Coenzyme Q10-containing medicine for improving heart activity and preparation method thereof

Abstract

The invention discloses a coenzyme Q10-containing medicine for improving heart activity and a preparation method thereof, and particularly belongs to the technical field of biological medicines. The medicine comprises functional components and auxiliary materials, wherein the functional components comprise a cactus extract, a calligonum mongolicum extract, an astragalus membranaceus extract, a sea-buckthorn extract and coenzyme Q10; the hypoxia survival time and the load-bearing swimming time of mice can be remarkably prolonged through low, medium and high dose groups of the medicine for improving the heart vitality, the requirement of fatigue caused by high labor intensity for oxygen is further met by enhancing the immunity of the organism, supply of nutrient substances to the brain, the heart, the bones and the muscles of the organism is enhanced, and the effect of improving the heart vitality is achieved. The composition can regulate the activity of central nervous system, promote the normal operation of the body circulation system, relieve and eliminate fatigue and damage to the body caused by fatigue and chronic fatigue, and quickly recover physical strength.

Description

Technical Field

[0001] The invention belongs to the technical field of biomedicine, and specifically relates to a medicine containing coenzyme Q10 for improving cardiac vitality and a preparation method thereof. Background Art

[0002] Coenzyme Q10 (CoQ10 for short) is a fat-soluble quinone compound widely present in the body's cells. It has many important physiological functions, especially in energy production, anti-oxidation and immune regulation. Coenzyme Q10 is an indispensable part of the mitochondrial respiratory chain, participating in the oxidative phosphorylation process, promoting the synthesis of ATP (adenosine triphosphate), and providing the necessary energy for cells. In addition, Coenzyme Q10 is also a powerful antioxidant that can protect cells from damage by free radicals and maintain the normal structure and function of cells.

[0003] In the field of heart health, the role of coenzyme Q10 is particularly significant. It can enhance the energy metabolism of myocardial cells, improve the contractility and endurance of the myocardium, and thus effectively prevent and treat a variety of heart diseases, such as heart failure, arrhythmia, myocardial ischemia, etc. In addition, coenzyme Q10 can also enhance the antioxidant capacity of myocardial cells, reduce the damage of oxidative stress to myocardial cells, and protect myocardial cells from adverse conditions such as hypoxia and ischemia.

[0004] With the acceleration of modern life and the increase of work pressure, people often face long-term physical or mental labor, which leads to physical fatigue, decreased endurance and other problems. At the same time, due to the influence of environmental pollution, bad living habits and other factors, the level of coenzyme Q10 in the body gradually decreases, which cannot meet the body's demand for energy, further aggravating fatigue and decreased endurance.

[0005] Therefore, the development of a composition, a drug and a preparation method thereof containing coenzyme Q10 that can significantly improve cardiac vitality, hypoxia resistance and fatigue resistance has important practical significance and clinical application value. Summary of the invention

[0006] In view of the deficiencies in the prior art, the present invention aims to provide a composition, a medicine and a preparation method thereof containing coenzyme Q10, which can significantly improve cardiac vitality, hypoxia resistance and fatigue resistance. The composition can not only provide sufficient energy support for the myocardium, enhance the contractility and endurance of the myocardium, but also enhance the body's antioxidant capacity and reduce the damage of oxidative stress to the body, thereby effectively relieving fatigue and improving the body's endurance and adaptability.

[0007] To achieve the above object, the present invention discloses the following technical solutions:

[0008] In a first aspect, the present invention provides a composition for improving cardiac vitality, comprising components: cactus extract, Calligonum rubrum extract, astragalus extract, seabuckthorn extract and coenzyme Q10.

[0009] Preferably, the following components are included by weight:

[0010]

[0011] Further preferably, the preparation method of the cactus extract comprises the following steps:

[0012] A1. Take the cactus and crush it with 0.75wt% citric acid aqueous solution, and then ultrasonically treat it at an ultrasonic frequency of 20kHz for 20min, and then soak it at 25-30℃ for 12h. After soaking, it was concentrated to 1 / 3 of the original volume by low-temperature distillation to obtain a concentrate;

[0013] A2. Add 3 times the amount of the concentrate with 95 v / v% ethanol aqueous solution, soak at 25-30°C for ≥24h, centrifuge, filter, discard the residue and retain the supernatant, remove the ethanol and concentrate, dry, crush, and pass through a ≥120 mesh sieve to obtain a cactus extract.

