Design for preparing composition product for preventing and treating senile sarcopenia

Abstract

The embodiment of the invention discloses a design for preparing a composition product for preventing and treating senile sarcopenia, and the composition is prepared from the following active ingredients: 2 to 6 parts of L-carnitine, 0.003 to 0.009 part of folic acid, 0.3 to 0.8 part of wormwood extract and 0.04 to 0.18 part of piperine. The invention also discloses application of the composition in preparation of products for preventing and treating senile sarcopenia. According to the application of the composition in preparation of products for preventing and treating senile sarcopenia, tests prove that after intervention of the composition, the grip strength, the 6m walking speed and the muscle mass of an intervention group are obviously improved compared with those before intervention.

Description

Technical Field

[0001] The embodiments of the present invention relate to the design of a composition product for preparing the prevention and treatment of sarcopenia in the elderly. Background Art

[0002] Sarcopenia is an age-related degenerative syndrome characterized by a decrease in skeletal muscle mass, muscle strength and / or physical activity. With the aging population and the increasing burden on the population, more and more elderly people will suffer from sarcopenia. It is reported that the prevalence of sarcopenia in people aged 60-70 is about 5%-13%, and it is estimated that it may increase to 11%-50% in people over 80 years old. Muscle attenuation increases the risk of falls and fractures, reduces the patient's ability to live in daily life, and is associated with heart disease, respiratory disease and cognitive impairment; it may cause patients to have motor dysfunction, decreased quality of life, loss of independent living ability, or long-term need for care from others, increase the risk of death, and also increase hospitalization costs and care costs.

[0003] Aging is often accompanied by a loss of muscle mass and function, which is caused by an imbalance between the rate of muscle protein synthesis and the rate of muscle protein breakdown. After the age of 40, muscle mass (lean body mass) decreases by about 8% per decade, and this decrease increases to 15% per decade after the age of 70.

[0004] The loss of muscle mass in older adults can affect health, leading to a variety of health and functional problems. As muscle mass decreases, patients may face reduced mobility, both in terms of speed and flexibility. As a result, independence decreases, which may subsequently cause patients to become depressed and isolated. This may in turn lead to a downward spiral, ultimately resulting in increased mortality. Therefore, sarcopenia is a major cause of disability, leading to reduced quality of life and increased risk of death.

[0005] At present, middle-aged and elderly people are paying more and more attention to muscle attenuation. In order to delay muscle attenuation, they mainly supplement high-quality protein, especially whey protein. Whey protein is rich in branched-chain amino acids, especially leucine, and is considered the most effective way to delay muscle attenuation. It can increase muscle and promote muscle synthesis. However, long-term excessive supplementation of whey protein may have a negative impact on the intestinal microbiota and increase the burden on the kidneys. Summary of the invention

[0006] To this end, the embodiments of the present invention provide a design for preparing a composition product for preventing and treating sarcopenia in the elderly, so as to solve the technical problem in the prior art due to the lack of effective products for treating sarcopenia in the elderly.

[0007] In order to achieve the above purpose, the embodiment of the present invention provides the following technical solutions:

[0008] The embodiment of the present invention provides a composition, which consists of the following effective ingredients: 2-6 parts of L-carnitine, 0.003-0.009 parts of folic acid, 0.3-0.8 parts of wormwood extract, and 0.04-0.18 parts of piperine.

[0009] In one embodiment of the present invention, the composition consists of the following effective ingredients: 3-5 parts of L-carnitine, 0.004-0.008 parts of folic acid, 0.4-0.7 parts of wormwood extract, and 0.05-0.17 parts of piperine.

[0010] In one embodiment of the present invention, the composition consists of the following effective ingredients: 4 parts of L-carnitine, 0.006 parts of folic acid, 0.5 parts of wormwood extract, and 0.1 parts of piperine.

[0011] In one embodiment of the present invention, the preparation method of the wormwood extract comprises:

[0012] Add hot water to the wormwood raw material, extract it under microwave heating at 50-70°C for 0.5-1.5 hours, the power of microwave heating extraction is 1000-1200W, filter it with filter paper that can filter less than 10μm, concentrate it under reduced pressure at 60-80°C and 6-7kpa to a Brix concentration of 15-25%, and further spray dry it to obtain the wormwood extract.

[0013] The present invention also provides the use of the above-mentioned composition in the preparation of products for preventing and treating sarcopenia in the elderly.

