CN111870626B - Pharmaceutical composition with blood fat reducing effect and preparation method and application thereof - Google Patents

Pharmaceutical composition with blood fat reducing effect and preparation method and application thereof Download PDF

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CN111870626B
CN111870626B CN202010670432.9A CN202010670432A CN111870626B CN 111870626 B CN111870626 B CN 111870626B CN 202010670432 A CN202010670432 A CN 202010670432A CN 111870626 B CN111870626 B CN 111870626B
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macroporous resin
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林熙
王国才
张玉波
张海鹏
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Guangdong Zhongji Gene Bioengineering Co ltd
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广东中暨基因生物工程有限公司
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K36/18Magnoliophyta (angiosperms)
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    • A61K36/73Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
    • A61K36/736Prunus, e.g. plum, cherry, peach, apricot or almond
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    • A61K2236/333Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/50Methods involving additional extraction steps
    • A61K2236/55Liquid-liquid separation; Phase separation

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Abstract

The invention relates to the technical field of traditional Chinese medicines, and particularly discloses a pharmaceutical composition with a blood fat reducing effect, and a preparation method and application thereof. The pharmaceutical composition with the function of reducing blood fat is prepared from the following raw materials in parts by weight: 10-15 parts of giant knotweed; 5-10 parts of miracle fruit kernels; 5-10 parts of seaweed; 3-8 parts of peach kernels; 3-6 parts of turtle shell. The invention takes giant knotweed rhizome, miracle fruit kernel, seaweed, peach kernel and turtle shell as raw materials to prepare the pharmaceutical composition with the function of reducing blood fat for the first time; the composition has excellent hypolipidemic effect; can be used as active ingredient for preparing medicine or health product with blood lipid reducing effect.

