HU199692B - Process for producing pharmaceutical compositions containing extract of black radish - Google Patents

Abstract

The present invention relates to a method for the preparation of a pharmaceutical composition comprising a black radish extract. The method of preventing and treating bile and gallstone diseases can be used as a pharmaceutical preparation, possibly as a medicament, as a pharmaceutical product, which, taking into account domestic eating habits, can effectively supplement or replace existing drug treatment. - Extraction of fresh, peeled black radish by extrusion - Black radish extract by lyophilization or otherwise dried and directly used or in various combinations - Applying the juice to the base granule - Use of the granules in various combinations with essential oils and / or extracts of other herbs - Granules Direct use - Removal of granules in capsules, tablets or other pharmaceutical forms. EN 199692 A Scope of the description: 4 pages without drawing -1-

Description

FIELD OF THE INVENTION The present invention relates to a process for the preparation of an extract of black frames and pharmaceutical compositions containing them for the treatment of indigestion.

Most of Hungary's population suffers from some form of indigestion. Of these, the malfunctioning caused by malfunctioning of the bile ducts is outstanding.

Our domestic medicinal treasure does not provide the right choice for those suffering from this disease, especially not in the area of natural substances. Our folk medicine, on the other hand, has diverse experience in the therapy of the digestive system.

Studying the suggestions of domestic and foreign folk observations and customs and folk medicine, we turned our attention to the use of black radish. Literature data support its effects on digestion and specifically on bile.

Thus, we found it expedient to produce a simple, low-component, functionally reliable, well-standardized product that would be technologically easy, quick to execute, and material and asset inputs should be within realistic limits.

Accordingly, we find the granulate as the most suitable dosage form to be most suitable.

After the preparation of the base granulate, the pressing liquid itself, printed from fresh peeled black radish, was used as the wetting agent as a granulating liquid. Subsequently, a piercing, dried and regranulated product was applied to the supplement - enhancing the effect - essential oil.

The finished dosage form almost loses the distinctive, unpleasant odor of the squeezed juice, and thus its enjoyment is enhanced, which can be further enhanced by the use of essential oils. The proceeds may be unchanged, that is to say, they may be in solid form, they may be dissolved in any beverage, or they may be used as ingredients in other pharmaceutical forms (eg tablets, capsules).

The consumption of spicy foods that are too fatty makes it difficult for the digestive process to function properly. Changing this dietary pattern, especially in the winter and in rural areas, is a very slow and almost ineffective process due to entrenched misconceptions and economic reasons. To solve these digestive problems, we have various preparations available in the pharmaceutical palette in Hungary.

According to old folk observations, we turned our attention to black radish. Namely, it was one of the foods regularly used in the Szeged homeland and is known for its black radish. It was eaten with, among other things, fatty broth. Black radish is widely used abroad in Nicaragua and Mexico and is consumed in various forms.

Nowadays, natural materials are becoming more and more popular in therapy. That is why we have considered it necessary to address this issue, thus expanding the range of natural substances in the treatment of indigestion that is a major issue in people's disease.

1.) Older Hungarian recipe collections contain the description and method of making radish candy.

2.) The book that deals with the processing and systematization of Argentine folk medicine deals with the therapeutic effect and use of radish in great detail. Among other indications, it highlights its very important role in the natural treatment of bile disorders.

3.) Mexico is famous for its increased use of natural materials. Based on their popular observations, a book has been published on plants that are useful, providing important and accurate information on the use of black radish.

4.) A Raphanus sativus L.var. niger (Mi 11)

S. Kerner, among the curative substances of black radish, is the mustard glycosides, essential oils, enzymes, enzyme inhibitors, vitamins B and C. Among its uses are dyspepsia, cholecystopathy, gall and gallstones. In addition, homoeopathic medicine recommends it for headaches and flatulence.

5.) The 1972 Order of Drugs (Issehutz B., - Issehutz L.) mentions the addition of a dragee called "Raphabil" containing black radish adsorbed on coal.

6.) Official preparation in Austria of "Kneipp Rettich - Pflanzensaft" (Rote Liste 1987)

7.) Injection marketed in Canada “Raphanus s. Potier (Laboratoires Sidel)

In vitro studies

The different types of bile stones (cholesterol, limestone, pigment stone) disintegrated in freshly squeezed black radish juice after a few days of storage under slight pressure.

Toxicity studies

Oral toxicity studies were performed on LATI OFA rats of both sexes. The animals were fasted for 24 hours prior to treatment. They were free to drink water. They weighed 120-150 g. With a 10% suspension of the preparation, LD ₅₀ could not be routinely determined by Litchfield-Wilcoxon as the substances were not toxic at 30 ml / kg or even 60 ml / kg. No toxic symptoms were observed in the animals within 24 hours.

Animal test for demonstration of effect

LATI CFY rats of mixed weight 240-260 g were anesthetized with 25% Urethan. (0.4 mL / 100 g). A small incision was made in the abdominal cavity under the pylorus to bind the thin-2WU ductus Wirsungianus to the intestine, a thin cannula was placed above the ductus and then sutured. Prior to closure of the abdominal cavity and skin, 5 animals received 5 ml of 10% MgSO ₄ solution orally and 5 animals received 5 ml of 10% oral solution. The animals were heated with a lamp to maintain a constant body temperature. The effluent bile was collected in tubes.

