WO2019011955A3 – May 16, 2019 – SOLUBILISATE WITH CURCUMIN AND OPTIONALLY AT LEAST ONE OTHER ACTIVE SUBSTANCE

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Inventors :

BEHNAM, Dariush - Schwalbenweg 9, 64380 Rossdorf

Owner :

AQUANOVA AG

Application Number :

WOEP18068731

Document Number :

WO2019011955A3

Priority Date :

January 1, 1970

Filing Date :

July 11, 2018

Date of Grant/ Publication :

May 16, 2019

Class :

; A61K47 / 26; A61K9 / 107; A61K31 / 12; A61K31 / 19; A61K36 / 324; A61P3 / 06; A61P3 / 04; A61P3 / 00; A61P25 / 16; A61P25 / 28; A61P29 / 00; A61P35 / 00; A61P37 / 00; A61P3 / 10; A61K38 / 48; A61K31 / 05; A61K31 / 122; A61K31 / 385; A61K36 / 185; A61K36 / 484

Abstract

In order to make available the health-promoting and healing properties of curcumin to the human or animal organism, and in combination with at least one other active substance, the invention provides a solubilisate consisting of or containing a proportion of curcumin equal to or smaller than 10% by weight, preferably equal to or smaller than 7.5% by weight, most preferably 6% by weight, and at least one emulsifier with an HLB value in a range below 18, preferably between 13 and 18, namely polysorbate 80 or polysorbate 20 or a mixture of polysorbate 20 and polysorbate 80, the average diameter of the curcumin-charged micelles ranging from 5 nm to 40 nm, preferably from 6 nm to 20 nm, most preferably from 7 nm to 10 nm, for use in particular as a food supplement and/or medicinal drug for treating and/or preventing diseases involving inflammation, cancer and other diseases.

Claim(s)

