Composition containing D-chiro-inositol as well as preparation method and application thereof

Abstract

The invention discloses a composition containing D-chiro-inositol as well as a preparation method and application of the composition. The composition comprises D-chiro-inositol, Myo-inositol and microcapsule powder, wherein the wall material of the microcapsule powder consists of anhydride modified edible protein and a polysaccharide compound; the edible protein is selected from at least one of spirulina protein, quinoa protein, whey protein and soybean protein; the polysaccharide compound comprises at least one of fucoidin and larch arabinogalactan. Active components are also embedded in the microcapsule powder, and comprise at least one of Omega-3, coenzyme Q10, astaxanthin and vitamin. According to the composition, the stability and bioavailability of fat-soluble active ingredients are improved through microencapsulation, and the composition has a synergistic effect with components such as D-chiro-inositol and Myoinositol, so that insulin resistance is effectively improved, female hormone balance is adjusted, and polycystic ovarian syndrome is improved. The process is simple, is suitable for large-scale production, and can be widely applied to dietary supplements or functional foods.

Description

Technical Field

[0001] This invention relates to the field of pharmaceutical technology, specifically to a composition containing D-chiral inositol, its preparation method, and its application. Background Technology

[0002] D-chiroinositol, a key mediator in the insulin signaling pathway, has been extensively studied and its significant effects in improving insulin resistance, regulating blood glucose, and alleviating symptoms associated with polycystic ovary syndrome (PCOS) have been confirmed. Clinical data show that plasma D-chiroinositol levels in PCOS patients are significantly lower than in healthy individuals, and their urinary clearance is increased, which is closely related to the degree of insulin resistance. Myo-inositol (MI) also participates in insulin signaling and follicle development regulation. The two are often used in combination in a certain ratio to synergistically improve insulin sensitivity, regulate sex hormone balance, and support ovulation. Currently, various dietary supplements containing D-chiroinositol and MI are available on the market, but most of them are in a simple physical mixture form.

[0003] In compound formulations targeting PCOS and metabolic syndrome, fat-soluble active ingredients such as Omega-3 (DHA / EPA), coenzyme Q10, astaxanthin, and fat-soluble vitamins are often incorporated to exert anti-inflammatory, antioxidant, and metabolic support effects. However, these ingredients are highly susceptible to oxidation, isomerization, or degradation during processing, storage, and oral administration due to factors such as light, oxygen, heat, and metal ions, leading to decreased potency, unpleasant flavors, and even harmful byproducts. Furthermore, direct mixing of fat-soluble ingredients with hydrophilic components (such as inositol, minerals, and plant extracts) can easily result in uneven dispersion, oil seepage, and clumping, affecting the uniformity, taste, and long-term stability of the formulation, thus limiting its clinical efficacy and commercial potential.

[0004] To improve the stability of lipid-soluble active ingredients, microencapsulation technology has been introduced into the fields of functional foods and formulations. Commonly used wall materials include proteins and polysaccharides, but their encapsulation efficiency, interfacial stability, and adaptability in complex formulations for multi-component lipid-soluble systems still need improvement. Especially for compound formulations targeting chronic metabolic disorders such as PCOS, the wall material needs to not only protect the active ingredient but also form a temporal synergistic effect with insulin-sensitizing components such as D-chiral inositol / MI in terms of release and absorption, thereby exerting a systemic regulatory effect in vivo. Therefore, developing a composition containing D-chiral inositol that can simultaneously improve the stability of the active ingredient, enhance component compatibility, and synergistically exert a metabolic regulatory effect has significant application value and market prospects. Summary of the Invention

[0005] In view of the shortcomings of the prior art, the present invention provides a composition containing D-chiral inositol, its preparation method and application.

[0006] To solve the above-mentioned technical problems, the technical solution adopted by the present invention is as follows: A composition containing D-chiral inositol, comprising D-chiral inositol, Myo-inositol, and microcapsule powder, wherein the wall material of the microcapsule powder is composed of anhydride-modified edible protein and polysaccharide compound, wherein the edible protein includes at least one selected from spirulina protein, quinoa protein, whey protein, and soy protein; and the polysaccharide compound includes at least one selected from fucoidan and larch arabinogalactan.

[0007] Preferably, the microcapsule powder further contains active ingredients embedded in the wall material, the active ingredients including at least one of Omega-3, coenzyme Q10, astaxanthin and vitamins.

[0008] Omega-3, coenzyme Q10, astaxanthin, and fat-soluble vitamins are typical fat-soluble / oil-soluble active ingredients, which are susceptible to oxidative degradation or isomerization due to factors such as oxygen, light, heat, and metal ions. Furthermore, in powder systems, they are prone to moisture absorption and clumping, migration and oil seepage, and accelerated deterioration due to contact with other components. Simultaneously, as oil-phase or hydrophobic solids, direct blending with hydrophilic powders such as Myo-inositol, D-chiral inositol, and mineral salts / plant extracts can easily lead to uneven dispersion and localized enrichment, resulting in fluctuations in single-bag dosage, decrease in effective ingredient content during storage, and reduced batch-to-batch consistency. To address these stability and uniformity challenges, this invention prepares the fat-soluble / oil-soluble active ingredients into spray-dried microcapsule powders, which are then compounded with hydrophilic components such as D-chiral inositol and MI, reducing active ingredient exposure from the source.

[0009] Preferably, the active ingredient Omega-3 is composed of DHA and EPA in a mass ratio of (4-8):1, and the vitamins include vitamin E and vitamin D, with a mass ratio of vitamin E to vitamin D of (10-20):1.