[0014] Further preferably, the preparation method of the red fruit Calligonum mongolicum extract comprises the following steps: taking the red fruit Calligonum mongolicum fruit powder, soaking it in 85v / v% ethanol aqueous solution at 50°C for ≥3h, centrifuging and filtering after soaking, discarding the residue and retaining the supernatant, removing the ethanol and concentrating, drying, crushing, and passing through a ≥120 mesh sieve to obtain the red fruit Calligonum mongolicum extract.

[0015] In a second aspect, the present invention provides a drug for improving cardiac vitality, characterized in that the drug comprises the composition for improving cardiac vitality as described in the first aspect;

[0016] The composition is added in an amount of 0.5-2 wt % in the medicine.

[0017] Preferably, the drug further comprises excipients;

[0018] The auxiliary materials include fillers, disintegrants, lubricants and flavoring agents.

[0019] More preferably, the filler is at least one of corn starch, maltodextrin, β-cyclodextrin, α-cyclodextrin, sorbitol, xylitol and lactose.

[0020] More preferably, the disintegrant is at least one of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, and cross-linked sodium carboxymethyl cellulose.

[0021] More preferably, the lubricant is magnesium stearate.

[0022] Further preferably, the flavoring agent is apple flavor.

[0023] In a third aspect, the present invention provides a method for preparing the drug for improving cardiac vitality according to the second aspect, characterized in that it comprises the following steps:

[0024] S1. The components of the composition for improving cardiac vitality are mixed to obtain a mixture;

[0025] S2. The mixture is mixed evenly with auxiliary materials and then compressed into tablets to obtain the drug for improving cardiac activity.

[0026] In a fourth aspect, the present invention provides the use of the composition for improving cardiac vitality described in the first aspect in the preparation of a pharmaceutical preparation or a health food having the health-care effects of relieving physical fatigue and / or resisting hypoxia.

[0027] In the present invention:

[0028] The cactus extract obtained by the extraction method of first extracting with water and then extracting with alcohol of the present invention contains multiple active ingredients, such as cactus polysaccharides, phenolic substances, alkaloid substances, sterols, triterpenes, saponins, vitamins, minerals, amino acids and other active ingredients. Medical theory believes that cactus is cold in nature and bitter in taste, and has the effects of detoxification, analgesia, swelling reduction and pus discharge, and qi and blood circulation. The chemical composition shows that cactus has multiple pharmacological effects such as regulating immunity, lowering blood sugar, lowering blood lipids, anti-oxidation, anti-inflammatory, analgesia, anti-virus, and anti-tumor.

[0029] The interior of the red-fruited Calligonum is rich in protein, fat, vitamins and other nutrients. After eating Calligonum, these nutrients can be quickly absorbed by the body and can effectively supplement the body's nutrition. In addition, Calligonum can also improve cell activity and the body's immunity.

[0030] Astragalus extract contains active ingredients such as astragaloside and astragaloside IV, which can enhance the body's immune function. Astragalus polysaccharide can enhance the phagocytic function of phagocytes, promote the immune response of spleen cells to sheep red blood cells, increase the weight of spleen and thymus, and thus enhance the body's nonspecific immunity. In addition, astragalus extract can increase the survival time of animals under hypoxic conditions. Studies have shown that astragalus polysaccharide can significantly prolong the survival time of mice under hypoxic conditions, indicating that astragalus extract has the effect of resisting hypoxia.

[0031] Sea buckthorn extract contains a variety of active ingredients, including flavonoids, phenolic compounds, vitamin C, vitamin E, carotenoids, etc., which can improve the body's heart vitality, hypoxia resistance and anti-fatigue ability. At the same time, sea buckthorn extract also has an immunomodulatory effect and can enhance the body's nonspecific immune function.

[0032] Coenzyme Q10 is a key auxiliary substance in the process of cellular energy production and is particularly important for heart health. As an electron carrier in the mitochondrial respiratory chain and a potential fat-soluble antioxidant, it can help improve myocardial energy metabolism, improve heart function, and increase heart vitality. Coenzyme Q10 is also crucial for the production of cellular energy and helps improve cells' tolerance to hypoxic conditions. Studies have shown that Coenzyme Q10 supplementation can significantly reduce fatigue symptoms.

