Oral composition

Incorporating ornithine and/or theanine into oral compositions with Rhodiola rosea extract significantly boosts the antioxidant activity, addressing the inadequacy of existing formulations.

JP2026100474APending Publication Date: 2026-06-19KOBAYASHI PHARMA CO LTD

Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
KOBAYASHI PHARMA CO LTD
Filing Date
2024-12-09
Publication Date
2026-06-19

AI Technical Summary

Technical Problem

Existing oral compositions containing Rhodiola rosea extract do not fully enhance its expected antioxidant effect.

Method used

Incorporating ornithine and/or theanine into an oral composition with Rhodiola rosea extract to improve its antioxidant activity.

Benefits of technology

The combination of Rhodiola rosea extract with ornithine and/or theanine enhances the antioxidant effect beyond the level achieved by Rhodiola rosea extract alone.

✦ Generated by Eureka AI based on patent content.

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Abstract

The object of this disclosure is to provide an oral composition containing Rhodiola rosea extract with enhanced antioxidant activity. [Solution] By incorporating ornithine and / or theanine into an oral composition containing Rhodiola rosea extract, the antioxidant effect is improved.
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Description

Technical Field

[0001] The present disclosure relates to an oral composition containing a rhaponticum extract.

Background Art

[0002] The rhaponticum extract contains various polyphenols and is known to have antioxidant activity (Non-Patent Document 1). Furthermore, the rhaponticum extract is known to have an anti-anxiety effect, an effect of improving falling asleep and sleep maintenance, a stress-reducing effect, an effect of improving relaxation, an effect of improving performance or concentration, an effect of improving the effect of rest, and an effect of promoting fatigue recovery, and is known to be orally administrable (Patent Document 1).

Prior Art Documents

Non-Patent Documents

[0003]

Non-Patent Document 1

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] In order to enhance the effectiveness of an oral composition containing a rhaponticum extract, a formulation that further enhances its expected antioxidant effect is desired. However, such formulations have not been fully studied.

[0006] Therefore, the present disclosure aims to provide an oral composition containing Rhodiola rosea extract with improved antioxidant activity. [Means for solving the problem]

[0007] The inventors, in their diligent efforts to solve the aforementioned problems, unexpectedly discovered that the antioxidant effect is improved by incorporating ornithine and / or theanine into an oral composition containing Rhodiola rosea extract. This disclosure was completed based on this finding and further investigations.

[0008] In other words, this disclosure provides inventions in the following embodiments. Item 1. An oral composition comprising (A) Rhodiola rosea extract, and (B) ornithine, theanine, and / or salts thereof. Item 2. The oral composition according to Item 1, comprising 0.01 to 50 parts by weight of component (B) per 1 part by weight of component (A). Item 3. An oral composition according to item 1 or 2, used as an antioxidant. [Effects of the Invention]

[0009] According to this disclosure, an oral composition containing Rhodiola rosea extract with enhanced antioxidant activity is provided. [Modes for carrying out the invention]

[0010] The oral composition of this disclosure is characterized by containing (A) Rhodiola rosea extract (hereinafter also referred to as "component (A)") and (B) ornithine and / or theanine (hereinafter also referred to as "component (B)"). The oral composition of this disclosure will be described in detail below. In this disclosure, the numerical range "X~Y" refers to a range of X or more and Y or less.

[0011] (A) Rhodiola extract The oral composition of the present disclosure contains a Raffia extract as component (A). Although the Raffia extract has an antioxidant effect, the oral composition of the present disclosure exhibits an antioxidant effect at a level exceeding the antioxidant effect corresponding to the blending amount of the Raffia extract.

[0012] Raffia (Apocynum venetum L.) means a plant belonging to the family Apocynaceae. Further, examples of the part of Raffia (extraction target part) used for the preparation of the Raffia extract include the whole herb, the aerial part, the leaves, the stems, and the like. As the extraction target part, one of these extraction target parts may be used alone, or two or more thereof may be used in combination. Among these extraction target parts, from the viewpoint of the antioxidant effect, the leaves of Raffia are preferably mentioned.

[0013] Regarding the extraction treatment for obtaining the Raffia extract, any common extraction method used for the production of plant extracts may be used, and examples thereof include solvent extraction treatment, supercritical extraction treatment, steam distillation treatment, and the like. Among these, preferably, solvent extraction treatment is mentioned.

[0014] Examples of the extraction solvent used in the solvent extraction treatment include water; monohydric alcohols having 1 to 6 carbon atoms such as methanol and ethanol; polyhydric alcohols such as propylene glycol and 1,3-butylene glycol; other polar solvents such as acetone and ethyl acetate; and mixed solvents thereof. Among these extraction solvents, preferably, water, monohydric alcohol, and mixed solvents thereof are mentioned, more preferably, water, ethanol, and aqueous ethanol are mentioned, and even more preferably, aqueous ethanol is mentioned.

