A composition for male health maintenance products and its preparation method, application and product

Abstract

The application provides a composition for male health maintenance products and a preparation method, application and product thereof, and belongs to the technical field of nutritional compositions. The composition provided by the application is composed of icariin and alpha-ketoglutaric acid or alpha-ketoglutarate, the composition can significantly improve the SOD antioxidant level of the body, up-regulate testosterone and FSH, repair the hypothalamus-pituitary-gonadal axis, improve sperm density and motility, improve oligoasthenospermia, effectively relieve physical fatigue, and also assist in regulating hypogonadism and inflammation of the reproductive system; the raw materials are safe and mild, long-term use has no obvious side effects, preparation only needs simple mixing, the process is simple, the product can be processed into ordinary food, health products or oral medicine, is suitable for preparing products for resisting fatigue, improving sperm quality, regulating male sex hormones and assisting in treating reproductive related diseases, and solves the defects of single composition and poor effect of existing maintenance products.

Description

Technical Field

[0001] This invention belongs to the field of nutritional composition technology, specifically relating to a composition for men's health maintenance products, its preparation method, application, and product. Background Technology

[0002] With the fast pace of modern life, increased work pressure, and the prevalence of unhealthy lifestyles such as prolonged sitting, staying up late, irregular eating habits, and lack of exercise, men's sub-health and reproductive health problems are showing a high incidence and affecting younger people, becoming a global public health issue. Related studies show that over the past four decades, global male sperm concentration and motility have been declining continuously, while the incidence of male reproductive health diseases has been increasing year by year. This is accompanied by a series of health problems such as physical fatigue, endocrine disorders, sex hormone imbalances, hypogonadism, and chronic inflammation of the reproductive system, seriously affecting men's physiological functions, quality of life, and reproductive health, and also placing a heavy burden on family health and public health systems.

[0003] Currently, intervention methods for male physical fatigue, reproductive dysfunction, and sex hormone imbalances are mainly divided into two categories: drug intervention and nutritional conditioning. Chemical drugs are fast-acting, but they generally have drawbacks such as significant side effects, poor compatibility, unsuitability for long-term use, and a tendency to cause dependence, failing to meet the daily health maintenance needs of the general public. Meanwhile, most commercially available health products are single-nutrient products or common food-medicine homologous compound formulas, with limited components and target points, only providing simple nutritional supplementation. They cannot provide synergistic conditioning from multiple dimensions, including metabolic regulation, endocrine balance, anti-oxidative damage, and reproductive function repair, resulting in limited overall intervention effects.

[0004] Icariin, the core active flavonoid component of the traditional medicinal and edible plant Epimedium, has been proven in both traditional Chinese medicine theory and modern pharmacological research to have the effects of tonifying the kidney and replenishing essence, improving reproductive function, anti-fatigue, and regulating the body's immunity. It can effectively improve male sperm quality and regulate the hypothalamic-pituitary-gonadal axis function, making it a classic active ingredient for regulating male reproductive health. However, icariin alone has problems such as poor water solubility, low absorption and utilization rate in the body, rapid metabolism, and weak effect when used alone, making it difficult to achieve long-term and stable health maintenance effects.

[0005] Alpha-ketoglutarate is a core intermediate metabolite in the tricarboxylic acid cycle, participating in the entire process of energy metabolism, amino acid synthesis, and anti-oxidative stress. It can effectively improve the body's energy metabolism level, relieve physical fatigue, scavenge free radicals, and reduce oxidative damage. Compared with free α-ketoglutarate, its salt derivatives have the advantages of better water solubility, stronger chemical stability, and higher bioavailability in the body, and can efficiently participate in the body's metabolic regulation and improve endocrine disorders. However, there is currently no technical solution for combining α-ketoglutarate or its salts with icariin for male health maintenance, and the synergistic effect of the two active ingredients has not been developed and utilized.

[0006] In summary, existing male health care products generally suffer from technical shortcomings such as single formula, limited scope of action, poor absorption, and insignificant intervention effects. There is a lack of a multi-target, synergistic, safe, and widely applicable compound nutritional composition that can simultaneously relieve physical fatigue, repair reproductive function, regulate sex hormone levels, and improve gonadal function. Summary of the Invention

[0007] To address the above shortcomings, the present invention provides a composition for men's health maintenance products, its preparation method, application, and the product thereof.

