A functional composition and uses thereof

Abstract

This invention provides a functional composition and its application, belonging to the field of functional food technology. The functional composition of this invention comprises the following components in parts by weight: 10-25 parts of Sichuan pepper extract, 5-10 parts of Gastrodia elata extract, and 2-5 parts of saffron extract; wherein the Sichuan pepper extract contains 60%-80% total flavonoids by weight, and the total flavonoids include hyperoside at 5%-15% by weight of the Sichuan pepper extract. The functional composition of this invention not only shortens sleep latency, but more importantly, it also reduces the frequency of nighttime awakenings, effectively reducing the number of nighttime awakenings at the root cause.

Description

Technical Field

[0001] This invention relates to the field of functional food technology, and more particularly to a functional composition and its application. Background Technology

[0002] With the fast pace of modern life and increasing work pressure, sleep disorders have become a significant factor affecting people's quality of life. Insomnia is one of the most common sleep problems, with clinical symptoms including difficulty falling asleep, sleep maintenance disorders (waking up ≥2 times per night), early awakening and difficulty falling back asleep, and fatigue and poor concentration upon waking. Many factors can cause or trigger insomnia, including psychological stress, physical condition, medication effects, and mental or physical illnesses. Long-term sleep deprivation or poor sleep quality not only leads to daytime fatigue, poor concentration, and memory loss, but can also cause a series of health problems, such as weakened immunity, cardiovascular disease, and depression. Therefore, the prevention and treatment of insomnia has always been an important topic in the field of health.

[0003] The clinical manifestations of sleep disorders vary considerably among individuals. Most patients present with only a single symptom, such as difficulty falling asleep but maintaining good sleep, or falling asleep quickly but experiencing frequent awakenings at night. Furthermore, the physiological mechanisms regulating the sleep onset process and maintaining sleep state also differ: (1) the synthesis of γ-aminobutyric acid (GABA) is more strongly correlated with promoting sleep onset and shortening sleep latency; (2) increased nighttime awakenings (i.e., sleep maintenance disorders) are more closely related to the regulatory mechanisms of melatonin and cortisol. Prolonged or excessive stress can lead to chronic stress causing overactivation of the hypothalamic-pituitary-adrenal (HPA) axis, resulting in elevated cortisol levels, which in turn inhibits normal melatonin secretion, disrupts circadian rhythm stability, and leads to sleep interruption and light sleep, increasing the risk of nighttime awakenings. Therefore, it is particularly necessary to develop sleep aids with clear mechanism-specific targeting for different types of sleep disorders.

[0004] Currently, most sleep aid health foods on the market use traditional Chinese medicinal herbs such as jujube seed, poria cocos, and lily bulb as their main ingredients, and are prepared using conventional water extraction processes. While these products do have some effect on improving sleep, they still have significant limitations. On the one hand, the mechanisms of action of the raw materials used are relatively broad, and the targets are relatively dispersed, resulting in limited effectiveness in specifically improving sleep problems. Moreover, most products mainly target difficulty falling asleep, with limited effect on improving sleep maintenance disorders (nighttime awakenings). On the other hand, these products generally have a slow onset of action, poor user compliance, and are difficult to maintain for long-term use.

[0005] In existing technologies, for example, patents CN120531134A and CN118872855B disclose health food formulas containing various nutrients and traditional Chinese medicines that improve sleep. However, their technical solutions mainly focus on the problem of difficulty falling asleep or their effects are mainly reflected in shortening sleep latency, without specifically addressing the problem of high frequency of nighttime awakenings. Patent CN120437274A discloses a sleep-aiding oral liquid with jujube seed, poria cocos, and lily plant fermentation liquid as the main ingredients. Its core mechanism lies in using jujube seed saponin A combined with γ-aminobutyric acid to directly regulate the GABAergic nervous system, thereby shortening sleep latency and effectively promoting sleep. This solution also does not significantly improve the frequency of nighttime awakenings. Furthermore, patent CN114191474B describes a jujube seed and poria cocos composition that improves sleep. It has broad targets and can improve problems such as frequent awakenings at night, difficulty falling asleep, and fatigue upon waking. However, in practical applications, its ability to improve the frequency of awakenings in the middle of the night is relatively weak, and it usually requires continuous use for more than a month to be effective. Patent CN116549462A discloses a sleep-improving composition containing active ingredients such as dopamine and melatonin, which can effectively prolong deep sleep time and improve sleep disorders such as frequent awakenings and vivid dreams. However, such neuromodulatory substances carry the risk of dependence and have various side effects with long-term use. Summary of the Invention

[0006] The purpose of this invention is to overcome the shortcomings of the prior art and provide a functional composition and its application that can improve sleep quality, especially effectively reduce the number of nighttime awakenings.