[0010] Preferably, the mass ratio of Myo-inositol to D-chiral inositol in the composition is (30-50):1.

[0011] Preferably, the composition further comprises folic acid, PQQ (pyrroloquinoline quinone), phenolic substances, plant extracts, fruit powder, vitamins, trace elements, magnesium citrate, and excipients.

[0012] Furthermore, the composition containing D-chiral inositol comprises the following raw materials by weight: 340-450 mg Myo-inositol, 7-50 mg D-chiral inositol, 0.2-1 mg folic acid, 8-20 mg PQQ, 30-70 mg phenolic substances, 80-130 mg plant extracts, 8-14 mg fruit powder, 50-150 mg vitamins, 10-20 mg trace elements, 80-160 mg magnesium citrate, 1.2-2 g microcapsule powder, and excipients to bring the total to 1.8-4.0 g.

[0013] Preferably, the trace element includes at least one of a zinc source and a selenium source; the zinc source is zinc gluconate and / or zinc citrate, and the selenium source is yeast selenium and / or sodium selenite.

[0014] Preferably, the plant extract includes any one of pomegranate seed extract, grape seed extract, and pumpkin seed extract.

[0015] Preferably, the phenolic substances include at least one of quercetin, resveratrol, catechin, and hesperidin.

[0016] Preferably, the fruit powder includes at least one of acai berry powder, blueberry powder, and cranberry powder.

[0017] Preferably, the excipients include at least one of maltodextrin and starch.

[0018] Microencapsulation encapsulates the active ingredients, forming a relatively dense interfacial film. This significantly reduces the direct effects of oxygen diffusion and light on the oil phase, minimizing oxidative degradation of the active ingredients during spray drying and subsequent storage, thereby improving stability and content retention. Simultaneously, microcapsules transform the originally easily permeable / agglomerated oil phase active ingredients into more fluid solid powder particles, improving their compatibility with hydrophilic powders such as Myo-inositol and D-chiral inositol, enhancing mixing uniformity, and making the effective dosage more controllable during storage. Furthermore, D-chiral inositol / MI, as an insulin sensitizer and a component related to insulin's second messenger, can promote glucose uptake and glycogen synthesis, reduce hyperinsulinemia, and weaken insulin-induced excessive androgen synthesis in the ovaries, thereby improving insulin resistance and related hyperandrogenemia and ovulation disorders. When microencapsulation ensures that antioxidant / metabolic support actives such as Omega-3, coenzyme Q10, astaxanthin, and fat-soluble vitamins maintain effective levels during storage, it can synergize with the insulin sensitivity-improving effect of D-chiral inositol / MI, which is more conducive to reducing the burden of PCOS-related chronic inflammation and oxidative stress, thus achieving a more stable comprehensive effect in menstrual cycle management, ovulation support, and improvement of androgen-related indicators.

[0019] A method for preparing a composition containing D-chiral inositol, comprising the following steps: (1) Preparation of microcapsule powder: Anhydride-modified edible protein is mixed with polysaccharide compounds to form a wall material solution; the active ingredients are encapsulated in the wall material, and microcapsule powder is obtained by emulsification, homogenization and spray drying; (2) Mix the microcapsule powder with the remaining ingredients, sieve, and package.

[0020] The reaction mechanism of this invention is as follows: The wall material of this invention uses quinoa protein as the main film-forming component. Succinic anhydride is used to acylate the reactive amino groups in the protein molecules, introducing succinyl groups and forming stable amide bonds, thereby introducing additional carboxyl groups onto the protein molecules, enhancing the negative charge of the protein, improving its hydrophilicity and solubility / dispersibility, and thus improving its adsorption and film-forming ability at the oil-water interface. During the reaction, the system is adjusted to a weakly alkaline state and the pH is maintained stably, so that succinic anhydride and protein amino groups preferentially undergo an acylation reaction. Subsequently, small molecule salts and free succinic acid are removed by dialysis to obtain modified protein. Further hydration of modified quinoa protein and polysaccharide compounds can form a thicker composite interface layer and steric barrier through hydrogen bonding, electrostatic interactions, and chain entanglement, making the emulsion droplet interface film denser and more resistant to stress during spray drying and storage. Therefore, this wall material can rapidly construct stable emulsion droplets during emulsification-homogenization and form a continuous coating structure after drying, achieving effective encapsulation and protection of Omega-3, coenzyme Q10, astaxanthin, and fat-soluble vitamins.

[0021] Preferably, the microcapsule powder is prepared as follows: Under light-protected conditions, mix 300-400 mg Omega-3 and 160-340 mg Coenzyme Q10, and stir at 35-45℃ and 300-500 rpm for 20-50 min; add 3-8 mg astaxanthin and 10-20 mg vitamins, and continue stirring for 10-30 min to obtain an oil phase mixture; The above oil phase mixture, wall material and water are mixed at a mass ratio of 1:(1-2):(5-10), and sheared at 10000-15000 rpm for 5-12 min to obtain a crude emulsion; then homogenized at 30-50 MPa 1-3 times to obtain a fine emulsion; spray dried to obtain microcapsule powder.

[0022] The wall material is prepared as follows: 2-6g of edible protein is dissolved in 80-140g of water and stirred at room temperature for 1-2 hours to obtain an edible protein solution; the pH of the solution is adjusted to 7.8-8.6 with 0.5-1.5mol / L sodium hydroxide; 0.4-1g of acid anhydride is added, and the pH is further adjusted to 7.8-8.6; the solution is stirred at 25-35℃ and 400-800rpm for 0.5-2 hours; the pH is adjusted to 6.8-7.2 with 0.5-2mol / L hydrochloric acid; and the solution is completely dialyzed with distilled water for 18-36 hours, changing the water 3-6 times during the process to remove small molecule salts and free succinic acid; the dialyzed solution is freeze-dried to obtain anhydride-modified edible protein. Mix all the acid anhydride-modified edible protein obtained above, 0.5-1.5g of polysaccharide compound and 80-180g of water, stir at 25-40℃ and 500-1000 rpm for 0.5-1.5h, let stand for hydration for 2-4h to obtain a homogeneous wall material solution; freeze-dry the wall material solution to obtain the wall material.

