A drug for enhancing cardiac vitality containing coenzyme Q10 and its preparation method

Abstract

The present invention discloses a drug containing coenzyme Q10 for enhancing cardiac vitality and its preparation method, specifically belonging to the technical field of biomedicine; the drug contains active components and excipients, and the active components include cactus extract, Calligonum rubicundum extract, Astragalus membranaceus extract, Hippohgae rhamnoides extract and coenzyme Q10; the low, medium and high dose groups of the drug for enhancing cardiac vitality provided by the present invention can significantly prolong the anoxic survival time and the load-bearing swimming time of mice. The drug can meet the oxygen demand of fatigue caused by high labor intensity by enhancing the body's immunity, enhance the supply of nutrients to the brain, heart and skeletal muscles of the body, regulate the vitality of the central nervous system, promote the normal operation of the body's circulatory system, relieve and eliminate fatigue and the damage caused by fatigue and chronic fatigue to the body, and quickly restore physical strength.

Description

Technical Field

[0001] The present invention belongs to the field of biomedical technology, and particularly relates to a drug containing coenzyme Q10 for enhancing cardiac vitality and its preparation method. Background Art

[0002] Coenzyme Q10 (Coenzyme Q10, abbreviated as CoQ10), as a lipophilic quinone compound widely present in body cells, has various important physiological functions, especially outstanding in energy production, antioxidant and immune regulation. Coenzyme Q10 is an indispensable part of the mitochondrial respiratory chain, participates in the oxidative phosphorylation process, promotes the synthesis of ATP (adenosine triphosphate), and provides necessary energy for cells. In addition, coenzyme Q10 is also a potent antioxidant, which can protect cells from damage by free radicals and maintain the normal structure and function of cells.

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

[0004] With the acceleration of the modern life rhythm and the increase of work pressure, people often face long-term physical or mental labor, resulting in problems such as fatigue and decreased endurance of the body. At the same time, due to the influence of factors such as environmental pollution and bad living habits, the level of coenzyme Q10 in the body gradually decreases, unable to meet the body's energy requirements, and further exacerbates the situation of fatigue and decreased endurance.

[0005] Therefore, developing a composition, drug containing coenzyme Q10 and its preparation method that can significantly enhance cardiac vitality, hypoxia tolerance and anti-fatigue has important practical significance and clinical application value. Summary of the Invention

[0006] Aiming at the deficiencies of the prior art, the purpose of the present invention is to provide a composition, drug containing coenzyme Q10 and its preparation method that can significantly enhance cardiac vitality, hypoxia tolerance and anti-fatigue. The composition can not only provide sufficient energy support for the myocardium, enhance the contractility and endurance of the myocardium, but also improve the antioxidant capacity of the body, reduce the damage of oxidative stress to the body, and thus effectively relieve fatigue and improve the body's endurance and adaptability.

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

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

[0009] Preferably, by mass parts, it comprises the following components:

[0010]

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

[0012] A1. Take the crushed cactus and soak it in a 0.75 wt% citric acid aqueous solution, perform ultrasonic treatment at an ultrasonic frequency of 20 kHz for 20 min, soak it at 25 - 30 °C for 12 h after ultrasonic treatment, and concentrate it by low-temperature distillation to 1 / 3 of the original volume to obtain a concentrated solution;

[0013] A2. Add an ethanol aqueous solution with a volume three times that of the concentrated solution and a concentration of 95 v / v%, soak it at 25 - 30 °C for ≥24 h, centrifuge, filter, discard the residue, keep the supernatant, remove ethanol, then concentrate, dry, pulverize, and pass through a sieve with a mesh size of ≥120 to obtain the cactus extract.

[0014] More preferably, the preparation method of the extract of Calligonum rubicundum comprises the following steps: Take the powder of the fruit of Calligonum rubicundum, soak it in an ethanol aqueous solution with a concentration of 85 v / v% at 50 °C for ≥3 h, centrifuge, filter, discard the residue, keep the supernatant, remove ethanol, then concentrate, dry, pulverize, and pass through a sieve with a mesh size of ≥120 to obtain the extract of Calligonum rubicundum.

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

[0016] The addition amount of the composition in the drug is 0.5 - 2 wt%.

[0017] Preferably, the drug further comprises excipients;

[0018] The excipients 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 essence.

[0023] In a third aspect, the present invention provides a method for preparing the drug for enhancing cardiac vitality described in the second aspect, which is characterized by comprising the following steps:

[0024] S1. Mix the components in the composition for enhancing cardiac vitality to obtain a mixture;

[0025] S2. Uniformly mix the mixture with excipients and then press into tablets to obtain the drug for enhancing cardiac vitality.

