Blood sugar reducing composition containing mulberry leaf extract and preparation method thereof

Abstract

The composition is prepared from folium mori, radix astragali, radix puerariae, rhizoma dioscoreae, poria cocos and pericarpium citri reticulatae in specific parts by weight, and the core of the composition is that the contents of key active ingredients 1-deoxynojirimycin and total flavonoids in the folium mori raw material are quantitatively screened; the preparation method adopts a step-by-step water extraction technology and a low-temperature concentration technology. The invention relates to the technical field of health food and traditional Chinese medicine pharmacy. By performing standardized quality control on the core raw materials and combining scientific compound compatibility and an optimized preparation process, the problems that in the prior art, due to the fact that the quality of the raw materials is not uniform, the product effect is unstable, and due to the simple formula, the action target spot is single are solved, and the prepared composition has the stable and efficient auxiliary blood sugar reducing effect and is suitable for being used for preparing the traditional Chinese medicine composition. And the composition can synergistically improve the metabolic state of the body, is high in safety and has remarkable popularization and application values.

Description

Technical Field

[0001] This invention relates to the field of health food and traditional Chinese medicine pharmaceutical technology, specifically a hypoglycemic composition containing mulberry leaf extract and its preparation method. Background Technology

[0002] With the continued rise in the global incidence of hyperglycemia and diabetes, effective postprandial blood glucose management has become a crucial issue in safeguarding public health. Against this backdrop, the discovery of safe and effective hypoglycemic active substances from natural plants has become a focus of attention for modern medicine and the health industry. Mulberry leaves, as a plant with a long history of being both a food and a medicine, have attracted considerable attention for their potential in regulating blood glucose. Modern pharmacological research reveals that 1-deoxynojirimycin (DNJ), unique to mulberry leaves, can effectively inhibit α-glucosidase and delay carbohydrate absorption, while its rich flavonoid compounds help with antioxidation and improve insulin resistance.

[0003] However, existing technologies for applying mulberry leaves to the development of hypoglycemic products generally face several deep-seated technical bottlenecks. The primary problem lies in the uncontrolled quality of raw materials. Existing products often overlook the decisive influence of factors such as mulberry variety and harvesting season on the content of key active ingredients such as DNJ and total flavonoids, leading to inconsistent effects between batches and significantly reduced stability and predictability of efficacy. Furthermore, many formulations are overly simplistic, focusing only on a single hypoglycemic target and failing to consider the holistic perspective of Traditional Chinese Medicine to comprehensively regulate the complex state of metabolic disorders. Simultaneously, their preparation processes are relatively crude, failing to optimize for the physicochemical properties of different medicinal materials in the compound formula, easily resulting in the loss of volatile or heat-sensitive components, thus weakening the overall efficacy of the product. Therefore, developing a novel hypoglycemic composition with controllable raw material standards, scientifically formulated combinations, and refined preparation processes to overcome the limitations of existing technologies has become an urgent technical challenge to be solved in this field.

[0004] Therefore, the present invention provides a hypoglycemic composition containing mulberry leaf extract and its preparation method to solve the above problems. Summary of the Invention

[0005] To address the shortcomings of existing technologies, this invention provides a hypoglycemic composition containing mulberry leaf extract and its preparation method, thus solving the aforementioned problems.

[0006] To achieve the above objectives, the present invention provides the following technical solution: a hypoglycemic composition containing mulberry leaf extract, made from the following raw materials in parts by weight: 10-30 portions of mulberry leaves; 10-20 parts of Astragalus membranaceus; 10-20 portions of kudzu root; 5-15 servings of yam; 5-15 parts of Poria cocos; 3-10 portions of dried tangerine peel; The mulberry leaf raw material was tested before use and found to have a 1-deoxynojirimycin (DNJ) content of not less than 0.5% and a total flavonoid content of not less than 1.0% on a dry weight basis.

[0007] The present invention further optimizes the above technical solution, wherein the composition is made from the following raw materials in parts by weight: Mulberry leaves 20 parts; Astragalus membranaceus 15 parts; Kudzu root 15 parts; Dioscorea opposita 10 parts; Poria cocos 10 parts; Tangerine peel 5 parts.

[0008] This invention specifies the preferred source of raw materials: the mulberry leaves are those harvested after the first frost in late autumn from the mulberry trees found in the Jiangsu and Zhejiang regions. The mulberry leaves at this stage have the highest accumulation of active ingredients. The astragalus is the dried root of *Astragalus membranaceus*, the kudzu root is the dried root of *Pueraria lobata*, and the poria is the dried sclerotium of the fungus *Poria cocos*, to ensure the authenticity and effectiveness of the raw materials.

