Microcrystalline structure of bitter melon extract with blood sugar regulating effect

Abstract

This invention provides a wild bitter melon extract granule that effectively protects the active ingredients of the wild bitter melon extract, improves its storage stability and bioavailability, and achieves excellent blood glucose regulation through multiple pathways such as inhibition of sugar-degrading enzymes, promotion of glucose oxidation, and hepatic glycogen accumulation, making it particularly suitable for the health management of diabetic patients and people at risk of hyperglycemia. [Solution] A fine particle of wild bitter melon extract having a blood glucose regulating effect, comprising a core-shaped spherical particle body 10 and a protective layer 20 covering the outside of the particle body, wherein the particle body is formed by uniformly mixing an effective amount of wild bitter melon extract 11 and a pharmaceutically acceptable binder 12 and granulating it, and the wild bitter melon extract contains at least bitter substances 111, bitter melon glycosides 112 and bitter melon polypeptides 113.

Description

Technical Field

[0001] The present invention relates to a particulate structure, and particularly to a particulate structure of Momordica charantia extract having a blood glucose regulating effect as a health product applicable to blood glucose regulation and related metabolic diseases.

Background Art

[0002] Diabetes is one of the chronic metabolic diseases spreading worldwide, mainly presenting symptoms of hyperglycemia, which is caused by insulin secretion deficiency or functional damage. Since hyperglycemia causes long-term damage to multiple organs, stabilizing blood glucose is an important step in health management.

[0003] People have been seeking substances derived from natural plants to assist in blood glucose management over a long period. According to research, Momordica charantia extract has various biological activities, and particularly shows remarkable effects in blood glucose lowering.

[0004] However, the active ingredients contained in natural plant extracts, especially proteins or peptide (e.g., polypeptide) substances, often face the problems of low stability and being easily decomposed and inactivated by environmental factors such as humidity, temperature, and light. Moreover, pure extracts may be released or decomposed early by the action of gastric acid or digestive enzymes in the digestive tract, resulting in insufficient bioavailability and affecting health effects. Therefore, the industry needs an improved technology that can effectively protect the active components of Momordica charantia extract and exert stable, highly efficient, and sustainable effects.

Summary of the Invention

Problems to be Solved by the Invention

[0005] In view of the above problems to be solved, we conceived the present invention, conducted discussions and prototypes, and after many modifications and improvements, we propose the present invention.

Means for Solving the Problems

[0006] This invention proposes a microgranular structure of wild bitter melon extract that has a blood glucose regulating effect. The wild bitter melon extract microgranular structure has a core-shaped microgranular structure body, which is formed by uniformly mixing an effective amount of wild bitter melon extract with a pharmaceutically acceptable binder and granulating it. The wild bitter melon extract contains at least bitter substances, bitter melon glycosides, and bitter melon polypeptides, and the structure of the microgranular structure body is suitable for achieving a good fluid, uniform, and controllable release effect of active ingredients in the digestive tract.

[0007] In one preferred embodiment of the present invention, a microcrystalline structure of wild bitter melon extract having a blood glucose regulating effect is proposed. The wild bitter melon extract microcrystalline structure further comprises a protective layer that coats the outside of the microcrystalline structure body, thereby preventing the influence of external environmental factors on the core activation of the microcrystalline structure body, thereby improving the storage stability of the microcrystalline structure, and allowing it to be designed as an enteric-coated or sustained-release coating layer, further increasing the absorption rate and duration of action of the wild bitter melon extract in the human body. [Effects of the Invention]

[0008] The primary objective of this invention, which involves the microcrystalline structure of bitter melon extract, is to provide physical protection to the active ingredient, enabling uniform and controllable release. Experimental verification has shown that the following multiple mechanisms work synergistically to achieve excellent blood glucose regulation: Inhibition of α-amylase reduces the breakdown of carbohydrates into disaccharides. Inhibition of glucosidase reduces the breakdown of disaccharides into monosaccharides (glucose). Activation of glucose oxidase promotes the conversion of monosaccharides (glucose). In hepatic glycogen accumulation, it promotes the accumulation of hepatic glycogen converted from glucose. [Brief explanation of the drawing]

