A β-carotene-grape seed extract eye-care preparation for protecting the retina

Abstract

The present invention discloses a β-carotene-grape seed extract eye-care preparation for retinal protection, relating to functional health foods. The preparation comprises active components and food-acceptable excipients. In parts by weight, the active components include 1–4 parts lutein, 0.5 –2 parts meso-zeaxanthin, 2 – 6 parts β-carotene, 8 – 25 parts blueberry extract, 5 – 18 parts grape seed extract, 0.2–1 part L-ergothioneine, 0.5–3 parts saffron extract, and 1–5 parts phosphatidylserine. The excipients comprise a filler, disintegrant, binder, and lubricant, with a weight ratio of active components to excipients of 1:1 to 1:4. By combining these eight components at specific ratios, the invention achieves synergistic effects, protects retinal health, and reduces blue-light damage. Dual-phase microencapsulation based on solubility, together with standardized preparation steps, improves stability and utilization efficiency.

Description

[0001] DESCRIPTION

[0002] A P-carotene-grape seed extract eye-care preparation for protecting the retina TECHNICAL FIELD

[0003] The present invention relates to the technical field of functional health foods, and in particular to a P-carotene-grape seed extract eye-care preparation for protecting the retina.

[0004] BACKGROUND ART

[0005] With the widespread use of electronic devices, the amount of time people spend each day in contact with screens such as mobile phones, computers, and tablets has increased substantially. The short- wavelength blue light emitted from screens can penetrate the cornea and crystalline lens and reach the retina directly. Long-term exposure to short- wavelength blue light can cause oxidative stress in retinal pigment epithelial cells, impair the function of photoreceptor cells, and further lead to discomfort such as visual fatigue, dry eyes, and blurred vision. In severe cases, it may also damage the macular region and cause irreversible harm to ocular health. At present, eye-care preparations have become the principal products used to alleviate blue-light injury and protect the retina. Eye-care preparations currently on the market generally use lutein, P-carotene, blueberry extract, grape seed extract, and the like as core raw materials. These raw materials themselves possess certain blue-light-blocking and antioxidant effects and can, to some extent, reduce blue-light-induced ocular injury and satisfy the basic daily need for eye protection.

[0006] Existing eye-care preparations have two core problems. First, component compounding is unreasonable: in most cases, the products are merely simple combinations of core raw materials, without grouping the ingredients according to lipid solubility and water solubility or strictly controlling the ratios among the ingredients, with the result that the ingredients cannot fully exert synergistic effects and comprehensive retinal protection is difficult to i DESCRIPTION achieve. Second, the preparation process has shortcomings: active ingredients are not subjected to targeted protective treatment, and direct mixing and granulation are commonly adopted, leading to easy oxidation of lipid-soluble ingredients, easy loss of water-soluble ingredients, and low utilization efficiency of the active ingredients, thereby preventing the raw materials from fully exerting their eye-protective effects.

[0007] SUMMARY OF THE INVENTION

[0008] The purpose of the present invention is to overcome the shortcomings of the prior art by providing a P-carotene-grape seed extract eye-care preparation for protecting the retina. By compounding eight active functional components at specific weight ratios, matching the same with food-acceptable excipients and defining the ratio therebetween, and simultaneously dividing the active components into a lipid-soluble group and a water-soluble group according to solubility for dual-phase microencapsulation, in combination with standardized preparation steps including raw-material pretreatment, mixing and granulation, final blending, and forming and packaging, the present invention develops the P-carotene-grape seed extract eye-care preparation for protecting the retina. The invention effectively solves the core problems of poor synergy among components, limited blue-light protection, easy oxidation and loss of active ingredients, and low utilization efficiency in conventional eye-care preparations. The resulting preparation exhibits excellent active-ingredient stability, dissolution, and cell-protective effect, can meet diverse eye-care needs through different ratios, and has clear preparation-process parameters suitable for large-scale production.

[0009] To solve the above technical problems, the present invention provides the following technical solutions. In one aspect, the present invention provides a P-carotene-grape seed extract eye-care preparation for protecting the retina, wherein the preparation consists of active functional components and food-acceptable excipients; in parts by weight, the active functional DESCRIPTION components comprise 1-4 parts of lutein, 0.5-2 parts of meso-zeaxanthin, 2-6 parts of 0-carotene, 8-25 parts of blueberry extract, 5-18 parts of grape seed extract, 0.2-1 part of L-ergothioneine, 0.5-3 parts of saffron extract, and 1-5 parts of phosphatidylserine;

[0010] The food-acceptable excipients comprise a filler, a disintegrant, a binder, and a lubricant, wherein the weight ratio of the active functional components to the excipients is 1:1 to 1:4.