[0009] The compositions of the present invention can be applied in various dosage forms, including oral liquids, granules, tablets, capsules, or solid beverages.

[0010] The present invention also provides a method for preparing the above-mentioned hypoglycemic composition containing mulberry leaf extract, comprising the following steps: S100. Raw material screening and pretreatment: Weigh each raw material according to the formula weight; Detect the mulberry leaf raw material using high performance liquid chromatography (HPLC) and screen out mulberry leaves that meet the standards of 1-deoxynojirimycin (DNJ) content not less than 0.5% and total flavonoid content not less than 1.0%; Wash and crush all qualified raw materials to 20-40 mesh for later use. S200, stepwise water extraction: S210. Place mulberry leaves, astragalus, kudzu root, yam, and poria in an extraction tank, add 8-12 times the total weight of the raw materials in purified water, and heat under reflux for 1-1.5 hours. S220. Add dried tangerine peel to the above extraction tank and continue to heat and reflux for 20-30 minutes. S230, repeat steps S210 and S220 once, and combine the two extracts; S300, Concentration: The combined extracts are filtered, and the filtrate is concentrated under reduced pressure at a vacuum of -0.06 to -0.08 MPa and a temperature of 50 to 70°C to obtain a concentrated extract with a relative density of 1.10 to 1.25 g / cm³. S400, Drying and Shaping: The concentrated extract is spray-dried to obtain a dry powder of the composition, and pharmaceutically acceptable excipients are added as needed to prepare a predetermined dosage form.

[0011] The present invention optimizes the process parameters in the preparation method: the heating reflux extraction temperature in step S210 is controlled at 90-100℃. In step S220, dried tangerine peel is added last to reduce the loss of its volatile components (such as hesperidin and limonene) and ensure its efficacy in regulating qi and resolving dampness.

[0012] In step S400, the excipient that can be added is at least one of maltodextrin, lactose, or microcrystalline cellulose, and the amount added is 30-100% of the dry matter weight of the concentrated extract, so as to improve the flowability and formability of the dry powder.

[0013] The method may further include, after step S400, performing wet granulation, tableting or aseptic filling on the prepared formulation according to its dosage form characteristics, and finally sterilizing it. Beneficial effects

[0014] This invention provides a hypoglycemic composition containing mulberry leaf extract and its preparation method. Compared with the prior art, it has the following advantages: (1) This invention fundamentally solves the problem of efficacy fluctuations caused by uneven raw material quality by quantitatively screening the key active ingredients DNJ and total flavonoids in the core raw material mulberry leaves. This ensures that the product has a high degree of standardization and quality stability, making its hypoglycemic effect clear, reliable and repeatable. At the same time, it breaks through the limitations of single-component effects by scientifically combining the principal ingredient mulberry leaves with multiple complementary medicinal and edible ingredients such as astragalus and kudzu root to construct a multi-target, multi-pathway synergistic system. This composition can not only inhibit sugar absorption, but also provide overall conditioning from the perspective of tonifying qi and strengthening the spleen and improving metabolism, achieving comprehensive health benefits that address both the symptoms and the root cause. Its effect is far superior to that of a single mulberry leaf or a simple formula combination.

[0015] (2) The refined preparation process, including stepwise water extraction and low-temperature concentration, employed in this invention is optimized for the characteristics of each component in the compound, effectively avoiding the loss of heat-sensitive and volatile components (such as the volatile oil in tangerine peel), maximizing the preservation of the overall bioactivity of the composition, and thus ensuring the full efficacy of the final product. Ultimately, since the selected raw materials are all highly safe medicinal and edible substances, this invention provides a highly effective health intervention solution suitable for long-term use, demonstrating significant market application prospects and practical value. Detailed Implementation

[0016] The technical solutions in the embodiments of the present invention will be clearly and completely described below. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention. Example

[0017] Preparation of a hypoglycemic composition granule containing mulberry leaf extract S100, Raw material screening and pretreatment: Weigh out 20kg of mulberry leaves, 15kg of astragalus, 15kg of kudzu root, 10kg of yam, 10kg of poria cocos, and 5kg of dried tangerine peel.

[0018] The mulberry leaf raw material was tested by high performance liquid chromatography (HPLC), and the DNJ content was found to be 0.58% (w / w) and the total flavonoid content was 1.3% (w / w), both of which met the standards.

[0019] All qualified raw materials were washed with purified water, dried at 60℃, then crushed, passed through a 30-mesh sieve, and mixed evenly for later use.