[0023] The anhydride is composed of succinic anhydride and octenyl succinic anhydride in a mass ratio of (0.5-2):(0.5-2).

[0024] When succinic anhydride and octenyl succinic anhydride are used synergistically to modify edible proteins, succinic anhydride undergoes acylation with amino groups such as lysine in the protein, introducing carboxyl groups and enhancing the protein's electronegativity and hydration capacity, thereby improving its dispersibility and interfacial film uniformity. Octenyl succinic anhydride, while introducing carboxyl groups, further introduces octenyl hydrophobic chains, giving the modified protein stronger amphiphilicity and oil-phase anchoring ability, forming a denser interfacial film and diffusion barrier layer. The combined use of these two materials can significantly improve the encapsulation efficiency and storage stability of active ingredients in microcapsule powders, reduce oxidative degradation and the formation of irritating oxidation products, thus enhancing their antioxidant and anti-inflammatory effects.

[0025] Preferably, the preparation method of the composition containing D-chiral inositol is as follows: premix folic acid, selenium source and half of the total amount of maltodextrin for 8-15 min; then add D-chiral inositol and Myo-inositol and premix for 3-8 min; add microcapsule powder, folic acid, PQQ, resveratrol, pomegranate seed extract, acai berry powder, quercetin, vitamin C, magnesium citrate, zinc source and the remaining maltodextrin and continue mixing for 8-16 min; sieve through 40-80 mesh and dispense to obtain the composition containing D-chiral inositol.

[0026] The composition is used in the preparation of dietary supplements or functional foods for improving insulin resistance, regulating female hormone balance, improving polycystic ovary syndrome and / or assisting in blood glucose management.

[0027] In this composition, Myo-inositol / D-chiral inositol, as an insulin-sensitizing nutritional factor, can promote glucose uptake and utilization, improve insulin resistance, and indirectly reduce the stimulation of ovarian androgen production by high insulin levels, thereby supporting the menstrual cycle and ovulation function; astaxanthin, a strong antioxidant, can reduce local oxidative stress in the ovary and help protect oocytes from lipid peroxidation damage; coenzyme Q10 participates in mitochondrial electron transport and energy metabolism, helping to improve oocyte energy supply and cell function stability; folic acid participates in one-carbon metabolism and nucleic acid synthesis, supporting germ cell division and early embryonic development and reducing homocysteine-related risks; PQQ helps improve cellular energy metabolism and mitochondrial homeostasis, synergistically enhancing the stress resistance of ovarian cells; resveratrol has antioxidant and anti-inflammatory properties, which can help improve PCOS-related chronic inflammation and support ovarian function; pomegranate seed extract is rich in polyphenolic antioxidants, which help alleviate oxidative stress and promote local microcirculation; acai berry powder contains polyphenols / anthocyanins and other components, which can help reduce inflammatory responses and support tissue repair; Quercetin, a natural flavonoid, possesses antioxidant, anti-inflammatory, and certain metabolic regulatory effects, which can help alleviate chronic inflammation and environmental stress damage in the reproductive system. Omega-3 (DHA / EPA) has anti-inflammatory and lipid-regulating effects, which can reduce the level of inflammatory factors in the ovaries / endometrium, improve membrane lipid composition and microcirculation, thereby reducing the interference of chronic inflammation on follicle development. Vitamin E, a lipid-phase antioxidant, can protect unsaturated fatty acids such as Omega-3 from oxidation and synergistically enhance mitochondrial protection with coenzyme Q10. Vitamin D participates in endocrine and immune regulation and is related to insulin sensitivity. Vitamin C, as an aqueous-phase antioxidant, can regenerate vitamin E and improve the stability of the polyphenol / carotenoid system. Zinc participates in the metabolism of various enzymes and hormones, helping to maintain normal ovarian secretion and antioxidant defense. Selenium is a key element in the antioxidant system, such as glutathione peroxidase, and can enhance the body's ability to clear peroxides. Magnesium (such as magnesium citrate) participates in enzyme reactions related to energy and glucose metabolism, which can help improve insulin action and support neuromuscular and stress regulation. The above-mentioned fat-soluble / oil-soluble active ingredients are preferably introduced in the form of microcapsules, which can further improve the stability of the powder and the uniformity of mixing, and make the effective dosage more controllable during the storage period.

[0028] The beneficial effects of this invention are as follows: This invention provides a composition containing D-chiral inositol, its preparation method, and its application. By using anhydride-modified edible protein and polysaccharide compounds to prepare microcapsule wall materials, a dense coating layer with good interfacial anchoring ability is formed. This structure can effectively block oxygen, light, and metal ions, significantly reducing the degradation loss of easily oxidized active ingredients such as Omega-3, coenzyme Q10, astaxanthin, and fat-soluble vitamins during processing, storage, and the gastrointestinal environment. Simultaneously, microencapsulation transforms oil-soluble components into highly fluid solid particles, greatly improving the mixing uniformity and physical stability of the formulation with hydrophilic components, ensuring the consistency and controllability of the dosage within the product's shelf life.

