Rare ginsenoside compound preparation with enzymatic hydrolysis activity and application of rare ginsenoside compound preparation in tonifying qi and blood and warming and tonifying kidney yang

Abstract

The invention provides a rare ginsenoside compound preparation with enzymatic hydrolysis activity, the rare ginsenoside compound preparation comprises ginsenoside, astragalus polysaccharide, Chinese angelica ferulic acid and icariin according to a mass ratio of (3-7): (2.5-4): (1.5-3): 1, the ginsenoside comprises ginsenoside Compound K and ginsenoside Rg3, and the mass ratio of the ginsenoside Compound K to the ginsenoside Rg3 is (0.5-1.5): 1. The preparation can promote the hematopoietic function, improve blood circulation, tonify the kidney and strengthen yang, thereby effectively relieving symptoms caused by deficiency of qi and blood and deficiency of the kidney, and improving the health level of a human body.

Description

Technical Field

[0001] The present invention belongs to the technical field of medical and health care preparations, and particularly relates to an enzymatically active rare ginsenoside compound preparation and its application in replenishing both qi and blood and warming and tonifying kidney yang. Background Art

[0002] Qi and blood deficiency and kidney deficiency are common sub-health conditions in Traditional Chinese Medicine (TCM) clinical practice, with widespread impacts on human health. Qi and blood deficiency can lead to symptoms such as sallow complexion, dizziness, palpitations, insomnia, and limb numbness, impacting quality of life and work efficiency. Kidney deficiency can cause weakness in the waist and knees, tinnitus and deafness, decreased sexual function, and frequent and urgent urination. It can also accelerate aging, weaken immunity, and increase the risk of disease.

[0003] Currently, there are numerous products on the market that treat Qi and blood deficiency and kidney deficiency, but most suffer from limited efficacy and slow onset. While traditional Chinese medicine formulas can provide some therapeutic benefits, they are complex, difficult to control, have a poor taste, and suffer from low patient compliance. While some chemically synthesized drugs work quickly, they often come with numerous side effects, and long-term use can pose potential health risks. Therefore, developing a compound preparation that can simultaneously regulate Qi and blood and the kidneys is of great practical significance. Summary of the Invention

[0004] The purpose of the present invention is to provide an enzymatically active rare ginsenoside compound preparation, which, through a reasonable ingredient ratio and a specific preparation method, fully exerts the synergistic effect of each component, achieves effective conditioning of qi, blood and kidneys, and at the same time improves the safety and bioavailability of the preparation.

[0005] To achieve the above object, the present invention adopts the following technical solutions:

[0006] A rare ginsenoside compound preparation with enzymatic hydrolysis activity comprises ginsenosides, astragalus polysaccharide, angelica ferulic acid and icariin in a mass ratio of (3-7): (2.5-4): (1.5-3): 1, wherein the ginsenosides comprise ginsenoside Compound K and ginsenoside Rg3, and the mass ratio of ginsenoside Compound K to ginsenoside Rg3 is (0.5-1.5): 1.

[0007] Optionally, the ginsenoside Compound K and the ginsenoside Rg3 are obtained by hydrolyzing total ginsenosides with β-glucosidase, and the total ginsenosides include ginsenoside Rb1, ginsenoside Rc and ginsenoside Rd in a mass ratio of (0.8-1.2):(0.8-1.2):1.

[0008] Optionally, the hydrolysis temperature is 30-60° C., the pH value is 4.5-6.5, and the hydrolysis time is 5-15 h.

[0009] Optionally, during the hydrolysis process, the dosage ratio of the β-glucosidase to the total ginsenosides is 1-10 U / mg.

[0010] Optionally, during the hydrolysis process, the usage ratio of the β-glucosidase to the total ginsenosides is 5 U / mg.

[0011] Optionally, during the hydrolysis process, the concentration of the total ginsenosides is 5-10 mg / mL.

[0012] Optionally, during the hydrolysis process, the concentration of the total ginsenosides is 7 mg / mL.

[0013] Optionally, during the hydrolysis process, the total ginsenosides include ginsenoside Rb1, ginsenoside Rc and ginsenoside Rd in a mass ratio of 1:1:1.

