Novel formulations and uses for curcuma extracts

a curcuma extract and formulation technology, applied in the field of curcuma extract formulations and uses, can solve the problems of inability to obtain the desired level of protection for consumers, fda, and the light absorption of sunscreen chemicals, and achieve the effect of enhancing the activity of compounds of interest and enhancing the activity of compounds

Inactive Publication Date: 2014-02-27
CALIFORNIA NORTHSTATE COLLEGE OF PHARMACY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0015]It should be appreciated that the term “purified” can be used to refer to an extract from a Curcuma longa plant, in some embodiments, such that the compounds of interest are isolated from the remainder of the plant in a soluble form. As such, one of skill will appreciate that the compounds of interest can sometimes be accompanied by other components of the plant that are carried along with the extract. For example, such other components can include those selected from the group consisting of hemicellulose, resins, oils, volatiles, inorganic salts, or any combination thereof. In some embodiments, the term “purified” can be used to refer to an extract consisting of, or consisting essentially of, any one or any combination of the compounds of interest. In some embodiments, the extract includes the extraction solvent. In some embodiments, an extract “consists essentially of” any one or any combination of the compounds of interest, where the presence of any other component from the plant has a negligible effect on the activity of the compounds of interest. The term “negligible effect” can be used to mean that the activity does not increase or decrease more than about 10% when compared to any one or any combination of the compounds of interest, respectively, without the other components. In some embodiments, the term “negligible effect” can be used to refer to a change of less that 10%, less than 9%, less than 8%, less than 7%, less than 6%, less than 5%, less than 4%, and less than 3%. In some embodiments, the term “negligible effect” can be used to refer to a change ranging from about 3% to about 10%, in increments of 1%. In some embodiments, the other components, for example, the hemicellulose, resins, oils, volatiles, inorganic salts, or any combination thereof, can enhance the activity of the compounds of interest. For example, the activity of the compounds of interest can be enhanced by an amount ranging from about 10% to about 300%, from about 20% to about 200%, from about 25% to about 250%, from about 30% to about 300%, from about 35% to about 275%, from about 40% to about 225%, from about 15% to about 100%, or any range therein in increments of 1%.

Problems solved by technology

A problem is that currently available sunscreen chemicals absorb light in either the UVA or UVB range.
As such, the desired level of protection for the consumer, as indicated by at least the FDA, is not readily available.
Significant problems still remain, however.
One problem is that the overlapping of peaks leaves skin exposed to weak protection in areas of the UV spectrum due to an inability to adequately overlap protection across the UV spectrum.
Another problem is that the titanium dioxide can penetrate the skin, and this makes it particularly problematic in that it can potentially convert to compounds that pose a cancer risk when exposed to the UV energy.
Extraction methods that currently exist suffer several problems.
One problem is that these methods incorporate undesirable chemicals at undesirable levels, for example, ethylene dichloride, methylene dichloride, and ethyl acetate.
Ethanol can also be used, but it can only be present to a limited extent for internal consumption, and topical application is also limited due to side effects.
As such, much effort has been spent trying to keep residual solvents below limits.
In view of at least the above, current extraction methods suffer from (i) use of toxic solvents that require steps to remove and risk the presence of toxic residuals; (ii) heating in multiple steps to extract and purify; (iii) use of a high pH up to 9.5 on Curcuma longa L., which degrades above pH 7.0; and, ipso facto (iv) multi-step processes that are complex and expensive.
There is currently no extraction process for Curcuma longa L. that uses a solvent that is suitable for both topical use and internal consumption.
A problem is that the current preparations are typically large in order to obtain a desired dosage, or multiple capsules have to be taken, resulting in an inconvenience to the consumer and, of course, non-compliance.

Method used

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  • Novel formulations and uses for curcuma extracts
  • Novel formulations and uses for curcuma extracts
  • Novel formulations and uses for curcuma extracts

Examples

Experimental program
Comparison scheme
Effect test

example 1

Extracting Curcuma longa L. Root with Ethanol

[0096]A variety of solvents may be used to extract the Curcuma longa L. root, and this example shows how the extraction can be done using ethanol.

[0097]Preparing Fresh Curcuma longa Root for Extraction

[0098]The extraction can be done with fresh Curcuma longa root, and the root can be prepared as follows:

[0099]Material

Fresh Curcuma longa root50 g

[0100]Method[0101]1. Wash the fresh root in water to remove any traces of soil or other contaminants;[0102]2. Drain to remove excess water;[0103]3. Pat dry with paper towel;[0104]4. Using a sharp knife or scapel, cut the root into pieces approximately ½″×1 / 2″; and,[0105]5. Use the moist, freshly-cut root pieces for extraction.