Solubilizate containing, in particular consisting of, In a proportion of less than or equal to 10% by weight comprises curcumin -, 7.5 wt. -% preferably less than or equal, particularly preferably 6% – wt. and at least one emulsifier having an HLB value in the range of less than 18, preferably between 13 and 18, polysorbate 80 or polysorbate 20 or polysorbate 20 is a mixture of and polysorbate 80, wherein the average diameter of the micelles loaded with between 5 nm and 40 nm comprises curcumin, preferably between 6 nm and 20 nm, particularly preferably between 7 nm and 10 nm is for use in the treatment of diseases associated with inflammation and/or preventing, cancer, Alzheimer’s, Parkinson’s, obesity, high cholesterol values, elevated blood sugar, Diabetes mellitus, metabolic syndrome and/or Autoimmune diseases, multiple sclerosis (msec), for reducing visceral fat, for thermogenesis, lowering of cholesterol, in particular LDL-cholesterol, and/or of glucose in the blood and/or Triglycerides in blood, for improving the Macular pigment density, and/or for reducing the accumulation for reducing oxidative stress of fat in the hepatocytes, in particular medicaments for the treatment of and/or preventing fatty liver, Ataxia Friedreich’s ataxia, lysophospholipid times diseases, in particular Tay -Sachs is’s disease, atherosclerosis, heart disease, arthritic solubilizate. containing, in particular consisting of, In a proportion of less than or equal to 10% by weight comprises curcumin -, 8 wt. -% preferably less than or equal, particularly preferably 3% – wt. 7 wt. -% to, and at least one further active compound and at least one emulsifier having an HLB value in the range less than 18, preferably between 13 and 18, in particular polysorbate 80 or polysorbate 20 or polysorbate 80 and a mixture of polysorbate 20.;
According to claim 2 solubilizate, characterized in that the at least one further active ingredient a Substance comprises one or more substances, is or are selected from the group consisting, which secondary plant substances, in particular Flavonoids, natural phenols, especially as CHALCONES xanhtohumol, plant extracts, in particular of the resin of the incense tree, from licorice, Cannabinoids, enzymes, in particular Serrapeptase , coenzyme q10, ?-lipoic acid, with resveratrol, comprises.;
Solubilizate according to claims 2 or 3, for use in the treatment of and/or Preventing inflammation-associated diseases, cancer, Alzheimer’s, Parkinson’s, obesity, high cholesterol values, elevated blood sugar, Diabetes mellitus, metabolic syndrome and/or Autoimmune diseases, multiple sclerosis (msec), for reducing visceral fat, for thermogenesis, lowering of cholesterol, in particular LDL-cholesterol, and/or of glucose in the blood and/or of triglycerides in the blood, for improving the Macular pigment density, and/or for reducing the accumulation for reducing oxidative stress of fat in the hepatocytes, in particular medicaments for the treatment of and/or preventing fatty liver, Ataxia Friedreich’s ataxia, lysophospholipid times diseases, in particular Tay -Sachs is’s disease, atherosclerosis, heart disease, arthritic.;
Solubilizate according to any of claims 1 to 3 for use as anti-inflammatory Food supplements and/or as a medicament having an anti-cancer activity, Alzheimer’s, Parkinson’s, obesity, high cholesterol values, increased Blood sugar, diabetes mellitus, metabolic syndrome and/or autoimmune diseases, multiple sclerosis (msec), for reducing visceral fat, for thermogenesis, cholesterinsekendes as medicaments, in particular on LDL-cholesterol, and/or as a medicament having an effect for reducing blood glucose and/or of triglycerides in the blood, for improving the macular pigment density, and/or for reducing the accumulation for reducing oxidative stress of fat in the hepatocytes, in particular a medicament having an activity against fatty liver, Ataxia Friedreich’s ataxia, lysophospholipid times diseases, in particular Tay -Sachs is’s disease, atherosclerosis, heart diseases, is arthritis.;
Solubilizate according to any preceding, characterized in that the total curcuminoids concentration in the human blood plasma after oral administration of 500 mg in the form of measured one hour comprises curcumin Solubilisats according to any preceding at about 500 ng ± 100 ng per ml of plasma per ml of plasma is curcuminoids curcuminoids.;
Solubilizate according to any preceding, characterized in that the total curcuminoids concentration in the human Over a period of 24 hours measured as blood plasma area under the curve of the total blood plasma concentration comprises curcumin – (burgundy-the local area the plasma concentration of Time totally comprises curcumin curve AUC ) in Range of about 9,500 to about 10,000 nmol h/l lies.;
Solubilizate according to any preceding, characterized in that the concentration of c-reactive protein antiinflamatorische activity measured as (CRP has) in Arthritic rats after single dose of blood serum in a dosage of 5 mg/kg of Solubilisats Body weight in the range of about 2100 pg/ml to about 2500 pg/ml is comprises curcumin.;