[0014] Optionally, the mass ratio of the ginsenoside, the astragalus polysaccharide, the angelica ferulic acid and the icariin is 5:3:2:1.

[0015] Optionally, the mass ratio of the ginsenoside Compound K to the ginsenoside Rg3 is 1:1.

[0016] Beneficial effects

[0017] (1) The enzymatically active rare ginsenoside compound preparation of the present invention achieves simultaneous conditioning of Qi, blood, and kidney function by combining ginsenosides, astragalus polysaccharides, angelica ferulic acid, and icariin in specific proportions. Ginsenoside Compound K and ginsenoside Rg3 possess multiple biological activities and synergize with astragalus polysaccharides, angelica ferulic acid, and icariin to promote hematopoiesis, improve blood circulation, and tonify the kidneys and enhance yang, thereby effectively alleviating symptoms caused by Qi and blood deficiency and kidney deficiency, and improving human health.

[0018] (2) β-glucosidase was used to hydrolyze ginsenosides to prepare ginsenoside Compound K and ginsenoside Rg3, which improved the yield and purity of the active ingredients. At the same time, the conditions such as temperature, pH value, time, enzyme-to-substrate ratio, and ginsenoside concentration during the hydrolysis process were optimized to ensure the efficient hydrolysis reaction and the stability of product quality, making the quality of the compound preparation controllable and the production process more scientific and reasonable. DETAILED DESCRIPTION

[0019] One embodiment of the present invention provides a compound preparation of rare ginsenosides with enzymatic hydrolysis activity, comprising ginsenosides, astragalus polysaccharides, angelica ferulic acid, and icariin in a mass ratio of (3-7): (2.5-4): (1.5-3): 1, wherein the ginsenosides include ginsenoside Compound K and ginsenoside Rg3, and the mass ratio of ginsenoside Compound K to ginsenoside Rg3 is (0.5-1.5): 1. By combining ginsenosides, astragalus polysaccharides, angelica ferulic acid, and icariin in specific proportions, simultaneous conditioning of qi, blood, and kidneys is achieved. Ginsenoside Compound K and ginsenoside Rg3 have multiple biological activities and synergistically act with astragalus polysaccharides, angelica ferulic acid, and icariin to enhance the body's immunity, promote hematopoietic function, improve blood circulation, and tonify the kidneys and strengthen yang, thereby effectively alleviating symptoms caused by qi and blood deficiency and kidney deficiency, and improving human health.

[0020] For example, ginsenoside Compound K and ginsenoside Rg3 are highly active components of ginsenosides. Ginsenoside Compound K exhibits excellent anti-tumor, anti-inflammatory, and immunomodulatory effects, while ginsenoside Rg3 demonstrates excellent anti-fatigue and cardiovascular health benefits. Astragalus polysaccharide has a potent Qi-tonifying effect, enhancing immunity, promoting hematopoiesis, and fueling Qi and blood production. Angelica ferulic acid invigorates and replenishes blood, improving circulation and promoting smoother Qi and blood flow. Icariin nourishes the kidneys and strengthens yang, enhancing kidney function. Combining these four ingredients in specific proportions can synergize in multiple ways, achieving the effect of harmonizing Qi, blood, and kidney function. When ginsenosides, astragalus polysaccharide, angelica ferulic acid, and icariin are within the aforementioned mass ratio range, the synergistic effects of the components are fully realized, resulting in the compound preparation achieving optimal results in regulating Qi, blood, and kidney function.

[0021] Optionally, the mass ratio of ginsenoside, astragalus polysaccharide, angelica ferulic acid and icariin can be 3:2.5:1.5:1, 4:3:2:1, 5:3:2:1, 6:4:3:1, etc. It is understood that the mass ratio of ginsenoside, astragalus polysaccharide, angelica ferulic acid and icariin can also be other options within the range of (3-7): (2.5-4): (1.5-3):1.

