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Aqueous solution comprising a polyphenol

a technology of aqueous solution and polyphenol, which is applied in the direction of pharmaceutical non-active ingredients, drug compositions, pharmaceutical delivery mechanisms, etc., can solve the problems of acidic ph, food additives, and difficult clinical use of stilbenoid, and achieve the effects of enhancing stilbenoid solubility and/or stability

Inactive Publication Date: 2018-08-02
OPTERION HEALTH AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent is about a solution containing at least 0.02% of a saccharide that can stabilize stilbenoids. The solution has a pH between 1 and 6, preferably between 3 to 3.5. This pH allows for the solubilization of stilbenoids in acidified glucose solutions, such as commonly used in peritoneal dialysis solutions. The solution also allows for heat sterilization without degrading the stilbenoid. Overall, the patent provides a technical solution to improve the stability of stilbenoids in aqueous solutions.

Problems solved by technology

However, many stilbenoids remain difficult to be employed clinically, as well as food additives, because of low aqueous solubility.
However, such acidic pH are not desired for many applications.

Method used

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  • Aqueous solution comprising a polyphenol
  • Aqueous solution comprising a polyphenol
  • Aqueous solution comprising a polyphenol

Examples

Experimental program
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examples

Methods:

Molecular Weight Measurement:

[0162]The saccharides are dissolved in extra-pure water in a concentration of 0.5% (w / v). The solutions are heated at 95° C. for 30 minutes. The polymers are analyzed using the following devices: Alliance chromatography system (Waters corporation, Milford, Mass., USA), DAWN-EOS light scattering detector (Wyatt Technology, Santa Barbara, USA) with λ0=658 nm and 16 detectors in the range of angles from 14.4 to 163.3°, K5 flow cell. The polymers are fractionated on a precolumn and three columns having the separation ranges 300-104, 5×104-2×106 and 106-108 (SUPREMA-Gel, PSS Polymer Standards Service GmbH, Mainz, Germany). 100 μl of solution are injected. The fractionation takes place at a temperature of 30° C. and a flow rate of 0.8 ml / min with 0.05M NaNO3 as eluent. The Astra V 5.1.8.0 program (from Wyatt Technology, Santa Barbara, USA) is used to analyze the molecular weight distribution of the samples. Same procedure can be used when molecular wei...

specific examples

[0169]Purity of tested stilbenoids were[0170]for resveratrol between 99.86% and 99.88%[0171]for piceid between 98.89% and 99.12%.

[0172]Major impurity in piceid was resveratrol of approximately 1%.

[0173]For analysis R and P and their impurities were separated by a C-18 column with a gradient system and UV-detection at 306 nm.

[0174]Increase of stability or solubility of a stilbenoid by presence of a saccharide, could only be measured within the range of solubility of the saccharide it self.

[0175]Solubility measurements after 1 hour stirring at RT generated some variability in-between measurement series, which might be due to low temperature variations, back-ground measurements and experimental imprecisions. Specifically, variations of concentration of Resveratrol in H2O, without any saccharide, between 0.3 and 6 mg / L were observed in-between different series. As a rule of thumb, for calculating factors of increased solubility, the minimal concentration value of Resveratrol in H2O was ...

example 1

[0176]Solubility and stability of Resveratrol and Piceid after one hour stirring at RT, as a function of glucose or icodextrin concentration in a solution, containing 5.4 g / L NaCl, 4.5 g / L NaLactate, 0.275 g / L CaCl2, and 0.051 g / L MgCl2, buffered at pH 3 or pH 7. Solubility was measured after one hour stirring at room temperature, in presence of excess solute, followed by filtering.

[0177]At 0% glucose or icodextrin, pH3 versus Ph7 stabilizes Resveratrol by 2 to 3 times and stabilizes Piceid 3 to 4 times and slightly increases solubility of both stilbenoids.

[0178]At pH7, 0.024% of glucose or Icodextrin stabilize tested stilbenoids 2 to 3 times. 0.075% of Glucose or Icodextrin stabilize tested stilbenoids 3 to 4 times.

[0179]High concentrations of Glucose (24 and 47%), but concentration of Icodextrin of only 0.075%, completely stabilize the tested stilbenoids within the limits of detection and increase their solubility within one hour by a factor 1.5 to 2.

[0180]Highest tested glucose c...

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Abstract

Aqueous solution, comprising, in dissolved state,—at least one stilbenoid—at least one saccharide, and method for increasing the solubility of a stilbenoid in water

Description

[0001]The present invention relates to an aqueous solution comprising a stilbenoid and to a method for increasing the solubility of stilbenoids in aqueous environment.BACKGROUND OF THE INVENTION[0002]Stilbenoids have been suggested as treatment and prevention against several diseases, including diabetes, cancer, inflammation and degenerative diseases. However, many stilbenoids remain difficult to be employed clinically, as well as food additives, because of low aqueous solubility. Various approaches like nanosizing, self-microemulsifying drug delivery systems (SMEDDS), microencapsulation, complexation, and solid dispersion can be used to increase the bioavailability of stilbenoids. Other possibilities lie in synthesis of stilbenoid derivatives with higher aqueous solubility. Solubility can be measured, at a given temperature, in different ways, as absolute solubility or as solubility within a limited time of stirring (e.g. one hour at room temperature). The latter is an important me...

Claims

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Application Information

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IPC IPC(8): A61K31/05A61K47/26A61K47/36A61K9/08A61P13/12
CPCA61K31/05A61K47/26A61K47/36A61K9/08A61P13/12A61M1/287
Inventor GRENTZMANN, GUIDO
Owner OPTERION HEALTH AG
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