[0033] Beneficial effects of the present invention:

[0034] The low, medium and high doses of the drug for improving cardiac activity provided by the present invention can significantly prolong the hypoxic survival time of mice and the weight-bearing swimming time of mice. The drug enhances the body's immunity, thereby responding to the demand for oxygen caused by fatigue due to high labor intensity, enhancing the supply of nutrients to the body's brain, heart and skeletal muscles, regulating the activity of the central nervous system, promoting the normal operation of the body's circulatory system, reducing and eliminating fatigue and damage to the body caused by fatigue and chronic fatigue, and quickly restoring physical strength. DETAILED DESCRIPTION

[0035] In order to make the purpose, technical scheme and advantages of the present invention more clearly understood, the present invention is further described in detail below in conjunction with specific embodiments. However, the following embodiments are only preferred embodiments of the present invention, not all. For the sake of clarity, all features of the actual embodiments are not described.

[0036] Based on the embodiments in the implementation manner, other embodiments obtained by those skilled in the art without making any creative work shall all fall within the protection scope of the present invention.

[0037] In the present invention:

[0038] Cactus: purchased from Anguo Jiuzhen Chinese Medicine Store;

[0039] Red fruit Calligonum affine: purchased from Anguo Jiuzhen Chinese Medicine Store;

[0040] Astragalus extract: purchased from Langlin Biotechnology, model NAT-018;

[0041] Sea buckthorn extract: purchased from Shaanxi Xinyanghe Biotechnology Co., Ltd., specification 30:1;

[0042] Coenzyme Q10: prepared according to the preparation method of Chinese patent CN115584357B "A fermentation extraction method of coenzyme Q10".

[0043] Preparation of Cactus Extract:

[0044] A1. Take the dried cactus, crush it with a universal high-speed grinder, soak it with a 0.75wt% citric acid aqueous solution, first ultrasonically treat it (frequency 20kHz) for 20min, soak it at 25-30℃ for 12h, and concentrate it to 1 / 3 of its original volume by low-temperature distillation after soaking to obtain a concentrate;

[0045] A2. Add 3 times the amount of the concentrate with 95 v / v% ethanol aqueous solution, soak at 25-30°C for ≥24h, centrifuge, filter, discard the residue and retain the supernatant, remove the ethanol and concentrate, dry, crush, and pass through a ≥120 mesh sieve to obtain a cactus extract.

[0046] Preparation of Calligonum rubrum extract:

[0047] Take the red fruit Calligonum fruit powder, soak it in 85v / v% ethanol aqueous solution at 50℃ for ≥3h, centrifuge and filter after soaking, discard the residue and keep the supernatant, remove the ethanol and concentrate, dry, crush and pass through a ≥120 mesh sieve to obtain the red fruit Calligonum fruit extract.

[0048] Preparation of the composition:

[0049] The raw materials were compounded and mixed according to the weight proportions in Table 1 to obtain a composition.

[0050] Table 1 Composition raw materials weight parts

[0051]

[0052] Note: “-” in the table means not added.

[0053] Preparation of Examples and Comparative Examples:

[0054] Step S1. Mixing the components in the above composition according to the mass ratio in Table 1 to obtain a mixture;

[0055] Step S2. The mixture is mixed evenly with the auxiliary materials and then pressed into tablets to obtain the drug for improving cardiac activity;

[0056] Specifically prepare according to the raw material mass percentage in Table 2.

[0057] Table 2 Mass percentage of drug raw materials

[0058]

[0059]

[0060] Note: “-” in the table means not added.

[0061] Performance Test:

[0062] 1. Materials

[0063] 1.1 Experimental Animals:

[0064] Male B6C3F1 mice weighing 20 ± 2 g were provided by Beijing Weitonglihua Experimental Animal Technology Co., Ltd.;

[0065] The animals were kept in an SPF animal room with a constant temperature of (25±1)°C and a constant humidity of (50±5)%, with a light-dark cycle of 12 h.

[0066] 1.2 Reagents:

[0067] Test sample: Tablets prepared in Examples 1-3 and Comparative Examples 4-8 (the recommended daily dose of the test sample is 3 g, and based on an adult body weight of 60 kg, the recommended dose of the sample is 0.050 g / kg.BW)

[0068] Soda lime was purchased from Tianjin Damao;

[0069] Other reagents were of analytical grade and ultrapure water was used in the experiments.