[0008] In this invention, the term "icariin (ICA)" refers to a naturally occurring flavonoid compound, a major active ingredient in plants of the genus *Epimedium* in the Berberidaceae family, widely found in various medicinal plants such as *Epimedium brevicornu*, *Epimedium sagittatum*, *Epimedium pubescens*, and *Epimedium koreanum*. Natural sources can be extracted and isolated from the rhizomes and leaves of *Epimedium* medicinal materials. Industrially, it can be prepared through plant extraction purification, biotransformation, or semi-synthesis. In this invention, the source of icariin is not limited. Whether obtained through natural extraction, industrial purification, biotransformation, chemical synthesis, or other known methods, as long as its chemical structure is consistent with the above definition, it falls within the scope of icariin as referred to in this invention. For example, any method may yield an *Epimedium* extract containing an amount equal to the icariin of this invention. The industrial purification method for icariin described in this invention includes, but is not limited to, water extraction, alcohol extraction, ultrasound-assisted extraction, and microwave-assisted extraction. All four of these industrial purification methods can be used individually or in combination. After conventional post-processing steps such as concentration, decolorization, column chromatography, crystallization, and drying, icariin products that meet pharmaceutical or food standards can be obtained.

[0009] The term "Epimedium extract" refers to a complex mixture of crude plant extracts obtained from the dried stems, leaves, and rhizomes of medicinal plants in the genus Epimedium (Berberis family), through conventional extraction methods such as water extraction and alcohol extraction, followed by concentration and drying. This mixture is characterized by its complex composition, inconsistent proportions of components, and significant batch-to-batch variations in active substance content. Flavonoids and flavonoid glycosides are the marker components of the extract and the only category possessing reproductive regulation-related activities; however, the content of the target active monomers is low, including a low proportion of icariin, and also containing icariin I, icariin II, icariin C, icariin D, and icariin E. The extract contains icariin, icariin I, icariin II, citronellol A, citronellol B, citronellol C, citronellol A, citronellol B, citronellol C, citronellol glycoside, dehydrated icariin, as well as common flavonoids and their glycoside derivatives such as quercetin, kaempferol, luteolin, isorhamnetin, hyperoside, and rutin. The commercially available crude extract of Epimedium contains only 0.5%-5% icariin by mass, with the vast majority being heteroflavonoid isomers without specific gonadal regulatory effects. Other components include Epimedium polysaccharides, tannins, terpenes, lignans, organic acids, amino acids, inorganic impurities, and plant fibers. In this invention, it is used only as a control material, corresponding to ratio 2, compounded with α-ketoglutarate or α-ketoglutarate.

[0010] In this invention, the term "α-ketoglutarate" refers to a naturally occurring five-carbon α-keto acid with the chemical formula C5H6O5. As a core intermediate metabolite of the tricarboxylic acid cycle, it is widely present in the cellular metabolism of animals, plants, and microorganisms. Natural sources can be extracted from animal and plant tissues (such as cereal germ, animal myocardium, and liver). Industrially, it can be prepared through microbial fermentation (such as fermentation and transformation by Corynebacterium glutamicum), chemical synthesis (such as the condensation reaction of diethyl oxalate and ethyl acetate), or bio-enzymatic catalysis. In this invention, the source of α-ketoglutarate is not limited. Whether obtained through natural extraction, microbial fermentation, chemical synthesis, or other known methods, as long as its chemical structure is consistent with the above definition, it falls within the scope of α-ketoglutarate as referred to in this invention.