Solubilizate according to any preceding, characterized in that the concentration of c-reactive protein antiinflamatorische activity measured as (CRP has) in Arthritic rats after single dose of blood serum in a dose of 10 mg/kg of Solubilisats Body weight in the range of about 1400 pg/ml to about 1800 pg/ml is comprises curcumin. Solubilizate according to any preceding, characterized in that the antiinflamatorische effect measured as concentration in blood serum arthritic rats of myeloperoxidase (is MPO) after a single administration of said In a dosage of 5 mg/kg of Solubilisats Body weight in the range of about 800/ml to about 900 comprises curcumin-mu-mu/ml.;
Solubilizate according to any preceding, for use in agriculture, horticulture and/or fish farming and/or in the area of food hygiene and/or for use as disinfectants and/or in the region of the Package, preferably in the packaging of Beef, poultry or fish, and/or Use as disinfectant.;
Solubilizate according to any preceding, characterized in that the emulsifier content, in particular Polysorbate proportion, at least 70% by weight -, 75 – 95% by weight and preferably in the range between -% by weight, particularly preferably in the range between 79% and 88% by weight by weight – – is.;
Solubilizate according to any preceding, characterized in that up to 20% by weight the solubilizate -, weight % preferably up to 15 – Ethanol. Solubilizate according to any preceding, characterized in that up to 25% by weight the solubilizate -, preferably between 12% – wt. 20 wt. -% and, up to 10% by weight more preferably – Contains glycerol.;
Solubilizate according to any preceding, characterized in that the solubilizate additionally contains up to 10 wt.% -, preferably up to 7 wt.% – Water.;
Solubilizate according to any preceding, characterized in that the diameter distribution of the micelles in a dilution of 1:500 in relation Solubilisats with distilled water under physiological conditions (pH of 1.1 and 37 °c) of about 6 nm to about d9o=20 nm=device DIO.;
Solubilizate according to any preceding, characterized in that the turbidity of less than 25 Solubilisats FNU , preferably less than 3 FNU is measured by Scattered light measurement with infrared light according to Rules at a dilution of 1:50 in ISO 7027 Solubilisats 1:500 in water at physiological conditions or ratio (1.1 and pH of 37 °c).;
Capsule filled with a solubilizate according to any preceding, characterized in that the capsule or as soft gelatin capsule Hard gelatin capsule or as soft, hard gelatin capsule or as free, gelatin free capsule, for example as cellulose capsule, is formed.;
Fluid containing a solubilizate according to one of Claims 1 to 17, characterized in that the fluid is selected from the group, wel food, food supplement, beverage, cosmetic and pharmaceutical products comprises.;
The fluid according to claim 19, characterized in that the fluid an aqueous dilution of the Solubilisats comprises.;
Method for treating and/or preventing diseases associated with inflammation, cancer, Alzheimer’s, Parkinson’s, obesity, high Cholesterol values, increased blood sugar, diabetes mellitus, metabolic syndrome and/or autoimmune diseases, multiple sclerosis (msec), for reducing visceral fat, for thermogenesis, lowering of cholesterol, in particular LDL-cholesterol, and/or of glucose in the blood and/or of triglycerides in the blood, for Improving the macula pigment density, and/or for reducing the accumulation for reducing oxidative stress of fat in the hepatocytes, in particular medicaments for the treatment of and/or preventing fatty liver, Ataxia Friedreich’s ataxia, lysophospholipid times Diseases, in particular Tay -Sachs is’s disease, Atherosclerosis, heart diseases, arthritic, characterized in that a solubilizate according to any of claims 1 to 17, in particular in a capsule according to claim 18 or 19 or 20 as fluid according to one of, the food supplement consumer or Patient, in particular orally, is administered.;
claim 19: 22. Method according to claim 21, characterized in that the solubilizate the consumer or patient in the food supplement – 0.5 mg/kg of body weight to a range of 1 mg contains curcumin dose/kg of Body weight, preferably at a dose of 0.81 mg/kg body weight, in particular once daily, administered.;
claim 20: 23. Method according to claims 21 or 22, characterized in that the solubilizate the consumer or patient – the food supplement in a 1 mg/kg body weight to Boswellia dose in the range of 2 mg/kg of Body weight, preferably at a dose of 1.62 mg/kg body weight, in particular once daily, administered.;
claim 21: 24. Method according to claim 21 or 22 and 23/and/or, characterized in that the solubilizate the consumer or patient – the food supplement in a 0.5 mg/kg body weight to 1 mg xanthohumol dose in the range of/kg body weight, preferably at a dose of 0.81 mg/kg body weight, the method of manufacturing a Solubilisats according to any of claims 2 to 17, comprising the steps of d is) and/or polysorbate 20 and/or 80 of Polysobat present a mixture of polysorbate 20 and Polysorbate 80 I) adding at least one other active ingredient, in particular Boswellia Serrata extract and/or xanhtohumol, f is) addition of curcumin powder wherein in step a) to a temperature in the range of 40 °c to 62 °c heating, preferably to a Temperature in the range of 45 °c to 57 °c, particularly preferably to a temperature in the range of 48 °c and 52 °c, is and wherein in step b) the temperature remains unchanged with respect to step a) heating to a temperature in the range of 60 °c to 75 °c or, preferably to a temperature in the range of 61 °c to 70 °c, particularly preferably to a temperature in the range of 63 °c and is 67 °c, and wherein in step c) heating at a temperature in the range of 82 °c to 97 °c, preferably to a Temperature in the range of 83 °c to 92 °c, particularly preferably to a temperature in the range of 85 °c and 89 °c takes place. A method according to claim 25, wherein before step b) a step BI) addition of water at a temperature in the range of 40 °c to 62 °c, preferably at a temperature ranging from 45 °c to 57 °c, particularly preferably at a temperature in the range of 48 °c and 52 °c, is performed.;
