Microparticles of bitter melon extract with blood sugar regulating properties

Abstract

A microparticle of bitter melon extract with blood sugar-regulating properties, comprising a microparticle body that is a solid spherical structure formed by granulation of an effective amount of bitter melon extract uniformly mixed with a pharmaceutically acceptable binder; wherein the bitter melon extract comprises at least charantin, momordicin and momordica peptides and wherein the structure of the particle body is designed to ensure good flowability and uniform, controlled release of the active ingredients in the gastrointestinal tract.

Description

Technical area

[0001] The utility model relates to a particulate structure, in particular a microparticle of bitter melon extract with blood sugar regulating properties, which is particularly suitable for products for blood sugar regulation and for the treatment of associated metabolic disorders. Technology in the background

[0002] Diabetes is a widespread chronic metabolic disease characterized primarily by hyperglycemia due to impaired insulin secretion or insulin sensitivity. Persistent hyperglycemia leads to long-term damage to multiple organs, making stable blood glucose control a crucial aspect of preventative healthcare.

[0003] Traditionally, people have sought natural plant sources to support blood sugar regulation. Research shows that extracts from bitter melon (Momordica charantia) possess several bioactive properties that have a particularly pronounced effect on lowering blood sugar levels.

[0004] The active ingredients in natural plant extracts, particularly protein or peptide substances (such as bitter melon peptides), often face challenges such as low stability and susceptibility to degradation and inactivation due to environmental factors like humidity, temperature, and light exposure. Furthermore, pure extracts can be prematurely released or degraded in the digestive tract due to stomach acid or digestive enzymes, resulting in insufficient bioavailability and diminished health benefits. Therefore, the industry requires improved technology capable of effectively protecting the active ingredients in bitter melon extracts while ensuring stable, efficient, and sustained release. Content of the utility model

[0005] The inventor thoroughly investigated the aforementioned problems. After several prototypes and refinement cycles, this utility model was finally developed.

[0006] The present utility model relates to a microparticle of bitter melon extract with blood sugar-regulating properties, consisting of: a microparticle body, which is a solid spherical structure formed by granulating an effective amount of bitter melon extract uniformly mixed with a pharmaceutically acceptable binder; wherein the bitter melon extract comprises at least charantin, momordicin and momordica peptides, and wherein the structure of the particle body is designed to ensure good flowability and a uniform, controlled release of the active ingredients in the gastrointestinal tract.

[0007] In a preferred embodiment of the present utility model, the bitter melon extract microparticles with blood sugar-regulating properties additionally comprise a protective layer. This protective layer encases the outer surface of the microparticle body to prevent external environmental factors from impairing the activity of the microparticle core. This improves the storage stability of the microparticle structure and can be designed as an enteric coating or as a delayed-release layer. This further improves the absorption rate and duration of action of the bitter melon extract in the human body.

[0008] The patented feature of the bitter melon extract particles with blood sugar-regulating effect in this patent lies in their particle structure, which provides physical protection to the active components while enabling a uniform, controlled release. Experimental verifications confirm that excellent blood sugar regulation is achieved through the synergistic interaction of the following several mechanisms: Inhibition of α-amylase: Reduces the breakdown of carbohydrates to disaccharides; Inhibition of glucosidase: Reduces the breakdown of disaccharides to monosaccharides (glucose); Promotion of glucose oxidase activity: Facilitates the conversion of monosaccharides (glucose); Promotion of glycogen accumulation: Facilitates the conversion of glucose to glycogen for storage. Description of the attached drawings Fig. Figure 1 is a three-dimensional sectional view of the present utility model. Fig. Figure 2 is a top view of the present utility model. Fig. 3 is a sectional view of Fig. 2 along the intersection line AA. Fig. Figure 4 is a schematic diagram of the present utility model, which is contained in a capsule. Fig. Figure 5 is a diagram illustrating the blood glucose regulation mechanism of the bitter melon extract particles of the present utility model. Fig. Figure 6 is an experimental diagram of the glucose oxidase inhibition rate of the bitter melon extract particles of the present utility model. Fig. Figure 7 is a diagram of the experimental α-amylase inhibition rate of the bitter melon extract particles of the present utility model. Fig. Figure 8 is a diagram of the glucose oxidase activity of the bitter melon extract particles of the present utility model. Fig. 9 is a test data sheet on glycogen accumulation for the microparticles of bitter melon extract in this utility model.