[0011] In this invention, the term "α-ketoglutarate" refers to a stable salt compound formed by ionic bonds between α-ketoglutarate and inorganic cations or basic amino acids. Its chemical formula uses the α-ketoglutarate anion as its core framework, forming a charge-balanced salt with the corresponding cation / amino acid cation. Its core biological activity is consistent with α-ketoglutarate, and compared to free α-ketoglutarate, it exhibits superior water solubility, stronger stability, and higher in vivo absorption and utilization efficiency, making it suitable for various formulation processes and applications in cosmetics, health products, and pharmaceuticals. The preparation of the α-ketoglutarate described in this invention is not particularly limited. It can be prepared by neutralization reaction of α-ketoglutarate with corresponding bases or basic amino acids in aqueous solution, or by existing conventional methods such as microbial fermentation or chemical synthesis. As long as it is a salt formed by α-ketoglutarate and the inorganic cations and amino acids specified in this invention, and is free of other impurities that affect the activity of the composition of this invention, it falls within the scope of the α-ketoglutarate described in this invention.

[0012] In this invention, α-ketoglutarate is divided into two main categories: inorganic acid salts and amino acid salts, specifically: Inorganic acid salts: These are salts formed by α-ketoglutarate and inorganic metal cations, including one or more of the following: calcium α-ketoglutarate, sodium α-ketoglutarate, potassium α-ketoglutarate, magnesium α-ketoglutarate, and zinc α-ketoglutarate. These salts are readily soluble in water, have simple preparation processes, and some of their cations (calcium, magnesium, zinc, and potassium) are essential mineral elements for the human body, which can form a synergistic effect of nutrition and biological activity with α-ketoglutarate. Amino acid salts refer to salts formed by α-ketoglutarate and the amino groups of basic amino acids, including one or more of α-ketoglutarate arginine salt, α-ketoglutarate ornithine salt, α-ketoglutarate lysine salt, α-ketoglutarate citrulline salt, and α-ketoglutarate histidine salt. These salts exhibit excellent biocompatibility, simultaneously releasing α-ketoglutarate and amino acids in vivo. This allows them to exert the metabolic regulatory and antioxidant effects of α-ketoglutarate while also supplementing amino acid nutrition, making them more suitable for the research and development needs of oral health supplements and injectable drugs. The α-ketoglutarate arginine salt used in this invention is also known as L-arginine-α-ketoglutarate, CAS number 16856-18-1.

[0013] The technical solution of this invention is as follows: On one hand, the present invention provides a composition comprising, by weight, 30-300 parts of icariin and 500-5000 parts of α-ketoglutarate or α-ketoglutarate.

[0014] Specifically, the composition contains, by weight, 30-35, 35-40, 40-45, 45-50, 50-55, 55-60, 60-65, 65-70, 70-75, 75-80, 80-85, 85-90, 90-95, 95-100, 100-105, 105-110, 110-115, 115-120, 120-125, 125-130, 130-135, 135-140, 140-145, 145-150, 150-155, 155-160, 160-165, 165-170 170-175, 175-180, 180-185, 185-190, 190-195, 195-200, 200-205, 205-210, 210-215, 215-220, 220-225, 225-230, 230-235, 235-240, 240-245, 245-250, 250-255, 255-260, 260-265, 265-270, 270-275, 275-280, 280-285, 285-290, 290-295 or 295-300 parts of icariin.

[0015] Preferably, the composition contains 35-40, 40-45, 45-50, 50-55, 55-60, 60-65, 65-70, 70-75, 75-80, 80-85, 85-90, 90-95 or 95-100 parts of icariin by weight.

[0016] More preferably, the composition contains 35-40, 40-45, or 45-50 parts by weight of icariin.

[0017] More preferably, the composition contains 36.5 parts by weight of icariin.

[0018] Specifically, the composition contains, by weight, 500-550, 550-600, 600-650, 650-700, 700-750, 750-800, 800-850, 850-900, 900-950, 950-1000, 1000-1050, 1050-1100, 1100-1150, 1150-1200, 1200-1250, 1250-1300, 1300-1350, 1350-1400, 1400-1450, 1450-1500, 1500-1550, 1550-1600, 1600-1650. 1650-1700, 1700-1750, 1750-1800, 1800-1850, 1850-1900, 1900-1950, 1950-2000, 2000-2050, 2050-2100, 2100-2150, 2150-2200, 2200-2250, 2250-2300, 2300-2350, 2350-2400, 2400-2450, 2450-2500, 2500-2550, 2550-2600, 2600-2650, 2650-2700, 2700-2750, 2750-280 0, 2800-2850, 2850-2900, 2900-2950, ​​2950-3000, 3000-3050, 3050-3100, 3100-3150, 3150-3200, 3200-3250, 3250-3300, 3300-3350, 3350-3400, 3400-3450, 3450-3500, 3500-3550, 3550-3600, 3600-3650, 3650-3700, 3700-3750, 3750-3800, 3800-3850, 3850-3900, 3900-3 950, 3950-4000, 4000-4050, 4050-4100, 4100-4150, 4150-4200, 4200-4250, 4250-4300, 4300-4350, 4350-4400, 4400-4450, 4450-4500, 4500-4550, 4550-4600, 4600-4650, 4650-4700, 4700-4750, 4750-4800, 4800-4850, 4850-4900, 4900-4950 or 4950-5000 parts of α-ketoglutaric acid or α-ketoglutarate.