[0011] Further, the lutein is derived from natural marigold and has a content of >5%; the meso-zeaxanthin has a content of >80%, and the weight ratio of meso-zeaxanthin to lutein is 1:2 to 1:4.

[0012] Furthermore, the P-carotene is derived from natural fermentation and has a content of >10%; the blueberry extract is derived from blueberry fruits and has an anthocyanin content of >25%, and the weight ratio of P-carotene to blueberry extract is 1:4 to 1:5.

[0013] Furthermore, the grape seed extract is derived from grape seeds and has a proanthocyanidin content of >95%; the L-ergothioneine is derived from biological fermentation and has a purity of >99%, and the weight ratio of grape seed extract to L-ergothioneine is 50:1 to 90:1.

[0014] Furthermore, the saffron extract is derived from saffron stigmas and has a crocin content of >3%; the phosphatidyl serine is derived from soybeans and has a content of >50%, and the weight ratio of saffron extract to phosphatidylserine is 1:2 to 1:6.

[0015] Furthermore, the excipients comprise 30-60 parts of a filler, 2-5 parts of a disintegrant, 1-3 parts of a binder, and 0.5-2 parts of a lubricant.

[0016] Furthermore, the filler is a mixture of microcrystalline cellulose and pregelatinized starch at a weight ratio of 3:1, the disintegrant is crospovidone, the binder is an aqueous ethanol solution having a volume fraction of 50%, and the lubricant is a mixture of magnesium stearate and silicon dioxide at a weight ratio of 4:1. DESCRIPTION

[0017] Furthermore, the active functional components are divided into lipid-soluble components and water-soluble components and are subjected to microencapsulation separately; the lipid-soluble components comprise lutein, meso-zeaxanthin, P-carotene, and phosphatidylserine, and the water-soluble components comprise blueberry extract, grape seed extract, L-ergothioneine, and saffron extract.

[0018] In another aspect, the present invention provides a method for preparing the P-carotene-grape seed extract eye-care preparation for protecting the retina, the method comprising the following steps:

[0019] 51. Raw-material pretreatment: weighing each active functional component and excipient according to the formula in parts by weight; passing each active functional component separately through an 80-100 mesh sieve and the excipients through an 80 mesh sieve; dividing the active functional components into lipid-soluble components and water-soluble components, and reserving the same for subsequent use;

[0020] 52. Dual-phase microencapsulation: mixing the lipid-soluble components with a mixture of maltodextrin and gum arabic at a weight ratio of 2:1 at a weight ratio of 1:2 to 1:3, dissolving the same in anhydrous ethanol, and subjecting the same to high-speed dispersion at 10000-12000 r / min for 15-20 min to obtain a lipid-soluble encapsulating solution; mixing the water-soluble components with the encapsulating agent at a weight ratio of 1:1.5 to 1:2.5, dissolving the same in purified water, and subjecting the same to ultrasonic emulsification at 300-500 W for 10-15 min to obtain a water-soluble encapsulating solution; spray-drying the two encapsulating solutions separately to obtain the corresponding encapsulated powders;

[0021] 53. Mixing and granulation: mixing the two encapsulated powders, adding the filler and binder, and mixing at 500-800 r / min for 15-30 min until uniform; adding an aqueous ethanol solution having a volume fraction of 50% to prepare a wet mass, passing the wet mass through a 20 mesh sieve to obtain DESCRIPTION wet granules, drying the wet granules with hot air at 50-60 °C until the moisture content is <3%, and passing the dried granules through an 18 mesh sieve for sizing;

[0022] 54. Final blending: placing the sized dry granules and the lubricant into a three-dimensional motion mixer and mixing at 300-500 r / min for 10-20 min until uniform, thereby obtaining a final blend;

[0023] 55. Forming and packaging: filling the final blend into empty gelatin capsules, controlling the fill-weight deviation within ±5%, performing aluminum-plastic blister packaging, and obtaining the finished product after inspection is passed.

[0024] Compared with the prior art, the P-carotene-grape seed extract eye-care preparation for protecting the retina provided by the present invention has the following beneficial effects:

[0025] I. By compounding eight active functional components, including lutein, meso-zeaxanthin, P-carotene, and blueberry extract, at specific weight ratios, the present invention achieves precise synergy among the components. Meso-zeaxanthin and lutein are combined at a ratio of 1:2 to 1 :4 to realize full-range protection of the macular region; P-carotene and blueberry extract synergistically enhance photoprotective capability; grape seed extract and L-ergothioneine construct an efficient antioxidant system; and saffron extract and phosphatidylserine protect the optic nerve. The preparation can effectively reduce blue-light-induced retinal injury, solve the problem that single ingredients have limited eye-protective effects and poor synergy, and comprehensively protect retinal health.