[0020] S200, stepwise water extraction: S210: Place mulberry leaves, astragalus, kudzu root, yam, and poria (total 70kg) into a 1000L multi-functional extraction tank, add 10 times the amount, i.e., 700L of purified water, turn on the jacket steam heating to 95℃, and perform reflux extraction for 1.5 hours.

[0021] S220: Add 5 kg of dried tangerine peel powder to the extraction tank and continue reflux extraction at 95℃ for 30 minutes.

[0022] S230: Discharge the first extract, add 8 times the amount of purified water (560L) to the residue again, and repeat steps S210 and S220 once. Combine the two extracts.

[0023] S300, Concentrated: The combined extracts were filtered through a 200-mesh filter cloth, and the filtrate was pumped into a vacuum concentration tank. The solution was concentrated under vacuum conditions of -0.07 MPa and 60°C until the relative density of the concentrate reached 1.20 g / cm³, thus obtaining a concentrated extract.

[0024] S400, Drying and Molding: The above concentrated extract was spray-dried (inlet air temperature 180°C, outlet air temperature 80°C) to obtain approximately 28 kg of dry powder of the composition.

[0025] Mix the dry powder with 14 kg of maltodextrin (accounting for 50% of the dry matter weight of the extract), granulate using a wet method, dry and granulate, and then package into 5 g granules per bag and seal them. Example

[0026] Preparation of a hypoglycemic composition tablet containing mulberry leaf extract S100, Raw material screening and pretreatment: Weigh out 10 kg of mulberry leaves, 10 kg of astragalus root, 10 kg of kudzu root, 5 kg of yam, 5 kg of poria cocos, and 3 kg of dried tangerine peel.

[0027] HPLC analysis showed that the DNJ content of the mulberry leaf raw material was 0.51% and the total flavonoid content was 1.1%, which met the standards.

[0028] All raw materials are cleaned, dried, and crushed through a 20-mesh sieve.

[0029] S200, stepwise water extraction: S210: Add 40 kg of mulberry leaves, astragalus, kudzu root, yam, and poria cocos to 8 times the amount of purified water, i.e., 320 L, and heat to 90 °C for reflux extraction for 1 hour.

[0030] S220: Add 3kg of dried tangerine peel powder and continue reflux extraction for 20 minutes.

[0031] S230: Repeat the extraction once and combine the two extracts.

[0032] S300, Concentrated: The filtered and combined extracts were concentrated under reduced pressure at a vacuum of -0.06 MPa and a temperature of 50 °C to obtain a concentrated extract with a relative density of 1.10 g / cm³.

[0033] S400, Drying and Molding: The concentrated extract was spray-dried to obtain approximately 15 kg of dry powder. Microcrystalline cellulose was added to the dry powder as an excipient, mixed thoroughly, and then compressed into tablets of 0.5 g each. Example

[0034] Preparation of an oral liquid containing mulberry leaf extract for lowering blood sugar S100, Raw material screening and pretreatment: Weigh out 30kg of mulberry leaves, 20kg of astragalus, 20kg of kudzu root, 15kg of yam, 15kg of poria cocos, and 10kg of dried tangerine peel.

[0035] HPLC analysis showed that the DNJ content of the mulberry leaf raw material was 0.65% and the total flavonoid content was 1.5%, which met the standards.

[0036] All raw materials are cleaned, dried, and pulverized through a 40-mesh sieve.

[0037] S200, stepwise water extraction: S210: Add 12 times the amount of purified water (1200L) of mulberry leaves, astragalus, kudzu root, yam, and poria cocos (total 100kg) to 1200L of purified water, heat to 100℃ and reflux for 1.5 hours.

[0038] S220: Add 10kg of dried tangerine peel powder and continue reflux extraction for 30 minutes.

[0039] S230: Repeat the extraction once and combine the two extracts.

[0040] S300, Concentrated: The filtered and combined extracts were concentrated under reduced pressure at a vacuum of -0.08 MPa and a temperature of 70 °C to obtain a concentrated extract with a relative density of 1.25 g / cm³.

[0041] S400, Molding: The concentrated extract was diluted with purified water to a fixed volume, and an appropriate amount of sweetener and preservative was added. The pH value was adjusted, and the mixture was stirred evenly. The mixture was then aseptically filled to produce 10 mL oral liquid vials.

[0042] Comparative Example 1: Lack of compound formulation According to the preparation method in Example 1, only 20 kg of standard mulberry leaf raw material was used for extraction and preparation, and the other auxiliary materials and process parameters were the same.