[0022] Preferably, the mass ratio of ginsenosides, astragalus polysaccharides, angelica ferulic acid, and icariin is 5:3:2:1. At this ratio, the synergistic effect between the ingredients is maximized, significantly enhancing the compound preparation's effects on regulating qi, blood, and the kidneys, and exhibiting superior efficacy compared to other ratios.

[0023] Optionally, in the ginsenosides, the mass ratio of ginsenoside Compound K to ginsenoside Rg3 is 0.5:1, 0.8:1, 1:1, 1.2:1, or 1.5:1.

[0024] Preferably, the mass ratio of ginsenoside Compound K to ginsenoside Rg3 is 1:1. When the mass ratio of the two is 1:1, their synergistic effect in the compound preparation can be maximized, showing the best comprehensive effects in regulating immunity, resisting fatigue, improving kidney function, etc., further enhancing the overall efficacy of the compound preparation.

[0025] In some embodiments, ginsenoside Compound K and ginsenoside Rg3 are obtained by hydrolyzing total ginsenosides with β-glucosidase, and the total ginsenosides include ginsenoside Rb1, ginsenoside Rc, and ginsenoside Rd in a mass ratio of (0.8-1.2): (0.8-1.2): 1. The preparation of Compound K and Rg3 by hydrolyzing total ginsenosides with β-glucosidase can improve the yield and purity of these two active ingredients, and is more efficient and environmentally friendly than traditional extraction methods. At the same time, limiting the mass ratio of Rb1, Rc, and Rd in total ginsenosides helps to ensure the stability of the hydrolysis process and the consistency of the product, thereby ensuring that the quality of the compound preparation is controllable.

[0026] Optionally, the mass ratio of ginsenoside Rb1, ginsenoside Rc, and ginsenoside Rd in the total ginsenosides may be 0.8:0.8:1, 1:1:1, or 1.2:1.2:1. It is understood that the mass ratio of ginsenoside Rb1, ginsenoside Rc, and ginsenoside Rd may also be selected within the range of (0.8-1.2):(0.8-1.2):1.

[0027] Preferably, the mass ratio of ginsenoside Rb1, ginsenoside Rc, and ginsenoside Rd is 1:1:1. This specific mass ratio makes the composition of total ginsenosides more balanced, and under the action of β-glucosidase, they can be more stably and efficiently hydrolyzed to produce the target products ginsenoside Compound K and ginsenoside Rg3, further improving the stability and controllability of the compound preparation.

[0028] Furthermore, the conditions such as temperature, pH value, time, enzyme-to-substrate ratio, and total ginsenoside concentration during the hydrolysis process were optimized to ensure the efficient hydrolysis reaction and the stability of product quality, making the quality of the compound preparation controllable and the production process more scientific and reasonable.

[0029] In some embodiments, the hydrolysis temperature is 30-60°C, the pH value is 4.5-6.5, and the hydrolysis time is 5-15 hours. Within this temperature and pH range, the activity of β-glucosidase can be fully exerted, the hydrolysis reaction can be carried out efficiently, and at the same time, enzyme inactivation or product degradation caused by excessively high temperatures or inappropriate pH values ​​can be avoided, thereby ensuring the yield and quality of ginsenoside Compound K and ginsenoside Rg3. For example, under these hydrolysis conditions, the yield of ginsenoside Compound K can reach more than 50%, and the yield of ginsenoside Rg3 can reach more than 30%.

[0030] Optionally, the hydrolysis temperature may be 30° C., 35° C., 40° C., 45° C., 50° C., 55° C., 60° C., etc. It is understood that the hydrolysis temperature may also be other suitable selections within the range of 30-60° C.

[0031] Optionally, the pH value may be 4.5, 4.8, 5, 5.5, 5.8, 6, 6.5, etc. It is understood that the pH value may also be other suitable selections within the range of 4.5-6.5.

[0032] Optionally, the hydrolysis time can be 5 h, 8 h, 10 h, 13 h, 15 h, etc. It is understandable that the hydrolysis time can also be other suitable selections within the range of 5-15 h.