MgSO _{4 is} very powerful in triggering bile secretion. The effect of the test product was even stronger. The amount of bile that was seized was even more. Thus, the test substance has a very strong effect on biliary production and excretion.

In terms of drug formulation, in terms of efficacy, technology and economics, granules have been found to be most suitable as stand-alone pharmaceutical formulations.

Digestion in the stomach is instantaneous, so absorption begins almost immediately after ingestion.

The technology is simple, the operation itself can be accomplished in a relatively short period of time, it does not require much equipment, and every aspect of it can be mechanized. Of the possible formulation options, this is the most economical and does not require too much energy.

It is not negligible from the application point of view that the present formulation almost completely loses the characteristic, unpleasant odor of the press juice. In fact, in combination with violet oils it becomes enjoyable. Not least, the shelf-life of the formulation is significantly better than that of the solid dosage form.

Of the various granulation processes, the wet process was chosen, in which base granules were mixed with the active ingredient as granulating fluid itself.

Ingredients of the granulate

The starting point is VII. In the Hungarian Pharmacopoeia, the composition of an official Granule Simplex was used.

The filler used was lactose and sucrose. The binder is required to achieve the proper breaking strength. We used a mixture of starch and polyvidone in the right proportions to ensure rapid disintegration, but also mechanical stability during storage.

The presence of a disintegrant in the composition of the granule is essential for rapid dissolution. For this purpose, ultraamylopectin V.N. (CMA) we found the most suitable.

The granulating liquid is provided by the pressed juice of fresh, peeled, cut black radish. The extraction takes approx. 20%.

Granulate

50-65 tr lactose

10-16 tr of sucrose

10-20 tr potato starch

2-10 tr polyvidone

2-8 tr CMA

10-20 tr of granulating fluid

The compositions of the invention are prepared as follows.

a) The black radish juice is mixed with honey and seasoned with the appropriate essential oil.

100 g of juice 100 g of honey

0.5 g of essential oil (well mixed) (fennel, anise, mint, cumin)

b) Half of the raw press juice is compacted and used directly, or the concentrate is mixed with an equal amount of honey and a small amount of essential oil relative to the starting juice.

Concentrate 100 g of juice to 50 g of concentrate 50 g of honey

0.5 g of essential oil (well mixed) (fennel, anise, mint, cumin)

c. The press juice is lyophilized and used as a powder. Lyophilization of 100 g of black radish juice using about 1 g of powder formulation, or 10 g of lyophilisate with 0.1 g of powdered Benedictine, or 0.05 g of powdered canine bark, or 0.05 g of powdered haemorrhoidal grass and / or 10 g of honey or mixed with herbal extracts to make herbal medicine.

d. ) 60 g lactose g sugar 15 g starch 5 g polyvinylpyrrolidone 4 g ultraamyl opectin

From the powder mixture, 15 g of black radish press juice is made into granules.

100 g granulate 100 g honey

0.5 g essential oil (fennel, mint, anise, caraway)

The preparation is well mixed.

Claims (1)

Patent Claim Point A process for the preparation of a pharmaceutical composition comprising black radish extract, comprising washing, peeling, rinsing the black radish, chopping the resulting pure radish, and then squeezing, settling and / or filtering, if necessary. a) Tr. 8-11 tr. pressed juice is formulated directly as a pharmaceutical composition, or optionally 8-11 tr. with honey, optionally 0.5-0.7 tr. combined with essential oil of fennel, anise, mint, cumin, or b.) crude 8-10 tr. The press juice is concentrated to 4-5 trillion and formulated directly as a liquid pharmaceutical formulation, or optionally 8-10 tr. with honey, optionally 0.3-0.6 tr. Combined with essential oil of fennel, anise, mint, cumin, or 3 -3HU 199692 A c. ) 95-100 tr. the juice is lyophilized or spray-dried to form it directly as a pharmaceutical formulation, or the 8-11 tr. lyophilisate optionally from 0.1 to 0.2 tr. pulvis Cardui benedicti herba, 0.05 to 0.1 tr. pulvis Fragulae cortex, 0.05-0.1 tr. pulvis Chelidonii herba drugs and / or 8-12 tr. mixed with honey or drugs extracts, or d. ) using 10 to 20 parts by weight of the press juice as a wetting liquid: granulate with 50 to 65 tr of lactose, 10 to 16 tr of sucrose, 10 to 20 tr of potato 6 or corn or wheat starch, 2 to 10 tr of polyvinylpyrrolidone, 2 to 8 tr of ultraamylopectin, the resulting granulate optionally with honey, 5 or optionally with essential oil of fennel, mint, anise, cumin and optionally the resulting lyophilisate and / or spray-dried product and / or press and / or granules are tabletted or encapsulated or may be delivered by means of a probe. sterile formulation