CN117838721A - Composition with synergistic long-acting blood glucose level regulation function and preparation method thereof - Google Patents
Composition with synergistic long-acting blood glucose level regulation function and preparation method thereof Download PDFInfo
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Abstract
The invention discloses a composition with synergistic long-acting blood glucose level regulation function and a preparation method thereof. The composition combines hyperbranched polylysine with ascorbic acid, the antioxidant activity of the hyperbranched polylysine can inhibit the oxidation of the ascorbic acid, the hyperbranched polylysine can adsorb ascorbic acid anions through electrostatic interaction, can be slowly degraded into lysine in vivo and slowly release the ascorbic acid, the rapid metabolism of the lysine and the ascorbic acid is avoided, and simultaneously the absorption and the utilization of the lysine in vivo can be promoted by the ascorbic acid, so that the lysine and the ascorbic acid can play a long-acting synergistic hypoglycemic effect. In addition, the combination of the two can also improve the level of antioxidant in the body and inhibit oxidative stress. The composition can realize the auxiliary treatment of diabetes by simultaneously reducing blood sugar and inhibiting oxidative stress, has definite components, simple composition, safety and innocuity, and has good application value and potential economic benefit.
Description
Technical Field
The invention belongs to the technical field of biological medicines, and particularly relates to a composition with a synergistic long-acting blood glucose level regulation function and a preparation method thereof.
Background
Diabetes is a chronic metabolic disease characterized by hyperglycemia, and increased oxidative stress and reduced antioxidant levels are the leading causes of diabetes. At present, diabetes mellitus has become the most common chronic disease in China. According to statistics, the number of diabetics in China exceeds 1.4 hundred million, and the first place of the world is occupied. Moreover, with the acceleration of the pace of life, people gradually develop bad lifestyles and eating habits, the incidence of diabetes rises year by year, and the ill population has a tendency to be younger.
At present, diabetes is difficult to radically cure, and long-term administration is required. The oral hypoglycemic medicine mainly comprises acarbose, metformin, glimepiride and the like. However, these drugs have unavoidable side effects on the liver, kidney and other organs of patients after long-term use, and the single drug therapy often has poor efficacy, and the dosage needs to be increased as the course of the disease is prolonged. The oral hypoglycemic drugs are used in combination with products for assisting in reducing blood sugar, so that the curative effect of the drugs can be improved, and the dosage can be reduced. However, most of the auxiliary hypoglycemic products on the market are composed of various traditional Chinese medicine components, the components are complex, and the specific components are not clear. Moreover, most of the auxiliary hypoglycemic products have insignificant effects, and some even have side effects. Based on the above, it is necessary to develop an auxiliary hypoglycemic product which has definite components, simple composition, long-acting hypoglycemic effect and safety and no toxicity for the auxiliary treatment of diabetes.
Disclosure of Invention
Aiming at the problems, the invention provides a composition with synergistic long-acting regulation of blood sugar level, which has definite ingredients, is safe and nontoxic, and can realize long-acting synergistic sugar control.
The technical scheme adopted by the invention is as follows:
a composition with synergistic long-acting regulation of blood sugar level mainly comprises hyperbranched polylysine and ascorbic acid as active ingredients.
The degradation product of the hyperbranched polylysine in vivo is human essential amino acid lysine. Lysine is safe and nontoxic, has antioxidant activity, and can promote insulin synthesis and secretion, and improve insulin receptor expression, thereby reducing blood sugar level and improving sensitivity of organism to insulin.
The hyperbranched polylysine can be slowly degraded into lysine in vivo, and can avoid rapid metabolism of lysine by organisms.
The ascorbic acid disclosed by the invention is a natural antioxidant, is widely used in various fruits and vegetables, is safe and nontoxic, can promote synthesis of glycogen, promote the body to fully utilize glucose, and improve the sensitivity of the body to insulin, so that the blood sugar level is reduced.
The composition combines hyperbranched polylysine with ascorbic acid, and the hyperbranched polylysine has antioxidant activity, can inhibit the oxidation of the ascorbic acid, and simultaneously, the hyperbranched polylysine is taken as a cation, and can adsorb ascorbic acid anions through electrostatic interaction, so that the ascorbic acid can be slowly released in vivo, and the ascorbic acid is prevented from being rapidly metabolized.
The composition combines hyperbranched polylysine with ascorbic acid, and the ascorbic acid can promote the absorption and utilization of lysine which is a degradation product of the hyperbranched polylysine by organisms.
The composition can realize long-acting synergistic blood sugar reduction.
The composition can improve the antioxidant level of the organism and inhibit the oxidative stress.
In the composition, the mass ratio of the hyperbranched polylysine to the ascorbic acid is 5:2-2:5.