[0007] To achieve the above objectives, the technical solution adopted by the present invention is as follows: In a first aspect, the present invention provides a functional composition comprising the following components in parts by weight: 10-25 parts of Sichuan pepper extract, 5-10 parts of Gastrodia elata extract, and 2-5 parts of saffron extract; wherein the Sichuan pepper extract contains 60%-80% total flavonoids by weight, and the total flavonoids contain hyperoside in 5%-15% by weight of the Sichuan pepper extract.

[0008] Studies have shown that Sichuan pepper extract can improve sleep maintenance ability; and the inventors have surprisingly discovered that when Sichuan pepper extract containing the above-mentioned specific content of total flavonoids is combined with gastrodia elata extract and saffron extract in the specific proportions of the present invention, the three can play a synergistic role, which significantly improves the sleep-improving effect of the functional composition of the present invention.

[0009] The functional composition of this invention not only shortens sleep latency, but more importantly, it also reduces the frequency of nighttime awakenings, effectively reducing the number of nighttime awakenings at the source.

[0010] In some embodiments, the Sichuan pepper extract contains 73%-75% total flavonoids by weight, and the hyperoside accounts for 8%-11% of the weight of the Sichuan pepper extract. Within this preferred range, the functional composition of the present invention is more effective in shortening sleep latency and reducing the frequency of nighttime awakenings.

[0011] In some preferred embodiments, the Sichuan pepper extract contains 75% total flavonoids by weight, and the hyperoside accounts for 11% of the weight of the Sichuan pepper extract.

[0012] In some embodiments, the preparation method of the Sichuan pepper extract includes the following steps: (1) Using Sichuan pepper as raw material, add an ethanol solution with a concentration of 70%-85% (v / v) to the Sichuan pepper for alcohol extraction to obtain an extract; (2) Concentrate the extract obtained in step (1), and then purify the concentrate by using macroporous resin. The elution solution used during purification is an ethanol solution with a concentration of 60%-70% (v / v).

[0013] In some preferred embodiments, the method for preparing the Sichuan pepper extract includes the following steps: (1) Weigh the pepper raw material, crush it, add 5-10 times the amount of 70%-85% ethanol solution according to the volume weight ratio, extract it at 70-80℃ 2-3 times, 1-2 hours each time, collect the extract, let it stand and filter, concentrate the filtrate, and freeze dry it. (2) The product freeze-dried in step (1) is purified with macroporous resin, and 60%-70% ethanol eluent is collected. The eluent is allowed to stand and filtered, the filtrate is concentrated, and freeze-dried to obtain Sichuan pepper extract.

[0014] In some embodiments, the Gastrodia elata extract contains 4%-10% by weight of 4-hydroxymethylphenyl-β-glucopyranoside. Preferably, the Gastrodia elata extract contains 8% by weight of 4-hydroxymethylphenyl-β-glucopyranoside.

[0015] In some embodiments, the saffron extract contains 0.3%-3% by weight of crocin. Preferably, the saffron extract contains 3% by weight of crocin.

[0016] In some embodiments, the functional composition comprises the following components in parts by weight: 18 parts Sichuan pepper extract, 6 parts Gastrodia elata extract, and 2 parts saffron extract. At this specific ratio, the functional composition of the present invention exhibits excellent effects in shortening sleep latency and reducing the frequency of nighttime awakenings.

[0017] In some embodiments, the functional composition further includes 5-10 parts by weight of magnesium supplementation, preferably 6 parts by weight. When magnesium supplementation is added to the extracts of Sichuan pepper, gastrodia elata, and saffron, the magnesium supplementation can soothe nerve excitability, block stress signal transmission, and synergize with these extracts to significantly improve sleep quality.

[0018] In some embodiments, the magnesium supplement is at least one of inorganic magnesium and organic magnesium acid; preferably, the inorganic magnesium is at least one of magnesium oxide, magnesium sulfate, magnesium chloride, and magnesium carbonate, and the organic magnesium acid is at least one of magnesium glycinate, magnesium citrate, magnesium lactate, and magnesium threonate. Using magnesium glycinate or magnesium threonate as the magnesium supplement not only results in high bioavailability but also enhances the sleep quality improvement effect of the functional composition of this invention.

[0019] In some embodiments, the magnesium purity in the glycine magnesium is 50%-70%.

