Use of an active ingredient combination that contains hydroxystilbene for preventing and/or treating diseases

a technology of active ingredients and hydroxystilbene, which is applied in the direction of biocide, plant ingredients, medical ingredients of coniferophyta, etc., can solve the problems of insufficient investigation of whether, metabolites, and the constituents of err 731® are degraded in the body, and do not provide verifiable technical teaching of the asserted pharmacological usability

Inactive Publication Date: 2013-02-07
HEGER PETER +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is about finding a new way to prevent and treat diseases that are associated with elevated levels of a protein called IL-6. These diseases can be treated using a selective estrogen receptorβ (ERβ) agonist. The invention is based on the use of a special combination of active ingredients that have been found to have a beneficial effect on IL-6 levels. This combination can be used to produce a pharmaceutical composition that is effective in treating disorders associated with elevated IL-6 levels.

Problems solved by technology

There has been only inadequate investigation of whether, and to which metabolites, the constituents of ERr 731® are degraded in the body for example after oral administration.
However, in fact, FR 2 835 185 does not provide a verifiable technical teaching for the asserted pharmacological usability, to say nothing of the asserted synergistic effect of the complex drug extract described therein.
In particular, experimental data proving the alleged usability for the treatment of disorders connected with free radicals, such as, for example, accelerated aging, cancer, arteriosclerosis, wrinkles, inflammatory phenomena and the like, are completely lacking.

Method used

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  • Use of an active ingredient combination that contains hydroxystilbene for preventing and/or treating diseases
  • Use of an active ingredient combination that contains hydroxystilbene for preventing and/or treating diseases
  • Use of an active ingredient combination that contains hydroxystilbene for preventing and/or treating diseases

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

Preparation of the Dry Extract ERr 731 from Rhapontic Rhubarb Root with an Aqueous Calcium Hydroxide Solution

[0202]A dry extract is prepared from rhapontic rhubarb root employing the following:

Drug (radix rheum rhaponticum) 50.0 kgCalcium oxide 5.0 kgPurified water190.0 kgAcetic acid (as necessary to adjust the required pH)

[0203]The yield which can be achieved in this case is between 2 and 3 kg per 50 kg of drug.

[0204]The preparation takes place in the following steps:

[0205]a) Firstly 5 kg of calcium oxide are introduced into a plastic tub and made into a slurry with 20 kg of purified water. The formation of calcium hydroxide (quicklime) which takes place under these conditions leads to a large rise in temperature of the solution. The calcium hydroxide can therefore be used further only after cooling. The temperature of the solution is then 30° C. to 35° C.

[0206]b) 50 kg of drug are introduced into a mixer, and the abovementioned quicklime is added. In order to remove the quicklime ...

preparation example 2

Preparation of a Dry Extract from Rhapontic Rhubarb Root with Various Organic Solvents

[0215]The constituents mainly detectable in the rhapontic rhubarb root used as drug here belong to the group of hydroxystilbenes. Present from this group in the roots are rhaponticin (Rh) with a content of about 6% and deoxyrhaponticin (DRh) with a content of about 4%.

[0216]It is possible by exposure to the solvent systems indicated below, in a 100-fold quantity at room temperature for 10 minutes with shaking or stirring, to extract the proportions summarized below:

Ethanol 86%Rh100.8%DRh99.5%Ethanol 15%Rh77.1%DRh75.5%AcetoneRh88.3%DRh96.6%Water, alkalineRh75.5%(pH 11, adjusted with CaO solution)DRh60.5%

[0217]No useful results were achieved with heptane.

[0218]The respective yields of crude extracts in proportions by mass (based on drug employed) are as follows:

Ethanol 86%35.5%Ethanol 15%32.2%Acetone21.4%Heptane  0%Water, alkaline 4.5%

[0219]Extraction of rhapontic rhubarb root with ethanol-water mixt...

formulation example 1

Production of a Solid Dosage Form—Minitablet

[0223]1. Production of the tablet core:

[0224]A solid tablet core is produced using the following active ingredients and ancillary substances in the stated ratios of amounts (P=parts by weight). The ingredients are mixed and tabletted in three different ways:

[0225]a) Tablet core formulation:

Purified dry extract according to3.6Ppreparation example 1 fromrhapontic rhubarb root (ERr 731 ®)Microcrystalline cellulose (e.g. Avicel ®)57.0P (±40%)Sorbitol8.0P (±40%)Talc2.5P (±40%)Makrogol 6000 (polyglycol)1.6P (±40%)Polyvidone (K value about 25, e.g. Kollidon ® 25)1.6P (±40%)Sodium dodecyl sulfate (e.g. Texapon ® K 12)0.5P (±40%)Magnesium stearate (vegetable)0.8P (±40%)75.6P (±40%)

[0226]It is possible by varying the weighed amount of ERr 731® and / or varying the amount of microcrystalline cellulose to obtain any desired ERr 731® contents in the untreated core (such as, for example, 2, 4, 6, 8, 10, 12 mg per tablet).

[0227]b) Mixing of drug and carrie...

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PUM

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Abstract

The invention relates to the use of a combination of active ingredients, selected from resveratrol and piceatannol precursors and functional derivatives thereof, in addition to the use of the stereoisomeric forms of said ingredients, in the form of salts or phenol respectively, for producing an agent for the prevention and / or treatment of diseases, whose occurrence and / or progress is associated with an increased IL-6 serum level and / or whose occurrence and / or progress can be treated by a dose of a selective oestrogen receptor .beta. (ER-β) agonist.

Description

RELATED APPLICATIONS[0001]This application is a continuation of U.S. application Ser. No.11 / 883,685, filed May 15, 2008, issued as U.S. Pat. No. 8,268,792, which is the U.S. national phase application, pursuant to 35 U.S.C. §371, of PCT international application Ser. No. PCT / EP2006 / 000951, filed Feb. 3, 2006, designating the United States and published in German on Aug. 10, 2006 as publication WO 2006 / 082068 A1, which claims priority to German application Ser. Nos. DE 10 2005 005 268.1, filed Feb. 4, 2005, DE 10 2005 005 270.3, filed Feb. 4, 2005, DE 10 2005 005 271.1, filed Feb. 4, 2005, DE 10 2005 005 273.8, filed Feb. 4, 2005, DE 10 2005 005 274.6, filed Feb. 4, 2005, DE 10 2005 005 275.4, filed Feb. 4, 2005, DE 10 2005 005 276.2, filed Feb. 4, 2005 and DE 10 2005 023 164.0, filed May 19, 2005. The entire contents of the aforementioned patent applications are incorporated herein by this reference.[0002]The invention relates to the use of hydroxystilbene-containing active ingredie...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/7034A61P35/00A61P25/06A61P29/00A61P25/24A61P25/22
CPCA23L1/3002A61K9/2054A61K9/2846A61K9/2866A61K31/085A61K31/7034A61K36/15A61K36/708A61K36/482A61K36/481A61K2300/00A23L33/105A61P13/02A61P13/08A61P25/06A61P25/22A61P25/24A61P29/00A61P35/00
InventorHEGER, PETERRETTENBERGER, REINHARDSPAICH, CARL-FRIEDRICH
OwnerHEGER PETER