[0029] This invention scientifically combines microencapsulated antioxidant and anti-inflammatory active ingredients (such as Omega-3 and Coenzyme Q10) with D-chiral inositol and Myo-inositol, which have proven insulin-sensitizing effects, and supplements them with folic acid, PQQ, resveratrol, minerals, and plant extracts. The microcapsule protection and delivery ensure the effective release and exposure of each active ingredient in vivo. Animal experiments have shown that this composition has significant advantages in improving insulin resistance, reducing local oxidative stress and chronic inflammation in the ovaries, regulating hormone balance, and thus comprehensively improving polycystic ovary syndrome and related metabolic disorders.

[0030] The preparation method of this invention has clear steps, mild and controllable conditions, and the emulsification, homogenization, spray drying and mixing and sieving involved are all mature unit operations, which are easy to realize industrial scale-up production and have good prospects for process transformation. Detailed Implementation

[0031] The invention will now be described in further detail with reference to specific embodiments, but it should not be construed as limiting the scope of the invention to the following embodiments.

[0032] The raw materials described in this application are partially described; all other raw materials not described are commercially available. Myo-inositol was purchased from Sichuan Bohaoda Biotechnology Co., Ltd.

[0033] The preparation method of D-chiral inositol is as follows: Genetically engineered Escherichia coli (containing the iolG mutant and the iolI gene) was inoculated into LB liquid medium (containing 50 mg / L chloramphenicol, 10 g / L peptone, 5 g / L yeast extract, and 10 g / L sodium chloride) and cultured at 37°C with shaking until the logarithmic growth phase. Then, 1-2‰ (v / v) was inoculated into seed culture medium (containing 50 mg / L chloramphenicol) and cultured at 37°C and 200 rpm for 10-12 hours. Seed culture was inoculated at 5-10 wt% into fermentation medium (potassium dihydrogen phosphate 13.4 g / L, ammonium sulfate 4 g / L, citric acid 1.8 g / L, antifoaming agent 300 μL / L, glucose 10 g / L, magnesium sulfate heptahydrate 0.6 g / L, trace element I 10 mL / L, chloramphenicol 50 mg / L). The temperature was controlled at 37℃, pH 6.5, dissolved oxygen (DO) ≥ 20%, and OD600 ≥ 20. The fermenter temperature was then adjusted to 25℃, and induction was performed with 0.5 M IPTG. The culture was continued for 18 h to obtain the fermentation broth. Cells were collected by centrifugation at 8000 rpm for 10 min. 200 g / L muscle inositol was dissolved in 50 mM HEPES buffer, and the pH was adjusted to 7.0 with sodium hydroxide. 100 g / L of cells were added, and the whole-cell catalytic reaction was carried out at 45℃ and 200 rpm for 4-6 h. The bacterial cells were separated by centrifugation, and the supernatant was decolorized with activated carbon. After filtration, the supernatant was separated by cation and anion exchange resins, concentrated to a supersaturated state, and anhydrous ethanol was added and stirred. The supernatant was crystallized at 4°C for 12-24 hours and then dried under vacuum at 40-50°C to constant weight to obtain pure D-chiral inositol with a purity ≥99%.

[0034] Maltodextrin was purchased from Jinan Mingde Chemical Co., Ltd., item number: 011.

[0035] Quinoa protein was purchased from Fufeng Sinote Biotechnology Co., Ltd., product number: SNT2609.

[0036] Fucoidan was purchased from Fufeng Sinote Biotechnology Co., Ltd., product number: SNT2563.

[0037] Larch arabinogalactan was purchased from Shanghai Zhenzhun Biotechnology Co., Ltd., product number: DEX-PS132. Example 1

[0038] A composition containing D-chiral inositol comprises the following ingredients by weight: 400 mg Myo-inositol, 15 mg D-chiral inositol, 0.4 mg folic acid, 10 mg PQQ, 50 mg phenolic substances, 100 mg plant extract, 10 mg acai berry powder, 100 mg vitamin C, 15 mg zinc source, 0.055 mg selenium source, 100 mg magnesium citrate, 1.5 g microcapsule powder, and maltodextrin excipient to bring the total to 3.0 g.

[0039] The zinc source is composed of zinc gluconate and zinc citrate in a mass ratio of 2:1.

[0040] The selenium source is sodium selenite.

[0041] The phenolic substances are composed of resveratrol and quercetin in a mass ratio of 4:1.

[0042] The plant extract is pomegranate seed extract.

[0043] The microcapsule powder is prepared as follows: Under light-protected conditions, 350 mg of Omega-3 and 200 mg of Coenzyme Q10 were mixed and stirred at 40°C and 400 rpm for 30 min; 5 mg of astaxanthin and 15 mg of vitamins were added, and stirring was continued for 20 min to obtain an oil phase mixture. The above oil phase mixture, wall material, and water were mixed at a mass ratio of 1:1.4:6 and sheared at 12000 rpm for 8 min to obtain a crude emulsion; then homogenized twice at 40 MPa to obtain a fine emulsion; and spray dried to obtain microcapsule powder.

[0044] The Omega-3 is a mixture of DHA and EPA in a mass ratio of 6:1.

[0045] The vitamins include vitamin E and vitamin D, wherein the mass ratio of vitamin E to vitamin D is 15:1.

[0046] The wall material is prepared as follows: 3g of edible protein is dissolved in 100g of a 0.02mol / L sodium phosphate buffer solution with pH=8; the solution is stirred at room temperature for 1.5h to obtain an edible protein solution; 0.8g of acid anhydride is added, and the pH is adjusted to 8.4. The solution is stirred at 30℃ and 600rpm for 1h, and the pH is adjusted to 7 with 1mol / L hydrochloric acid. The solution is completely dialyzed with distilled water for 24h, with the water changed 5 times during the process to remove small molecule salts and free succinic acid. The dialyzed solution is freeze-dried to obtain anhydride-modified edible protein; the edible protein is spirulina protein; the acid anhydride is composed of succinic anhydride and octenyl succinic anhydride in a mass ratio of 2:1.