[0020] In some embodiments, the functional composition further includes the following components in parts by weight: 2-5 parts 5-hydroxytryptophan, 0.05-0.2 parts vitamin B5, and 0.03-0.1 parts vitamin B6. 5-hydroxytryptophan, as a precursor for endogenous melatonin synthesis, works synergistically with vitamin B6 and vitamin B5 to provide raw materials for the melatonin synthesis pathway, effectively supplementing melatonin deficiency caused by factors such as circadian rhythm disorders, and achieving the effect of rapidly improving sleep and inhibiting wakefulness.

[0021] In some preferred embodiments, the functional composition contains 2 parts by weight of 5-hydroxytryptophan, 0.2 parts by weight of vitamin B5, and 0.1 parts by weight of vitamin B6.

[0022] In some embodiments, the purity of the 5-hydroxytryptophan is 96%-99%, the purity of the vitamin B5 is 96%-99%, and the purity of the vitamin B6 is 96%-99%.

[0023] In some embodiments, the functional composition comprises the following components in parts by weight: 10-25 parts of Sichuan pepper extract, 5-10 parts of Gastrodia elata extract, 2-5 parts of saffron extract, 5-10 parts of magnesium supplement, 2-5 parts of 5-hydroxytryptophan, 0.05-0.2 parts of vitamin B5, and 0.03-0.1 parts of vitamin B6; the Sichuan pepper extract contains 60%-80% total flavonoids by weight, and the total flavonoids include 5%-15% hyperoside (i.e., quercetin-3-O-β-D-galactopyranoside) by weight of the Sichuan pepper extract; the Gastrodia elata extract contains 4%-10% 4-hydroxymethylphenyl-β-glucopyranoside by weight; the saffron extract contains 0.3%-3% crocin by weight; and the organic magnesium acid is at least one of magnesium glycine and magnesium threonate.

[0024] In a preferred embodiment, the functional composition comprises the following components in parts by weight: 18 parts Sichuan pepper extract, 6 parts Gastrodia elata extract, 2 parts saffron extract, 6 parts magnesium supplement, 2 parts 5-hydroxytryptophan, 0.2 parts vitamin B5, and 0.1 parts vitamin B6. At this ratio, the functional composition of the present invention exhibits optimal effects in shortening sleep latency and reducing the frequency of nighttime awakenings.

[0025] The preparation method of the functional composition of the present invention includes the following steps: mixing the components of the functional composition according to the specified proportions. For example, the functional composition of the present invention is prepared using the following preparation method: (1) Mix the pepper extract, gastrodia extract and saffron extract in the prescribed amounts evenly, and pass them through a 60-100 mesh sieve to obtain mixed powder A; (2) Take the prescribed amounts of 5-hydroxytryptophan, vitamin B6, vitamin B5 and magnesium supplement, mix them, and pass them through a 100-200 mesh sieve to obtain mixed powder B; (3) Mix the obtained mixed powder A and mixed powder B thoroughly and stir evenly to obtain a functional composition.

[0026] Secondly, the present invention provides the use of the above-described functional composition in improving sleep quality or in the preparation of products that improve sleep quality.

[0027] In some embodiments, the product for improving sleep quality is a functional food.

[0028] In some embodiments, the functional composition is used to shorten sleep latency and / or reduce nighttime awakening frequency, or to prepare products that shorten sleep latency and / or reduce nighttime awakening frequency.

[0029] Thirdly, the present invention provides a functional food comprising the above-mentioned functional composition.

[0030] In some embodiments, the dosage form of the functional food is capsules, tablets, or granules.

[0031] Fourthly, the present invention provides the use of (a) the above-described functional composition or the above-described functional food in combination with (b) a melatonin preparation for improving sleep quality or in the preparation of a combination product for improving sleep quality.

[0032] Melatonin reduces cortisol secretion by inhibiting the stress response of the HPA axis. In normal individuals, endogenous melatonin peaks between 2 and 3 a.m. Orally administered melatonin reaches peak plasma concentration 20-30 minutes after administration and remains elevated for approximately 90 minutes. Melatonin formulations using sustained-release technology can replenish melatonin levels during the night, preventing sleep disruption caused by the decline in its secretion.

[0033] The functional composition of this invention uses Sichuan pepper extract as the main functional ingredient, supplemented with various medicinal and edible raw materials and nutritional supplements. While its onset of action is relatively slow, it can fundamentally regulate the sleep maintenance mechanism, reduce the number of nighttime awakenings, and help alleviate anxiety and tension, thereby improving morning mental state. The melatonin preparation, with melatonin as the main functional ingredient, can take effect rapidly and works synergistically with the functional composition of this invention in the initial stage to achieve a comprehensive effect of improving sleep and inhibiting awakenings.