[0019] Preferably, the composition contains, by weight, 750-800, 800-850, 850-900, 900-950, 950-1000, 1000-1050, 1050-1100, 1100-1150, 1150-1200, 1200-1250, 1250-1300, 1300-1350, or 1350-140 parts. 0, 1400-1450, 1450-1500, 1500-1550, 1550-1600, 1600-1650, 1650-1700, 1700-1750, 1750-1800, 1800-1850, 1850-1900, 1900-1950 or 1950-2000 parts of α-ketoglutaric acid or α-ketoglutarate.

[0020] More preferably, the composition contains 1000-1050, 1050-1100, 1100-1150, 1150-1200, 1200-1250, 1250-1300, 1300-1350, 1350-1400, 1400-1450, 1450-1500, 1500-1550, 1550-1600, 1600-1650, 1650-1700, 1700-1750, 1750-1800, 1800-1850, 1850-1900, 1900-1950, or 1950-2000 parts by weight of α-ketoglutaric acid or α-ketoglutarate.

[0021] More preferably, the composition contains 1000 parts by weight of α-ketoglutaric acid or α-ketoglutarate.

[0022] Specifically, the α-ketoglutarate includes one or more of pharmaceutically acceptable inorganic acid salts and amino acid salts of α-ketoglutarate.

[0023] Preferably, the inorganic acid salt includes one or more of the following: calcium α-ketoglutarate, sodium α-ketoglutarate, potassium α-ketoglutarate, magnesium α-ketoglutarate, and zinc α-ketoglutarate.

[0024] Preferably, the amino acid salt includes one or more of the following: α-ketoglutarate arginine salt, α-ketoglutarate ornithine salt, α-ketoglutarate lysine salt, α-ketoglutarate citrulline salt, and α-ketoglutarate histidine salt.

[0025] In some specific embodiments of the present invention, the inorganic acid salt is calcium α-ketoglutarate.

[0026] In some specific embodiments of the present invention, the amino acid salt is α-ketoglutarate arginine salt.

[0027] On the other hand, the present invention provides a method for preparing the composition described in any of the above claims, the method comprising mixing icariin and α-ketoglutarate or α-ketoglutarate in parts by weight until homogeneous.

[0028] In another aspect, the present invention provides the use of the composition described in any one of the above claims in the preparation of a male health maintenance product, said male health maintenance product comprising any one or more of the following: (1) Products that relieve physical fatigue; (2) Medications that improve male sperm motility; (3) Medications to improve oligospermia; (4) Medications for diseases related to regulating male sex hormone levels; (5) Medications used as adjunctive treatment for male hypogonadism; (6) Medications that help improve inflammatory diseases of the reproductive system.

[0029] In another aspect, the present invention provides a product comprising the composition described in any one of the above claims or the composition prepared by the above preparation method.

[0030] Specifically, the products also include any one or more of nutritional additives and food-medicine homologous ingredients.

[0031] Preferably, the nutritional additive includes one or more of dietary fiber, prebiotics, protein, lipids, minerals, and vitamins.

[0032] More preferably, the minerals include one or more of calcium, magnesium, zinc, selenium, potassium, iron, copper, and manganese.