[0043] Comparative Example 2: Mulberry leaf raw materials were not screened. According to the formula and preparation method of Example 1, 20 kg of ordinary commercially available mulberry leaves without DNJ and total flavonoid content testing (the DNJ content was only 0.21% and the total flavonoid content was 0.6%) were used, and the other raw materials and process parameters were the same.

[0044] Comparative Example 3: Using conventional integrated extraction process The formula of Example 1 was followed, but the extraction method was changed: all raw materials (75 kg), including dried tangerine peel, were added to the extraction tank at once, along with 10 times the amount of water, and the mixture was refluxed and extracted twice, each time for 2 hours. The remaining process parameters were the same as in Example 1.

[0045] Comparative Example 4: A simplified three-herb formula was used. The formula uses three medicinal ingredients: mulberry leaves, dried tangerine peel, and yam. Following the process described in Example 1, 20 kg of mulberry leaves, 10 kg of yam, and 5 kg of dried tangerine peel meeting the standards were weighed and prepared.

[0046] Experimental Example: Evaluation of the hypoglycemic effect of the composition of the present invention Experimental animals: SPF-grade male SD rats, weighing 180-220g.

[0047] Modeling method: After feeding rats with a high-sugar, high-fat diet for 4 weeks, a type 2 diabetic rat model was established by intraperitoneal injection of streptozotocin (STZ) 35 mg / kg. A fasting blood glucose level ≥11.1 mmol / L was used as the criterion for successful modeling.

[0048] Grouping and administration: The successfully modeled rats were randomly divided into 8 groups, with 10 rats in each group.

[0049] Normal control group: Normal rats were given an equal volume of physiological saline.

[0050] Model control group: diabetic rats were given an equal volume of physiological saline.

[0051] Positive control group: Metformin hydrochloride (100 mg / kg) was administered.

[0052] Example 1 group: Administered the granules prepared in Example 1 (calculated based on human equivalent dose).

[0053] Comparative Example 1: The granules prepared in Comparative Example 1 were administered.

[0054] Comparative Example 2: The granules prepared in Comparative Example 2 were administered.

[0055] Comparative Example 3: The granules prepared in Comparative Example 3 were administered.

[0056] Comparative Example 4: The granules prepared in Comparative Example 4 were administered.

[0057] Each group was given the medication by gavage once daily for four consecutive weeks.

[0058] Detection indicators and methods: Fasting blood glucose (FBG) was measured in rats in each group before administration and 4 weeks after administration.

[0059] An oral glucose tolerance test (OGTT) was performed after the last administration. After fasting for 12 hours, rats were given glucose (2 g / kg) by gavage. Blood glucose levels were measured by tail vein sampling at 0, 30, 60, and 120 minutes, and the area under the blood glucose curve (AUC) was calculated.

[0060] Experimental results: The experimental results are shown in Table 1 below.

[0061] Table 1. Comparison of blood glucose levels and glucose tolerance in rats of different groups (x̄ ± s, n=10)

[0062] Where x̄ is the sample mean and s is the sample standard deviation.

[0063] As can be seen from Table 1: Compared with the model control group, the Example 1 group significantly reduced the area under the curve of fasting blood glucose and postprandial blood glucose in diabetic rats (P<0.01), and its hypoglycemic effect was comparable to that of the positive control drug metformin, and even numerically superior.

[0064] Example 1 group vs. Comparative Example 1 group: The hypoglycemic effect of Example 1 group was significantly better than that of Comparative Example 1 group which contained only mulberry leaves, proving that the compound formulation of the present invention has a significant synergistic effect.

[0065] Example 1 vs. Comparative Example 2: Comparative Example 2, which used unscreened inferior mulberry leaf raw materials, showed no significant difference in blood sugar lowering effect compared to the model group, highlighting the necessity and inventiveness of the present invention in quantitatively screening the active ingredients of mulberry leaf raw materials.

[0066] Example 1 vs. Comparative Example 3: Example 1, which uses a stepwise extraction process, has a significantly better blood sugar lowering effect than Comparative Example 3, which uses a conventional integrated extraction process. This shows that the optimized process of the present invention can better preserve active ingredients and improve product efficacy.

[0067] Example 1 vs. Comparative Example 4: The complete formula of six herbs in Example 1 is significantly better than that in Comparative Example 4, which contains only three herbs, proving that the formula of the present invention is more scientific and comprehensive.

[0068] In summary, the hypoglycemic composition prepared by this invention through strict quality control of raw materials, scientific compound formulation, and optimized preparation process has a clear, stable, and efficient hypoglycemic effect. Its comprehensive effect is superior to existing technologies or simplified technical solutions, and it has significant progressiveness and practical value.