[0047] All the acid anhydride-modified edible protein obtained above, 1g of larch arabinogalactan and 100g of water were mixed and stirred at 30℃ and 800 rpm for 1h, and allowed to stand for hydration for 3h to obtain a homogeneous wall material solution; the wall material solution was freeze-dried to obtain the wall material.

[0048] The preparation method of the composition containing D-chiral inositol is as follows: folic acid, selenium source and half of the total amount of maltodextrin are premixed for 10 min; then D-chiral inositol and Myo-inositol are added and premixed for 5 min; microcapsule powder, folic acid, PQQ, resveratrol, pomegranate seed extract, acai berry powder, quercetin, vitamin C, magnesium citrate, zinc source and the remaining maltodextrin are added and mixed for another 10 min; the mixture is sieved through a 60-mesh sieve and dispensed to obtain the composition containing D-chiral inositol. Example 2

[0049] It is basically the same as Example 1, except that in the preparation method of the wall material, the edible protein is quinoa protein. Example 3

[0050] It is basically the same as Example 1, except that in the preparation method of the wall material, the edible protein is soybean protein. Example 4

[0051] It is basically the same as Example 1, except that in the preparation method of the wall material, the edible protein is whey protein. Example 5

[0052] The method is basically the same as in Example 1, except that the anhydride used in the preparation method of the wall material is succinic anhydride. Example 6

[0053] The method is basically the same as in Example 1, except that the anhydride used in the preparation method of the wall material is octenyl succinic anhydride.

[0054] Comparative Example 1 The difference from Example 1 is that microcapsule powder was not used. The specific preparation method is as follows: A composition containing D-chiral inositol, comprising the following ingredients by weight: 400 mg Myo-inositol, 15 mg D-chiral inositol, 0.4 mg folic acid, 10 mg PQQ, 40 mg resveratrol, 100 mg pomegranate seed extract, 10 mg acai berry powder, 10 mg quercetin, 100 mg vitamin C, 15 mg zinc source, 0.055 mg selenium source, 100 mg magnesium citrate, 350 mg Omega-3, 200 mg coenzyme Q10, 5 mg astaxanthin, 15 mg vitamin C, and maltodextrin as an excipient to bring the total to 3.0 g.

[0055] The zinc source is composed of zinc gluconate and zinc citrate in a mass ratio of 2:1.

[0056] The selenium source is sodium selenite.

[0057] The Omega-3 is a mixture of DHA and EPA in a mass ratio of 6:1.

[0058] The vitamins include vitamin E and vitamin D, wherein the mass ratio of vitamin E to vitamin D is 15:1.

[0059] The preparation method of the composition containing D-chiral inositol is as follows: premix folic acid, selenium source and half of the total amount of maltodextrin for 10 min; then add D-chiral inositol and Myo-inositol and premix for 5 min; add Omega-3, coenzyme Q10, astaxanthin, vitamin, folic acid, PQQ, resveratrol, pomegranate seed extract, acai berry powder, quercetin, vitamin C, magnesium citrate, zinc source and the remaining maltodextrin and continue mixing for 10 min; sieve through 60 mesh and dispense to obtain the composition containing D-chiral inositol. Comparative Example 2

[0060] It is basically the same as Example 1, except that in the preparation method of the wall material, the acid anhydride is maleic anhydride. Comparative Example 3

[0061] The method is basically the same as in Example 1, except that in the preparation method of the wall material, the acid anhydride is composed of succinic anhydride and maleic anhydride in a mass ratio of 2:1. Comparative Example 4

[0062] It is basically the same as Example 1, except that: larch arabinogalactan is not added in the preparation method of the wall material. Comparative Example 5

[0063] It is basically the same as Example 1, except that D-chiral inositol is not added to the composition. Test Example 1

[0064] Animal experiments using a polycystic ovary syndrome (PCOS) model: Experimental animals and housing conditions: Female 8-10 week old SD rats, weighing 250-300g, SPF grade, were selected. Animals were acclimatized for at least 7 days after purchase. The housing environment was: temperature 20℃, relative humidity 50%-60%, 12h light / dark cycle, with free access to food and water. DHEA was weighed and dissolved in sesame oil (or an equivalent vegetable oil carrier) to prepare a 30 mg / mL solution. Dissolution was aided by shaking in a 37-40℃ water bath. The solution was prepared fresh for immediate use or stored briefly at 4℃ in the dark.

[0065] Modeling method: Except for the normal group, the remaining rats were injected subcutaneously with DHEA at a fixed time every day at a dose of 6 mg / 100g body weight (i.e., 60 mg / kg), with an administration volume of 2 mL / kg, for 21 consecutive days. The normal group was injected subcutaneously with an equal volume of carrier (sesame oil) every day, and other feeding conditions were the same. The normal group was fed according to routine conditions. From the 7th day of modeling, vaginal smears were examined at a fixed time every morning. The estrous cycle was observed under a microscope using physiological saline wet mounts or methylene blue / Giemsa staining. Rats that successfully established the model were randomly divided into stratified groups according to body weight: model blank group, comparative examples 1-5, and examples 1-6; each group consisted of 10 rats. The 10 rats in the normal group did not participate in the modeling.

[0066] Administration: Administer by gavage once daily at a fixed time.