[0033] Preferably, the medicinal and edible ingredients include cloves, star anise, sword bean, fennel, thistle, yam, hawthorn, purslane, black-striped snake, dried plum, papaya, hemp seed, bitter orange flower, Solomon's seal, licorice, angelica, ginkgo, white hyacinth bean, white hyacinth bean flower, longan pulp, cassia seed, lily, nutmeg, cinnamon, amla, bergamot, almond, sea buckthorn, oyster, fox nut, Sichuan pepper, red adzuki bean, donkey-hide gelatin, chicken gizzard lining, malt, kelp, jujube, monk fruit, apricot kernel, honeysuckle, green plum, houttuynia cordata, ginger, Japanese raisin tree fruit, wolfberry, gardenia, amomum villosum, sterculia lychnophora, poria cocos, citron, elsholtzia ciliata, peach kernel, mulberry. Leaves, mulberries, tangerine peel, platycodon root, alpinia oxyphylla, lotus leaves, radish seeds, lotus seeds, galangal, bamboo leaves, fermented soybean, chrysanthemum, chicory, yellow mustard seeds, polygonatum, perilla, perilla seeds, kudzu root, black sesame, black pepper, sophora japonica buds, sophora japonica flowers, dandelion, honey, torreya nuts, jujube seeds, fresh imperata root, fresh reed root, viper, tangerine peel, mint, coix seed, allium macrostemon, raspberry, patchouli, angelica, galangal, saffron, cardamom, turmeric, long pepper, codonopsis, cistanche, dendrobium officinale, American ginseng, astragalus, ganoderma, cornus officinalis, gastrodia elata, eucommia ulmoides leaves, rehmannia glutinosa, ophiopogon japonicus, asparagus cochinchinensis, and tangerine peel.

[0034] In another aspect, the present invention provides a method for maintaining male health, the method comprising using the composition or product described in any of the preceding claims.

[0035] Specifically, the method includes administering to a subject an effective amount of any of the compositions or products described above.

[0036] Preferably, the subject is a mammal.

[0037] More preferably, the subject is a human being.

[0038] The beneficial effects of this invention are as follows: The composition of the present invention combines icariin with α-ketoglutarate or its salt in a specific ratio. The two pathways complement each other and have a synergistic effect, achieving multiple physiological effects at the same time: (1) Antioxidant: Increase the level of SOD in the body, clear free radicals, and reduce oxidative stress damage to the testes and epididymis; (2) Regulate reproductive endocrine: Significantly increase serum testosterone T and follicle-stimulating hormone FSH, repair the damaged hypothalamus-pituitary-gonadal axis, and improve hypogonadism and sex hormone disorders; (3) Improve sperm quality: Increase sperm density and sperm motility, and effectively intervene in oligospermia and asthenospermia symptoms; (4) Effectively relieve physical fatigue: Prolong the sinking time and exhaustion time of weight-bearing swimming mice, and improve the body's energy supply and exercise endurance; (5) Assist in improving chronic inflammation of the reproductive system and assist in regulating hypogonadism-related diseases.

[0039] The composition of this invention has high safety and is suitable for long-term use. The formula is adaptable to various dosage forms of different products such as food, health products, and pharmaceuticals. Preparation only requires simple mixing, and the process is simple and easy to industrialize. It can be used as a basic nutritional compound raw material to develop daily care foods and functional health products for ordinary men. It can also be used to prepare drugs for adjuvant treatment of oligospermia, asthenospermia, hypogonadism, and sex hormone imbalance, thus solving the defects of existing products with single ingredients and limited effects. Attached Figure Description

[0040] Figure 1 The results show the levels of T, FSH, and SOD in serum; compared with the normal control group, ns This indicates no significant difference. p<0.05, p<0.01, p<0.0001; compared with the model control group, #ns There was no significant difference. #### p<0.0001.

[0041] Figure 2 The results show the sperm density and sperm motility measurements; compared to the normal control group, the figures in the image show... ns There was no significant difference. p<0.01, p<0.001, p<0.0001; compared with the model control group, #ns This indicates no significant difference. # p<0.05, ## p<0.01, ### p<0.001, #### p<0.0001.

