for the preparation of herbal extracts for the treatment of renal and bladder disorders, comprising dried powder containing 25-35% angelica root, 15-25% starch horsetail, 15-25% gold canary grass, 15-25% leechinella, containing, if desired, known excipient (s),

the. ) by extraction by cooking in a manner known per se, or

b. ) Soak for 1-4 hours in water at 40-70 ° C, squeeze and / or centrifuge the resulting slurry, if necessary, soak the residue again in water and re-squeeze and / or centrifuge, and then press the resulting juice to concentrate. an adsorbent is placed in the path of the exhaust gases and vapors, which is flushed with solvent at the end of the concentration, and the resulting solution is combined with the remaining concentrate after solvent removal.

In carrying out the methods of the present invention, the herbs to be used are dried, comminuted and, if sterility problems are encountered in the manufacturing process, preferably the initial mixture is sterilized by radiation treatment. Alternatively, the final product may be sterilized, preferably by radiation sterilization.

If radiation sterilization is not used, the water-soaked mixture may be boiled or pasteurized for desiccation if desired.

In process (a) of the present invention, the novel starting mixture is worked up in a manner known per se, for example as described in U.S. Patent No. 189,162. The concentrate thus obtained has a novel, very advantageous spectrum of action resulting from the new starting composition. This process, of course, yields a lower yield and lower aroma and essential oil content than process b), but is significantly more advantageous than those known in the art.

In carrying out the process according to the invention, which is much more preferred, b), the starting mixture is swollen in 2 to 5 times its weight, preferably 3 times its weight, for 1 to 4 hours, preferably 2 to 2.5 hours. The water used in the swelling (digestion) is preferably acidic (H = 1.0-4.0). For acidification, for example, citric acid may be used. If radiation sterilization is not used, the mixture may be boiled or pasteurized for desiccation if desired.

The temperature used during digging is a very important factor. Although yields of up to 40 ° C can be achieved which are not much worse than conventional processes, yields of 60-65 ° C yield extremely high active ingredient, volatile and aroma yields. At temperatures above 70 ° C, many valuable components undergo decomposition (these components are conventional

Losses are significantly greater in slack processes).

After digestion, the resulting pulp is separated from the solid residues by filtration or centrifugation, and the residue is squeezed and / or subjected to vigorous centrifugation. If centrifugation is used, it is preferable to use at least 10,000 rpm. The preferred solution is pressing, in which case it is advisable to use a screw press or press extractor in this step. It is desirable to rinse the press residue (spin residue) several times, preferably twice, with mild acidic water. The resulting mixture was cooled (20-30 ° C) and filtered.

The filtrate is concentrated by vacuum evaporation to a volume of 0.10.2. Here, too, gentle conditions are used (pressure is 6-8 x ^{10 3} Pa, preferably 7 x ^{10 3} Pa, temperature 30-40 ° C, preferably 35 ° C).

In a preferred embodiment of the present invention, an adsorbent, preferably granular activated carbon, is added in front of the cooling unit (condenser) to bind the flavoring and volatile substances. Of course, other materials suitable for solvent and temperature conditions, such as silica gel, Al ₂ O ₃ , synthetic adsorbents, and the like, may also be used as adsorbents. At the end of the distillation, the adsorbent is washed with a non-toxic organic solvent, preferably ethyl acetate. The resulting flavoring solution is also degassed under gentle conditions. The resulting aroma concentrate is blended with the main weight of the product at any stage of the further processing, preferably in the final step.

Flavorings may also be recovered by extracting flavorings from a condensed aqueous solution in the receiver.

The resulting concentrate can be converted into a formulation conventional in pharmaceutical products using methods and additives known per se. It is preferred that the resulting concentrate be lyophilized and spray dried, in which case the aroma extract may be added to the product after lyophilization.

The process of the invention will be described in more detail below.

EXAMPLE 7 g medical angel root (Angelicae radix et rhizoma) g horseradish (Equiseti herba) g golden parsley (Solidaginis herba) g chestnut root (Levistici radix) (the plants are used in dried form) grind to mmes. The flour is swelled in 300 g of 0.25% citric acid in water for at least 2 hours and at most 3 hours at 65 ° C. The drug pulp is then passed through a screw press (pressurized 6.0-7.0 x ^{10 6} Pa). The press juice is collected (200-220 ml) and the drug is washed with 200 g, also 0.25% citric acid water. The resulting extract (340-370 ml) was cooled to ambient temperature (20-25 ° C) and filtered through a Hyflo supercell filter bed (20 g) to dryness (crude and solid free). wash with water, add the wash solution to the filtrate (360-390 mL solution).

A laboratory vacuum evaporator is assembled by inserting a G3 glass-bottomed tube section with a suitable abrasive (sealed) connection between the evaporator flask and the cooling condenser into which 20 g of granulated activated carbon is inserted and the vapor is passed through.

The above approx. The extract (360-390 ml) was concentrated to a volume of 65 ml on the above vacuum evaporator.