[0067] Dosage: Comparative groups 1-5 were administered the samples of Comparative Groups 1-5 by gavage, and Examples 1-6 were administered the samples of Examples 1-6 by gavage, at a dose of 2.3 g / kg·d for 21 consecutive days. The normal group and the model blank group were administered an equal volume of 0.9% physiological saline by gavage.

[0068] Preparation of the administration solution: The sample was converted into a dose based on the body weight of the day and prepared into a homogeneous solution / suspension with 0.9% physiological saline. The administration volume was controlled at 10 mL / kg, and the solution was kept mixed during administration to ensure the accuracy of the actual intake dose.

[0069] Detection: 24 hours after the last administration, all rats were fasted for ≥12 hours (with free access to water). Blood was collected under anesthesia via the orbital rim or abdominal aorta. Serum was separated by centrifugation at 3000 rpm for 10 min and stored at -20℃ for analysis. Serum levels of T, FSH, LH, and AMH were detected using ELISA (according to the kit instructions). The effects on improving estrous cycle and endocrine abnormalities were comprehensively evaluated in conjunction with vaginal smear results. All data are expressed as mean ± standard deviation (x ± s), and the results are shown in Table 1.

[0070] Table 1. Results of Polycystic Ovary Syndrome (PCOS) Test

[0071] Test Example 2 Stability test: The compositions containing D-chiral inositol prepared in Examples 1-6 and Comparative Examples 1-5 were bottled and sealed, and placed in an environment of 48°C for 3 months. Samples were taken at 0 months (initial) and 3 months for testing. After being restored to room temperature of 25°C, the composition showed no significant change in appearance and no clumping, indicating that the stability was qualified. The results are shown in Table 2.

[0072] Peroxide value test: Weigh 5.00 g of powder sample into a stoppered conical flask.

[0073] Add 20 mL of petroleum ether (30–60℃) or n-hexane, shake / vortex for 1 min, sonicate for 10 min, and allow to stand to separate into layers; collect the supernatant. Repeat the extraction 3 times and combine the organic phases.

[0074] The organic phase was dried with anhydrous sodium sulfate and then filtered. The solvent was removed by rotary evaporation under reduced pressure below 40°C to obtain the extracted oil.

[0075] Weigh out the extracted oil mass m (g), protect it from light, and purify it with nitrogen (optional) before testing; PV determination of samples from the same batch should be completed on the same day.

[0076] PV determination (iodometric titration) Weigh 1.00 g (±0.05 g) of the extracted oil into an iodine flask.

[0077] Add 30 mL of an acetic acid-isooctane mixture (3:2, v / v) to completely dissolve the oil.

[0078] Add 1.0 mL of saturated potassium iodide solution, seal tightly, and react in the dark for 1 min; then add 30 mL of deionized water.

[0079] Titrate with 0.01 mol / L sodium thiosulfate standard solution until pale yellow, add 1 mL of 1% starch indicator, and continue titrating until the solution is no longer blue as the endpoint.

[0080] Perform a blank test using the same method and record the sample titration volume V (mL) and the blank volume V0 (mL).

[0081] Peroxide value PV (mmol / kg, or meq O2 / kg) is calculated using the following formula: PV = (V − V0) × c × 1000 / m Where: V and V0 are titration volumes (mL); c is the sodium thiosulfate concentration (mol / L); and m is the oil mass (g). Each sample was measured in triplicate, and the results are expressed as x ± s.

[0082] Table 2. Results of stability and peroxide value tests stability PV (0 months) PV (3 months) Example 1 No abnormalities, no lumps 2.0±0.1 6.2±0.4 Example 2 No abnormalities, no lumps 2.2±0.2 6.7±0.6 Example 3 No abnormalities, no lumps 2.4±0.2 7.2±0.7 Example 4 No abnormalities, no lumps 2.3±0.3 6.9±0.5 Example 5 No abnormalities, no lumps 2.6±0.4 8.2±0.7 Example 6 No abnormalities, no lumps 2.7±0.3 8.5±0.8 Comparative Example 1 There are lumps and many spots. 3.8±0.3 24.6±1.7 Comparative Example 2 No abnormalities, no lumps 3.2±0.2 9.8±0.8 Comparative Example 3 No abnormalities, no lumps 2.8±0.2 9.0±0.9 Comparative Example 4 No lumps, but a few spots 3.0±0.2 11.8±1.1 Comparative Example 5 No abnormalities, no lumps 2.3±0.2 7.0±0.5 Test Example 3

[0083] Evaluation of in vitro anti-inflammatory and antioxidant activities: This test case aims to evaluate the anti-inflammatory and antioxidant activities of the compositions of the present invention through in vitro cell experiments. An inflammation model was established using lipopolysaccharide (LPS)-induced mouse macrophages (RAW264.7). The effects of the examples and comparative samples were evaluated by detecting changes in the levels of key inflammatory factors (TNF-α) and endogenous antioxidant enzymes (SOD).

[0084] Cell Culture and Processing: Cell Line: RAW264.7 mouse macrophage cell line was selected. Culture Conditions: Cells were placed in DMEM medium containing 10% fetal bovine serum (FBS), 100 U / mL penicillin, and 100 U / mL streptomycin, and cultured routinely in an incubator at 37℃, 5% CO2, and saturated humidity (95%). Cells were passaged at 80%-90% density. To determine the safe test concentration of the sample, a preliminary cytotoxicity experiment was first performed using the CCK-8 assay. RAW264.7 cells were cultured at 5 × 10⁻⁶ cells / mL. 3 Cells were seeded per well in 96-well plates and cultured for 24 hours. The medium was then replaced with culture medium containing different concentrations (e.g., 0, 50, 100, 200, 400, 800 μg / mL) of the composition samples of this invention, and cultured for another 24 hours. Cell viability was then assessed according to the CCK-8 reagent instructions. Results showed that cell viability was greater than 90% at concentrations ≤200 μg / mL, with no significant difference compared to the normal control group (P>0.05). Therefore, 200 μg / mL was selected as the non-toxic concentration for subsequent anti-inflammatory and antioxidant experiments.