[0009] [Figure 1] Figure 1 is a three-dimensional cross-sectional view of the present invention. [Figure 2] Figure 2 is a plan view of the present invention. [Figure 3]Figure 3 is a cross-sectional view of the present invention along line AA in Figure 2. [Figure 4] Figure 4 is a schematic diagram of the gel sac filling method of the present invention. [Figure 5] Figure 5 is a diagram illustrating the blood glucose regulation mechanism based on the microparticle structure of the bitter melon extract according to this invention. [Figure 6] Figure 6 is an experimental chart showing the inhibition rate of the microparticle structure of the bitter melon extract of this invention against glucosidase. [Figure 7] Figure 7 is an experimental chart showing the inhibition rate of the granular structure of the bitter melon extract of this invention against α-amylase. [Figure 8] Figure 8 is an experimental diagram showing the activation of glucose oxidase by the microparticle structure of the bitter melon extract according to the present invention. [Figure 9] Figure 9 is an experimental chart showing liver glycogen accumulation due to the microparticle structure of the bitter melon extract according to the present invention. Forms for implementing a utility model

[0010] We will now further describe the present invention in conjunction with drawings of preferred embodiments of the present invention so that those skilled in the art may carry out the present invention in accordance with the description herein.

[0011] First, referring to Figures 1 and 2, the microparticle structure of bitter melon extract with blood glucose regulating effect according to the present invention comprises a microparticle structure body 10 and a protective layer 20.

[0012] The fine particle structure body 10 contains a wild bitter melon extract 11 and a binder 12, and the wild bitter melon extract 11 refers to an extract containing active ingredients such as bitter substances 111 (Bitters), bitter melon glycosides 112 (Charantin), and bitter melon polypeptides 113 (10,000 Dalton Polypeptides) with a molecular weight of approximately 10,000 Daltons. More preferably, the wild bitter melon extract 11 contains 6.0% or more of bitter substances 111, 5.0% or more of bitter melon glycosides 112, and 1.5% or more of bitter melon polypeptides 113 with a molecular weight of approximately 10,000 Daltons. Furthermore, the in vitro bioactivity indicators of the bitter melon extract 11 correspond to a glucose dialysis delay index (GDRI) of 35-50 and a glucose uptake EC50 of 5-9 mg / mL. The fine particle body 10 is in the shape of a solid heart and is formed by uniformly mixing the bitter melon extract 11 and the binder 12 and granulating them, with an average particle size range between 100 microns and 800 microns. The binder 12 consists of a pharmaceutically acceptable material, such as starch, a cellulose derivative (hydroxypropyl methylcellulose, etc.), polyvinylpyrrolidone (PVP), or other pharmaceutical or food-grade polymer, and plays the role of agglomerating the bitter melon extract 11 powder to form a fine particle structure 10 having a specific physical structure.

[0013] As shown in Figures 1 and 3, the protective layer 20 covers the outside of the microparticle structure body 10. The protective layer 20 can be selected from shellac varnish, gelatin, or various polymers (such as acrylic resin or ethylcellulose), and can be designed as an enteric coating layer or a sustained-release coating layer. The protective layer 20 plays the roles of: 1) enhancing the stability of the microparticles to prevent moisture and oxidation, and 2) controlling the release characteristics to gradually release the microparticle structure in the intestines and maximize the bioavailability of active ingredients such as bitter melon polypeptide.

[0014] When taking the granular structure of bitter melon extract, which has a blood glucose regulating effect, in addition to direct oral administration, it is possible to fill a predetermined amount of the granular structure into a gel sac 30 and swallow the gel sac 30, as shown in Figure 4.

[0015] Referring to Figure 5, which shows a diagram of the blood glucose regulation mechanism 40, the effects of this invention are evident in many ways. First, the microcrystalline structure of the bitter melon extract acts on the digestive tract, reducing the breakdown of carbohydrates into disaccharides through its inhibitory effect on α-amylase 41, and reducing the breakdown of disaccharides into monosaccharides (glucose) through its inhibitory effect on glucosidase 42, thereby fundamentally slowing down glucose absorption. Second, in cellular metabolism, the microcrystalline structure of the bitter melon extract accelerates the conversion of glucose into energy (adenosine triphosphate) through its promoting effect on glucose oxidase activation 43, and accumulates liver glycogen converted from excess glucose through its promoting effect on liver glycogen accumulation 44, thereby achieving the effect of comprehensively regulating blood glucose levels.

[0016] To verify the effect of the wild bitter melon extract microparticle structure of this invention, we conducted in vitro experiments, and the results are shown below.

[0017] (1) Experiment on inhibition of sugar-degrading enzymes: Refer to Experimental Chart 50 in Figure 6, which shows the inhibition rate against glucosidase, and Experimental Chart 60 in Figure 7, which shows the inhibition rate against α-amylase. The experimental results show that the granular structure of the bitter melon extract has an inhibitory effect of approximately 8.3% against glucosidase and approximately 7.3% against α-amylase. The granular structure of the bitter melon extract can be said to have its active ingredients act effectively in the digestive tract and slow down glucose absorption.