[0026] II. By dividing the active functional components into lipid-soluble and water-soluble groups and applying dual-phase microencapsulation under specific DESCRIPTION parameters, in combination with standardized steps of mixing and granulation, final blending, and forming and packaging, the present invention effectively solves the problems that active ingredients are readily lost and have low utilization efficiency in conventional preparation processes. The dual-phase microencapsulation can effectively avoid oxidative deterioration of lipid-soluble components and reduce the loss of water-soluble components, thereby improving the stability and bioavailability of each active ingredient.

[0027] Other advantages, objectives, and features of the present invention will be set forth in part in the following description and in part will become apparent to those skilled in the art upon examination of the following disclosure, or may be learned from practice of the invention.

[0028] BRIEF DESCRIPTION OF THE DRAWINGS

[0029] To describe the technical solutions in the embodiments of the present invention or in the prior art more clearly, the drawings required for describing the embodiments or the prior art are briefly introduced below. Obviously, the drawings in the following description merely illustrate certain embodiments of the present invention, and those of ordinary skill in the art can derive other drawings therefrom without inventive effort.

[0030] Figure 1 is a flow chart of the preparation method of the P-carotene-grape seed extract eye-care preparation for protecting the retina;

[0031] Figure 2 is a schematic diagram of classification of the lipid-soluble and water-soluble active functional components according to the present invention;

[0032] Figure 3 is a schematic flow chart of the dual-phase microencapsulation process according to the present invention.

[0033] DETAILED DESCRIPTION DESCRIPTION

[0034] In order to further illustrate the technical means and effects adopted by the present invention to achieve the intended objectives, the specific implementation, structure, features, and effects of the present invention are described in detail below in conjunction with the accompanying drawings and preferred embodiments.

[0035] Embodiment 1:

[0036] The present embodiment provides a P-carotene-grape seed extract eye-care preparation for protecting the retina, the composition and ratio of the preparation being as follows:

[0037] In parts by weight, the active functional components comprise 2 parts of lutein, 1 part of meso-zeaxanthin, 4 parts of P-carotene, 15 parts of blueberry extract, 10 parts of grape seed extract, 0.5 part of L-ergothioneine, 1.5 parts of saffron extract, and 3 parts of phosphatidylserine. The excipients comprise 40 parts of a filler, 3 parts of a disintegrant, 2 parts of a binder, and 1 part of a lubricant, wherein the filler is a mixture of microcrystalline cellulose and pregelatinized starch at a weight ratio of 3:1, the disintegrant is crospovidone, the binder is an aqueous ethanol solution having a volume fraction of 50%, and the lubricant is a mixture of magnesium stearate and silicon dioxide at a weight ratio of 4:1. The weight ratio of the active functional components to the excipients is 1:2.

[0038] As shown in Figure 1, the preparation method of the preparation comprises steps S1-S5, and the specific preparation method is as follows:

[0039] SI . Raw-material pretreatment: each active functional component and excipient is accurately weighed according to the above formula in parts by weight. Each active functional component is separately passed through a 90 mesh standard sieve, and the undersize is collected for subsequent use; the excipients are uniformly passed through an 80 mesh standard sieve, and the undersize is collected for subsequent use. The active functional components are divided into lipid-soluble components and water-soluble components DESCRIPTION according to solubility. As shown in Figure 2, the lipid-soluble components comprise lutein, meso-zeaxanthin, 0-carotene, and phosphatidylserine, and the water-soluble components comprise blueberry extract, grape seed extract, L-ergothioneine, and saffron extract. The classified components are sealed and stored for subsequent use.

[0040] 52. Dual-phase microencapsulation: as shown in Figure 3, a mixture of maltodextrin and gum arabic at a weight ratio of 2:1 is weighed as an encapsulating agent. The lipid-soluble components are mixed with the encapsulating agent at a weight ratio of 1:2.5, anhydrous ethanol is added until complete dissolution, and the resulting mixed solution is placed in a high-speed disperser and dispersed at 11000 r / min for 18 min to obtain a uniform lipid-soluble encapsulating solution. The water-soluble components are mixed with the above encapsulating agent at a weight ratio of 1:2, purified water is added until complete dissolution, and the resulting mixed solution is placed in an ultrasonic emulsifier and ultrasonically emulsified at 400 W for 12 min to obtain a uniform water-soluble encapsulating solution. The two encapsulating solutions are separately introduced into a spray-drying apparatus for drying, the inlet air temperature is controlled at 180 °C and the outlet air temperature at 80 °C, and the dried powdery encapsulates are collected to obtain the lipid-soluble encapsulated powder and the water-soluble encapsulated powder.

