CN107982389B - Composition for resisting atherosclerosis - Google Patents

Composition for resisting atherosclerosis Download PDF

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Publication number
CN107982389B
CN107982389B CN201711469863.3A CN201711469863A CN107982389B CN 107982389 B CN107982389 B CN 107982389B CN 201711469863 A CN201711469863 A CN 201711469863A CN 107982389 B CN107982389 B CN 107982389B
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composition
extract
curcumin
parts
saw
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CN107982389A (en
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胡文波
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Jiangsu Eachy Biomedical Co ltd
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Jiangsu Eachy Biomedical Co ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/12—Ketones
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/01—Hydrocarbons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/889—Arecaceae, Palmae or Palmaceae (Palm family), e.g. date or coconut palm or palmetto
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs

Abstract

The invention provides an anti-atherosclerosis composition, which comprises 95-105 parts of curcumin, 50-170 parts of saw palmetto extract, 20-40 parts of lycopene and 4-10 parts of piperine in sequence by weight; the composition has effect in resisting atherosclerosis better than curcumin alone.

Description

Composition for resisting atherosclerosis
Technical Field
The invention relates to a composition, in particular to a composition capable of effectively resisting arteriosclerosis, and belongs to the technical field of medicines/foods.
Background
Atherosclerosis (AS) is the leading cause of coronary heart disease, cerebral infarction, peripheral vascular disease. With the improvement of living standard of people in China and the change of eating habits, atherosclerotic diseases become common diseases seriously harming the health of people, most of the atherosclerotic diseases are seen in middle-aged and old people over 40 years old, but the clinical onset age of the atherosclerotic diseases has a trend of being younger in recent years. The symptoms of which depend mainly on the vascular pathology and the degree of ischemia of the affected organs. Atherosclerosis of the aorta is often without specific symptoms; for coronary atherosclerosis, if the caliber is narrowed to more than 75%, angina pectoris, myocardial infarction, arrhythmia, and even sudden death can occur; cerebral atherosclerosis can cause cerebral ischemia, brain atrophy, or cause rupture of cerebral vessels to bleed. It can be seen that atherosclerosis is a disease which is difficult to detect in an early stage and serious in consequences, and therefore, treatment of atherosclerosis should be initiated prophylactically.
Prevention of atherosclerosis is divided into two stages: the first-level prevention is light diet, no smoking, no spirit drinking, emotional comfort and the like; the second-level prevention is to use aspirin for anti-thrombus and statins for lipid regulation for the life. Among them, aspirin is known to irritate gastrointestinal tract, and is liable to cause gastric mucosa injury, gastric ulcer and gastric bleeding after long-term use, while statins induce type 2 diabetes at a risk of up to 46%. Obviously, the health cost of this solution for preventing AS is too heavy, and therefore, there is an urgent need for a safer and more effective anti-atherosclerosis drug/functional food to protect the health of the general population.
Curcumin is a chemical component extracted from rhizomes of some plants in Zingiberaceae and Araceae, and experiments prove that curcumin belongs to a nontoxic substance and has no potential mutagenic and teratogenic effects. Curcumin has a great number of pharmacological activities, such as anticancer, anti-inflammatory, anti-oxidation, free radical scavenging, anti-atherosclerosis, kidney protection and the like, but no finished product with any efficacy is available at present due to the limitations of curcumin property, activity intensity and the like. In addition, the mechanism of atherosclerosis is very complex and has not yet been fully elucidated, and thus, it is difficult to achieve a complete cure or a good prevention of atherosclerosis by means of a single ingredient.
Disclosure of Invention
The technical problem to be solved by the invention is to provide a composition with anti-atherosclerosis function, and provide a measure for effectively avoiding or relieving the atherosclerosis condition for people with high atherosclerosis incidence who do not show symptoms.