[0042] Figure 3 The figures show the results of the exhaustion time and the first sinking time; compared with the normal control group, p<0.0001. Detailed Implementation

[0043] The following non-limiting embodiments are intended to enable those skilled in the art to gain a more comprehensive understanding of the present invention, but do not limit the invention in any way. The following content is merely an exemplary description of the scope of protection claimed by the present invention, and those skilled in the art can make various changes and modifications to the present invention based on the disclosed content, and such changes should also fall within the scope of protection claimed by the present invention.

[0044] The present invention will be further described below by way of specific embodiments. Unless otherwise specified, all instruments, devices, equipment, reagents, products, etc., used in the embodiments of the present invention are obtained through conventional commercial means.

[0045] Example 1 A composition for a male health maintenance product comprises 36.5 parts of icariin and 1000 parts of α-ketoglutarate, which are directly mixed to obtain the product.

[0046] Example 2 A composition for a male health maintenance product, comprising 50 parts of icariin and 2000 parts of α-ketoglutarate, obtained by directly mixing the two.

[0047] Example 3 A composition for a male health maintenance product, comprising 100 parts of icariin and 750 parts of α-ketoglutarate, obtained by directly mixing the two.

[0048] Example 4 A composition for a male health maintenance product, comprising 300 parts of icariin and 500 parts of α-ketoglutarate, obtained by directly mixing the two.

[0049] Example 5 A composition for a male health maintenance product, comprising 30 parts of icariin and 5000 parts of α-ketoglutarate, obtained by directly mixing the two.

[0050] Example 6 A composition for a male health maintenance product comprises 36.5 parts of icariin and 1000 parts of α-ketoglutarate. The α-ketoglutarate is a calcium α-ketoglutarate salt, obtained by directly mixing the two.

[0051] Example 7 A composition for a male health maintenance product comprises 36.5 parts of icariin and 1000 parts of α-ketoglutarate. The α-ketoglutarate is α-ketoglutarate arginine salt, obtained by directly mixing the two.

[0052] Comparative Example 1 A composition for a male health maintenance product, comprising 1000 parts of icariin and 36.5 parts of α-ketoglutarate, obtained by directly mixing the two.

[0053] Comparative Example 2 A composition for a male health maintenance product comprises 36.5 parts of Epimedium extract and 1000 parts of α-ketoglutarate, which are directly mixed together to obtain the product.

[0054] Comparative Example 3 A composition for a male health maintenance product, comprising 36.5 parts of icariin and 1000 parts of creatine, obtained by directly mixing the two.

[0055] Experimental Example 1 This experiment used male SPF-grade SD rats, weighing 130-150g, which were placed in an acclimatization environment for one week. During the rearing period, they were provided with normal food and free access to water. The rearing conditions were controlled at a temperature of (22 ± 2)℃, humidity of (50 ± 10)%, and a 12-hour light-dark cycle. They were randomly divided into 14 groups, including a normal control group, a model control group, Example 1-Example 7 groups, Comparative Example 1-Comparative Example 3 groups, an icariin group, and an α-ketoglutarate group, with 5 rats in each group.

[0056] Administering high doses of hydrocortisone to animals is a classic method for establishing a model of oligoasthenospermia due to kidney yang deficiency. Symptoms of oligoasthenospermia include reduced sperm count, decreased sperm motility, decreased libido, fatigue, and weakness. The model control group, Examples 1-7, Comparative Examples 1-3, α-ketoglutarate group, and icariin group were administered hydrocortisone 27 mg / kg intramuscularly daily for 21 consecutive days to construct the animal model. The normal control group received an equal volume of physiological saline as a control.

[0057] Examples 1-7 and Comparative Examples 1-3 were administered the corresponding compositions via gavage at a daily rate of 150 mg / kg. The icariin group was administered icariin via gavage at a daily rate of 150 mg / kg, and the α-ketoglutarate group was administered α-ketoglutarate via gavage at a daily rate of 150 mg / kg. Administered at fixed times daily for 4 consecutive weeks. The experimental groupings and administration details are shown in Table 1.

[0058] Table 1

[0059] Rats were fasted for 24 hours prior to the last administration but allowed free access to water. One hour after the last administration, SD rats were anesthetized with inhaled isoflurane, and samples were collected. Blood was collected from the abdominal aorta. The blood from the procoagulant collection tube was centrifuged at 4500 rpm for 5 minutes at 4°C, and the supernatant serum was separated and stored at -80°C for serum biochemical analysis. After euthanizing the rats, epididymal tissue was collected for relevant indicator examinations. Spleen tissue was collected and flash-frozen in liquid nitrogen for Western blotting.

