DE4033530A1 - Crystallisation inhibitor for treating kidney stone disorders - contains an ethanolic extract of madder contg. 0.2-1.0 per cent ruberythric acid - Google Patents

Abstract

A crystallisation inhibitor consists of an ethanolic extract of madder contg. 0.2-1.01 ruberythrin acid. The inhibitor contains 0.1-0.4g Na-Cu-chlorophyllin, opt. 0.05-0.2g vitamin B1, opt. 0.2-0.5 g vitamin B6, opt. 5.0g ethanol in 15g water and ethanolic madder extract contg. 0.2-0.9% ruberythrin acid to 100g. USE/ADVANTAGE - The crystallisation inhibitor can be used in the prophylactic and metaphylactic treatment of kidney stone disorders. The extracts inhibits the formation of kidney stones and accelerate the removal of such stones. The inhibition are effective, well tolerated, easy to apply, simple to prepare and galenically stable. In an example 0.4 Na-Cu- chlorophyllin was completely dissolved in 5g ethanol and 15g water. 0.3g vitamin B6 and 0.1g vitamin B1 and 1.0g tween 80 were successively dissolved in Ca 50% of the total amt. of ethanolic madder extract necessary. The two solns. were then stirred together and made up to 100g with ethanolic madder extrac

Description

The invention relates to a crystallization inhibitor for prophylactic and metaphylactic treatment of Urinary stone disorders. The invention effectively prevents that Formation of urinary stones and accelerates the finish once formed stones.

This takes in the order of the urological clinical pictures Urinary stone disease in many European countries and With a prevalence of around 5%, it can definitely be one of the Widespread diseases are counted.

Urinary stones consist of their main components or as Pure substrates of approximately 70-75% calcium oxalate and 5-10% from calcium phosphate. This fact and still high Recurrence rates force one to deal with the genesis of this calcium-containing stones as well as for the search for suitable ones therapeutic and metaphylactic measures.

With a variety of different types of medication Influence urinary colic, a spontaneous discharge of the To achieve concretions or renewed through long-term therapy To prevent stone formation.

Already at Hippocrates there are references to vegetable Medicines for urinary stones. Phytopreparations are on the ground their often spasmolytic and diuretic effects for the Stone abortion and in long-term prophylaxis even today up to date again.

Rubia-tinctorum drug extracts are used in various urinary stone medications such as Cystium ^R , Cystenal ^R , Urol ^R , Nieron ^R and others.

The extremely minimal content of inhibitor substances is disadvantageous (Madder hydroxyanthraquinones) in these preparations. He leaves them crystallization-inhibiting properties do not come into effect.

These preparations do not prevent stone formation, but rather accelerate their ability to leave at best. Partial kick however, significant colic.

Another is also under therapy with these preparations Growth to larger urinary stones has been observed. In the sense of her Use as an inhibitor preparation is an increase in Application dose required 100 to 1000 times. This is but not possible due to intolerance. Likewise the combination substances would then be overdosed and thus unwanted side effects not excluded.

The invention is based on the object of an effective well-tolerated and easy-to-use agent that the Prevents formation of urinary stones and the exit of already formed Urinary stones accelerated.

The drug is said to be comparatively easy to manufacture and galenic be stable.

According to the invention, the object is achieved by using madder extract with a Content of 0.2 to 1.0% of ruberythric acid dissolved. The application dose in humans is 3 × 1 daily Tablespoon.

The stone formation inhibiting effect is achieved by the addition of 0.1 to 0.4 g Na-Cu chlorophylline increased. 1.0 g of Tween 80 serves as Solution mediator and solution stabilizer.

A composition of

• 0.1 to 0.4 g of Na-Cu chlorophylline,
• - 0.05 to 0.2 g of vitamin B ₁ ,
• - 0.2 to 0.5 g of vitamin B ₆ ,
• - 1.0 g Tween 80
• - 5.0 g ethanol in 15 g water and
• - ethanolic madder extract 0.2 to 0.9% ruberythric acid made up to 100 g

improves the inhibition of stone formation.  