[0014] In one embodiment of the present invention, the product comprises the above-mentioned composition and one or more pharmaceutically acceptable carriers.

[0015] The one or more pharmaceutically acceptable excipients are selected from one or more diluents, lubricants, glidants, wetting agents, disintegrants and stabilizers. The diluent is selected from one or more of the following: mannitol, lactose, corn starch and microcrystalline cellulose.

[0016] In one embodiment of the present invention, it further comprises a glidant, a lubricant or both.

[0017] In one embodiment of the present invention, the glidant is colloidal anhydrous silicon dioxide, and the lubricant is magnesium stearate.

[0018] In one embodiment of the present invention, the composition is in the form of powder, tablet or capsule.

[0019] In an embodiment, the present disclosure provides a pharmaceutical composition in the form of a hard or soft gelatin capsule or tablet, comprising a pharmaceutical composition of the present invention and one or more excipients.

[0020] In an embodiment, the present disclosure provides a pharmaceutical composition in the form of a hard or soft gelatin capsule or tablet, comprising a dry powder mixture of the pharmaceutical composition and one or more excipients.

[0021] According to this embodiment, the one or more excipients may be selected from one or more diluents, lubricants, glidants, wetting agents, disintegrants and stabilizers.

[0022] The terms "diluent", "filler" and "bulking agent" are used interchangeably herein. According to this embodiment, the amount of the composition in the powder mixture is 10-60 wt%, with the remainder being filled by one or more excipients.

[0023] In an embodiment, the one or more excipients comprise a diluent or a combination of diluents. Suitable diluents include lactose, corn starch and microcrystalline cellulose. In an embodiment, in addition to the diluent, the one or more excipients further comprise a glidant, a lubricant or both a glidant and a lubricant. Typically, a glidant is a material that reduces friction between particles, such as colloidal anhydrous silicon dioxide; and a lubricant is a material that reduces adhesion of the powder to the metal, such as magnesium stearate.

[0024] In an embodiment, the one or more excipients may further include a wetting agent, such as sodium lauryl sulfate, and a disintegrant, preferably a super disintegrant, such as sodium starch glycolate, cross-linked carboxymethylcellulose or cross-linked povidone.

[0025] Examples of diluents suitable for tablets or capsules include calcium carbonate, calcium lactate, calcium phosphate, calcium silicate, calcium sulfate, cellulose butyl acetate, cellulose acetate, microcrystalline cellulose, powdered cellulose, silicified microcrystalline cellulose, corn starch, corn syrup solids, dextrates, dextrin, dextrose, erythritol, ethylcellulose, palmitic acid glyceride, hydroxypropyl cellulose, inulin, kaolin, lactitol, lactose, lactose monohydrate and co-processed with povidone, lactose monohydrate and powdered cellulose, magnesium carbonate, magnesium oxide, maltitol, maltodextrin, maltose, maltodextrin, maltose, mannitol, medium chain triglycerides, polydextrose, polyethylene glycol, sodium propylparaben, dimethicone, sodium bicarbonate, sodium carbonate, sodium chloride, sorbitol, starch, sucrose, sugar, sunflower oil, talc, trehalose, xylitol.

[0026] Examples of suitable disintegrants for tablets or capsules include agar, alginic acid, asparagine, calcium alginate, calcium carboxymethylcellulose, sodium carboxymethylcellulose, cellulose, carob bean gum, chitosan, colloidal silicon dioxide, corn starch and pregelatinized starch, cross-linked sodium carboxymethylcellulose, cross-linked polyvinylpyrrolidone, glycine, guar gum, hydroxypropylcellulose, hydroxypropyl starch, lactose monohydrate and corn starch, magnesium aluminum, maltose, methylcellulose, polacrilin potassium, povidone, sodium alginate, sodium starch glycolate, starch.

[0027] Examples of suitable binders for tablets or capsules include gum arabic, agar, alginic acid, ammonium alginate, attapulgite, calcium carbonate, calcium lactate, calcium polycarbophil, carboxymethylcellulose calcium, hydroxymethylcellulose sodium, cellulose acetate phthalate, carob bean gum, chitosan, rosin, copovidone, corn syrup solids, dextrates, dextrin, dextrose, anhydrous glucose, ethylcellulose, ethylene glycol and vinyl alcohol graft copolymers, gelatin, glucose Sugar, glyceryl behenate, guar gum, hydroxyethylcellulose, hydroxypropylcellulose, hydroxyethylmethylcellulose, hypromellose, isomalt, lactose monohydrate, magnesium aluminum silicate, maltitol, maltodextrin, maltose, methylcellulose, polycarbophil, polydextrose, polyethylene oxide, polymethacrylate, povidone, sodium propylparaben, sodium alginate, starch, sucrose, sugar, vegetable oil, vitamin E polyethylene glycol succinate, zein.