claim 22: Method according to claims 25 or 26, wherein in step BI) adding ethanol at a temperature ranging from 40 °c also to 62 °c, preferably at a temperature ranging from 45 °c to 57 °c, particularly preferably at a temperature in the range of 48 °c and 52 °c, is performed.;
claim 23: A method of manufacturing a Solubilisats according to any of claims 2 to 17 comprising the steps of a is) preparing a first approach and/or polysorbate 80/20 and by initially introducing Polysobat polysorbate 20 and polysorbate 80 or a mixture of at least one first active ingredient and, in particular alpha-lipoic acid, b is) producing a second approach of water and at least one additional drug by present, especially Serrapeptase d) adding at least one further active compound, in particular xanthohumol and/or, and/or and/or Glavonoid Boswellia serrata extract Resveratrol and/or coenzyme q10, and adding to the second approach of curcumin powder Step b) d is) combining the first approach of step a) and the second approach of step c), wherein the temperature during the execution of the steps a) to d) in the range of 18 °c to 22 °c is, s) heating to a temperature in the range of 80 °c to 97 °c, preferably to a temperature in the range of 83 °c to 92 °c, particularly preferably to a temperature in the range of 85 °c and 89 °c.;
claim 24: A method according to claim 28, wherein in step d) the addition of ethanol and/or glycerol also and/or/and/or polysorbate 20 or polysorbate MCT oil and 80 and/or a mixture of Polysorbate 20 and polysorbate 80 takes place.;
claim 25: A method of manufacturing a Solubilisats according to any of claims 2 to 17 comprising the steps of b is) and/or polysorbate 20 and/or 80 of Polysobat present a mixture of polysorbate 20 and Polysorbate 80 and of glycerol and ethanol, and b) adding at least one other active ingredient, in particular an ethanolic extract of the Hard resins from hops, in particular PU powder Xantho -type Flav , wherein in step a) to a temperature in the range of 40 °c to 62 °c heating, preferably to a Temperature in the range of 45 °c to 57 °c, particularly preferably to a temperature in the range of 48 °c and 52 °c, is and wherein in step b) heating to a temperature in the range of 60 °c to 75 °c a, preferably to a Temperature in the range of 61 °c to 70 °c, particularly preferably to a temperature in the range of 63 °c and is 67 °c, d) addition of curcumin powder at a temperature in the Range of 70 °c to 92 °c, preferably at a temperature in the range of 75 °c to 87 °c, particularly preferably at a temperature in the range of 78 °c and 82 °c, d is) adding Glavonoid under heating to a Temperature in the range of 80 °c to 97 °c, preferably to a temperature in the range of 83 °c to 92 °c, particularly preferably to a temperature in the range of 85 °c and 89 °c.;
claim 26: A method of manufacturing a Solubilisats according to any of claims 2 to 17, by mixing a Curcuminsolubilisats and at least one additional drug solubilisats , more preferably of the 1:1 of the individual solutes to each other.;
claim 27: A method of manufacturing a Solubilisats xanhtohumol -, in particular for use in a method according to claim 31, comprising the steps a) providing a ethanolic extract of the hard resins from hops, in particular PU powder Xantho -type Flav , b is) and/or polysorbate 20 and/or 80 Polysobat adding a mixture of polysorbate 20 and Polysorbate 80, wherein in step b) to a temperature in the range of 80 °c to 95 °c heating, preferably to a Temperature in the range of 81 °c to 90 °c, particularly preferably to a temperature in the range of 83 °c and 87 °c takes place.;
claim 28: A method according to claim 32 wherein before step b) a step BI) dissolving the ethanolic extract of the hard resins from hops, in particular PU powder Xantho -type Flav , in ethanol under heating to a temperature in the range of 40 °c to 62 °c, preferably to a temperature in the range of 45 °c to 57 °c, particularly preferably to a temperature in the Range of 48 °c and 52 °c, is performed.;
claim 29: A method for producing a enzyme Solubilisats , especially a Serrapeptase type Solubilisats , in particular for use in a method according to claim 31, comprising the steps of, a is) of water and enzyme present, in particular Serrapeptase , b is) addition of MCT oil d) addition of polysorbate 20 or polysorbate 80 and/polysorbate 20 and polysorbate 80 and/or a mixture of, wherein the temperature during the execution of the Step a) in the range of 18 °c to 22 °c lies, and wherein in step b) heating at a Temperature in the range of 77 °c to 93 °c, preferably to a temperature in the range of 80 °c to 90 °c, particularly preferably to a temperature in the range of 83 °c and 87 °c, takes place.

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