The composition also comprises auxiliary materials.
The formulation of the composition is a tablet.
In the composition, hyperbranched polylysine and ascorbic acid are prepared into enteric coated tablets which can be taken orally.
In the composition, the auxiliary materials comprise modified starch, stearic acid, micro silica gel, microcrystalline cellulose and talcum powder.
The composition comprises the following components in percentage by weight: 10-50% of hyperbranched polylysine, 10-50% of ascorbic acid, 3-15% of modified starch, 0.1-1% of stearic acid, 0.1-1% of micro powder silica gel, 5-45% of microcrystalline cellulose and 3-6% of talcum powder.
Compared with the prior art, the invention has the remarkable beneficial effects that:
the hyperbranched polylysine and the ascorbic acid are combined for use, the hyperbranched polylysine can inhibit the oxidation of the ascorbic acid and adsorb the ascorbic acid, so that the ascorbic acid can be slowly released, and the hyperbranched polylysine can be slowly degraded into the lysine, thereby avoiding the rapid metabolism of the lysine and the ascorbic acid, simultaneously the ascorbic acid can promote the absorption and the utilization of the lysine in the body, and the combination of the two can cooperatively play a long-acting hypoglycemic effect. At the same time, the antioxidant level of the organism is improved, and the oxidative stress is inhibited. The composition disclosed by the invention has definite components and simple composition, the degradation product of the hyperbranched polylysine serving as an active component is the human essential amino acid lysine, and the ascorbic acid is a natural antioxidant, so that the composition is safe and nontoxic and can be taken for a long time.
Drawings
FIG. 1 is a graph showing the change in blood glucose in mice after administration of the compositions prepared in example 1, comparative example 1 and comparative example 2.
FIG. 2 shows MDA (a) and SOD (b) contents in blood of mice after taking the compositions prepared in example 1, comparative example 1 and comparative example 2.
FIG. 3 shows the amounts of Lys (a) and AA (b) in blood of mice after administration of the compositions prepared in example 1 and comparative example 3.
Detailed Description
The foregoing aspects of the invention are explained in further detail below with reference to specific embodiments and the accompanying drawings.
Example 1: preparation of hyperbranched polylysine-ascorbic acid (HBPL-AA) enteric coated tablets
The embodiment provides a composition with synergistic long-acting regulation of blood glucose level, comprising the following components in percentage by weight: 25% of hyperbranched polylysine, 30% of ascorbic acid, 10% of modified starch, 0.75% of stearic acid, 0.25% of micro-powder silica gel, 30% of microcrystalline cellulose and 4% of talcum powder.
The preparation method comprises the following steps:
step 1, mixing hyperbranched polylysine solution and ascorbic acid solution for 30min under the stirring condition, and then freeze-drying the mixture for standby;
step 2, respectively sieving the freeze-dried powder obtained in the step 1, modified starch, stearic acid, micro silica gel, microcrystalline cellulose and talcum powder by a 100-mesh sieve, and then mixing and sieving by a 20-mesh sieve to obtain particles obtained by mixing the freeze-dried powder and auxiliary materials;
and 3, mixing the granules obtained in the step 2 with magnesium stearate and talcum powder into a tablet press for tabletting to obtain the HBPL-AA tablet. And preparing shellac coating solution for coating and spraying tablets, and drying to obtain the HBPL-AA enteric coated tablets.
Comparative example 1: preparation of hyperbranched polylysine (HBPL) enteric coated tablets
The weight percentages of the components are as follows: 55% of hyperbranched polylysine, 10% of modified starch, 0.75% of stearic acid, 0.25% of micro silica gel, 30% of microcrystalline cellulose and 4% of talcum powder.
The preparation method comprises the following steps: the hyperbranched polylysine, modified starch, stearic acid, micro silica gel, microcrystalline cellulose and talcum powder are sieved by a 100-mesh sieve, and then are mixed and sieved by a 20-mesh sieve. And mixing the obtained granules, magnesium stearate and talcum powder into a tablet press for tabletting to obtain the HBPL tablet. And then preparing shellac coating solution for coating and spraying tablets, and drying to obtain the HBPL enteric coated tablets.
Comparative example 2: preparation of an enteric coated tablet of Ascorbic Acid (AA)
The weight percentages of the components are as follows: 55% of ascorbic acid, 10% of modified starch, 0.75% of stearic acid, 0.25% of micro silica gel, 30% of microcrystalline cellulose and 4% of talcum powder.
An AA enteric-coated tablet was prepared in the same manner as in comparative example 1.