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

[0027] In the present invention:

[0028] The cactus extract obtained by the extract method of first water extraction and then alcohol extraction of the present invention contains various active ingredients, such as cactus polysaccharides, phenolic substances, alkaloid substances, sterols, triterpenoids, saponin substances, 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 detoxifying and relieving pain, detumescence and discharging pus, promoting qi and activating blood circulation. From the chemical composition, cactus has various pharmacological effects such as regulating immunity, lowering blood sugar, lowering blood lipid, antioxidant, anti-inflammatory, analgesic, antiviral, and anti-tumor.

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

[0030] Astragalus extract contains effective ingredients such as astragalus polysaccharides and astragaloside IV, and has the effect of enhancing the body's immune function. Astragalus polysaccharides can enhance the phagocytic function of phagocytes, promote the immune response of splenocytes to sheep red blood cells, and increase the weights of the spleen and thymus, thereby enhancing the body's non-specific immunity. In addition, astragalus extract can increase the survival time of animals under hypoxic conditions. Research shows that astragalus polysaccharides can significantly prolong the survival time of mice under hypoxic conditions, indicating that astragalus extract has the effect of anti-hypoxia.

[0031] The various active ingredients contained in sea buckthorn extract, including flavonoid compounds, phenolic compounds, vitamin C, vitamin E, carotenoids, etc., have the effects of enhancing the body's cardiac vitality, anti-hypoxia ability and anti-fatigue ability. At the same time, sea buckthorn extract also has an immune regulatory effect and can enhance the body's non-specific 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, cardiac function, and enhance cardiac vitality. Coenzyme Q10 is also crucial for cellular energy production and helps improve the tolerance of cells to hypoxic conditions. Research shows that coenzyme Q10 supplements can significantly reduce fatigue symptoms.

[0033] Advantages of the present invention:

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

[0035] To make the objectives, technical solutions, and advantages of the present invention clearer, the following further elaborates on the present invention in detail with reference to specific embodiments. However, the following embodiments are only preferred embodiments of the present invention and not all of them. For clarity, not all features of the actual embodiments are described.

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

[0037] In the present invention:

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

[0039] Calligonum rubicundum: Purchased from Anguo Jiuzhen Chinese Herbal Medicine Store;

[0040] Astragalus extract: Purchased from Langlin Biology, 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 crusher, soak it in a 0.75 wt% citric acid aqueous solution, first perform ultrasonic treatment (frequency 20 kHz) for 20 min, then soak it at 25 - 30 °C for 12 h, and after soaking, concentrate it by low-temperature distillation to 1 / 3 of the original volume to obtain a concentrated solution;

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

[0046] Preparation of the extract of Calligonum rubicundum:

[0047] Take the powder of the fruits of Calligonum rubicundum, soak it in an ethanol aqueous solution of 85 v / v% at 50 °C for ≥3 h, centrifuge and filter after soaking, discard the residue, and retain the supernatant. After removing the ethanol, concentrate, dry, crush, and pass through a sieve with ≥120 meshes to obtain the extract of Calligonum rubicundum.

[0048] Preparation of the composition:

[0049] Compound and mix according to the mass parts of the raw materials in Table 1 to obtain the composition.

[0050] Table 1 Mass parts of the raw materials of the composition

[0051]

[0052] Note: "-" in the table indicates not added.

[0053] Preparation of the examples and comparative examples:

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

[0055] Step S2. Mix the mixture with excipients evenly and then press it into tablets to obtain the drug for enhancing cardiac vitality;

[0056] Specifically, prepare it according to the mass percentages of the raw materials in Table 2.

[0057] Table 2 Mass percentages of the raw materials of the drug

[0058]

[0059]

[0060] Note: "-" in the table indicates 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 Vital River Laboratory Animal Technology Co., Ltd.

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

[0066] 1.2 Reagents:

[0067] Test samples: Tablets prepared in Examples 1 - 3 and Comparative Examples 4 - 8 (the recommended daily dose of the test sample for humans is 3 g. Calculated 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 all of analytical grade, and the experimental water was ultrapure water.

[0070] 2. Methods

[0071] 2.1 Animal grouping and administration method:

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

[0073] Table 3 Animal grouping and corresponding doses

[0074]

[0075]

[0076] Note: In the table, the blank control group: fed with placebo (the placebo was prepared by lacking the composition in the raw material formula of Example 2 and only retaining the excipients); low dose group: test sample 0.250 g / kg.BW, equivalent to 5 times the human recommended dose; medium dose group: test sample 0.500 g / kg.BW, equivalent to 10 times the human recommended dose; high dose group: test sample 1.500 g / kg.BW, equivalent to 30 times the human recommended dose.

[0077] Before the experiment, the test samples were ground into powder and dissolved with distilled water as the solvent to prepare each dose, and then mixed evenly for testing.