[0034] Additionally, (a) the above-mentioned functional composition or the above-mentioned functional food and (b) melatonin preparation can be formulated into various oral preparations for combined use.

[0035] In some embodiments, the (a) functional composition or the functional food described above is used in combination with (b) a melatonin preparation to shorten sleep latency and / or reduce the frequency of nighttime awakenings, or a combined product for shortening sleep latency and / or reducing the frequency of nighttime awakenings is prepared.

[0036] In some embodiments, the method of combining (a) the functional composition or the functional food with (b) the melatonin preparation is as follows: first, (a) the functional composition or the functional food is taken together with (b) the melatonin preparation (e.g., both are taken together for 7-20 days), and then (a) the functional composition or the functional food is taken alone in subsequent stages. Preferably, the frequency of administration is once daily.

[0037] Melatonin preparations are intended for short-term use only, aiming to quickly establish a sleep rhythm while avoiding user dependence and reducing the risk of side effects that may result from long-term use of exogenous melatonin.

[0038] In some embodiments, the method of combining (a) the functional composition or the functional food with (b) the melatonin preparation is as follows: first, (a) the functional composition or the functional food is taken together with (b) the melatonin preparation for 14 days, and then (a) the functional composition or the functional food is taken alone once daily. Preferably, the time of administration is before bedtime, for example, between 9 and 10 pm.

[0039] In some embodiments, the melatonin formulation is a melatonin sustained-release formulation.

[0040] In some embodiments, the melatonin formulation comprises the following components in parts by weight: 0.03-0.1 parts melatonin, 0.09-0.2 parts β-cyclodextrin, and 0.1-0.25 parts hydroxypropyl methylcellulose.

[0041] Fifthly, the present invention provides a combination product for improving sleep quality, comprising: (a) the above-mentioned functional composition or the above-mentioned functional food; and (b) Melatonin preparations.

[0042] In some embodiments, the melatonin formulation is a melatonin sustained-release formulation.

[0043] In some embodiments, the melatonin formulation comprises the following components in parts by weight: 0.03-0.1 parts melatonin, 0.09-0.2 parts β-cyclodextrin, and 0.1-0.25 parts hydroxypropyl methylcellulose.

[0044] In a preferred embodiment, the melatonin preparation comprises the following components in parts by weight: 0.06 parts melatonin, 0.12 parts β-cyclodextrin, and 0.18 parts hydroxypropyl methylcellulose.

[0045] In some embodiments, the hydroxypropyl methylcellulose contains 27%-30% methoxy groups and 7%-10.5% hydroxypropoxy groups by mass. Preferably, the hydroxypropyl methylcellulose contains 28% methoxy groups and 8.5% hydroxypropoxy groups by mass.

[0046] In some embodiments, the melatonin formulation exhibits a release rate of 40-50% after 4-5 hours of administration and an 85% release rate after 7-8 hours. Preferably, the melatonin formulation exhibits a release rate of 45% after 4 hours of administration and an 85% release rate after 7 hours.

[0047] In some embodiments, the melatonin formulation is in the form of capsules, tablets, or granules.

[0048] In some embodiments, the functional composition or the functional food is in the form of capsules, tablets or granules.

[0049] Compared with the prior art, the beneficial effects of the present invention are as follows: In light of the current lack of sleep aids for improving sleep maintenance disorders, this invention provides a functional composition that improves sleep quality, shortens sleep latency, and effectively reduces the number of nighttime awakenings at the root cause. This functional composition enhances the safety, effectiveness, and durability of the product, while reducing dependence and side effects.

[0050] The present invention further combines the above-mentioned functional composition with a melatonin preparation, and the two work synergistically to achieve the comprehensive effect of improving sleep and inhibiting wakefulness.

[0051] This invention addresses the shortcomings of existing technologies in improving nighttime sleep maintenance disorders, such as insufficient effectiveness, slow onset of action, and high risk, and has significant practical implications and necessity for application. Detailed Implementation

[0052] To make the objectives, technical solutions, and advantages of this invention clearer, the technical solutions of this invention will be clearly and completely described below. Obviously, the described embodiments are only some embodiments of this invention, not all embodiments. Based on the embodiments of this invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of this invention.