[0041] 53. Mixing and granulation: the lipid-soluble encapsulated powder and the water-soluble encapsulated powder are introduced into a mixer and pre-mixed at low speed for 5 min. The filler and the binder in parts by weight are then added, and mixing is carried out at 650 r / min for 22 min until the system is uniform. The binder is added dropwise to the mixed system to prepare a wet mass; when the wet mass reaches a state in which it forms a ball when held by hand and readily disperses upon light pressure, liquid addition is stopped. The wet mass is passed through a 20 mesh standard sieve to obtain DESCRIPTION wet granules, the wet granules are spread flat on trays and dried in a hot-air drying oven at a constant temperature of 55 °C, and drying is stopped when the moisture content of the granules reaches 2.5%. The dried granules are then passed through an 18 mesh standard sieve for sizing, and the sized granules are collected for subsequent use.

[0042] 54. Final blending: the sized granules are introduced into a three-dimensional motion mixer, the lubricant is added, and mixing is performed at 400 r / min for 15 min. During the mixing process, the materials in the mixer are ensured to tumble fully, and the final blend is obtained after the system becomes uniform.

[0043] 55. Forming and packaging: the final blend is fed into a capsule-filling apparatus for filling into empty gelatin capsules. During filling, the fill weight is monitored in real time, and the fill-weight deviation is controlled within ±4%. After filling is completed, the capsules are subjected to aluminum-plastic blister packaging. A full-item inspection is carried out after packaging, and the finished product is obtained after inspection is passed.

[0044] In summary, the present embodiment adopts a medium ratio within the formula range of the present invention. In the preparation process, all process parameters are controlled at intermediate values within the ranges defined by the present invention. The sieve mesh used in raw-material pretreatment is adapted to the particle size of the components; the dispersion parameters, emulsification parameters, and spray-drying temperature in the dual-phase microencapsulation process are optimal matching values; the wet-mass state, granule moisture, and sizing specification in mixing and granulation all conform to the preparation requirements; and the fill-weight deviation during forming and packaging is controlled accurately. Upon testing, the preparation obtained in the present embodiment has a lipid-soluble component oxidation rate of 0.8%, a water-soluble component retention rate of 99.2%, an in vitro dissolution rate of active ingredients at 45 min of 92.5%, and a retinal DESCRIPTION pigment epithelial cell survival rate after blue-light induction of 89.7%. All test indexes are excellent, fully demonstrating the synergistic advantages of the formula and process of the present invention.

[0045] Embodiment 2

[0046] The present embodiment provides a P-carotene-grape seed extract eye-care preparation for protecting the retina, the composition and ratio of the preparation being as follows:

[0047] In parts by weight, the active functional components comprise 1 part of lutein, 0.5 part of meso-zeaxanthin, 2 parts of P-carotene, 8 parts of blueberry extract, 5 parts of grape seed extract, 0.2 part of L-ergothioneine, 0.5 part of saffron extract, and 1 part of phosphatidylserine. The excipients comprise 30 parts of a filler, 2 parts of a disintegrant, 1 part of a binder, and 0.5 part of a lubricant, wherein the filler is a mixture of microcrystalline cellulose and pregelatinized starch at a weight ratio of 3:1, the disintegrant is crospovidone, the binder is an aqueous ethanol solution having a volume fraction of 50%, and the lubricant is a mixture of magnesium stearate and silicon dioxide at a weight ratio of 4:1. The weight ratio of the active functional components to the excipients is 1:4.

[0048] The preparation method of the preparation comprises steps S1-S5, and the specific preparation method is as follows:

[0049] SI . Raw-material pretreatment: each active functional component and excipient is accurately weighed according to the above formula in parts by weight. Each active functional component is separately passed through an 80 mesh standard sieve, and the undersize is collected for subsequent use; the excipients are uniformly passed through an 80 mesh standard sieve, and the undersize is collected for subsequent use. The active functional components are divided into lipid-soluble components and water-soluble components according to solubility. The lipid-soluble components comprise lutein, meso-zeaxanthin, P-carotene, and phosphatidylserine, and the water-soluble io DESCRIPTION components comprise blueberry extract, grape seed extract, L-ergothioneine, and saffron extract. The classified components are sealed and stored for subsequent use.

[0050] 52. Dual-phase microencapsulation: a mixture of maltodextrin and gum arabic at a weight ratio of 2:1 is weighed as an encapsulating agent. The lipid-soluble components are mixed with the encapsulating agent at a weight ratio of 1:2, anhydrous ethanol is added until complete dissolution, and the resulting mixed solution is placed in a high-speed disperser and dispersed at 10000 r / min for 15 min to obtain a uniform lipid-soluble encapsulating solution. The water-soluble components are mixed with the above encapsulating agent at a weight ratio of 1:1.5, purified water is added until complete dissolution, and the resulting mixed solution is placed in an ultrasonic emulsifier and ultrasonically emulsified at 300 W for 10 min to obtain a uniform water-soluble encapsulating solution. The two encapsulating solutions are separately introduced into a spray-drying apparatus for drying, the inlet air temperature is controlled at 170 °C and the outlet air temperature at 75 °C, and the dried powdery encapsulates are collected to obtain the lipid-soluble encapsulated powder and the water-soluble encapsulated powder.