[0009] In the characters: 10 particle bodies; 11 Bitter melon extract; 111 Charantin; 112 Momordicin; 113 Momordica peptides; 12 binders; 20 Protective coating; 30 capsules; 40 Diagram of the blood glucose regulation mechanism; 41 α-Amylase-inhibiting effect; 42 Glucosidase-inhibiting effect; 43 Increase in glucose oxidase activity; 44 Promotion of glycogen accumulation; 50 Experimental table on the glucosidase inhibition rate; 60 Experimental table on the α-amylase inhibition rate; 70 Experimental table on glucose oxidase activity; 80 Experimental table on glycogen accumulation Detailed description

[0010] The following further explanation is given in conjunction with the schematic representations illustrating preferred embodiments of the present utility model, so that those skilled in the art can implement the utility model on the basis of the description contained herein.

[0011] Firstly, the present utility model refers to the Fig. 1 and Fig. 2 on microparticles of bitter melon extract which have blood sugar regulating effects and comprise: a microparticle body 10 and a protective layer 20.

[0012] The microparticle body 10 comprises: bitter melon extract 11 and a binder 12, wherein the bitter melon extract 11 is an extract containing active components such as bitter substances 111 (bitters), charantin 112 (charantin), and bitter melon polypeptides 113 (10,000-Dalton polypeptides) with a molecular weight of approximately 10,000 Daltons. Preferably, the content of bitter substance 111 in the bitter melon extract 11 is at least 6.0%, the content of charantin 112 is at least 5.0%, and the content of 10,000-Dalton polypeptides 113 is at least 1.5%. Furthermore, the in vitro bioactivity indicators of bitter melon extract are: Glucose Dialysis Delay Index (GDRI) of 35-50 and glucose uptake EC50 of 5-9 mg ml-1.The microparticle body 10 is a solid, spherical particle formed by uniformly mixing the bitter melon extract 11 with a binder 12 and has an average particle size in the range of 100 to 800 micrometers. The binder 12 comprises medically safe materials such as starch, cellulose derivatives (e.g., hydroxypropyl methylcellulose), polyvinylpyrrolidone (PVP), or other polymers of pharmaceutical or food-grade quality. The binder serves to agglomerate the bitter melon extract powder 11, thus forming the particle body 10 with a specific physical structure.

[0013] With reference to the Fig. 1 and Fig. 3. The protective layer 20 is applied to the outer surface of the microparticle body 10. This protective layer 20 can be made of materials such as shellac, gelatin, or various polymers (e.g., acrylic resin, ethylcellulose). The protective layer can function as an enteric coating or as a delayed-release coating. Its functions are: 1. Improving particle stability and preventing moisture absorption or oxidation; 2. Controlling the release properties to enable gradual release in the intestinal tract and maximize the bioavailability of active ingredients such as bitter melon peptides.

[0014] The bitter melon extract particles with blood sugar-regulating effects can be administered directly orally. Alternatively, as described in Fig. Figure 4 shows that a predetermined amount of particles are encapsulated in capsule 30 for ingestion.

[0015] See Fig. , which the in Fig. The mechanism of blood glucose regulation is illustrated in Figure 5. The efficacy of this invention manifests itself in several ways: First, the bitter melon extract particles act in the digestive tract. By inhibiting α-amylase, they reduce the breakdown of carbohydrates to disaccharides. Simultaneously, by inhibiting glucosidase, they decrease the conversion of disaccharides to monosaccharides (glucose), thus delaying glucose uptake at its source. Second, at the cellular metabolic level, the microparticles of bitter melon extract accelerate the conversion of glucose to energy (adenosine triphosphate) by promoting glucose oxidase activity and facilitate the conversion of excess glucose to glycogen for storage by promoting glycogen accumulation. This results in comprehensive blood glucose regulation.