[0106]Preparing Dried Curcuma longa Root for Extraction

[0107]The Curcuma longa L. root may have been dried, for example, for storage. The dried root can be prepared for extraction as follows:

[0108]Material

Dried Curcuma longa root30 g

[0109]Method[0110]1. Wash the dried root in ...

example 2

Extracting Curcuma longa L. Root with Sesame Oil

[0158]The extracts removed using oils that are at least substantially non-toxic, as discussed herein, can be considered as highly favorable to those in the art, as the extracts can be included directly into topical or oral formulations without the use of additional separation steps that include, for example, removal of the extract from the extraction solvent prior to making an at least substantially non-toxic formulation for use.

[0159]Material

Prepared Curcuma longa root50 g

[0160]Method[0161]1. Transfer the prepared Curcuma longa root to a 250 mL beaker;[0162]2. Pour sesame oil into the beaker until it covers the prepared material;[0163]3. Allow to macerate for 48 hours, with mixing after 24 hours;[0164]4. Decant the clear solvent;[0165]5. Add a second amount of sesame oil to cover the prepared Curcuma longa root in the beaker;[0166]6. Allow to macerate for a further 48 hours;[0167]7. Decant the clear solvent;[0168]8. Filter the remaini...

example 3

Assessing Extraction Efficiency of Different Solvent Systems

[0171]The extraction efficacy of different solvent systems were investigated for extraction of curcumin, deoxy curcumin, bis-deoxy curcumin and possibly other curcumin derivatives and related substances (collectively “curcuminoids” hereafter) from plants of the family Zingerberaceae, especially Curcuma longa L. While not intending to be bound by any theory or mechanism of action, it may be desired to utilize the whole extract, since plant components are believed to work together to modulate component activities. Biocompatible solvents were the focus, for at least the reasons set-forth herein, including the ability to use the extract in the liquid form (including the extraction solvent) directly in pharmaceutical formulations that are at least substantially non-toxic and acceptable for human use, topically or orally.

[0172]Material

[0173]Liquid paraffin (light and heavy), glycerin, sesame oil, ethanol, cotton seed oil, polyeth...

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Abstract

Formulations and uses of extracts of Curcuma longa L. plants for safe use topically, orally, rectally, or vaginally, for example, are provided. A sunscreen containing an extract of Curcuma longa L. is provided, the sunscreen having an absorption that spans the UVA and UVB ranges in a manner that meets updated FDA recommendations without requiring the addition of titanium dioxide. A process of producing the extract is also provided, using an extraction solvent that is at least substantially non-toxic and useful also as a pharmaceutically acceptable carrier in liquid dosage forms. The extraction process also produces a significantly higher yield from a single extraction than the state-of-the-art. Liquid dosage forms can be produced directly from the extraction process without requiring removal of the extraction solvent, reducing complexity and cost of processing over the state-of-the-art. Microemulsions and nanoemulsions are also provided to enhance the bioavailability and stability of the extracts.

Description

BACKGROUND[0001]1. Field of the Invention[0002]The teachings provided herein generally relate to formulations and uses of extracts of Curcuma longa L. plants for safe use topically, orally, rectally, or vaginally, for example.[0003]2. Description of Related Art[0004]A New Use of Curcuma longa L. Extract as a Sunscreen[0005]The teachings provided herein shows that the Curcuma longa L. extract, surprisingly, has very good ultraviolet energy absorption properties across the entire wavelength range of interest, making it very attractive as a sunscreen agent. Moreover, the constituents of Curcuma longa L. have been shown to provide other therapeutic benefits. For example, antioxidant and anti-inflammatory effects have been shown, and treatments for Alzheimer's disease, Parkinson's disease, cystic fibrosis, liver injury, alcohol-induced liver disease, multiple sclerosis, human immunodeficiency virus (HIV), and cancer have been proposed. As such, the use of Curcuma longa L. extract as a su...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/12A61Q17/04A61K8/35
CPCA61K31/12A61K8/35A61Q17/04A61K36/23A61K8/9789A61K8/9794A61P17/00A61P17/02A61P17/16A61P29/00A61P3/02A61P39/06A61K2300/00
Inventor PATHER, INDIRANWOLDEMARIAM, TIBEBE ZEWDIE
Owner CALIFORNIA NORTHSTATE COLLEGE OF PHARMACY
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