[0028] Examples of suitable lubricants for tablets or capsules include calcium stearate, castor oil, glyceryl behenate, glyceryl monostearate, glyceryl palmitostearate, leucine, magnesium stearate, mineral oil, myristic acid, palm oil, palmitic acid, poloxamer, polyethylene glycol, potassium glycol, potassium benzoate, sodium benzoate, sodium lauryl sulfate, sodium stearate, sodium stearyl fumarate, stearic acid, sucrose stearate, talc, vegetable oil, zinc stearate.

[0029] Examples of suitable glidants for tablets or capsules include cellulose, colloidal silicon dioxide, hydrophobic colloidal silicon dioxide, magnesium oxide, magnesium silicate, magnesium trisilicate, sodium stearate and talc.

[0030] In the present invention, the preparation method of the wormwood extract can better retain the effective ingredients. The wormwood extract of the present invention has a common synergistic effect with L-carnitine, folic acid and piperine, which can enhance muscle strength, improve muscle quality, and reduce muscle physiological function decline, so that the combination has the effect of effectively preventing and treating muscle wasting syndrome.

[0031] The embodiments of the present invention have the following advantages:

[0032] The present invention provides an application of a composition in the preparation of a product for preventing and treating sarcopenia in the elderly. Experiments have shown that after intervention with the composition of the present invention, the grip strength, 6m walking speed and muscle mass of the intervention group are significantly improved after intervention compared with before intervention. DETAILED DESCRIPTION

[0033] Embodiment 1, powder

[0034] The composition for treating sarcopenia provided in this embodiment is composed of the following ingredients in parts by mass: 4 parts of L-carnitine, 0.006 parts of folic acid, 0.5 parts of wormwood extract, and 0.1 parts of piperine.

[0035] In this embodiment, the wormwood extract is prepared according to the following process: 3 kg of wormwood raw material is added to 40 kg of 40-80°C hot water, extracted under 60°C microwave heating for 1 hour, the microwave heating extraction power is 1100W, and filtered with filter paper that can filter particles below 10 μm, and then reduced pressure concentration is performed at 70°C and 6.7kPa to a Brix concentration of 20%, and further spray dried to obtain a powdered wormwood extract.

[0036] Example 2, Tablets

[0037] The composition for treating sarcopenia provided in this embodiment is composed of the following ingredients in parts by mass: 3 parts of L-carnitine, 0.005 parts of folic acid, 0.4 parts of wormwood extract, and 0.05 parts of piperine.

[0038] The preparation method of the tablet of this embodiment comprises the following steps:

[0039] 30 g of L-carnitine, 0.05 g of folic acid, 4 g of wormwood extract and 0.5 g of piperine, a total of 34.55 g, are mixed thoroughly, 10.6 g of starch is added, 2.7 g of 10% starch slurry is added and mixed thoroughly, granulated through a 20-mesh sieve, dried, granulated through a 20-mesh sieve, 0.07 g of magnesium stearate is added, mixed thoroughly, and pressed into tablets to obtain 100 tablets.

[0040] In this embodiment, the wormwood extract is prepared according to the following process: 3 kg of wormwood raw material is added to 40 kg of hot water, extracted under 55°C microwave heating for 40 minutes, the microwave heating extraction power is 1000 W, and after filtering with filter paper that can filter particles below 10 μm, it is reduced pressure concentrated at 65°C and 6.5 kPa to a Brix concentration of 18%, and further spray dried to obtain a powdered wormwood extract.

[0041] Embodiment 3, powder

[0042] The composition for treating sarcopenia provided in this embodiment is composed of the following ingredients in parts by mass: 5 parts of L-carnitine, 0.007 parts of folic acid, 0.6 parts of wormwood extract, and 0.15 parts of piperine.

[0043] In this embodiment, the wormwood extract is prepared according to the following process: 3 kg of wormwood raw material is added to 40 kg of hot water, extracted under microwave heating at 65°C for 1.5 hours, the microwave heating extraction power is 1150 W, and after filtering with filter paper that can filter particles below 10 μm, it is reduced pressure concentrated at 75°C and 6.8 kPa to a Brix concentration of 22%, and further spray dried to obtain a powdered wormwood extract.