[0060] (1) Determination of serum T, FSH and SOD levels The levels of testosterone (T), follicle-stimulating hormone (FSH), and superoxide dismutase (SOD) in rat serum were measured according to the ELISA kit instructions. The results are shown in Table 2 and... Figure 1 As shown: Table 2

[0061] Note: Compared with the normal control group, ns This indicates no significant difference. p<0.05, p<0.01, p<0.0001; compared with the model control group, #ns This indicates no significant difference. #### p<0.0001.

[0062] The results showed that, compared with the normal control group, the model control group rats exhibited significantly reduced serum testosterone (T), follicle-stimulating hormone (FSH), and antioxidant superoxide dismutase (SOD) levels after hydrocortisone modeling. This confirmed the successful establishment of the kidney-yang deficiency oligospermia model, indicating that the rats suffered from insufficient sex hormone secretion, severe oxidative stress damage, and reproductive endocrine dysfunction. The compositions of Examples 1-7 of this invention can significantly increase serum T, FSH, and SOD levels in model rats, repairing the hypothalamic-pituitary-gonadal axis endocrine function, scavenging free radicals, reducing oxidative damage to the reproductive system, and possessing multiple pharmacological activities including anti-fatigue, improved sperm quality, regulation of male sex hormones, and intervention in gonadal hypofunction.

[0063] (2) Measurement of sperm density and sperm motility Take one epididymis, cut it into small pieces, and place it in 1 mL of physiological saline at 37°C. Shake for 15 minutes. Place one drop of this liquid in a hemocytometer and count the sperm cells under a microscope to obtain the number of sperm cells per milliliter of diluted solution. Place another drop of this liquid in the hemocytometer and observe 200 sperm cells under a microscope. Record the number of motile sperm cells and grade their motility. Sperm motility is typically classified into four grades: Grade A indicates excellent motility, with rapid, straight forward movement; Grade B indicates very good motility, with straight forward movement; Grade C indicates moderate motility, with forward curved movement; and Grade D indicates poor motility, with only stationary wriggling. Calculate the sperm motility rate using the following formula.

[0064] Sperm motility rate = (a+b)×100 / 200; where a represents the number of grade a sperm and b represents the number of grade b sperm.

[0065] The measurement results are shown in Table 3 and Figure 2 As shown: Table 3

[0066] Note: Compared with the normal control group, ns There was no significant difference. p<0.01, p<0.001, p<0.0001; compared with the model control group, #ns There was no significant difference. # p<0.05, ## p<0.01, ### p<0.001, #### p<0.0001.

[0067] The results showed that, compared with the normal control group, the model control group rats, after being induced by hydrocortisone, exhibited a significant decrease in epididymal sperm count and a substantial reduction in sperm motility, confirming that the kidney yang deficiency model was accompanied by typical oligospermia and asthenospermia pathological characteristics. The composition of this invention, by enhancing the body's antioxidant levels to reduce epididymal oxidative damage and maintaining sperm motility, can simultaneously improve oligospermia and asthenospermia.

[0068] Experimental Example 2 This experiment used SPF-grade male Kunming mice, weighing 35-40g, which were placed in an acclimatization environment for one week. During this period, they were provided with normal food and free access to water. The rearing conditions were controlled at a temperature of 22 ± 2℃, humidity of 50% ± 10%, and a 12-hour light-dark cycle. For the first 3 days of the experiment, the mice were fed water once daily at a depth where their tails could not support their bodies, and a water temperature of approximately 25 ± 1℃. The mice were allowed to swim acclimatizingly without their tails bearing weight, and were removed within 5 minutes to mitigate experimental errors caused by stress. They were randomly divided into a normal control group and groups 1 through 7, with 5 mice in each group.

[0069] Groups 1-7 were administered the corresponding composition by gavage at a fixed time each day for 4 consecutive weeks. The normal control group and the model control group were given an equal volume of physiological saline. The experimental groups and administration details are shown in Table 4.