[0033] In some embodiments, during the hydrolysis process, the ratio of β-glucosidase to ginsenosides is 1-10U / mg. The appropriate ratio of enzyme to substrate is the key to ensuring that the hydrolysis reaction is fully carried out. When the ratio is within this range, it is possible to avoid waste of enzyme and reduce production costs while ensuring hydrolysis efficiency. Optionally, during the hydrolysis process, the ratio of β-glucosidase to ginsenosides is 1U / mg, 3U / mg, 5U / mg, 7U / mg, 10U / mg, etc.

[0034] Preferably, during the hydrolysis process, the ratio of β-glucosidase to total ginsenosides is 5 U / mg. This ratio achieves an optimal balance between yield and efficiency in the hydrolysis reaction, enabling the production of high-purity and high-yield ginsenoside Compound K and ginsenoside Rg3 at a low cost, further improving the quality and economic benefits of the compound preparation.

[0035] In some embodiments, the concentration of total ginsenosides during the hydrolysis process is 5-10 mg / mL. Controlling the concentration of total ginsenosides within this range enables the hydrolysis reaction to be carried out in a suitable system, avoiding incomplete reaction due to excessively high concentration or affecting production efficiency due to excessively low concentration, thereby ensuring the stability of the hydrolysis process and the uniformity of product quality. For example, during the hydrolysis process, the concentration of total ginsenosides is 5 mg / mL, 6 mg / mL, 7 mg / mL, 8 mg / mL, 9 mg / mL, 10 mg / mL, etc.

[0036] Preferably, the concentration of total ginsenosides during the hydrolysis process is 7 mg / mL. At this concentration, the various indicators of the hydrolysis reaction perform optimally, better ensuring the yield and purity of ginsenoside Compound K and ginsenoside Rg3, thereby providing more reliable assurance for the quality of the compound preparation.

[0037] Another embodiment of the present invention provides a method for preparing the above-mentioned enzymatically active rare ginsenoside compound preparation, comprising the steps of uniformly mixing ginsenosides, astragalus polysaccharide, angelica ferulic acid, and icariin. It will be appreciated that after uniformly mixing ginsenosides, astragalus polysaccharide, angelica ferulic acid, and icariin, suitable excipients may be added to prepare a corresponding dosage form. For example, the enzymatically active rare ginsenoside compound preparation may be in the form of a capsule, tablet, or the like.

[0038] Example 1

[0039] In this embodiment, the preparation method of the enzymatically active rare ginsenoside compound preparation is as follows:

[0040] S101: Ginsenoside Rb1, ginsenoside Rc, and ginsenoside Rd are weighed in a 1:1:1 mass ratio to prepare a 7 mg / mL total ginsenoside solution. β-glucosidase is added at a ratio of 5 U / mg to total ginsenosides at 45°C and a pH of 5.5 for 12 hours to hydrolyze the solution. After the reaction, ginsenosides are separated and purified to obtain ginsenosides, including Compound K and ginsenoside Rg3 in a 1:1 mass ratio.

[0041] S102: Weigh the ginsenosides, astragalus polysaccharide, angelica ferulic acid and icariin prepared above in a mass ratio of 5:3:2:1, mix them thoroughly and evenly, and prepare them into capsules using a conventional preparation process.

[0042] Example 2

[0043] Compared with Example 1, the difference of Example 2 is that the mass ratio of ginsenoside, astragalus polysaccharide, angelica ferulic acid and icariin in S102 is 3:2.5:1.5:1.

[0044] Example 3

[0045] Compared with Example 1, the difference of Example 3 is that the mass ratio of ginsenoside, astragalus polysaccharide, angelica ferulic acid and icariin in S102 is 7:4:3:1.

[0046] Example 4

[0047] Compared with Example 1, Example 4 is different in that the mass ratio of ginsenoside Rb1, ginsenoside Rc and ginsenoside Rd in S101 is 0.8:0.8:1.

[0048] Example 5

[0049] Compared with Example 1, Example 5 is different in that the mass ratio of ginsenoside Rb1, ginsenoside Rc and ginsenoside Rd in S101 is 1.2:1.2:1.