[0069] Furthermore, any content not described in detail in this specification is existing technology known to those skilled in the art.

[0070] It should be noted that, in this document, relational terms such as "first" and "second" are used only to distinguish one entity or operation from another, and do not necessarily require or imply any such actual relationship or order between these entities or operations. Furthermore, the terms "comprising," "including," or any other variations thereof are intended to cover non-exclusive inclusion, such that a process, method, article, or apparatus that comprises a list of elements includes not only those elements but also other elements not expressly listed, or elements inherent to such process, method, article, or apparatus.

[0071] Although embodiments of the invention have been shown and described, it will be understood by those skilled in the art that various changes, modifications, substitutions and alterations can be made to these embodiments without departing from the principles and spirit of the invention, the scope of which is defined by the appended claims and their equivalents.

Claims

1. A hypoglycemic composition containing mulberry leaf extract, characterized in that, Made from the following parts by weight of raw materials: 10-30 portions of mulberry leaves; 10-20 parts of Astragalus membranaceus; 10-20 portions of kudzu root; 5-15 servings of yam; 5-15 parts of Poria cocos; 3-10 portions of dried tangerine peel; The mulberry leaf raw material was tested before use and found to have a 1-deoxynojirimycin content of not less than 0.5% and a total flavonoid content of not less than 1.0% on a dry weight basis.

2. The hypoglycemic composition containing mulberry leaf extract according to claim 1, characterized in that, Made from the following parts by weight of raw materials: 20 portions of mulberry leaves; 15 portions of Astragalus membranaceus; 15 portions of kudzu root; 10 portions of yam; 10 parts of Poria cocos; Five portions of dried tangerine peel.

3. The hypoglycemic composition containing mulberry leaf extract according to claim 1, characterized in that, The mulberry leaves mentioned are those of the Hu mulberry tree harvested after the first frost in late autumn.

4. The hypoglycemic composition containing mulberry leaf extract according to claim 1, characterized in that, The Astragalus membranaceus is the dried root of Astragalus membranaceus, the Pueraria lobata is the dried root of Pueraria lobata, and the Poria cocos is the dried sclerotium of the fungus Poria cocos.

5. The hypoglycemic composition containing mulberry leaf extract according to claim 1, characterized in that, The dosage form of the composition is oral liquid, granules, tablets, capsules, or solid beverage.

6. A method for preparing a hypoglycemic composition containing mulberry leaf extract as described in any one of claims 1-5, characterized in that, Includes the following steps: S100. Raw material screening and pretreatment: Weigh the corresponding weights of each raw material; use high performance liquid chromatography to detect the mulberry leaf raw materials and screen out the mulberry leaves that meet the standards for 1-deoxynojirimycin and total flavonoid content; wash and crush all qualified raw materials to 20-40 mesh for later use. S200, stepwise water extraction: S210. Place mulberry leaves, astragalus, kudzu root, yam, and poria in an extraction tank, add 8-12 times the total weight of purified water, and heat under reflux for 1-1.5 hours. S220. Add dried tangerine peel to the above extraction tank and continue to heat and reflux for 20-30 minutes. S230, repeat steps S210 and S220 once, and combine the extracts from both times; S300, Concentration: The combined extracts are filtered, and the filtrate is concentrated under reduced pressure at a vacuum of -0.06 to -0.08 MPa and a temperature of 50 to 70°C to obtain a concentrated extract with a relative density of 1.10 to 1.25 g / cm³. S400, Drying and Shaping: The concentrated extract is spray-dried to obtain a dry powder of the composition, and pharmaceutically acceptable excipients are added as needed to prepare a predetermined dosage form.

7. The method for preparing a hypoglycemic composition containing mulberry leaf extract according to claim 6, characterized in that, The heating reflux extraction temperature in step S210 is controlled at 90-100℃.

8. The method for preparing a hypoglycemic composition containing mulberry leaf extract according to claim 6, characterized in that, The addition of dried tangerine peel at the end of step S200 is intended to reduce the loss of its volatile components.

9. The method for preparing a hypoglycemic composition containing mulberry leaf extract according to claim 6, characterized in that, In step S400, the added excipient is at least one of maltodextrin, lactose, or microcrystalline cellulose, and the amount added is 30-100% of the dry matter weight of the concentrated extract.

10. The method for preparing a hypoglycemic composition containing mulberry leaf extract according to claim 6, characterized in that, The method further includes, after step S400, performing wet granulation, tableting or aseptic filling on the prepared formulation according to its dosage form characteristics, and finally sterilizing it.

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