[0053] In the following examples and comparative examples, both the Gastrodia elata extract and the saffron extract are commercially available. Specific purchase information is as follows: Gastrodia elata extract: The manufacturer was Xi'an Tianguangyuan Biotechnology Co., Ltd. In Examples 1-13 and Comparative Examples 1-8, the specification was: gastrodin ≥5%; in Example 14, the specification was: gastrodin 4%; in Example 15, the specification was: gastrodin ≥10%.

[0054] Saffron extract: Purchased from Shaanxi Jiahe Biotechnology Co., Ltd. In Examples 1-13 and Comparative Examples 1-8, the specification was: crocin ≥3%; in Example 14, the specification was: crocin 0.3%; in Example 15, the specification was: crocin ≥2%.

[0055] Example 1 One embodiment of the functional composition of the present invention is shown in Table 1.

[0056] In this embodiment, the Sichuan pepper extract contains 75% total flavonoids by weight, and the total flavonoids include hyperoside at 11% by weight of the Sichuan pepper extract; the gastrodia extract contains 8% 4-hydroxymethylphenyl-β-glucopyranoside by weight; the saffron extract contains 3% crocin by weight; and the magnesium supplement is magnesium glycine.

[0057] In this embodiment, the preparation method of Sichuan pepper extract is as follows: Sichuan pepper raw material is taken, washed, dried, and pulverized. An 80% (v / v) ethanol solution is added at a material-to-liquid ratio of 1:10, and extraction is performed at 80°C in a constant temperature water bath for 3 extractions, each lasting 1 hour. The extracts are combined, allowed to stand, filtered, and the filtrate is collected and concentrated. After freeze-drying, the extract is purified using a D161 macroporous adsorption resin with 70% ethanol solution as the eluent. The eluent fraction is collected, concentrated, freeze-dried, and pulverized to obtain the Sichuan pepper extract. The total flavonoids in this extract are 75% by mass, and hyperoside is 11% by mass.

[0058] The preparation method of the functional composition in this embodiment is as follows: Mix all components in the formulated functional composition evenly and pass through a 100-mesh sieve to obtain the functional composition.

[0059] Furthermore, the above-mentioned functional composition is encapsulated to obtain a capsule dosage form product.

[0060] Examples 2-10 and Comparative Examples 1-7 The component compositions of the functional compositions of Examples 2-10 and Comparative Examples 1-7 are shown in Table 1. The Sichuan pepper extract, Gastrodia elata extract, and saffron extract used in the functional compositions of Examples 2-10 and Comparative Examples 1-7, as well as their preparation methods, are the same as in Example 1.

[0061] The functional compositions and their capsule formulations in Examples 2-10 and Comparative Examples 1-7 were prepared according to the preparation method of Example 1.

[0062] Table 1

[0063] Examples 11-15 Examples 11-15: The functional compositions consist of the following components in parts by weight: 18 parts of Sichuan pepper extract, 6 parts of Gastrodia elata extract, 2 parts of saffron extract, 6 parts of magnesium supplement, 2 parts of 5-hydroxytryptophan, 0.2 parts of vitamin B5, and 0.05 parts of vitamin B6. The contents of total flavonoids and hyperoside in Sichuan pepper extract, the contents of 4-hydroxymethylphenyl-β-glucopyranoside in Gastrodia elata extract, and the contents of crocin in saffron extract are shown in Table 2 below.

[0064] Table 2

[0065] In Example 11, the preparation method of Sichuan pepper extract differs from that in Example 1 in that: (1) the extraction conditions are as follows: 75% ethanol solution is added at a material-to-liquid ratio of 1:8, and the extraction is carried out at 75°C for 3 times, each time for 2 hours; (2) 65% ethanol solution is used as the eluent during purification. All other operations are the same as the preparation method of Sichuan pepper extract in Example 1.

[0066] In Example 12, the preparation method of Sichuan pepper extract differs from that in Example 1 in that: (1) the extraction conditions are as follows: add 70% ethanol solution at a material-to-liquid ratio of 1:5, and extract twice at 70°C for 1 hour each time; (2) 60% ethanol solution is used as the eluent during purification. All other operations are the same as the preparation method of Sichuan pepper extract in Example 1.

[0067] In Example 13, the preparation method of the Sichuan pepper extract differs from that in Example 1 in that the extraction conditions are as follows: an 85% ethanol solution is added at a material-to-liquid ratio of 1:10, and the extraction is carried out at 80°C for 3 times, 2 hours each time. All other operations are the same as those in Example 1.

[0068] In Examples 14 and 15, the preparation method of the Sichuan pepper extract is the same as in Example 1.