[0044] Comparative Example 1

[0045] The composition tablet provided in this comparative example is composed of the following ingredients in parts by mass: 3 parts of L-carnitine, 0.005 parts of folic acid and 0.05 parts of piperine.

[0046] The preparation method of the tablet of this embodiment comprises the following steps:

[0047] 30 g of L-carnitine, 0.05 g of folic acid and 0.5 g of piperine, a total of 30.55 g, are mixed thoroughly, 14.6 g of starch is added, 2.7 g of 10% starch slurry is added and mixed thoroughly, granulated through a 20-mesh sieve, dried, granulated through a 20-mesh sieve, 0.07 g of magnesium stearate is added, mixed thoroughly, and pressed into tablets to obtain 100 tablets.

[0048] Test Example 1

[0049] 1. The research subjects were selected from the screened patients with sarcopenia, and 203 volunteers were recruited in this study in accordance with the principle of informed consent.

[0050] The inclusion criteria were: (1) age 60 to 85 years old; (2) relative skeletal muscle mass index was calculated using Inbody 720 = skeletal muscle mass of the limbs / height squared (m 2 ), male <7.0 kg / m 2 , women <5.7kg / m 2 ; (3) Grip strength: male <26kg, female <18kg (or normal walking speed <0.8m / s for both men and women); (4) Good compliance and willingness to sign the informed consent.

[0051] Exclusion criteria are: (1) patients with mental disorders; (2) patients with sensory disabilities that significantly affect data collection, such as severe hearing loss, blindness, etc.; (3) patients with other major physical illnesses (diabetes with serious complications, patients with severe kidney disease, malignant tumors, etc.); (4) patients who are participating in other clinical trials; (5) patients who are considered by researchers to be unsuitable for clinical trials for other reasons.

[0052] 2. Grouping and treatment of research subjects

[0053] This study is a double-blind randomized controlled trial. 203 eligible elderly people with sarcopenia were screened and matched according to gender, age, and randomly divided into an intervention group and a placebo group. There were 100 people in the intervention group and 103 people in the placebo group, and they received different intervention treatments respectively. The intervention time was 12 months, and follow-up was conducted once a month. During the study, the subjects maintained their usual eating habits and lifestyles, and did not disrupt their daily routines at will.

[0054] (1) Intervention Group 1 (100 people): The product of Example 2 of the present invention, 1 tablet (about 0.5 g) per day, twice a day, drink with warm water half an hour after a meal.

[0055] (2) Placebo group (103 people): The product of comparative example 1 was administered in the same manner as the intervention group.

[0056] 3. Research content and methods

[0057] Before the intervention and after 12 months of intervention, all subjects used dual-energy X-ray absorptiometry (DXA) to measure skeletal muscle index (ASMI), grip strength, 6m walking time and other indicators. The measurement of various physical indicators was carried out by specially trained investigators. The measurement methods of each indicator are as follows:

[0058] 3.1 Anthropometric measurements

[0059] (1) Body composition analysis: The bioelectrical impedance method is used to analyze the body composition of the test subject. Before the test, the test subject cannot exercise or engage in other physical activities, eat, bathe or take a sauna. The room temperature is maintained between 20℃ and 25℃.

[0060] (2) Grip strength measurement: Use an electronic handgrip dynamometer (CAMRY) to measure grip strength. The subject sits with both feet placed naturally on the ground, knees and hips flexed 90 degrees. Shoulders adducted to neutral position. Elbows flexed 90 degrees, forearms in neutral position, wrist flexed between 0° and 30°, and 0° to 15° ulnar deviation. Grip the handgrip dynamometer firmly and record the reading. Measure three times, and then take the average value as the measured value.

[0061] (3) 6m walking time: The subjects were asked to walk 6m at their normal walking speed and record the time taken. The test was repeated twice and the average of the two times was taken as the measurement result.

[0062] 4. Statistical analysis

[0063] SPSS 21.0 software was used for statistical analysis. The test level α was 0.05, and the test was two-sided. All data were entered into the Epidata 3.02 database using the double entry method, with logical check conditions set and random sampling of data to ensure the accuracy of the entry.