[0018] (2) Glucose metabolism promotion test: Refer to experimental chart 70 in Figure 8 showing glucose oxidase activation, and experimental chart 80 in Figure 9 showing hepatic glycogen accumulation. Compared to the control group, the palmitic acid-induced cell model with added bitter melon extract granules significantly promoted glucose oxidase activation, increasing the activity to approximately 111%, and promoted hepatic glycogen accumulation, increasing the accumulated amount to approximately 105%.

[0019] These results verify that the micro-particle structure of the Momordica charantia extract used in the present invention not only delays glucose absorption, but also promotes the utilization and accumulation of glucose by cells, achieving blood glucose regulation through multiple mechanisms. This micro-particle structure enables the active ingredients to reach the action site stably, thereby exerting these excellent physiological functions.

[0020] Due to the structure of the above specific embodiments, the following beneficial effects may occur.

[0021] 1. Improvement in stability and protection: The structure of the micro-particle structure body 10 provides physical protection for activated ingredients such as Momordica charantia polypeptide, effectively preventing decomposition or inactivation due to environmental factors.

[0022] 2. Optimization of absorption and action time: By controlling the release of active ingredients through the external protective layer 20 (which can be designed as an enteric coating layer or a sustained-release coating layer) and stably releasing them in the intestine, the bioavailability and action time are increased.

[0023] 3. Synergistic action of multiple mechanisms: According to experimental verification, the present invention can achieve a comprehensive and excellent blood glucose regulation effect through the inhibition of carbohydrase (the inhibition rate against α-amylase is about 7.3%, and the inhibition rate against glucosidase is about 8.3%), the promotion of glucose oxidase activation (increasing the activity to about 111%), and the promotion of liver glycogen accumulation (the accumulation amount increases to about 105%).

[0024] 4. Uniform and highly efficient release: The micro-particle structure realizes the effect of uniformly and controllably releasing active ingredients.

Explanation of symbols

[0025] 10-Microparticle structure; 11-Bitter melon extract; 111-Bitter substance; 112-Bitter melon glycoside; 113-Bitter melon polypeptide; 12-Binding agent; 20-Protective layer; 30-Coagulant; 40-Diagram of blood glucose regulation mechanism; 41-Inhibitory effect on α-amylase; 42-Inhibitory effect on glucosidase; 43-Promoting effect on glucose oxidase activation; 44-Promoting effect on hepatic glycogen accumulation; 50-Diagram showing the inhibition rate of glucosidase; 60-Diagram showing the inhibition rate of α-amylase; 70-Diagram showing glucose oxidase activation; 80-Diagram showing hepatic glycogen accumulation

Claims

1. The product has a core-shaped granular structure, which is formed by uniformly mixing and granulating an effective amount of bitter melon extract and a pharmaceutically acceptable binder; the bitter melon extract contains at least bitter substances, bitter melon glycosides, and bitter melon polypeptides; and the structure of the granular structure is suitable for achieving good fluidity, uniformity, and controllable release of active ingredients in the digestive tract. A micro-particle structure of bitter melon extract with blood glucose regulating properties.

2. The microparticle structure of bitter melon extract having a blood glucose regulating effect according to claim 1, further comprising a protective layer covering the outside of the microparticle structure body.

3. The microparticle structure of bitter melon extract having a blood glucose regulating effect according to claim 2, characterized in that the protective layer is an enteric-coated coating layer or a sustained-release coating layer.

4. The microparticle structure of the wild bitter melon extract having a blood glucose regulating effect according to claim 1, characterized in that the molecular weight of the bitter melon polypeptide contained in the wild bitter melon extract is approximately 10,000 daltons.

5. The bitter substance content of the aforementioned bitter melon extract is 6.0% or more, the bitter melon glycoside content is 5.0% or more, and the bitter melon polypeptide content is 1.5% or more. The microparticle structure of bitter melon extract having a blood glucose regulating effect as described in feature 1.

6. The microparticle structure of bitter melon extract having a blood glucose regulating effect according to claim 1, characterized in that the average particle size of the microparticle structure itself is in the range of 100 microns and 800 microns.

7. The binder is selected from a combination of starch, cellulose derivatives, polyvinylpyrrolidone (PVP), or other pharmaceutical or food-grade polymers. The microparticle structure of bitter melon extract having a blood glucose regulating effect as described in feature 1.

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