[0015] The solvent extraction treatment can be carried out by immersing the part of Raffia to be extracted, which has been subjected to treatments such as drying, cutting, and pulverization as necessary to enhance the extraction efficiency, in the extraction solvent and stirring as necessary. For example, the solvent extraction treatment can be carried out by immersing it in an extraction solvent having a volume 2 to 100 times the dry weight of the part of Raffia to be extracted and carrying out the treatment at, for example, 60°C or higher, preferably at the heating reflux temperature, for about 0.5 to 24 hours.

[0016] After the extraction process, the crude extract is obtained in the form of an extract solution by removing solids through solid-liquid separation. The obtained extract solution may be subjected to purification treatment by filtration treatment; various chromatographies and other adsorption treatments using columns filled with carriers such as polystyrene gel (polystyrene-divinylbenzene copolymer, etc.), ion exchange resin, activated carbon, etc., if necessary. Further, the obtained extract solution may be used as it is as a non-concentrated extract, may be subjected to a concentration step and used as a soft extract if necessary, or may be further subjected to a drying step and used as an extract powder.

[0017] The crude extract contains hyperoside and isoquercitrin, which are flavonoid compounds. Examples of the content of hyperoside per 100 parts by weight of the dry weight of the crude extract include, for example, 1 to 10 parts by weight, preferably 1.5 to 10 parts by weight, or 1.5 to 5 parts by weight. Examples of the content of isoquercitrin per 100 parts by weight of the dry weight of the crude extract include, for example, 1 to 10 parts by weight, preferably 1.5 to 10 parts by weight, or 1.5 to 5 parts by weight.

[0018] The content of the component (A) in the oral composition of the present disclosure may be appropriately set according to the degree of antioxidant effect required, but in terms of dry weight, for example, it is 15 to 40% by weight, preferably 20 to 30% by weight.

[0019] (B) Ornithine, theanine, and / or salts thereof The oral composition of the present disclosure contains ornithine, theanine, and / or their salts as the component (B). Ornithine, theanine, and their salts do not have an antioxidant effect by themselves, but in the oral composition of the present disclosure, when combined with the component (A), the antioxidant effect is improved.

[0020] Ornithine and theanine may be in the L-form or the D-form, but preferably the L-form. [[ID=2))

[0021] The salts of ornithine or theanine are not particularly limited as long as they are pharmaceutically acceptable. Examples include inorganic acid salts (such as hydrochloride, sulfate, nitrate, phosphate, etc.), organic acid salts (such as acetate, maleate, fumarate, citrate, malate, lactate, α-ketoglutarate, gluconate, caprylate, etc.), ammonium salts (such as ammonium salt, tetramethylammonium salt, etc.), and metal salts (such as alkali metal salts like sodium salt and potassium salt, alkaline earth metal salts like magnesium salt and calcium salt, aluminum salt, zinc salt, etc.). These salts may be used alone or in combination of two or more.

[0022] In the oral composition of the present disclosure, as the component (B), one kind may be selected and used from ornithine, ornithine salts, theanine, and theanine salts, or two or more kinds may be used in combination.

[0023] In the oral composition of the present disclosure, the ratio of the component (A) to the component (B) is not particularly limited and may be appropriately set according to the degree of antioxidant effect required. However, in terms of the content (total amount) of the component (B) per 1 part by weight (dry weight) of the component (A), for example, it is 0.01 to 50 parts by weight, preferably 0.05 to 10 parts by weight, more preferably 0.1 to 5 parts by weight, still more preferably 0.3 to 3 parts by weight, even more preferably 0.5 to 2 parts by weight, particularly preferably 0.5 to 1.5 parts by weight or 0.7 to 1.3 parts by weight.

[0024] The specific content of the component (B) in the oral composition of the present disclosure is determined by the content of the above-mentioned component (A) and the ratio of the component (A) and the component (B). In terms of the total amount, preferably it is 1 to 30% by weight, more preferably 10 to 27% by weight, still more preferably 15 to 25% by weight.

[0025] Other ingredients The oral compositions of this disclosure may or may not contain other nutritional and / or pharmacological components in addition to the components (A) and (B) described above. Such optional nutritional and / or pharmacological components are not particularly limited as long as they are usable in food or oral medicine, but examples include vitamins, other amino acids, minerals, carbohydrates, fatty acids, other plant extracts, other antioxidants, hypoglycemic agents, anticholinergic agents, and immunostimulants. These components may be used individually or in combination of two or more. The content of these components may be appropriately determined depending on the type of additive used or the intended use of the oral composition.