The invention provides an anti-atherosclerosis composition, which comprises curcumin, saw palm extract and piperine. The curcumin, the saw palm extract and the piperine are sequentially 95-105 parts, 50-170 parts and 4-10 parts by weight. Wherein the curcumin can also be Curcuma rhizome extract containing more than 95% curcumin; the saw palmetto extract has two kinds of powder and oil, and can be selected according to the requirements of preparing different dosage forms; the piperine can also be black pepper extract with piperine not less than 90%, and has effect of improving curcumin bioavailability.
The effect of curcumin on resisting arteriosclerosis is proved by a plurality of animal experiments, but the dosage is higher, the dosage is between 200 and 1000mg/kg (body weight) per day, the curcumin needs to be taken by an adult according to 60kg, and about 0.5 to 5g of curcumin is also needed by the adult with 60kg per day in consideration of the difference of medication between humans and animals, and the dosage is very large; in addition, curcumin has poor solubility and low bioavailability, the effect of the conventional dosage form is very little, special treatment is needed, such as preparation of solid lipid nanoparticles, micelles, self-emulsifying systems, solid dispersions and the like, the actual dosage can be further increased, the compliance of people taking the product is inevitably influenced, and the long-term consistent taking is difficult, so that the purpose of resisting atherosclerosis cannot be realized. In the process of studying curcumin, the inventor finds that the anti-atherosclerosis effect of the curcumin can be obviously improved by matching the curcumin with a specific dosage of the saw palmetto extract. Compared with curcumin used alone, the composition of the invention can reduce indexes of TC, TG and LDL in blood and raise HDL by more than 20% after the total taking amount of the active ingredients is reduced by half. The saw palmetto extract is mainly used for treating prostate diseases, and the report on the aspects of heart and cerebral vessels is not found.
Preferably, the composition of the present invention further comprises lycopene, wherein the weight part of the lycopene is 20-40 parts. Although the addition of the lycopene in the amount has no obvious difference compared with the addition of no lycopene, the addition of the lycopene has certain beneficial effect, namely, the addition of the lycopene can further reduce the three indexes of TC, TG and LDL by about 5 percent.
The curcumin, the saw palm extract, the lycopene and the piperine (or the black pepper extract) can be obtained commercially or extracted by self according to a disclosed method, and all the raw materials are sieved by a sieve of 80 meshes for later use.
When the saw palmetto extract in the composition of the invention is solid extract, the content is not lower than 30 percent, and the dosage is 80-170 parts, preferably 100-170 parts; when the oily extract is selected, the content is more than 85%, and the dosage is 50-80 parts.
The composition of the present invention further preferably comprises 100 parts of curcumin, 110-150 parts of saw palmetto extract, 20-30 parts of lycopene and 4-7 parts of piperine. In a preferred embodiment, the composition comprises 100 parts curcumin, 130 parts saw palm extract, 25 parts lycopene and 5 parts piperine.
The composition also contains one or more than one pharmaceutically or dietetically acceptable auxiliary materials or excipients. Can be made into common dosage forms such as capsule, tablet, granule, etc. by conventional method; can also be prepared into preparation forms which are beneficial to improving the bioavailability of the curcumin, such as nanoparticles, liposome, micelle, solid dispersion, self-emulsifying system and the like. Proper and proper auxiliary materials or excipients are selected according to different preparation forms.
The inventors further verified the technical effects of the present invention through experiments.
Restated again: the following tests are merely illustrative of the many tests that have been performed during the development of the present invention and are not intended to cover or exhaust all of the tests that have been performed by the inventors and are intended to be illustrative of the effects of different formulations of the present invention on the effects of atherosclerosis.
The test method comprises the following steps:
50 SD rats were randomly divided into 5 groups:
10 control groups were fed basal diet;
10 models were fed with high fat diet (3% cholesterol, 0.5% sodium cholate, 0.2% propylthiouracil, 5% white sugar, 10% lard, balance basal diet);
feeding high-fat feed and 500 mg/kg/day curcumin to 10 curcumin groups;
composition 1 group of 10 animals fed high fat diet +250 mg/kg/day of the mixture of the effective ingredients of the composition of example 1 (i.e., without adjuvant, the same below);
composition 2 group 10 were fed with high fat diet +250 mg/kg/day of the mixture of the functional ingredients of the composition of example 2.