[0064] 5. Experimental results

[0065] According to the established inclusion and exclusion criteria, a total of 203 volunteers were screened and included in this study, with 100 in the intervention group and 103 in the placebo group. No one withdrew from the study during the intervention period, and all 203 people completed the intervention. The average age of the intervention group was 71.1±2.5 years old. The average age of the placebo group was 73.3±3.4 years old. Before the intervention, there was no significant difference between the intervention group and the placebo group in skeletal muscle content of the limbs, grip strength, and 6m walking time (P>0.05). The results after the intervention are shown in the table below:

[0066] Table 1 Comparison of grip strength between the two groups of patients before and after intervention (x±s)

[0067]

[0068] As shown in Table 1, before the intervention, there was no significant difference in grip strength between the intervention group and the placebo group; after the intervention, the grip strength of the intervention group was significantly improved compared with that before the intervention, and after the intervention, the grip strength of the intervention group was significantly different from that of the placebo group (P < 0.05).

[0069] Table 2 Comparison of gait speed between the two groups of patients before and after intervention (x±s)

[0070]

[0071] As shown in Table 2, before the intervention, there was no significant difference in gait speed between the intervention group and the placebo group; after the intervention, the gait speed of the intervention group was significantly improved compared with that before the intervention, and after the intervention, the gait speed of the intervention group was significantly increased compared with that of the placebo group (P < 0.05).

[0072] Table 3 Comparison of muscle mass between the two groups of patients before and after intervention (x±s)

[0073]

[0074] As shown in Table 3, before the intervention, there was no significant difference in muscle mass between the intervention group and the placebo group; after the intervention, the muscle mass increase in the intervention group was significantly improved compared with that before the intervention, and after the intervention, the muscle mass increase in the intervention group was significantly different from that in the placebo group (P < 0.05).

[0075] In summary, the composition of L-carnitine, folic acid, wormwood extract and piperine of the present invention has a significant improvement effect on improving and treating sarcopenia in the elderly compared to the combination of L-carnitine, folic acid and piperine in Comparative Example 1. The addition of the wormwood extract of the present invention, in effective combination with other components of L-carnitine, folic acid and piperine, has a synergistic effect, which greatly improves sarcopenia in the elderly. This may be because the active ingredients in the wormwood extract of the present invention are combined with other components to synergistically enhance the effect of increasing muscle mass, improving muscle strength, and reducing muscle physiological function decline.

[0076] Although the present invention has been described in detail above by general description and specific embodiments, it is obvious to those skilled in the art that some modifications or improvements can be made to the present invention. Therefore, these modifications or improvements made without departing from the spirit of the present invention all belong to the scope of protection claimed by the present invention.

Claims

1. A composition, characterized in that The composition consists of the following effective ingredients: 2-6 parts of L-carnitine, 0.003-0.009 parts of folic acid, 0.3-0.8 parts of wormwood extract, and 0.04-0.18 parts of piperine.

2. The composition according to claim 1, characterized in that The composition consists of the following effective ingredients: 3-5 parts of L-carnitine, 0.004-0.008 parts of folic acid, 0.4-0.7 parts of wormwood extract, and 0.05-0.17 parts of piperine.

3. The composition according to claim 1, characterized in that The composition consists of the following effective ingredients: 4 parts of L-carnitine, 0.006 parts of folic acid, 0.5 parts of wormwood extract and 0.1 parts of piperine.

4. A composition according to any one of claims 1 to 3, characterized in that The preparation method of the wormwood extract comprises: The wormwood raw material is added with hot water, extracted under microwave heating at 50-70°C for 0.5-1.5 hours, the microwave heating extraction power is 1000-1200W, filtered with filter paper below 10μm, concentrated under reduced pressure at 60-80°C and 6-7kpa to a Brix concentration of 15-25%, and further spray-dried to obtain the wormwood extract.

5. Use of the composition according to any one of claims 1 to 3 in the preparation of products for preventing and treating sarcopenia in the elderly.

6. The use according to claim 1, characterized in that The product comprises the composition according to any one of claims 1 to 3, and one or more pharmaceutically acceptable carriers. The one or more pharmaceutically acceptable excipients are selected from one or more diluents, lubricants, glidants, wetting agents, disintegrants and stabilizers; Wherein, the diluent is selected from one or more of the following: mannitol, lactose, corn starch and microcrystalline cellulose.

7. The use according to claim 5, characterized in that: The composition may also include a glidant and / or a lubricant.

8. The use according to claim 7, characterized in that: The glidant was colloidal anhydrous silicon dioxide, and the lubricant was magnesium stearate.

9. The use according to claim 7, characterized in that The composition is in the form of powder, tablet or capsule.

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