[0070] 2. Methods

[0071] 2.1 Animal grouping and dosing method:

[0072] Healthy male B6C3F1 mice weighing 20±2g were randomly divided into a blank control group and a test sample group according to their body weight. The 11 test sample groups were correspondingly marked as Examples 1-3 and Comparative Examples 1-8. Each test sample group was divided into low, medium and high dose groups, with 10 replicates in each group, as shown in Table 3.

[0073] Table 3 Animal groups and corresponding doses

[0074]

[0075]

[0076] Note: In the table, blank control group: placebo was administered (placebo was administered in accordance with the raw material formula of Example 2 without the composition, and only the auxiliary materials were retained); low-dose group: 0.250 g / kg.BW of the test sample, equivalent to 5 times the recommended human dose; medium-dose group: 0.500 g / kg.BW of the test sample, equivalent to 10 times the recommended human dose; high-dose group: 1.500 g / kg.BW of the test sample, equivalent to 30 times the recommended human dose.

[0077] Before the test, the test samples were ground into powder, dissolved in distilled water as solvent to prepare various doses, and mixed well for testing.

[0078] After 7 days of adaptive feeding, mice in the experimental group were gavaged with the test sample solution at a corresponding dose every morning for 15 days. During the experiment, each group had free access to food and water. The mice were weighed every 3 days and their growth was observed.

[0079] 2.2 Normal pressure closed oxygen-deficient test:

[0080] 30 minutes after the last oral administration, the mice were placed in a 250 ml wide-mouth bottle containing 5 g of soda lime and filter paper. The bottle cap was sealed with vaseline and the timer was immediately started. The last respiratory cessation of the mouse (the mouse suddenly became limp after struggling and convulsing, and the chest no longer rose and fell) was taken as the sign of death. The body weight of each mouse and the survival time of hypoxia in normal pressure (ST) were observed and recorded, and the volume of the wide-mouth bottle (V) was accurately measured.

[0081] 2.3 Mouse weight-bearing swimming test:

[0082] Add water at 25-27℃ to a depth of 30cm in a swimming box of 100cm×80cm×50cm. 40min after the last gavage of mice, load the base of the tail of the mice with a weight of 3% of their body weight, gently put them in the swimming box and start timing. Record the swimming time when the mice are exhausted (they show obvious movement disorders when swimming, until they sink into the water, and still cannot swim to the surface after 10s; after emerging from the water, they breathe deeply and rapidly, their eyes are dull, their reactions are slow, they are slow to escape from strong stimulation, and their body position is prone or sitting; when the tail of the mice is lifted, their limbs hang down, and there is no sign of struggle).

[0083] 3 Statistical analysis

[0084] All experimental data were expressed as "mean ± standard deviation". SPSS24.0 statistical software was used for statistical analysis, and P < 0.05 was considered statistically significant, and P < 0.01 was considered statistically significant.

[0085] 4 Results Analysis

[0086] The effects of the embodiments and comparative examples on the body weight of mice, the survival time of mice under normal pressure and closed hypoxia, and the weighted swimming time of mice are shown in Tables 4 and 5.

[0087] Table 4 Effects on mouse body weight

[0088]

[0089]

[0090] According to Table 4, during the experiment, there was no bite in each group of animals, the coat color was normal, and the body weight increased with the extension of feeding days. Compared with the blank control group, there was no significant difference in the body weight of mice in the test sample group (P>0.05), indicating that low, medium and high doses of the test samples had no adverse effects on the weight gain of mice.

[0091] Table 5 Effects on the survival time of mice under normal pressure and closed hypoxia and the weight-bearing swimming time of mice

[0092]

[0093]

[0094] Note: a indicates that Examples 1-3 are significantly different from the blank control group (p < 0.05), aa indicates that the difference is extremely significant (p < 0.01); b indicates that Example 2 is significantly different from Comparative Examples 1-8 at the same dosage level (p < 0.05), bb indicates that the difference is extremely significant (p < 0.01).