[0050] Comparative Example 1

[0051] Compared with Example 1, the difference of Comparative Example 1 is that the mass ratio of ginsenoside, astragalus polysaccharide, angelica ferulic acid and icariin in S102 is 2:1:1:1.

[0052] Comparative Example 2

[0053] Compared with Example 1, the difference of Comparative Example 2 is that the mass ratio of ginsenoside, astragalus polysaccharide, angelica ferulic acid and icariin in S102 is 8:5:5:1.

[0054] Comparative Example 3

[0055] Compared with Example 1, the difference of Comparative Example 3 is that the ginsenosides are ginsenosides obtained by extracting ginseng from ginseng using a conventional ethanol extraction method.

[0056] Blank example

[0057] In the blank example, compared with Example 1, the preparation only contained excipients.

[0058] Test Case

[0059] Mice were tested using the preparations in the Examples, Comparative Examples, and Blank Examples. The hematopoietic function indices and renal function indices are shown in the following table.

[0060]

[0061] As can be seen from the above table, the enzymatically active rare ginsenoside compound preparation of the present invention has a significant effect of harmonizing qi, blood and kidney through a scientific and reasonable ingredient ratio and preparation method. Compared with the comparative example and the blank example, it has obvious advantages in promoting hematopoietic function and improving kidney function.

[0062] The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention. Any modifications, equivalent substitutions and improvements made within the spirit and principles of the present invention should be included in the scope of protection of the present invention.

[0063] For those skilled in the art, according to the concept of the present invention, there may be changes in the specific implementation methods and application scope. In summary, the content of this specification should not be understood as limiting the present invention.

Claims

1. A rare ginsenoside compound preparation with enzymatic activity, characterized in that: It comprises ginsenosides, astragalus polysaccharides, angelica ferulic acid and icariin in a mass ratio of (3-7): (2.5-4): (1.5-3): 1, wherein the ginsenosides comprise ginsenoside Compound K and ginsenoside Rg3, and the mass ratio of the ginsenoside Compound K to the ginsenoside Rg3 is (0.5-1.5):

1.

2. The enzymatically active rare ginsenoside compound preparation according to claim 1, characterized in that: The ginsenoside Compound K and the ginsenoside Rg3 are obtained by hydrolyzing total ginsenosides with β-glucosidase, and the total ginsenosides include ginsenoside Rb1, ginsenoside Rc and ginsenoside Rd in a mass ratio of (0.8-1.2): (0.8-1.2):

1.

3. The enzymatically active rare ginsenoside compound preparation according to claim 2, characterized in that: The hydrolysis temperature is 30-60° C., the pH value is 4.5-6.5, and the hydrolysis time is 5-15 hours.

4. The enzymatically active rare ginsenoside compound preparation according to claim 2, wherein: During the hydrolysis process, the dosage ratio of the β-glucosidase to the total ginsenosides is 1-10 U / mg.

5. The enzymatically active rare ginsenoside compound preparation according to claim 4, characterized in that: During the hydrolysis process, the dosage ratio of the β-glucosidase to the total ginsenosides is 5 U / mg.

6. The enzymatically active rare ginsenoside compound preparation according to claim 2, wherein: During the hydrolysis process, the concentration of the total ginsenosides is 5-10 mg / mL.

7. The enzymatically active rare ginsenoside compound preparation according to claim 6, characterized in that: During the hydrolysis process, the concentration of the total ginsenosides was 7 mg / mL.

8. The enzymatically active rare ginsenoside compound preparation according to claim 2, wherein: During the hydrolysis process, the total ginsenosides include ginsenoside Rb1, ginsenoside Rc and ginsenoside Rd in a mass ratio of 1:1:

1.

9. The enzymatically active rare ginsenoside compound preparation according to any one of claims 1 to 8, characterized in that: The mass ratio of the ginsenoside, the astragalus polysaccharide, the angelica ferulic acid and the icariin is 5:3:2:

1.

10. The enzymatically active rare ginsenoside compound preparation according to any one of claims 1 to 8, characterized in that: The mass ratio of the ginsenoside Compound K to the ginsenoside Rg3 is 1:1.

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