The advantage of a pronounced and additional diuretic and stone abortion effects good galenic stability has the following composition

• - 0.4 g Na-Cu chlorophylline,
• - 0.3 g vitamin B ₆ ,
• - 0.1 g vitamin B ₁ ,
• - 1.0 g Tween 80,
• - 5.0 g ethanol in 15 g water and
• - ethanolic madder extract 0.2 to 0.9% ruberythric acid made up to 100 g.

The dosage in humans is 3 × 1 tablespoons daily.

An optimum of an efficient combination of active ingredients and galenic The stability of the preparation is with this combination of active ingredients given.

In addition to known spasmolytic, diuretic and anti-inflammatory effects of extracts from Radix Rubiae tinctorum (madder root) becomes the previously unknown anti-crystallization effect of madder hydroxyanthraquinones used effectively.

The inhibitory effect on the model of is very pronounced intrarenal calcium oxalact crystallization in rabbits intraperitoneal glyoxalatin injection. This effect is through oral doses supported by Na-Cu-chlorophylline. From madder Anthraquinones and chlorophyllin is among the many Results of an investigation a mechanism of action in the sense of a specific surface adsorption of these natural products Crystal seeds and crystal growth centers proved. Are from it the reduced crystal formation and the difficult Incremental growth derivable.

In addition to this finding, the use of vitamins B ₆ and B _{1 leads to} a further improvement in the crystallization-inhibiting effect, so that these vitamins are recommended as combination active ingredients in combination with Na-Cu-chlorophylline and the madder extract for metaphylactic use in calcium oxalt stone disease.

The anthraquinone glycosides (hydroxyanthraquinones) of the Madder root extracts act as inhibitors of the intrarenal Crystallization and growth of calcium oxalate in particular. These substances also act against stone formation from calcium and Magnesium phosphates (infection stones).

Na-Cu-chlorophylline also acts as an intrarenal inhibitor Crystallization and growth of calcium oxalate.

Vitamin B ₆ is very effective in the metabolism of glyoxylic acid as a biogenetically relevant precursor of oxalic acid. This means that less stone-forming oxalate ions are excreted in the urine and the critical calcium oxalate oversaturation is reduced. Even a small decrease in the oxalate concentration in the urine is pathogenetically effective.

Vitamin B ₁ activates the metabolism of glyoxylic acid.

Water and ethanol serve as solvents for the active ingredients.

Tween 80 is a solubilizer and solution stabilizer for the ethanolic-aqueous active ingredient mixtures.

The effect of the mixture of substances of the pharmaceutical preparation results from the individual effects described. The Crystallization and stone growth inhibiting effect of Inhibitors is due to the oxalic acid lowering effect of the vitamins supported.

The following is the methodology for making the Active substance mixtures described:

Solution 1:
Na-Cu-chlorophylline is completely dissolved in 5 g of ethanol and 15 g of water.

Solution 2:
In approximately 50% of the total amount of madder extract required, vitamin B ₆ , vitamin B ₁ and Tween 80 are dissolved in succession.

Both solutions are combined with stirring and on the Final quantity (100 g) filled up with madder extract.

Claims (4)

1. Crystallization inhibitor consisting of ethanolic Madder extract with a content of 0.2 to 1.0% Ruberythric acid. 2. Crystallization inhibitor according to claim 1, characterized by a composition

• 0.1 to 0.4 g Na-Cu chlorophylline,
• - 1.0 g Tween 80,
• - ethanolic madder extract 0.2 to 0.9% ruberythric acid made up to 100 g.

3. crystallization inhibitor according to claim 2, characterized by a composition

• 0.1 to 0.4 g Na-Cu chlorophylline,
• - 0 05 to 0.2 g of vitamin B ₁ ,
• - 0.2 to 0.5 g of vitamin B ₆ ,
• - 1.0 g Tween 80,
• - 5.0 g ethanol in 15 g water,
• - ethanolic madder extract 0.2 to 0.9% ruberythric acid made up to 100 g.

4. Crystallization inhibitor according to claim 3, characterized by a composition

• - 0.4 g Na-Cu chlorophylline,
• - 0.3 g vitamin B ₆ ,
• - 0.1 g vitamin B ₁ ,
• - 1.0 g Tween 80,
• - 5.0 g ethanol in 15 g water,
• - ethanolic madder extract 0.2 to 0.9% ruberythric acid made up to 100 g.