JP-2026075037-A - Powdered preparation for improving brain function, etc., and method for manufacturing the same.

Abstract

[Problem] To provide a stabilized formulation (formulation for improving brain function, etc.) of alariadiol for use as a pharmaceutical or functional food, and a method for producing the same. [Solution] A powder formulation containing alariadiol, dextrin, and cyclodextrin. Preferably further containing high molecular weight polysaccharides. [Selection Diagram] None

Inventors

• 若山 史佳
• ワイズ 里沙
• 高橋 達治
• 小島 弘之
• 藤根 俊昭

Assignees

• 一丸ファルコス株式会社

Dates

Publication Date

20260507

Application Date

20250522

Priority Date

20241021

Claims (8)

1. A powder formulation containing alariadiol, dextrin, and cyclodextrin for improving brain function.
2. The powder formulation according to claim 1, further comprising high-molecular-weight polysaccharides.
3. The powder formulation according to claim 1 or 2, wherein the cyclodextrin is contained in an amount of 20% by mass or more relative to the total amount of the powder formulation.
4. The powder formulation according to claim 1 or 2, wherein the cyclodextrin comprises γ-cyclodextrin.
5. The powder formulation according to claim 2, wherein the high-molecular-weight polysaccharide is gum arabic or ghati gum.
6. A powder formulation according to claim 1 or 2 for stabilizing alariadiol as an active ingredient.
7. A step of mixing alariadiol, dextrin, and cyclodextrin to obtain a mixture, A step of homogenizing the aforementioned mixture to prepare an emulsified solution, The process of drying the emulsified liquid, A method for producing a powder formulation for improving brain function, including [the specified ingredient].
8. The method for producing a powder formulation according to claim 8, wherein the cyclodextrin comprises γ-cyclodextrin.

Description

An application has been submitted for an exception to the loss of novelty. This invention relates to a stabilized alariadiol-containing powder formulation for use in humans and other organisms, and to a method for producing the same. Gotu kola (Centella asiatica; also known as Centella asiatica) is a herb native to India, Indonesia, China, and Southeast Asia, and is used in Ayurveda, the traditional Indian system of medicine. It is known to have a wide range of effects, including antipyretic, analgesic, anti-inflammatory, and cognitive function-improving properties. For example, administration of gotu kola extract to rats has been reported to reduce oxidative stress and improve cognitive function, suggesting its potential as a treatment for Alzheimer's disease (see, for example, Non-Patent Document 1). Incidentally, in order to develop such active ingredients as pharmaceuticals or functional foods, it is desirable that they can be stored stably at room temperature for a certain period of time or longer. For example, a technique has been reported in which vitamins and coenzyme Q10 , which are incorporated into pharmaceuticals and foods, are encapsulated in cyclodextrin to form a powder composition in order to stabilize them (see, for example, Patent Document 1). Md Sahab Uddin et al. , Nootropic and Anti-Alzheimer’s Actions of Medicinal Plants: Molecular Insight into Therapeutic Potential to Alleviate Alzheimer's Neuropathology. Mol Neurobiol. 2019 Jul;56(7):4925-4944. Japanese Patent Publication No. 2005-2005 Figure 1 is a flow chart showing the manufacturing process of alariadiol in one embodiment.Figure 2 is a flow chart showing the process for manufacturing a powder formulation containing alariadiol.Figure 3 shows the flowchart for Test Example 5 (Human Monitor Test). The Stroop test has two purposes: "to perform an activity that fatigues the brain" and "to evaluate brain function (concentration, judgment, reaction speed) because good results were obtained." The 15 minutes of the 100-square calculation are broken down as follows: "the first 5 minutes are for multiplication, intended to confuse the brain," and the following 10 minutes are for addition, which is used as a test to evaluate brain function (concentration, calculation ability, judgment, reaction speed). This invention relates to a powder formulation containing at least alariadiol, dextrin, and cyclodextrin, and more preferably to a powder formulation further containing high molecular weight polysaccharides. The following describes the components included in a typical embodiment of the powder formulation. (Alariadiol) The formulation of this embodiment is the following formula (I): The product contains alariadiol (CAS No. 1354638-93-9), represented by formula (I), as an active ingredient. The compound represented by formula (I) above contains chiral carbon atoms at positions 3 and 8, and the double bond between carbon atoms at positions 9 and 10 has a cis (Z) conformation. Therefore, the active ingredient may be an optical isomer, a racemic mixture, and/or a geometric isomer with respect to these positions. Naturally occurring alariadiol has also been isolated from an ethanol extract of Aralia cordata leaves and has been reported to have inhibitory activity on the proliferation of human breast cancer cells (Cheng WL et al. (2011) Planta Med; 77:164-168). Alariadiol can be produced from medicinal plants such as Gotu Kola and Aralia cordata by organic solvent extraction and purification by column chromatography. Furthermore, this active ingredient may also be in the form of a salt or derivative. Examples of salts where the hydroxyl group of the compound represented by formula (I) has a suitable acidity include metal salts such as aluminum, alkali metal salts such as lithium, sodium, or potassium, alkaline earth metal salts such as calcium or magnesium, and ammonium or substituted ammonium salts, such as salts with lower alkylamines like triethylamine, hydroxyalkylamines such as 2-hydroxyethylamine, bis-(2-hydroxyethyl)-amine, or tri-(2-hydroxyethyl)-amine, or cycloalkylamines such as bicyclohexylamine, or salts with pyridine-type bases such as procaine, dibenzylpiperidine, N-benzyl-β-phenethylamine, dehydroabiethylamine, N,N'-bisdehydroabiethylamine, glucamine, N-methylglucamine, or pyridine, colidine, quinine, or quinoline. In addition, the hydroxyl group of the compound represented by formula (I) may be acylated, alkylated, phosphorylated, or boronated derivatives. Therefore, in this specification, the term "alariadiol" includes the compound represented by formula (I) above, its isomers or derivatives, or salts thereof. The amount of alariadiol in the formulation of this embodiment is not particularly limited, but it is sufficient to include an effective amount of alariadiol to exert a desired effect (for example, an effect of preventing or treating a disease or condition that exhibits impaired brain function). For example, if the entire form