Comparative example 3: preparation of [ lysine+ascorbic acid ] ([ Lys+AA ]) enteric coated tablets
The weight percentages of the components are as follows: 25% of lysine, 30% of ascorbic acid, 10% of modified starch, 0.75% of stearic acid, 0.25% of micro silica gel, 30% of microcrystalline cellulose and 4% of talcum powder.
An enteric coated tablet [ Lys+AA ] was prepared in the same manner as in example 1.
The hypoglycemic and antioxidant effects of example 1, comparative example 1 and comparative example 2 were evaluated by the following methods: a diabetic mouse model was established by intraperitoneal injection of tetraoxapyrimidine (160 mg/kg) into 6-8-week-old C57BL/6 mice, after which diabetic mice were intragastrically coated with the composition HBPL-AA enteric coated tablet prepared in example 1, the HBPL enteric coated tablet prepared in comparative example 1, and the AA enteric coated tablet prepared in comparative example 2, respectively. A normal control group (healthy mice) and a model control group (non-diabetic mice) were additionally set, and the stomach was irrigated with physiological saline. The mice were dosed once every two days for four weeks, once a week with blood glucose monitoring. After blood glucose was measured at the fourth week, the blood of each group of mice was collected and the mice were sacrificed, and the content of Malondialdehyde (MDA) and superoxide dismutase (SOD) in the blood was measured.
As shown in fig. 1, the blood glucose level of the model control group is significantly increased compared with that of the normal control group; after the diabetes mouse model is subjected to gastric lavage in example 1, the blood sugar level is gradually reduced along with the time extension, and the effect is obviously better than that of comparative examples 1 and 2, so that the composition prepared by the invention has long-acting synergistic blood sugar reducing effect.
The detection results of MDA and SOD are shown in figure 2, and compared with the normal control group, the model control group has the advantages that the MDA content of lipid peroxidation products is increased, and the SOD content of antioxidant enzymes is reduced; after the diabetes mouse model is subjected to gastric lavage in example 1, the rise of MDA and the reduction of SOD are effectively inhibited, and the effect is obviously better than that of comparative example 1 and comparative example 2, so that the composition prepared by the invention has a synergistic antioxidation effect.
The metabolic status of example 1 and comparative example 3 in vivo was evaluated using the following method: SD rats of 6-8 weeks of age were selected, and the SD rats were perfused with the respective example 1 and comparative example 3, and blood was collected through the orbit at various time points after the lavage. After that, the plasma was collected by centrifugation and the lysine (Lys) and AA contents in the plasma were detected by high performance liquid chromatography. As shown in fig. 3 a, b, lys and AA were rapidly metabolized in vivo after comparative example 3 was administered by gavage; after gavage administration of example 1, the concentration of Lys and AA in the blood increased significantly, indicating that the compositions prepared according to the invention avoided rapid metabolism of Lys and AA.
Claims (7)
1. A composition with synergistic long-acting regulation of blood sugar level is characterized in that the composition contains active ingredients hyperbranched polylysine and ascorbic acid which are combined through physical acting force, can synergistically reduce blood sugar, and can also contain auxiliary materials.
2. The composition with synergistic long-acting regulation of blood glucose levels of claim 1, wherein the mass ratio of hyperbranched polylysine to ascorbic acid is 5:2-2:5.
3. The composition with synergistic effect for regulating blood glucose level as claimed in claim 1, wherein the adjuvant is one or more of modified starch, stearic acid, aerosil, microcrystalline cellulose, and pulvis Talci.
4. The composition with synergistic long-acting regulation of blood glucose levels of claim 1, comprising the following components in weight percent: 10-50% of hyperbranched polylysine, 10-50% of ascorbic acid, 3-15% of modified starch, 0.1-1% of stearic acid, 0.1-1% of micro powder silica gel, 5-45% of microcrystalline cellulose and 3-6% of talcum powder.
5. The composition having a synergistic effect in regulating blood glucose levels as claimed in claim 1, wherein the dosage form of the composition is a tablet.
6. The composition with synergistic extended release for regulating blood glucose levels as claimed in claim 5, wherein the tablet is an enteric coated tablet, which is directly taken orally.
7. A method of preparing a composition having synergistic long-acting regulation of blood glucose levels as claimed in claim 1, which method comprises: and (3) stirring and mixing the hyperbranched polylysine solution and the ascorbic acid solution, freeze-drying, mixing the freeze-dried powder with auxiliary materials, granulating, tabletting, coating, spraying and drying to obtain the enteric coated tablet.
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| CN202311719520.3A CN117838721A (en) | 2023-12-14 | 2023-12-14 | Composition with synergistic long-acting blood glucose level regulation function and preparation method thereof |
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|---|---|
| CN (1) | CN117838721A (en) |
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2023
- 2023-12-14 CN CN202311719520.3A patent/CN117838721A/en active Pending
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