[0085] Experimental Groups: The experiment included a normal control group (without LPS and samples), a model blank group (with LPS only), Examples 1-6, and Comparative Examples 1-5. Drug Administration and Model Establishment: Cells in the logarithmic growth phase were injected with 1×10⁻⁶ cells... 6 Cells were seeded at a density of 1 cell / well in 6-well plates, with 2 mL of culture medium added to each well. After 24 h of culture, the culture medium was replaced. Except for the normal control group and the model blank group, the corresponding sample solution was added to each of the other groups (ensuring a final sample concentration of 200 μg / mL) for 1 h of pretreatment. Subsequently, except for the normal control group, LPS (final concentration of 1.0 μg / mL) was added to all wells, and the cells were cultured for another 24 h to induce an inflammatory response.

[0086] Indicator Detection: I. Anti-inflammatory Activity Assay: After culture, the culture supernatant of each group of cells was collected. The concentration of tumor necrosis factor-α (TNF-α) was detected using a commercially available ELISA kit. II. Antioxidant Activity Assay: Cells from each group were collected, washed with PBS, lysed, and centrifuged at 12,000 rpm for 5 min at 4°C. The activity level of superoxide dismutase (SOD) in the cell lysate was detected using a SOD activity assay kit. Data Analysis: All experiments were repeated three times, and results are expressed as mean ± standard deviation (x ± s).

[0087] The test data obtained based on the above experimental methods are summarized in Table 3.

[0088] Table 3 Results of anti-inflammatory and antioxidant tests TNF-α concentration (pg / mL) SOD activity (U / mg) Example 1 132.7±12.5 26.5±3.2 Example 2 145.3±15.1 25.8±2.4 Example 3 160.8±18.2 26.1±5.0 Example 4 150.1±16.5 25.6±1.6 Example 5 220.5±20.9 22.4±2.8 Example 6 240.6±22.3 23.1±3.1 Comparative Example 1 480.2±40.1 21.5±1.3 Comparative Example 2 310.7±28.8 22.1±2.2 Comparative Example 3 285.9±25.4 22.7±2.4 Comparative Example 4 350.1±33.7 21.2±2.0 Comparative Example 5 450.8±38.2 24.1±3.6 Model blank group 550.5±45.3 14.0±0.4 normal group 60.2±8.1 25.2±2.1 The results above show that the composition containing D-chiral inositol prepared by the present invention has a good effect on the treatment of polycystic ovary syndrome and can extend the shelf life of the product.

[0089] As shown in Table 1, compared with the blank control group, the administration of the present invention in Examples 1-6 can improve the overall endocrine disorder trend in PCOS model rats, with a decrease in serum T level and a return of gonadotropin level to the normal group; indicating that the composition of the present invention can exert an intervention effect. The main reason is that the combination of D-chiral inositol and Myo-inositol in the composition can improve the abnormal regulation of insulin signaling and ovarian steroid production, and reduce excessive androgen production driven by high insulin; the microcapsule delivery significantly inhibits the oxidative degradation of active substances such as Omega-3, coenzyme Q10, astaxanthin and fat-soluble vitamins in the gastrointestinal environment and during storage, improves the consistency of the arrival and exposure of effective ingredients, and thus forms a synergistic effect in anti-inflammation, anti-oxidation and improvement of ovarian microenvironment.

[0090] Examples 2, 3, and 4 differed only in that the edible protein in the wall material was replaced with quinoa protein, soy protein, and whey protein, respectively. The different proteins exhibited variations in interfacial adsorption capacity, film-forming density, and the amphiphilic structure formed after modification with anhydride. This resulted in differences in the strength of the interfacial film formed during emulsification, the stability of the glassy framework of the wall material obtained through spray drying, and its ability to block oxygen and metal ions, thus affecting the protective strength and in vivo release consistency of the lipophilic active ingredients. Therefore, Examples 1-4 all demonstrated effects in improving PCOS-related hormone indicators, but the differences in interfacial film-forming and antioxidant shielding capabilities resulting from different protein sources led to variations in the degree of improvement; Example 1, which used spirulina protein, was generally more conducive to obtaining a more robust overall effect.

[0091] Example 5 used only succinic anhydride, and Example 6 used only octenyl succinic anhydride for protein modification; Comparative Example 2 used maleic anhydride instead. The type of anhydride determines the degree of hydrophobic segment introduction, the distribution of charged / hydrophilic groups, and the amphiphilic balance of the modified protein, thus affecting the ability of the wall material to form a dense film at the oil-water interface and the barrier performance of the microcapsules. Compared with the synergistic modification of succinic anhydride and octenyl succinic anhydride used in Example 1, single anhydride modification often fails to simultaneously achieve strong interfacial adsorption and sufficient hydrophobic barrier, resulting in a relatively weakened synergistic effect on the protection and delivery of lipophilic actives; while the maleic anhydride modification in Comparative Example 2, due to its different structure and post-reaction polarity and charge characteristics, may result in an interfacial film structure and hydration layer characteristics that are inferior to the synergistic anhydride system, and the improvement effect on PCOS-related indicators is not as sufficient as in Example 1.