[0051] 53. Mixing and granulation: the lipid-soluble encapsulated powder and the water-soluble encapsulated powder are introduced into a mixer and pre-mixed at low speed for 5 min. The filler and the binder in parts by weight are then added, and mixing is carried out at 500 r / min for 15 min until the system is uniform. The binder is added dropwise to the mixed system to prepare a wet mass; when the wet mass reaches a state in which it forms a ball when held by hand and readily disperses upon light pressure, liquid addition is stopped. The wet mass is passed through a 20 mesh standard sieve to obtain wet granules, the wet granules are spread flat on trays and dried in a hot-air drying oven at a constant temperature of 50 °C, and drying is stopped when n DESCRIPTION the moisture content of the granules reaches 2.0%. The dried granules are then passed through an 18 mesh standard sieve for sizing, and the sized granules are collected for subsequent use.

[0052] 54. Final blending: the sized granules are introduced into a three-dimensional motion mixer, the lubricant is added, and mixing is performed at 300 r / min for 10 min. During the mixing process, the materials in the mixer are ensured to tumble fully, and the final blend is obtained after the system becomes uniform.

[0053] 55. Forming and packaging: the final blend is fed into a capsule-filling apparatus for filling into empty gelatin capsules. During filling, the fill weight is monitored in real time, and the fill-weight deviation is controlled within ±3%. After filling is completed, the capsules are subjected to aluminum-plastic blister packaging. A full-item inspection is carried out after packaging, and the finished product is obtained after inspection is passed.

[0054] In summary, the present embodiment adopts a low ratio within the formula range of the present invention. In the preparation process, all process parameters adopt the lower-limit values defined by the present invention; an 80 mesh sieve is used throughout raw-material pretreatment to meet the mixing requirements of low-ratio components; the dispersion speed, emulsification power, and related parameters in the dual-phase microencapsulation process are the minimum values within the defined ranges; the spray-drying temperature is adapted to the drying characteristics of a low-concentration encapsulating solution; the mixing speed and time in mixing and granulation conform to the mixing pattern of low-ratio materials; and the fill-weight deviation in forming and packaging is controlled with high precision. Upon testing, the preparation obtained in the present embodiment has a lipid-soluble component oxidation rate of 1.2%, a water-soluble component retention rate of 97.5%, an in vitro dissolution rate of active ingredients at 45 min of 88.3%, and a retinal pigment epithelial cell survival DESCRIPTION rate after blue-light induction of 82.4%. All test indexes comply with the technical requirements of the present invention and are suitable for daily eye-care scenarios requiring a low dosage.

[0055] Embodiment 3

[0056] The present embodiment provides a P-carotene-grape seed extract eye-care preparation for protecting the retina, the composition and ratio of the preparation being as follows:

[0057] In parts by weight, the active functional components comprise 4 parts of lutein, 2 parts of meso-zeaxanthin, 6 parts of P-carotene, 25 parts of blueberry extract, 18 parts of grape seed extract, 1 part of L-ergothioneine, 3 parts of saffron extract, and 5 parts of phosphatidylserine. The excipients comprise 60 parts of a filler, 5 parts of a disintegrant, 3 parts of a binder, and 2 parts of a lubricant, wherein the filler is a mixture of microcrystalline cellulose and pregelatinized starch at a weight ratio of 3:1, the disintegrant is crospovidone, the binder is an aqueous ethanol solution having a volume fraction of 50%, and the lubricant is a mixture of magnesium stearate and silicon dioxide at a weight ratio of 4:1. The weight ratio of the active functional components to the excipients is 1:1.

[0058] The preparation method of the preparation comprises steps S1-S5, and the specific preparation method is as follows:

[0059] SI . Raw-material pretreatment: each active functional component and excipient is accurately weighed according to the above formula in parts by weight. Each active functional component is separately passed through a 100 mesh standard sieve, and the undersize is collected for subsequent use; the excipients are uniformly passed through an 80 mesh standard sieve, and the undersize is collected for subsequent use. The active functional components are divided into lipid-soluble components and water-soluble components according to solubility. The lipid-soluble components comprise lutein, meso-zeaxanthin, P-carotene, and phosphatidylserine, and the water-soluble DESCRIPTION components comprise blueberry extract, grape seed extract, L-ergothioneine, and saffron extract. The classified components are sealed and stored for subsequent use.