[0095] According to Table 5, compared with the blank control group, the low, medium and high doses of Examples 1-3 can significantly prolong the hypoxic survival time of mice (P < 0.01). Compared with Comparative Examples 1-8, the hypoxic survival time of Example 2 at the same dose is significantly longer than that of the Comparative Examples;

[0096] Compared with the blank control group, the weight-bearing swimming time of mice in the low, medium and high dose groups of Examples 1-3 was significantly prolonged (P < 0.01). Compared with Comparative Examples 1-8, the weight-bearing exhaustive swimming time of Example 2 was significantly longer than that of the Comparative Examples at the same dose.

[0097] That is to say, the low, medium and high dose compositions provided by the present invention can effectively improve the hypoxia resistance and fatigue resistance of mice, and the effect of the components in the composition when used in combination is more obvious than when used alone; compared with the results of Example 2 and Comparative Examples 4, 5 and 8, it can be seen that when one of the cactus extract and coenzyme Q10 is missing, the performance is most affected, and the difference is extremely significant, indicating that the cactus extract and coenzyme Q10 play a major role in the entire formula, and the astragalus extract, the red fruit calligonum extract and the sea buckthorn extract play an auxiliary role in the formula.

[0098] Although the specific embodiments of the present invention are described above, it should be understood by those skilled in the art that this is only for illustration and the protection scope of the present invention is defined by the appended claims. Those skilled in the art may make various changes or modifications to these embodiments without departing from the principles and essence of the present invention, but these changes and modifications all fall within the protection scope of the present invention.

Claims

1. A composition for improving cardiac vitality, characterized in that: Contains the following ingredients: cactus extract, calligonum red fruit extract, astragalus extract, sea buckthorn extract and coenzyme Q10.

2. The composition for improving cardiac vitality according to claim 1, characterized in that: By mass, it contains the following components:

3. The composition for improving cardiac vitality according to claim 2, characterized in that: The preparation method of the cactus extract comprises the following steps: A1. Take the cactus and crush it with 0.75wt% citric acid aqueous solution, and then ultrasonically treat it at an ultrasonic frequency of 20kHz for 20min. After ultrasonic treatment, continue to soak at 25-30℃ for 12h, and then distill and concentrate to 1 / 3 of the original volume to obtain a concentrate; A2. Add 3 times the amount of the concentrate with 95 v / v% ethanol aqueous solution, soak at 25-30°C for ≥24h, centrifuge, filter, discard the residue and retain the supernatant, remove the ethanol and concentrate, dry, crush, and pass through a ≥120 mesh sieve to obtain a cactus extract.

4. The composition for improving cardiac vitality according to claim 2, characterized in that: The preparation method of the red fruit Calligonum mongolicum extract comprises the following steps: taking red fruit Calligonum mongolicum fruit powder, soaking it in 85v / v% ethanol aqueous solution at 50°C for ≥3h, centrifuging and filtering after soaking, discarding the residue and retaining the supernatant, removing the ethanol and concentrating, drying, crushing, and passing through a sieve of ≥120 meshes to obtain the red fruit Calligonum mongolicum extract.

5. A drug for improving cardiac activity, characterized in that: The medicine comprises the composition for improving cardiac vitality according to any one of claims 1 to 4, and the composition is added to the medicine in an amount of 0.5 to 2 wt%.

6. The drug for improving cardiac activity according to claim 5, characterized in that: The medicine further comprises excipients, which include fillers, disintegrants, lubricants and flavoring agents.

7. The drug for improving cardiac activity according to claim 6, characterized in that: The filler is at least one of corn starch, maltodextrin, β-cyclodextrin, α-cyclodextrin, sorbitol, xylitol and lactose.

8. The drug for improving cardiac activity according to claim 6, characterized in that: The disintegrant is at least one of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, and cross-linked sodium carboxymethyl cellulose.

9. The method for preparing a drug for improving cardiac vitality according to any one of claims 5 to 8, characterized in that: The following steps are involved: S1. The components of the composition for improving cardiac vitality are mixed to obtain a mixture; S2. The mixture is mixed evenly with auxiliary materials and then pressed into tablets to obtain the drug for improving cardiac activity.

10. Use of the composition for improving cardiac vitality according to any one of claims 1 to 4 in the preparation of a pharmaceutical preparation or health food having the health-care effects of relieving physical fatigue and / or resisting hypoxia.

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