[0016] To validate the efficacy of the microparticles from bitter melon extract in this utility model, in vitro experiments were carried out with the following results: (1) Glycosidase inhibition test: See Fig. 6, which illustrates the glucose glycosidase inhibition rate (experimental diagram 50), and Fig. Figure 7 illustrates the α-amylase inhibition rate (experimental diagram 60). The experimental results show that the microparticles from bitter melon extract exhibit an inhibitory effect on glucosidase (approx. 8.3%) and α-amylase (approx. 7.3%). These microparticles ensure that the active ingredient works effectively in the digestive tract, thus delaying glucose absorption. (2) Test to promote glucose metabolism: See Fig. 8 to illustrate glucose oxidase activity (diagram 70) and Fig.Figure 9 illustrates glycogen accumulation (Diagram 80). In a palmitic acid-induced cell model, the addition of bitter melon extract microparticles resulted in a significant increase in: glucose oxidase activity: activity increased to approximately 111%; glycogen accumulation: accumulation increased to approximately 105%.

[0017] These results demonstrate that the bitter melon extract microparticles used in this novel application not only delay carbohydrate absorption but also promote the cellular utilization and storage of glucose, thus achieving multimechanistic regulation of blood glucose levels. The microparticle structure ensures a stable delivery of the active ingredients to their target sites, thereby enabling these superior physiological effects.

[0018] The structure of the above-mentioned specific embodiments offers the following advantages: 1. Improved stability and protection: The structure of the microparticle body 10 provides physical protection for active components such as bitter melon peptides, thus effectively preventing their degradation and inactivation by environmental influences. 2. Optimized absorption and duration of action: The outer protective layer 20 (which can be designed as an enteric-coated or sustained-release layer) enables a controlled release of the active ingredients. This facilitates their stable release in the intestinal tract, thereby improving bioavailability and extending the duration of action. 3. Synergistic Multi-Mechanism Action: Experimental evidence confirms that this composition achieves comprehensive and superior blood glucose regulation by inhibiting carbohydrate-digesting enzymes (α-amylase inhibition rate approx. 7.3%, glucosidase inhibition rate approx. 8.3%), increasing glucose oxidase activity (activity increased to approximately 111%), and promoting glycogen accumulation (accumulation increased to approximately 105%), thereby achieving comprehensive and excellent blood glucose regulation. 4. Uniform and efficient release: The microparticle structure enables a uniform and controllable release of the active ingredients.

Claims

[1] A microparticle of bitter melon extract with blood glucose-regulating properties, comprising a microparticle body that is a solid spherical structure formed by granulation of an effective amount of bitter melon extract uniformly mixed with a pharmaceutically acceptable binder; wherein the bitter melon extract comprises at least charantin, momordicin and momordica peptides and wherein the structure of the particle body is designed to ensure good flowability and uniform, controlled release of the active substances in the gastrointestinal tract. [2] A microparticle made of bitter melon extract with blood sugar regulating properties according to claim 1, further comprising a protective layer that envelops the outside of the microparticle body. [3] A microparticle of bitter melon extract with blood sugar regulating properties according to claim 2, wherein the protective layer is an enteric coating or a delayed-release coating. [4] A microparticle of bitter melon extract with blood sugar regulating properties according to claim 1, wherein the molecular weight of the bitter melon peptide contained in the bitter melon extract is about 10,000 Daltons. [5] A microparticle of bitter melon extract with blood sugar regulating properties according to claim 1, wherein the bitter melon extract contains not less than 6.0% charantin, not less than 5.0% momordicin and not less than 1.5% momordic peptide. [6] A microparticle made of bitter melon extract with blood sugar regulating properties according to claim 1, wherein the average particle size of the microparticle body is in the range of 100 micrometers to 800 micrometers. [7] A microparticle of bitter melon extract with blood sugar regulating properties according to claim 1, wherein the binder is selected from the group consisting of starch, cellulose derivatives, polyvinylpyrrolidone (PVP) or other polymers of pharmaceutical or food grade.

Images