[0060] 52. Dual-phase microencapsulation: a mixture of maltodextrin and gum arabic at a weight ratio of 2:1 is weighed as an encapsulating agent. The lipid-soluble components are mixed with the encapsulating agent at a weight ratio of 1:3, anhydrous ethanol is added until complete dissolution, and the resulting mixed solution is placed in a high-speed disperser and dispersed at 12000 r / min for 20 min to obtain a uniform lipid-soluble encapsulating solution. The water-soluble components are mixed with the above encapsulating agent at a weight ratio of 1:2.5, purified water is added until complete dissolution, and the resulting mixed solution is placed in an ultrasonic emulsifier and ultrasonically emulsified at 500 W for 15 min to obtain a uniform water-soluble encapsulating solution. The two encapsulating solutions are separately introduced into a spray-drying apparatus for drying, the inlet air temperature is controlled at 190 °C and the outlet air temperature at 85 °C, and the dried powdery encapsulates are collected to obtain the lipid-soluble encapsulated powder and the water-soluble encapsulated powder.

[0061] 53. Mixing and granulation: the lipid-soluble encapsulated powder and the water-soluble encapsulated powder are introduced into a mixer and pre-mixed at low speed for 5 min. The filler and the binder in parts by weight are then added, and mixing is carried out at 800 r / min for 30 min until the system is uniform. The binder is added dropwise to the mixed system to prepare a wet mass; when the wet mass reaches a state in which it forms a ball when held by hand and readily disperses upon light pressure, liquid addition is stopped. The wet mass is passed through a 20 mesh standard sieve to obtain wet granules, the wet granules are spread flat on trays and dried in a hot-air drying oven at a constant temperature of 60 °C, and drying is stopped when DESCRIPTION the moisture content of the granules reaches 3.0%. The dried granules are then passed through an 18 mesh standard sieve for sizing, and the sized granules are collected for subsequent use.

[0062] 54. Final blending: the sized granules are introduced into a three-dimensional motion mixer, the lubricant is added, and mixing is performed at 500 r / min for 20 min. During the mixing process, the materials in the mixer are ensured to tumble fully, and the final blend is obtained after the system becomes uniform.

[0063] 55. Forming and packaging: the final blend is fed into a capsule-filling apparatus for filling into empty gelatin capsules. During filling, the fill weight is monitored in real time, and the fill-weight deviation is controlled within ±5%. After filling is completed, the capsules are subjected to aluminum-plastic blister packaging. A full-item inspection is carried out after packaging, and the finished product is obtained after inspection is passed.

[0064] In summary, the present embodiment adopts a high ratio within the formula range of the present invention. In the preparation process, all process parameters adopt the upper-limit values defined by the present invention. A fine 100 mesh sieve is used for the active functional components to improve the mixing uniformity of the high-ratio components; the dispersion speed, emulsification power, and processing time in the dual-phase microencapsulation process are the maximum values within the defined ranges to ensure the uniformity of the high-concentration encapsulating solution; the spray-drying temperature is adapted to the drying requirement of the high-concentration encapsulating solution; the mixing speed and time in mixing and granulation are increased to ensure sufficient mixing of the high-ratio materials; and the fill-weight deviation in forming and packaging is controlled within the defined range. Upon testing, the preparation obtained in the present embodiment has a lipid-soluble component oxidation rate of 0.9%, a water-soluble component retention rate of 98.8%, an in vitro dissolution rate DESCRIPTION of active ingredients at 45 min of 91.8%, and a retinal pigment epithelial cell survival rate after blue-light induction of 88.9%. All test indexes are excellent and are suitable for eye-care scenarios involving high-intensity blue-light exposure.

[0065] Comparative Example 1

[0066] The composition and ratio of the preparation in the present comparative example are as follows:

[0067] In parts by weight, the preparation contains only four active functional components: 2 parts of lutein, 4 parts of P-carotene, 15 parts of blueberry extract, and 10 parts of grape seed extract. The excipients are of the same types, ratios, and composition as those in Embodiment 1, namely 40 parts of a filler, 3 parts of a disintegrant, 2 parts of a binder, and 1 part of a lubricant, wherein the filler is a mixture of microcrystalline cellulose and pregelatinized starch at a weight ratio of 3:1, the disintegrant is crospovidone, the binder is an aqueous ethanol solution having a volume fraction of 50%, and the lubricant is a mixture of magnesium stearate and silicon dioxide at a weight ratio of 4:L The weight ratio of the active functional components to the excipients is 1:2.

[0068] The specific preparation method is as follows:

[0069] 51. Raw-material pretreatment: each active functional component and excipient is accurately weighed according to the above formula in parts by weight. All active functional components and excipients are jointly introduced into a sieving device and uniformly passed through an 80 mesh standard sieve. After the undersize is collected, the materials are mixed, sealed, and stored for subsequent use. The active functional components are not divided according to solubility.