[0026] Furthermore, the oral compositions of this disclosure may or may not contain, in addition to the aforementioned components (A) and (B), a base and / or additives, as necessary, in order to prepare them into a desired formulation. Such bases and / or additives, whether present or absent, are not particularly limited as long as they are usable in food or oral pharmaceuticals, but examples include excipients, disintegrants, lubricants, binders, thickeners, monohydric alcohols with 1 to 5 carbon atoms, higher alcohols with 6 or more carbon atoms, oils and fats, water-soluble polymers, surfactants, polyhydric alcohols, pH adjusters, buffers, antioxidants, preservatives, chelating agents, water, etc. These components may be used individually or in combination of two or more. The content of these components is appropriately determined according to the type of base and / or additive used and the dosage form of the oral composition.

[0027] Dosage form / form The dosage form of the oral composition of this disclosure is not particularly limited as long as it can be taken orally, and may be solid (specifically, powder, granules, tablets, capsules, etc.), semi-solid (specifically, paste, gel, etc.), or liquid. Of these dosage forms, a solid form is preferred from the viewpoint of stability, etc.

[0028] The formulation of the oral composition of this disclosure is not particularly limited as long as it can be taken orally, and may be either food or pharmaceutical, but food is preferred. Examples of food and beverages include foods for special dietary uses and health functional foods (nutrient function foods, foods with functional claims, foods for specified health uses, etc.), and general foods (nutritional supplements, health supplements, fortified foods, nutritional adjustment foods, supplements, etc.). Food and beverages include food and beverages for human use and feed for non-human animals (livestock feed, livestock supplements, pet food, pet supplements, etc.).

[0029] Purpose The oral compositions of this disclosure can be used in applications that utilize the known effects of Rhodiola rosea extract, and / or applications that utilize the known effects of ornithine, theanine, and / or salts thereof. The oral compositions of this disclosure are preferably used as antioxidants because the combination of ornithine, theanine, and / or salts thereof provides an antioxidant effect at a level exceeding that of the amount of Rhodiola rosea extract.

[0030] More specific uses of the oral composition disclosed herein include improving sleep quality, improving satisfaction with sleep upon waking, improving sleep onset, improving sleep maintenance, anti-anxiety effects, stress reduction, improved relaxation, improved performance, improved concentration, improved rest effects, accelerated fatigue recovery, improvement of temporary mood swings before menstruation, and improvement of menstrual discomfort. [Examples]

[0031] The present disclosure will be described in detail below with reference to examples, but the present disclosure is not limited to these examples.

[0032] Following the procedure for the DPPH antioxidant capacity measurement kit (Dojin Chemical Laboratories), assay buffer (included in the kit) and DPPH (1,1-diphenyl-2-picrylhydrazyl) solution were added to a 96-well microplate. Furthermore, the components listed in Tables 1 and 2 were added to reach the final concentrations indicated. For the Rhodiola rosea extract, a dried powder (containing 2% by weight of hyperoside and 2% by weight of isoquercitrin) obtained by heating and refluxing dried Rhodiola rosea leaves with aqueous ethanol was used. Both ornithine hydrochloride and theanine were L-forms.

[0033] DPPH is a stable, purple radical compound that becomes colorless upon reduction by antioxidants. The absorbance at 517 nm (at 25°C, 30 minutes after the start of measurement) was measured using a plate reader. The radical scavenging rate was evaluated as the antioxidant activity value based on the following formula. The results are shown in Tables 1 and 2.

[0034] [ka]

[0035] [Table 1]

[0036] [Table 2]

[0037] As shown in Tables 1 and 2, neither theanine nor ornithine hydrochloride exhibited antioxidant activity (Comparative Examples 2 and 4). However, compared to the antioxidant activity of Rhodiola rosea extract alone (Comparative Examples 1 and 3), the combination of Rhodiola rosea extract with theanine or ornithine hydrochloride improved the antioxidant activity (Examples 1 and 2).

[0038] Prescription examples Tablet compositions were prepared according to the formulations shown in Table 3, and 230 mg tablets were prepared. In all cases, the inclusion of ornithine hydrochloride or theanine resulted in improved antioxidant effects.

[0039] [Table 3]

Claims

1. An oral composition comprising (A) Rhodiola rosea extract, and (B) ornithine, theanine, and / or salts thereof.

2. The oral composition according to claim 1, comprising 0.01 to 50 parts by weight of component (B) per 1 part by weight of component (A).

3. An oral composition according to claim 1 or 2, used as an antioxidant.