[0069] The functional compositions and their capsule formulations in Examples 11-15 were prepared according to the method in Example 1.

[0070] Comparative Example 8 The functional composition of Comparative Example 8 differs from that of Example 7 only in that 5-hydroxytryptophan is replaced with tryptophan, otherwise it is the same as Example 7.

[0071] Comparative Example 8: The functional composition and its capsule formulation were prepared according to the preparation method of Example 1.

[0072] Experimental Example This experimental example tests the effects of the products prepared in the above embodiments and comparative examples.

[0073] According to the "Methods for Functional Testing and Evaluation of Health Foods (2023 Edition)," this experiment verified the sleep-improving effect of the test substance on C57BL / 6J mice by observing its effects on direct sleep, pentobarbital-induced sleep duration prolongation, subthreshold dose pentobarbital-induced sleep onset rate, and pentobarbital-induced sleep latency. Details are as follows: Experimental animals: 1080 SPF-grade male C57BL / 6J mice (purchased from Spiford (Beijing) Biotechnology Co., Ltd.), 270 mice each for direct sleep experiment, prolonged sodium pentobarbital sleep time experiment, subthreshold dose sodium pentobarbital hypnosis experiment, and sodium barbital sleep latency experiment), weighing 18-22g. Animal housing environment: temperature 23±2℃, humidity 30%-70%, alternating light and dark for 12 hours daily, with free access to water. After 5 days of acclimatization, mice in each experimental group were randomly divided into a negative control group and experimental groups, with 10 mice in each group. The negative control group was administered physiological saline by gavage at 10 mL / kg BW. Each experimental group was administered a solution prepared from the contents of the capsules obtained in Examples 1-15 + melatonin preparation A, Example 7 + melatonin preparation B, Example 7 + melatonin preparation C, Comparative Examples 1-8 + melatonin preparation A, and Example 7 + melatonin preparation D by gavage at 10 mL / kg BW. This was done once daily for 30 consecutive days, with relevant indicators measured at the end of the administration. The composition of the melatonin capsule formulation is as follows: Melatonin Formulation A: 0.06 parts by weight of melatonin, 0.12 parts by weight of β-cyclodextrin, and 0.18 parts by weight of hydroxypropyl methylcellulose. The preparation method of Melatonin Formulation A is as follows: Take the components in the prescribed amounts, mix them, dry them, and pass them through a 100-200 mesh sieve to obtain the melatonin formulation; encapsulate the melatonin formulation to obtain the capsule dosage form product of the melatonin formulation.

[0074] Melatonin formulation B: 0.03 parts by weight of melatonin, 0.09 parts by weight of β-cyclodextrin and 0.1 parts by weight of hydroxypropyl methylcellulose, prepared in the same way as melatonin formulation A.

[0075] Melatonin preparation C: 0.1 parts by weight of melatonin, 0.2 parts by weight of β-cyclodextrin and 0.25 parts by weight of hydroxypropyl methylcellulose, prepared in the same way as melatonin preparation A.

[0076] Melatonin preparation D: 0.06 parts by weight of melatonin and 0.12 parts by weight of β-cyclodextrin, prepared in the same way as melatonin preparation A.

[0077] In the above-mentioned melatonin preparations A, B, C, and D, the methoxy group content of hydroxypropyl methylcellulose is 28%, and the hydroxypropoxy group content is 8.5%.

[0078] Direct sleep experiment: Twenty minutes after the last administration of the test substance, the mice were turned over, and the righting reflex was observed to determine whether they had fallen asleep. Sleep was defined as the disappearance of the righting reflex. When a mouse was placed in a dorsal position, it should be able to immediately right itself. If it could not right itself within 30-60 seconds, the righting reflex was considered to have disappeared, and the mouse had entered sleep. The recovery of the righting reflex was considered awakening. The period from the disappearance to the recovery of the righting reflex was the animal's sleep time. The number of animals falling asleep and the sleep time were recorded in the negative control group and the drug-treated group. The experimental results are shown in Table 3.

[0079] Experiment to prolong pentobarbital sodium sleep time: Two hours after the last administration of the test substance to mice, 45 mg / kg of pentobarbital sodium was injected intraperitoneally (0.2 mL / 20 g). The disappearance of the righting reflex was used as an indicator to observe whether the test substance could prolong pentobarbital sodium sleep time. The experimental results are shown in Table 4.

