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Methods of increasing solubility of poorly soluble compounds and methods of making and using formulations of such compounds

A technology of chemical compounds and organic compounds, which can be used in skin care preparations, active ingredients of hydroxyl compounds, cosmetic preparations, etc., and can solve problems such as the illusion of safety of sunscreens

Inactive Publication Date: 2013-09-25
API起源有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Sunscreen use may sometimes create a false sense of safety when an individual is overexposed to the sun

Method used

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  • Methods of increasing solubility of poorly soluble compounds and methods of making and using formulations of such compounds
  • Methods of increasing solubility of poorly soluble compounds and methods of making and using formulations of such compounds
  • Methods of increasing solubility of poorly soluble compounds and methods of making and using formulations of such compounds

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Experimental program
Comparison scheme
Effect test

preparation example Construction

[0387] Polysorbates are a class of emulsifiers used in the preparation of some medicines or foods. They are often used in cosmetics to solubilize essential oils in water-based products. Polysorbates are oily liquids derived from PEGylated sorbitol (a derivative of sorbitol) esterified with fatty acids. Surfactants that are esters of fatty acid-containing mono (non-PEGylated) sorbitol are commonly known as Spans.

[0388] ・Polysorbate 20 (polyoxyethylene (20) sorbitan monolaurate)

[0389] · Polysorbate 40 (polyoxyethylene (20) sorbitan monopalmitate)

[0390]· Polysorbate 60 (polyoxyethylene (20) sorbitan monostearate)

[0391] · Polysorbate 80 (polyoxyethylene (20) sorbitan monooleate)

[0392] The number 20 after the polyoxyethylene moiety refers to the oxyethylene-(CH 2 CH 2 O) - total number of groups. The number following the polysorbate portion relates to the type of fatty acid associated with the polyoxyethylene sorbitan portion of the molecule. Monolaurate is r...

Embodiment 1

[0566] Example 1. Solubility in Polysorbate

[0567]The product made from apigenin and polysorbate 80 is called "A / PS80". A / PS80 is made through the following steps:

[0568] Mix unprocessed apigenin powder and viscous liquid polysorbate 80 (PS80) with a ratio of about 5-10wt% apigenin and 95-90wt% polysorbate 80 and a small amount of deionized and any Optionally also acetone and / or ethanol mixed in the beaker;

[0569] The mixture is then stirred well to form a thick paste mixture;

[0570] • The mixture is then slowly heated to a relatively high temperature while stirring. The heating process is accompanied by evaporation of water and volatile components present in polysorbate 80. The heating process is carefully controlled to avoid overflowing of the mixture from the beaker due to foaming caused by the heating process;

[0571] Upon removal of volatiles and heating to a temperature in excess of about 200 to 300°C, a dark brown clear liquid is produced such that all of ...

Embodiment 2

[0586] Example 2. Determination of Solubility of Selected Flavonoids in Polysorbate 80 and PEG400 by HPLC

[0587] The aim of this work was to quantify a total of six different flavonoids in PS80 and PEG-400. Samples were also analyzed qualitatively to look for signs of solvent degradation due to the high temperatures required during heat treatment.

[0588] The program was divided into three distinct phases: method validation / development, quantification of various flavonoids, and qualitative analysis to look for signs of PS80 / PEG400 degradation. Method development was performed to determine whether the previously used high performance liquid chromatography (HPLC) method for apigenin was suitable for quantification of remaining flavonoids in PEG400 or PS80.

[0589] Table IX provides the HPLC concentrations of flavonoids in PS80 and PEG-400 in the flavonoid concentrates prepared by the heat treatment process.

[0590]

[0591] Statistical analysis software was used to loo...

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Abstract

The subject invention relates to novel soluble forms of planar ring structured organic compounds including flavonoids, and their production. The invention also includes the use of these novel formulations of planar ring structured organic compounds in the preparation of formulations and products. The invention also relates to a wide variety of applications of the formulations of the invention. The subject invention includes novel soluble forms and various formulations of flavonoids. Further, the invention includes novel methods of manufacturing the flavonoid formulations. The invention also relates to a wide variety of applications of the flavonoid formulations.

Description

[0001] This application is a continuation of U.S. Application No. 13 / 064,882, filed April 22, 2011, a PCT application filed October 22, 2010 that has claimed priority to U.S. Application No. 61 / 253,857, filed October 22, 2009 Part continuation of / US2010 / 002821. This application is also a continuation-in-part of PCT / US2010 / 002821, filed October 22, 2010, which has claimed priority from US application 61 / 253,857, filed October 22, 2009. All of these applications are incorporated by reference in their entirety into this application. technical field [0002] The subject invention relates to novel soluble forms of planar ring-structured organic compounds including flavonoids and preparations thereof. The present invention also includes the application of these novel planar ring-structured organic compound preparations in preparation of preparations and products. The invention also relates to various uses of the formulations of the invention. Background technique [0003] fla...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K9/00A61K31/00A61Q17/04A61K8/49A61K31/353
CPCA61K8/498A61K9/0014A61K9/7023A61K31/00A61K31/353A61K2800/412A61K2800/592A61K2800/652A61Q19/00A61P17/00A61P17/06A61P17/10A61P17/14A61P17/16A61P19/02A61P31/10A61P35/00A61P37/02A61P37/06A61P43/00A61K31/7048A61K31/05
Inventor 菲利普·J·比尔巴拉
Owner API起源有限责任公司
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