[0070] Table 4

[0071] Thirty minutes after the last administration, mice were secured to their tails with lead wire weighing approximately 5% of their body weight (2.1-2.4g). The mice were then allowed to swim in a smooth-walled swimming tank at a water temperature of 25±1℃ and a depth of 30cm. This was a weighted swimming experiment, with the water temperature and depth identical to the adaptive swimming conditions. If any mouse stopped swimming by arching its back or hovered to rest, the water around it was gently stirred with a glass rod to encourage continued swimming, avoiding direct pricking of the mouse's body. Before recording the time to exhaustion, an adaptive no-weighted swimming test was conducted for 3-5 minutes to screen out mice that could not swim, thus avoiding affecting the results. A normal control group underwent the swimming experiment without weight-bearing conditions. The time to exhaustion (from the moment of entry into the water until the mouse's nostrils sink below the surface and there is no spontaneous resurfacing within 10 seconds) and the time of first sinking were recorded for each mouse. After determination, the mice were immediately removed from the water, dried, and kept warm.

[0072] The measurement results are shown in Table 5 and Figure 3 As shown: Table 5

[0073] Note: Compared with the normal control group, #### p<0.0001; compared with the model control group, p<0.0001.

[0074] The test results showed that the weighted swimming exhaustion test is a classic in vivo model for evaluating the body's anti-fatigue and endurance capabilities. Higher values ​​for exhaustion time and first sinking time indicate a more sufficient energy supply and stronger fatigue tolerance. Compared with the normal control group, the mice in each embodiment of this invention showed a highly significant prolongation in both the first sinking time and exhaustion swimming time, indicating that the composition of this invention can significantly improve the exercise endurance of mice, delay the onset of physical fatigue, and possess excellent fatigue-relieving effects.

[0075] Finally, it should be noted that the above content is only used to illustrate the technical solution of the present invention, and is not intended to limit the scope of protection of the present invention. Simple modifications or equivalent substitutions made by those skilled in the art to the technical solution of the present invention do not depart from the essence and scope of the technical solution of the present invention.

Claims

1. A composition for use in male health maintenance products, characterized in that, The composition comprises, by weight, 30-300 parts of icariin and 500-5000 parts of α-ketoglutarate or α-ketoglutarate.

2. The composition according to claim 1, characterized in that, The composition comprises, by weight, 35-100 parts of icariin and 750-2000 parts of α-ketoglutarate or α-ketoglutarate.

3. The composition according to claim 1, characterized in that, The α-ketoglutarate includes one or more of pharmaceutically acceptable inorganic acid salts and amino acid salts of α-ketoglutarate.

4. The composition according to claim 3, characterized in that, The inorganic acid salts include one or more of the following: calcium α-ketoglutarate, sodium α-ketoglutarate, potassium α-ketoglutarate, magnesium α-ketoglutarate, and zinc α-ketoglutarate.

5. The composition according to claim 3, characterized in that, The amino acid salts include one or more of the following: α-ketoglutarate arginine salt, α-ketoglutarate ornithine salt, α-ketoglutarate lysine salt, α-ketoglutarate citrulline salt, and α-ketoglutarate histidine salt.

6. A method for preparing the composition according to any one of claims 1-5, characterized in that, The preparation method includes mixing icariin and α-ketoglutarate or α-ketoglutarate in proportion to weight.

7. The use of the composition according to any one of claims 1-5 or the composition prepared by the preparation method according to claim 6 in the preparation of male health maintenance products.

8. The application according to claim 7, characterized in that... The aforementioned male health maintenance products include any one or more of the following: (1) Products that relieve physical fatigue; (2) Medications that improve male sperm motility; (3) Medications to improve oligospermia; (4) Medications for diseases related to regulating male sex hormone levels; (5) Medications used as adjunctive treatment for male hypogonadism; (6) Medications that help improve inflammatory diseases of the reproductive system.

9. A product characterized in that, The product comprises the composition according to any one of claims 1-5 or the composition prepared by the preparation method according to claim 6.

10. The product according to claim 9, characterized in that, The products also include any one or more of the following: nutritional additives and ingredients that are both food and medicine.

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