The suspension was gavaged once a day (gavage water for control and model groups) for 8 weeks. At the end of the 8 th week of the experiment, after fasting for 12 hours, the experimental rats were anesthetized with a 20% urethane solution and then blood was taken from the abdominal aorta, and after treatment, the Total Cholesterol (TC), Triglyceride (TG), low density lipoprotein cholesterol (LDL-C), and high density lipoprotein (HDL-C) contents were measured using a full-automatic biochemical analyzer, respectively, and the results are detailed in table 1.
TABLE 1 blood lipid results (mmol/L) for each group
n TC TG LDL-C HDL-C
Control group 10 1.51±0.34 0.64±0.17 0.75±0.20 0.87±0.41
Model set 10 2.88±0.30* 1.70±0.25* 1.49±0.42* 0.66±0.27
Curcumin group 10 2.43±0.18 1.26±0.22※ 1.14±0.36※ 0.73±0.16
Composition 1 group 10 1.87±0.43※▲ 0.86±0.31※▲ 0.90±0.39※▲ 0.94±0.30※▲
Composition 2 group 10 1.72±0.27※▲ 0.79±0.33※▲ 0.83±0.24※▲ 1.01±0.35※▲
Note: p < 0.05 compared to blank; in comparison with the set of models,※p is less than 0.05; compared with the curcumin group, the curcumin-enriched food has the advantages that,▲p＜0.05。
TABLE 2 comparison of the degree of float of each index with the model set
TC TG LDL-C HDL-C
Curcumin group 15.6％ 25.9％ 23.5％ 10.6％
Composition 1 group 35.0％ 49.4％ 39.6％ 42.4％
Composition 2 group 40.3％ 53.5％ 44.3％ 53.0％
The experimental results show that the composition and the curcumin alone can affect the levels of triglyceride and cholesterol, but the composition is lower in use amount (50%) and has more remarkable effect. No significant difference was observed between composition 1 and composition 2, but composition 2 had a greater ability to regulate blood lipids.
In addition to the above experiments, the inventors also performed repetitive experiments, including adjusting the amounts of the components in the composition within a certain range, adding conventional adjuvants to make different dosage forms, etc., which can achieve the objectives of the present invention.
Detailed Description
Example 1
Formula (1000 granules): curcumin 100g saw palm extract 170g piperine 7g
Microcrystalline cellulose 80g magnesium stearate 30g
The process comprises the following steps: mixing curcumin, Serenoa repens extract, piperine and microcrystalline cellulose, adding 6% PVPk30 ethanol solution to make soft mass, granulating, drying, adding magnesium stearate, mixing, and making into capsule.
Example 2
Formulation (1000 tablets): curcumin 95g saw palm extract 150g piperine 4g
30g of lycopene, 60g of microcrystalline cellulose, 15g of sodium carboxymethyl starch and 3g of superfine silica gel powder
The process comprises the following steps: mixing curcumin, saw palmetto extract, lycopene, piperine and microcrystalline cellulose, adding 7% PVPk30 ethanol solution to make soft mass, granulating, drying, adding silica gel micropowder, mixing, and tabletting.
Example 3
Formula (1000 granules): curcumin 105g saw palm extract 110g piperine 5g
Lycopene 20g poloxamer 188900 g
The process comprises the following steps: weighing poloxamer 188 according to a formula ratio, heating in 70 ℃ water bath until the poloxamer 188 is molten, adding curcumin dissolved by absolute ethyl alcohol, continuously stirring until uniform transparent liquid is formed and almost no alcohol smell exists, solidifying for 8 hours at-4 ℃, then drying for 8 hours in vacuum at 50 ℃, taking out and crushing, sieving by a 80-mesh sieve to obtain curcumin solid dispersion, uniformly mixing with piperine, lycopene and saw palmetto extract, and encapsulating into 1000 capsules.
Example 4
Formula (1000 granules): curcumin 100g saw palm extract 90g piperine 7g poloxamer 188850 g
The process comprises the following steps: same as example 3
Example 5
Formula (1000 granules): curcumin 100g saw palm extract (oil) 80g piperine 10g
130g of olive oil, 80300 g of Tween 80300 g of polyethylene glycol 40060 g
The process comprises the following steps: 1. adding curcumin, piperine and saw palmetto extract into olive oil, and mixing to obtain oil phase;
2. grinding and mixing Tween 80 and polyethylene glycol 400, and stirring in water bath at 30 deg.C for 1 hr to completely dissolve to obtain emulsified phase; 3. mixing the oil phase and the emulsified phase, stirring at high speed to obtain emulsified concentrated solution, and encapsulating into soft capsule.
Example 6
Formula (1000 granules): curcumin 100g saw palm extract (oil) 50g piperine 6g
Lycopene 40g olive oil 160g Tween 80320 g polyethylene glycol 40070 g
The process comprises the following steps: same as example 4 except for step 1.
1. Adding curcumin, piperine, lycopene and saw palmetto extract into oleum Olivarum, and mixing to obtain oil phase.
The above are only some examples of the present invention, which are further intended to illustrate the present invention and not to limit the scope of the present invention. Modifications and variations of the above-described embodiments may be made by anyone without departing from the scope and spirit of the invention, and are intended to be covered by the appended claims.