[0070] 52. Mixing and granulation: the sieved mixed materials are introduced into a mixer, the filler and the binder in parts by weight are added, and mixing is carried out at 650 r / min for 22 min until the system is uniform. The binder DESCRIPTION is added dropwise to the mixed system to prepare a wet mass; when the wet mass reaches a state in which it forms a ball when held by hand and readily disperses upon light pressure, liquid addition is stopped. The wet mass is passed through a 20 mesh standard sieve to obtain wet granules, the wet granules are spread flat on trays and dried in a hot-air drying oven at a constant temperature of 55 °C, and drying is stopped when the moisture content of the granules reaches 2.5%. The dried granules are then passed through an 18 mesh standard sieve for sizing, and the sized granules are collected for subsequent use.

[0071] 53. Final blending: the sized granules are introduced into a three-dimensional motion mixer, the lubricant is added, and mixing is performed at 400 r / min for 15 min. When the system becomes uniform, mixing is stopped to obtain the final blend.

[0072] 54. Forming and packaging: the final blend is fed into a capsule-filling apparatus for filling into empty gelatin capsules, and the fill-weight deviation is controlled within ±4%. After filling is completed, the capsules are subjected to aluminum-plastic blister packaging. A full-item inspection is carried out after packaging, and the finished product is obtained after inspection is passed.

[0073] In summary, the present comparative example adopts a conventional quaternary core formula for an eye-care preparation. The four active ingredients meso-zeaxanthin, L-ergothioneine, saffron extract, and phosphatidylserine used in the present invention are not added; the active functional components are not divided into lipid-soluble and water-soluble groups; and the dual-phase microencapsulation process of the present invention is not adopted. The preparation method is the traditional direct mixing and granulation process and does not have the core innovative technical features of the present invention. Upon testing, the preparation obtained in the present comparative example has a lipid-soluble component DESCRIPTION oxidation rate as high as 15.6%, a water-soluble component retention rate of only 72.3%, an in vitro dissolution rate of active ingredients at 45 min of 65.7%, and a retinal pigment epithelial cell survival rate after blue-light induction of 65.2%. All test indexes are far lower than those of the embodiments of the present invention and cannot solve the core defects of conventional eye-care preparations.

[0074] Performance comparison table of embodiments and comparative example: DESCRIPTION

[0075] It can be seen from the above table that all three embodiments adopt the combination of the eight active functional components defined by the present invention, and dual-phase microencapsulation is carried out after grouping into lipid-soluble and water-soluble components. The process parameters are all within the ranges defined by the present invention, with differences only in formula ratios and specific process-parameter values. The test data show that the oxidation rate of lipid-soluble components in all three embodiments is below 1.5%, the retention rate of water-soluble components is above 97%, the in vitro dissolution rate of active ingredients at 45 min is above 88%, and the survival rate of retinal pigment epithelial cells after blue-light induction is above 82%. Among them, Embodiment 1, having the medium ratio, shows the best overall indexes; Embodiment 3, having the high-end ratio, is the next best; and Embodiment 2, having the low ratio, is suitable for basic eye-care needs. Comparative Example 1 adopts a conventional quaternary formula and process without grouping or encapsulation treatment; its oxidation rate of lipid-soluble components increases sharply, its retention rate of water-soluble components decreases significantly, and its dissolution rate of active ingredients and survival rate of retinal pigment epithelial cells are far lower than those of the embodiments of the present invention. This fully proves that, by combining precise compounding of eight active components with the dual-phase microencapsulation process, the present invention can effectively solve the core problems of easy loss of ingredients, low utilization efficiency, and poor eye-protective effect in conventional eye-care preparations, and that the components and process form a significant synergistic enhancement effect. DESCRIPTION

[0076] The above descriptions are merely preferred embodiments of the present invention and do not limit the present invention in any form. Although the present invention has been disclosed above by preferred embodiments, the same are not intended to limit the present invention. Any person skilled in the art may, without departing from the scope of the technical solutions of the present invention, make certain changes or modifications to the disclosed technical content so as to obtain equivalent embodiments with equivalent variations. However, any simple modification, equivalent variation, or modification made to the above embodiments according to the technical substance of the present invention without departing from the technical solutions of the present invention shall still fall within the scope of the technical solutions of the present invention.

Claims

CLAIMS1. A P-carotene-grape seed extract eye-care preparation for protecting the retina, characterized in that the preparation consists of active functional components and food-acceptable excipients; in parts by weight, the active functional components comprise 1-4 parts of lutein, 0.5-2 parts of meso-zeaxanthin, 2-6 parts of P-carotene, 8-25 parts of blueberry extract, 5-18 parts of grape seed extract, 0.2-1 part of L-ergothioneine, 0.5-3 parts of saffron extract, and 1-5 parts of phosphatidylserine;The food-acceptable excipients comprise a filler, a disintegrant, a binder, and a lubricant, wherein the weight ratio of the active functional components to the excipients is 1:1 to 1:4.