[0080] Subthreshold dose-induced hypnosis experiment with sodium pentobarbital: Two hours after the last administration of the test substance to mice, 30 mg / kg of sodium pentobarbital was injected intraperitoneally (0.2 mL / 20 g). The number of mice falling asleep within 30 minutes was recorded, and the incidence of falling asleep was calculated. The experimental results are shown in Table 5.

[0081] Sodium barbital sleep latency test: 20 minutes after the last administration of sodium barbital, mice in each group were intraperitoneally injected with 200 mg / kg sodium barbital (injection volume 0.2 mL / 20 g). The effect of the test substance on the sleep latency of sodium barbital was observed and recorded using the disappearance of the righting reflex as an indicator. The experimental results are shown in Table 6.

[0082] Table 3 Results of the direct sleep experiment in mice

[0083] As shown in Table 3, after 30 days of oral administration, neither the negative control group nor the administered group experienced direct sleep. This indicates that the mice did not develop dependence on the functional composition of this invention or the melatonin preparation.

[0084] Table 4. Results of experiments prolonging sodium pentobarbital sleep time

[0085] Different letters indicate significant differences between groups (p < 0.05).

[0086] Table 5 Results of subthreshold dose hypnotic experiments with sodium pentobarbital

[0087] Different letters indicate significant differences between groups (p < 0.05).

[0088] Table 6 Results of the sodium barbital sleep latency experiment

[0089] Different letters indicate significant differences between groups (p < 0.05).

[0090] As shown in Tables 4, 5, and 6, the experimental results indicate that: ① Compared with Comparative Examples 1, 2, and 3, Example 2 further increased the sleep duration of mice by combining Sichuan pepper extract, Gastrodia elata extract, and saffron extract; and Comparative Examples 1, 2, and 3 all lacked one extract compared with Example 2, resulting in a sharp decrease in the sleep duration of mice, indicating that Sichuan pepper extract, Gastrodia elata extract, and saffron extract have a synergistic effect.

[0091] ② Based on the effects of using the functional compositions of Examples 2-7, Examples 9 and 10, and Comparative Example 7 in combination with melatonin preparation A, it is evident that when the functional composition of the present invention is composed of the following components in parts by weight: 10-25 parts of Sichuan pepper extract, 5-10 parts of Gastrodia elata extract, 2-5 parts of saffron extract, 5-10 parts of magnesium supplement, 2-5 parts of 5-hydroxytryptophan, 0.05-0.2 parts of vitamin B5, and 0.03-0.1 parts of vitamin B6, it not only shortens sleep latency but also reduces the frequency of nighttime awakenings, effectively reducing the number of nighttime awakenings from the root cause. In particular, when the functional composition is composed of the following components in parts by weight: 18 parts of Sichuan pepper extract, 6 parts of Gastrodia elata extract, 2 parts of saffron extract, 6 parts of magnesium supplement, 2 parts of 5-hydroxytryptophan, 0.2 parts of vitamin B5, and 0.05 parts of vitamin B6, its effect in shortening sleep latency and reducing the frequency of nighttime awakenings is optimal.

[0092] ③ Comparing the effects of using the functional compositions of Example 2, Example 8 and Comparative Example 5 together with melatonin preparation A, it is shown that magnesium supplementation is beneficial to the improvement of sleep quality by the functional compositions of the present invention.

[0093] ④ Comparing Example 2, Example 8 and Comparative Example 6, it is shown that 5-hydroxytryptophan, vitamin B5 and vitamin B6 can significantly and rapidly improve sleep and inhibit wakefulness.

[0094] ⑤ Comparing the effects of using the functional compositions of Comparative Example 8 and Example 7 together with melatonin preparation A, it can be seen that 5-hydroxytryptophan in the functional compositions of the present invention cannot be replaced by other substances.

[0095] Experiment Example 2: Human Trial Verification Experiment To assess the efficacy of capsule formulations of the functional compositions obtained in Examples 1-15 and Comparative Examples 1-8 of this invention in improving nighttime awakening frequency, a self-assessment test was conducted on 560 individuals aged 40-65 years who did not have difficulty falling asleep but had long-term nighttime awakening symptoms. These individuals were randomly divided into 28 groups of 20 each. Each group took either capsule formulation A (from Examples 1-15 and Comparative Examples 1-8) or melatonin formulation for two weeks, followed by one week of taking capsule formulations of the functional compositions obtained in Examples 1-15 and Comparative Examples 1-8 alone, once daily. The capsules were taken half an hour before 10 PM each night with warm water. No other medications were taken during the test period or in the two weeks prior to and following the test.