[0078] After 7 days of adaptive feeding, continuous gavage was carried out for 15 days. The mice in the experimental groups were gavaged with the corresponding dose of the test sample solution every morning. During the experiment, the mice in each group were allowed to freely eat and drink water. The body weight was measured once every 3 days, and the growth status of the mice 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 25-27℃ water 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 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 there is a significant difference between Examples 1-3 and the blank control group (p < 0.05), and aa indicates a highly significant difference (p < 0.01); b indicates that there is a significant difference between Example 2 and Comparative Examples 1-8 at the same dose level (p < 0.05), and bb indicates a highly significant difference (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 hypoxia survival time of mice (P < 0.01). When Example 2 is compared with Comparative Examples 1-8, at the same dose, the hypoxia survival time is significantly longer than that of the comparative examples;

[0096] Compared with the blank control group, the load-bearing swimming time of mice in the low, medium, and high dose groups of Examples 1-3 is significantly prolonged (P < 0.01). When Example 2 is compared with Comparative Examples 1-8, at the same dose, the load-bearing exhaustion swimming time is significantly longer than that of the comparative examples;

[0097] That is to say, the low, medium, and high dose compositions provided by the present invention can effectively improve the hypoxia tolerance and fatigue tolerance of mice. At the same time, the combined use of the components in the composition has a more obvious effect than when used alone. By comparing the results of Example 2 with those of Comparative Examples 4, 5, and 8, it can be seen that when either cactus extract or coenzyme Q10 is missing, the performance is most affected, and the difference is extremely significant, indicating that cactus extract and coenzyme Q10 play a major role in the whole formula, and astragalus extract, Calligonum rubicundum extract, and seabuckthorn extract play an auxiliary role in the formula.

[0098] Although the specific embodiments of the present invention have been described above, those skilled in the art should understand that this is only for illustration purposes. The protection scope of the present invention is defined by the appended claims. Without departing from the principles and essence of the present invention, those skilled in the art can make various changes or modifications to these embodiments, but these changes and modifications all fall within the protection scope of the present invention.

Claims

1. A composition for enhancing cardiac vitality, characterized in that, By mass parts, the composition consists of the following components: Cactus extract: 5 - 10 parts; Calligonum rubicundum extract: 1 - 5 parts; Astragalus membranaceus extract: 0.2 - 2 parts; Hippophae rhamnoides extract: 2 - 5 parts; Coenzyme Q10: 0.01 - 0.1 part.

2. The composition for enhancing cardiac vitality according to claim 1, wherein, The preparation method of the cactus extract includes the following steps: A1. Take the cactus, crush it, soak it in a 0.75wt% citric acid aqueous solution, perform ultrasonic treatment at an ultrasonic frequency of 20kHz for 20min, continue to soak it at 25 - 30°C for 12h after ultrasonic treatment, and then concentrate it by low-temperature distillation to 1 / 3 of the original volume to obtain a concentrated solution; A2. Add an ethanol aqueous solution with a volume three times that of the concentrated solution and a concentration of 95v / v%, soak it at 25 - 30°C for ≥24h, centrifuge, filter, discard the residue and retain the supernatant, concentrate, dry, crush, and pass through a sieve with a mesh size of ≥120 to obtain the cactus extract.

3. The composition for enhancing cardiac vitality according to claim 1, wherein The preparation method of the Calligonum rubicundum extract includes the following steps: Take the powder of Calligonum rubicundum fruits, soak it in an ethanol aqueous solution with a concentration of 85v / v% at 50°C for ≥3h, centrifuge, filter, discard the residue and retain the supernatant after soaking, concentrate, dry, crush, and pass through a sieve with a mesh size of ≥120 to obtain the Calligonum rubicundum extract.

4. A drug for enhancing cardiac vitality, characterized in that, The drug contains the composition for enhancing cardiac vitality according to any one of claims 1 - 3, and the addition amount of the composition in the drug is 0.5 - 2wt%.

5. The drug for enhancing cardiac vitality according to claim 4, wherein The drug also contains excipients, and the excipients include fillers, disintegrants, lubricants, and flavoring agents.

6. The drug for enhancing cardiac vitality according to claim 5, characterized in that, The filler is at least one of corn starch, maltodextrin, β-cyclodextrin, α-cyclodextrin, sorbitol, xylitol, and lactose.

7. The drug for enhancing cardiac vitality according to claim 5, characterized in that, The disintegrant is at least one of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, and cross-linked carboxymethyl cellulose sodium.

8. The preparation method of the drug for enhancing cardiac vitality according to any one of claims 4-7, characterized in that, It includes the following steps: S1. Mix the components in the composition for enhancing cardiac vitality to obtain a mixture; S2. Mix the mixture with the excipients evenly and press them into tablets to obtain the drug for enhancing cardiac vitality.

9. Use of the composition for enhancing cardiac vitality according to any one of claims 1 - 3 in the preparation of a pharmaceutical preparation or health food having the health care effects of relieving physical fatigue and / or anti-hypoxia.

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