After disassembly of the vacuum evaporator, the adsorbent was washed with 50 ml of ethyl acetate at 20-25 ° C. The solution was collected in a 100 ml round-bottomed flask, and the solvent was removed on a Rotavapor vacuum evaporator by evaporation of ethyl acetate. The remaining approx. Check the absence of ethyl acetate in 0.5 ml of oil by gas chromatography. If the oil is ethyl acetate free, it is added to the concentrate with stirring.

The analytical results of the 65 ml concentrate obtained above are described below.

the. Dry solids content: 0.32 g / ml (based on 100 g of starting mixture: 20.8 g).

b. Essential oil content: 0.5 mg / ml (based on 100 g of starting mixture: 32.5 mg).

c. Flavonide, expressed as (total) rutoside:

2.3 mg / ml (155 mg per 100 g starting mixture).

Flavonoid components: isoquercitrin, luteolin, quercetin mono- and diglycosides.

d. Umbelliferone content: 4.6 mg / ml (calculated on a 100 g starter mixture: 299 mg).

Example 2

Starting from the composition of Example 1, and

As described in Example 1, 360-390 ml of herb-filtered herbal extract is obtained.

Concentration of the extract is carried out with the exception that no carbon adsorbent is used. Concentration is also performed by vacuum distillation (65 ml final volume). After the distillation is complete, the condensed water (about 300 mL) from the collecting flask is transferred to a shaking funnel and extracted with 3 x 50 mL of ethyl acetate. The combined solutions were de-solvented as described in Example 1. 0.28 g of an oil is obtained which is combined with the concentrate with stirring.

The analytical results of the 65 ml concentrate obtained above are described below.

the. Dry solids content: 0.32 g / ml (based on 100 g of starting mixture: 20.8 g).

b. Essential oil content: 0.3 mg / ml (calculated as 100 g of starting mixture: 19.5 mg).

c. Flavonide, expressed as (total) rutoside:

HU 209 652 A

2.3 mg / ml (calculated as 100 g of the starting mixture: 155 mg).

d.) Umbelliferone content: 4.6 mg / ml (calculated on a 100 g starter mixture: 299 mg).

Example 3 (Reference Example)

Starting from the herb mixture of Example 1. The flour is swelled with 300 g of water for 2.5 hours and then the thick, non-agitated pulp is stirred by addition of 700 g of water. The operation is carried out in a 3 L round bottom flask, after dilution, the flask is refluxed and heated with a flask crater. The heating is continued to reflux and the mixture is refluxed for 15 minutes. The mixture was then cooled to 20-30 ° C and the solid was collected by filtration. The filtered material was rinsed with 200 g of water and the washing solution was combined with the filtrate. The resulting approx. Filter 980 ml of extract sharply on a 20 g Hyflo supercell filter bed. The filter bed is washed with 20 ml of water and the washing liquid is added to the extract. The resulting approx. 1000 ml of herbal extract are then concentrated on a vacuum evaporator (without adsorbent) to a volume of 65 ml.

The analytical results of the concentrate obtained as described above are described below.

the. Dry solids content: 0.30 g / ml (calculated as 100 g of starting mixture: 19.5 g).

b. ) Essential oil content: None.

c. Flavonide expressed as (total) rutoside:

1.4 mg / ml (calculated as 100 g of the starting mixture: 91 mg).

d. Umbelliferone content: 3.3 mg / ml (calculated on a 100 g starter mixture: 214.5 mg).

Example 4

The preparation of Example 1 is carried out except that the initial herb mixture is not soaked but first soaked in water at room temperature, then boiled abruptly, then cooled to 60-65 ° C with cold water and the active ingredient is recovered. continued at this temperature as described in Example 1, with the other exception that the drug pulp was separated from the solution by accelerated filtration.

Claims (5)

PATIENT INDIVIDUAL POINTS 1. A method for producing a herbal extract for kidney and bladder disorders, comprising: 2535% angel root, 15-25% horsetail, 1525% gold cane, 15-25% dried lard containing 15-25% lecithin, known as excipient also contains the. ) is extracted by cooking in a manner known per se b. ) Is soaked in water at 40-70 ° C for 1 to 4 hours, the liquid from the resulting pulp is squeezed and / or centrifuged, if desired, the residue is again soaked in water and re-extruded and / or centrifuged, and the resulting slurry is compressed, if desired. in the path of the exhaust gases and vapors, an adsorbent is placed, which is washed with a solvent at the end of the concentration, and the solution thus obtained is combined with the remainder of the condensation after removal of the solvent. Process according to claim 1, characterized in that an acidic aqueous solution is used for soaking. 3. Process according to any one of claims 1 to 5, characterized in that water is used in the amount of 2-5 times that of the dried mill during soaking. 4. Referring to 1-3. Process according to any one of claims 1 to 5, characterized in that carbon is used as the adsorbent. 5. Process according to any one of claims 1 to 5, characterized in that ethyl acetate is used to wash the adsorbent.