[0096] The efficacy evaluation criteria were formulated with reference to the "Guiding Principles for Clinical Research of New Traditional Chinese Medicine Drugs," employing a three-level evaluation standard. **Marked Effect:** A significant reduction in the frequency of nighttime awakenings per week (reduction ≥3 nights) or a significant reduction in the frequency of nighttime awakenings per day (reduction ≥3 times); **Effective (Improved):** A reduction in the frequency of nighttime awakenings per week (reduction 1-2 nights) or a significant reduction in the frequency of nighttime awakenings per day (reduction 1-2 times); **Ineffective:** No reduction in the frequency of nighttime awakenings per week or no reduction in the frequency of nighttime awakenings per day. The percentage of participants at each level was statistically analyzed, and the results are shown in Table 7 below.

[0097] Table 7. Percentage of people at each level in the examples and comparative examples

[0098] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention, and not to limit them; although the present invention has been described in detail with reference to the foregoing embodiments, those skilled in the art should understand that modifications can still be made to the technical solutions described in the foregoing embodiments, or equivalent substitutions can be made to some of the technical features; and these modifications or substitutions do not cause the essence of the corresponding technical solutions to deviate from the spirit and scope of the technical solutions of the embodiments of the present invention.

Claims

1. A functional composition, characterized in that, The product comprises the following components in parts by weight: 10-25 parts of Sichuan pepper extract, 5-10 parts of gastrodia elata extract, and 2-5 parts of saffron extract; wherein the Sichuan pepper extract contains 60%-80% total flavonoids by weight, and the total flavonoids contain 5%-15% hyperoside by weight of the Sichuan pepper extract. Preferably, the Sichuan pepper extract contains 73%-75% total flavonoids by weight, and the hyperoside accounts for 8%-11% of the weight of the Sichuan pepper extract.

2. The functional composition according to claim 1, characterized in that, The preparation method of the Sichuan pepper extract includes the following steps: (1) Using Sichuan pepper as raw material, add an ethanol solution with a concentration of 70%-85% (v / v) to the Sichuan pepper for alcohol extraction to obtain an extract; (2) Concentrate the extract obtained in step (1), and then purify the concentrate by using macroporous resin. The elution solution used during purification is an ethanol solution with a concentration of 60%-70% (v / v).

3. The functional composition according to claim 1 or 2, characterized in that, The Gastrodia elata extract contains 4%-10% by weight of 4-hydroxymethylphenyl-β-glucopyranoside; And / or, the saffron extract contains 0.3%-3% crocin by weight.

4. The functional composition according to any one of claims 1-3, characterized in that, The functional composition also includes 5-10 parts by weight of magnesium supplement; Preferably, the magnesium supplement is at least one of inorganic magnesium and organic magnesium acid; more preferably, the inorganic magnesium is at least one of magnesium oxide, magnesium sulfate, magnesium chloride, and magnesium carbonate, and the organic magnesium acid is at least one of magnesium glycine, magnesium citrate, magnesium lactate, and magnesium threonate.

5. The functional composition according to claim 4, characterized in that, The functional composition further includes the following components in parts by weight: 2-5 parts of 5-hydroxytryptophan, 0.05-0.2 parts of vitamin B5, and 0.03-0.1 parts of vitamin B6.

6. The use of the functional composition according to any one of claims 1-5 in the preparation of a product for improving sleep quality; preferably, the functional composition is used to prepare a product for shortening sleep latency and / or reducing the frequency of nighttime awakenings.

7. A functional food, characterized in that, Includes the functional composition according to any one of claims 1-5; preferably, the dosage form of the functional food is capsules, tablets or granules.

8. The use of the functional composition of any one of claims 1-5 or the functional food of claim 7 in combination with a melatonin preparation in the preparation of a combined product for improving sleep quality; preferably, the melatonin preparation comprises the following components in parts by weight: 0.03-0.1 parts melatonin, 0.09-0.2 parts β-cyclodextrin, and 0.1-0.25 parts hydroxypropyl methylcellulose.

9. The application according to claim 8, characterized in that, The functional composition or functional food is combined with melatonin preparations to prepare a combination product for shortening sleep latency and / or reducing the frequency of nighttime awakenings.

10. A combination product for improving sleep quality, characterized in that, include: (a) The functional composition according to any one of claims 1-5 or the functional food according to claim 7; as well as (b) Melatonin preparations; Preferably, the melatonin preparation comprises the following components in parts by weight: 0.03-0.1 parts melatonin, 0.09-0.2 parts β-cyclodextrin, and 0.1-0.25 parts hydroxypropyl methylcellulose.

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