[0092] Comparative Example 1 did not use microcapsule powder to encapsulate the lipid-soluble active ingredients, while Comparative Example 4 did not add larch arabinogalactan to the wall material. The absence of microcapsules makes Omega-3, Coenzyme Q10, astaxanthin, etc., more susceptible to oxidation, aggregation, or phase separation during processing, storage, and in vivo transport, leading to a decrease in the retention rate of active ingredients and poorer dosing consistency, thus weakening the overall improvement effect; this is consistent with the stability degradation phenomena such as clumping and spots observed in Comparative Example 1 in Table 2. Larch arabinogalactan, as a film-forming / glassy framework and hydration stabilizing component, can form a continuous polysaccharide phase during spray drying and improve the structural integrity and anti-agglomeration ability of the wall material; Comparative Example 4 reduces the film-forming uniformity and the ability to inhibit oxidative propagation of the wall material, therefore, although it may still maintain some improvement, the overall effect and stability are weaker than the examples containing this component.

[0093] Comparative Example 5 did not add D-chiral inositol to the composition. Since D-chiral inositol is a key component in the inositol system that is closely related to insulin signaling and the regulation of ovarian steroid production, the absence of D-chiral inositol will weaken the intervention intensity for high insulin and high androgen levels, thus limiting the decrease in T levels and the extent of gonadotropin reversion. This indicates that the beneficial effects of the present invention do not simply come from antioxidant / nutritional supplementation, but from the synergistic effect of D-chiral inositol-Myo-inositol metabolic regulation and microcapsule stable delivery of lipid-soluble active ingredients.

[0094] Examples 1-6 showed no abnormalities or clumping after being accelerated at 48°C for 3 months, and the peroxide value (PV) of the extracted oils only increased slightly and remained at a low level. This indicates that the present invention can effectively inhibit the primary oxidation reaction of lipophilic active ingredients through microencapsulation, thereby significantly improving the physical and chemical stability of lipophilic active ingredients and the overall composition. In contrast, Comparative Example 1 showed clumping and more spots, and its PV increased significantly, indicating that the oils were more prone to oxidative deterioration and powder clumping and oxidative discoloration when not microencapsulated. Although no clumping was observed in Comparative Example 4, a small number of spots appeared, and its PV increase was between that of the Example group and Comparative Example 1. This further proves that microcapsules and polysaccharide backbone components can enhance film density and form a stable glassy structure, inhibit phase separation, oxidation propagation and powder clumping, thereby achieving better stability.

[0095] Table 3 shows that Examples 1-6 can significantly inhibit the release of LPS-induced macrophage inflammatory factor TNF-α and enhance intracellular SOD activity, indicating that the composition has good anti-inflammatory and antioxidant properties. Among them, Example 1 has the best effect. The comparative examples showed varying degrees of decrease in activity due to the lack of key components (such as D-chiral inositol, microcapsules, specific anhydrides or polysaccharides), which further verifies the functional synergy of the components in the formulation of this invention.

Claims

1. A composition containing D-chiral inositol, characterized in that, It contains D-chiral inositol, Myo-inositol, and microcapsule powder. The wall material of the microcapsule powder is composed of anhydride-modified edible protein and polysaccharide compounds. The edible protein includes at least one of spirulina protein, quinoa protein, whey protein, and soy protein. The polysaccharide compounds include at least one of fucoidan and larch arabinogalactan.

2. The composition containing D-chiral inositol according to claim 1, characterized in that, The anhydride is composed of succinic anhydride and octenyl succinic anhydride in a mass ratio of (0.5-2):(0.5-2).

3. The composition containing D-chiral inositol according to claim 1 or 2, characterized in that, The microcapsule powder also contains active ingredients embedded in the wall material, including at least one of Omega-3, coenzyme Q10, astaxanthin, and vitamins.

4. The composition containing D-chiral inositol according to claim 3, characterized in that, The active ingredient Omega-3 is composed of DHA and EPA in a mass ratio of (4-8):1, and the vitamins include vitamin E and vitamin D, with a mass ratio of vitamin E to vitamin D of (10-20):

1.

5. The composition containing D-chiral inositol according to any one of claims 1-4, characterized in that, The mass ratio of Myo-inositol to D-chiral inositol in the composition is (15-50):

1.

6. The composition containing D-chiral inositol according to claim 5, characterized in that, The composition also includes folic acid, PQQ, phenolic substances, plant extracts, fruit powder, vitamins, trace elements, magnesium citrate, and excipients.

7. The composition according to claim 6, characterized in that, The trace elements include at least one of zinc source and selenium source; the zinc source is zinc gluconate and / or zinc citrate, and the selenium source is yeast selenium and / or sodium selenite.

8. A method for preparing a composition containing D-chiral inositol as described in any one of claims 1-7, characterized in that, Includes the following steps: (1) Preparation of microcapsule powder: Succinic anhydride-modified edible protein is mixed with polysaccharide compounds to form a wall material solution; the active ingredients are encapsulated in the wall material, and microcapsule powder is obtained by emulsification, homogenization and spray drying; (2) Mix the microcapsule powder with the remaining ingredients, sieve, and package.

9. The preparation method according to claim 8, characterized in that, The preparation of the wall material solution in step (1) includes: dissolving edible protein and adjusting the pH to 8.4, adding succinic anhydride to react, dialysis, and freeze-drying to obtain modified protein; mixing the modified protein with a polysaccharide compound and hydrating to obtain the wall material solution.

10. The use of a composition according to any one of claims 1-7 in the preparation of a dietary supplement or functional food for improving insulin resistance, regulating female hormone balance, improving polycystic ovary syndrome and / or assisting in blood glucose management.

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