Claims (8)

1. The raw materials of the composition comprise, by weight, 95-105 parts of curcumin, 4-10 parts of saw palmetto extract and piperine, wherein the saw palmetto extract is 80-170 parts of solid extract and 50-80 parts of oily extract.
2. The composition of claim 1, further comprising lycopene.
3. The composition of claim 2 wherein the lycopene is present in an amount of from 20 to 40 parts by weight.
4. The composition of claim 1, wherein the saw palm extract is 100-170 parts by weight when the saw palm extract is a solid extract.
5. The composition of claim 1, wherein the saw palmetto extract is present in an amount of not less than 30% when the saw palmetto extract is a solid extract.
6. The composition of claim 1, wherein the saw palm extract is not less than 85% when the saw palm extract is an oily extract.
7. The composition as claimed in claim 1, which comprises 100 parts of curcumin, 110 parts of saw palm solid extract, 20-30 parts of lycopene and 4-7 parts of piperine.
8. The composition according to any one of claims 1 to 7, wherein said composition further comprises one or more pharmaceutically or dietetically acceptable adjuvants or excipients.
CN201711469863.3A 2017-12-29 2017-12-29 Composition for resisting atherosclerosis Active CN107982389B (en)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1456309A (en) * 2003-03-18 2003-11-19 于水 Antilipemic antiatherosclerosis medicine composition and preparing method, application thereof
CN106692153A (en) * 2017-01-12 2017-05-24 中国人民解放军第四军医大学 Compound rhizoma curcumae longae tablet

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6627227B2 (en) * 2000-05-09 2003-09-30 Kenneth Weisman Use of saw palmetto to prevent atherosclerosis

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1456309A (en) * 2003-03-18 2003-11-19 于水 Antilipemic antiatherosclerosis medicine composition and preparing method, application thereof
CN106692153A (en) * 2017-01-12 2017-05-24 中国人民解放军第四军医大学 Compound rhizoma curcumae longae tablet

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"番茄红素抗动脉粥样硬化的研究进展";胡敏予;《中国动脉硬化杂志》;20071231;第15卷(第6期);摘要。 *

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