2. The P-carotene-grape seed extract eye-care preparation for protecting the retina according to claim 1, characterized in that the lutein is derived from natural marigold and has a content of >5%; the meso-zeaxanthin has a content of >80%, and the weight ratio of meso-zeaxanthin to lutein is 1:2 to 1:4.

3. The P-carotene-grape seed extract eye-care preparation for protecting the retina according to claim 1, characterized in that the P-carotene is derived from natural fermentation and has a content of >10%; the blueberry extract is derived from blueberry fruits and has an anthocyanin content of >25%, and the weight ratio of P-carotene to blueberry extract is 1:4 to 1:5.

4. The P-carotene-grape seed extract eye-care preparation for protecting the retina according to claim 1, characterized in that the grape seed extract is derived from grape seeds and has a proanthocyanidin content of >95%; the L-ergothioneine is derived from biological fermentation and has a purity of >99%, and the weight ratio of grape seed extract to L-ergothioneine is 50: 1 to 90:1.

5. The P-carotene-grape seed extract eye-care preparation for protecting the retina according to claim 1, characterized in that the saffron extract is derived from saffron stigmas and has a crocin content of >3%; the phosphatidylserine is derived from soybeans and has a content of >50%, andCLAIMS the weight ratio of saffron extract to phosphatidylserine is 1:2 to 1:6.

6. The P-carotene-grape seed extract eye-care preparation for protecting the retina according to claim 1, characterized in that the excipients comprise 30-60 parts of a filler, 2-5 parts of a disintegrant, 1-3 parts of a binder, and 0.5-2 parts of a lubricant.

7. The P-carotene-grape seed extract eye-care preparation for protecting the retina according to claim 6, characterized in that the filler is a mixture of microcrystalline cellulose and pregelatinized starch at a weight ratio of 3:1, the disintegrant is crospovidone, the binder is an aqueous ethanol solution having a volume fraction of 50%, and the lubricant is a mixture of magnesium stearate and silicon dioxide at a weight ratio of 4:1.

8. The P-carotene-grape seed extract eye-care preparation for protecting the retina according to claim 1, characterized in that the active functional components are divided into lipid-soluble components and water-soluble components and are subjected to microencapsulation separately; the lipid-soluble components comprise lutein, meso-zeaxanthin, P-carotene, and phosphatidylserine, and the water-soluble components comprise blueberry extract, grape seed extract, L-ergothioneine, and saffron extract.

9. The P-carotene-grape seed extract eye-care preparation for protecting the retina according to claim 1, characterized in that the preparation method thereof comprises the following steps:

51. Raw-material pretreatment: weighing each active functional component and excipient according to the formula in parts by weight; passing each active functional component separately through an 80-100 mesh sieve and the excipients through an 80 mesh sieve; dividing the active functional components into lipid-soluble components and water-soluble components, and reserving the same for subsequent use;52. Dual -phase microencapsulation: mixing the lipid-soluble components with a mixture of maltodextrin and gum arabic at a weight ratio of 2:1 at aCLAIMS weight ratio of 1:2 to 1:3, dissolving the same in anhydrous ethanol, and subjecting the same to high-speed dispersion at 10000-12000 r / min for 15-20 min to obtain a lipid-soluble encapsulating solution; mixing the water-soluble components with the encapsulating agent at a weight ratio of 1:1.5 to 1:2.5, dissolving the same in purified water, and subjecting the same to ultrasonic emulsification at 300-500 W for 10-15 min to obtain a water-soluble encapsulating solution; spray-drying the two encapsulating solutions separately to obtain the corresponding encapsulated powders;53. Mixing and granulation: mixing the two encapsulated powders, adding the filler and binder, and mixing at 500-800 r / min for 15-30 min until uniform; adding an aqueous ethanol solution having a volume fraction of 50% to prepare a wet mass, passing the wet mass through a 20 mesh sieve to obtain wet granules, drying the wet granules with hot air at 50-60 °C until the moisture content is <3%, and passing the dried granules through an 18 mesh sieve for sizing;54. Final blending: placing the sized dry granules and the lubricant into a three-dimensional motion mixer and mixing at 300-500 r / min for 10-20 min until uniform, thereby obtaining a final blend;55. Forming and packaging: filling the final blend into empty gelatin capsules, controlling the fill-weight deviation within ±5%, performing aluminum-plastic blister packaging, and obtaining the finished product after inspection is passed.

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