Description

Pharmaceutical composition with blood fat reducing effect and preparation method and application thereof
Technical Field
The invention relates to the technical field of traditional Chinese medicines, in particular to a pharmaceutical composition with a blood fat reducing effect, and a preparation method and application thereof.
Background
Hyperlipidemia refers to the condition of high blood lipid level in human body, which can directly cause diseases seriously harming human health, such as atherosclerosis, coronary heart disease, pancreatitis and the like. The blood fat content can be effectively controlled and reduced by taking western lipid-lowering medicines; however, if the western medicine for reducing blood fat is taken for a long time, the physical health of the patient is damaged due to the side effect of the medicine. Based on the above, more traditional Chinese medicine hypolipidemic drugs are developed, more drug choices can be provided for patients with hyperlipidemia, and damage to the body caused by long-term administration of one or more hypolipidemic drugs can be prevented.
The rhizoma Polygoni Cuspidati is dried rhizome and root of Polygonum cuspidatum Sieb. et Zucc. of Polygonaceae; has effects in promoting diuresis, eliminating jaundice, clearing away heat and toxic materials, dispelling blood stasis, relieving pain, relieving cough, and eliminating phlegm. The Sargassum is the algae of Sargassum fusiforme and Sargassum pallidum of Sargassaceae, and has the effects of softening hard masses, eliminating phlegm, promoting diuresis, and relieving swelling. The Chinese medicinal semen Persicae is dried mature seed of Prunus persica (L.) Batsch belonging to Rosaceae, and has effects of promoting blood circulation, removing blood stasis, loosening bowel to relieve constipation, and relieving cough and asthma. Carapax Trionycis is the dorsal scale of Trionycis of Trionychidae, and has effects in nourishing yin, suppressing yang, softening and resolving hard mass, and relieving fever and steaming. The fruit stone of Synsepalum dulcificum Daniell is the fruit stone of Synsepalum dulcificum Daniell of Sapotaceae.
At present, no report exists for preparing the blood fat reducing medicine by taking giant knotweed rhizome, miracle fruit kernel, seaweed, peach kernel and turtle shell as raw materials.
Disclosure of Invention
The invention aims to solve the technical problem of providing a medicinal composition with a brand-new composition and a blood fat reducing effect.
The technical scheme of the invention is as follows:
a pharmaceutical composition with a blood fat reducing effect is prepared from the following raw materials in parts by weight:
10-15 parts of giant knotweed; 5-10 parts of miracle fruit kernels; 5-10 parts of seaweed; 3-8 parts of peach kernels; 3-6 parts of turtle shell.
Preferably, the pharmaceutical composition with the function of reducing blood fat is prepared from the following raw materials in parts by weight:
10-12 parts of giant knotweed; 6-8 parts of miracle fruit kernels; 6-8 parts of seaweed; 5-6 parts of peach kernels; and 4-5 parts of turtle shell.
Most preferably, the pharmaceutical composition with the function of reducing blood fat is prepared from the following raw materials in parts by weight:
10 parts of giant knotweed; 8 parts of miracle fruit kernels; 8 parts of seaweed; 5 parts of peach kernel; and 4 parts of turtle shell.
The inventor firstly adopts the theory of traditional Chinese medicine to preferably select a large amount of traditional Chinese medicine prescriptions with the function of reducing blood fat, and then carries out verification on the effect of reducing blood fat through a blood fat reduction pharmacological experiment; the results show that the composition prepared from the raw materials of giant knotweed, miracle fruit kernel, seaweed, peach kernel and turtle shell has a good blood fat reducing effect. The composition can be used as an active ingredient to prepare medicines or health products with the function of reducing blood fat.
The preparation method of the pharmaceutical composition with the function of reducing blood fat is characterized by comprising the following steps:
mixing rhizoma Polygoni Cuspidati, semen Synsepalum dulcificum, Sargassum, semen Persicae and carapax Trionycis, extracting with water under heating, concentrating the extractive solution, and drying to obtain the pharmaceutical composition with blood lipid reducing effect.
The preparation method of the pharmaceutical composition with the function of reducing blood fat is characterized by comprising the following steps:
mixing giant knotweed rhizome, miracle fruit kernel, seaweed and peach kernel, heating and refluxing the mixture by using 50 to 95 volume percent of ethanol, and concentrating an extracting solution to obtain a traditional Chinese medicine ethanol extract;
extracting carapax Trionycis with water under reflux, concentrating the extractive solution, and drying to obtain carapax Trionycis extract;
mixing the traditional Chinese medicine alcohol extract and the turtle shell extract to obtain the pharmaceutical composition.
The inventor further researches and discovers that the blood fat reducing activity of the obtained pharmaceutical composition is different by taking giant knotweed rhizome, miracle fruit kernel, seaweed, peach kernel and turtle shell as raw materials and different preparation methods; if the method is adopted, the polygonum cuspidatum, the miracle fruit kernel, the seaweed and the peach kernel are extracted by ethanol, and the activity of reducing blood fat of the pharmaceutical composition prepared by extracting the turtle shell by water is better than that of the pharmaceutical composition prepared by extracting the polygonum cuspidatum, the miracle fruit kernel, the seaweed, the peach kernel and the turtle shell by water.
Preferably, the preparation method of the pharmaceutical composition with the effect of reducing blood fat comprises the following steps:
mixing giant knotweed rhizome, miracle fruit kernel, seaweed and peach kernel, heating and refluxing the mixture by using 50 to 95 volume percent of ethanol, and concentrating an extracting solution to obtain a traditional Chinese medicine ethanol extract; further enriching the effective components of the Chinese medicinal alcohol extract by using a macroporous resin column to obtain the effective parts of the Chinese medicinal materials;
extracting carapax Trionycis with water under reflux, concentrating the extractive solution, and drying to obtain carapax Trionycis extract;
mixing the effective parts of the traditional Chinese medicine with the turtle shell extract to obtain the pharmaceutical composition.
Preferably, the specific method for enriching the active ingredients of the Chinese medicinal alcohol extract by using the macroporous resin column comprises the following steps:
loading the traditional Chinese medicine alcohol extract to a macroporous resin column, and eluting by using ethanol with the volume fraction of 18% and 3-6 times of the column volume; and then eluting with 42% ethanol with 3-6 times of column volume, collecting the effective parts eluted by 42% ethanol, concentrating and drying to obtain the effective parts of the traditional Chinese medicine.
Most preferably, the specific method for further enriching the active ingredients of the traditional Chinese medicine alcohol extract by using a macroporous resin column comprises the following steps:
loading the Chinese medicinal alcohol extract on macroporous resin column, eluting with ethanol with volume fraction of 18% 5 times of column volume; then eluting with 42% ethanol with 5 times column volume, collecting 42% ethanol eluted effective components, concentrating and drying to obtain the Chinese medicinal effective components.
The inventor further researches and discovers that the blood fat reducing effect of the traditional Chinese medicine composition obtained by mixing the traditional Chinese medicine effective part obtained by enriching the effective components of the traditional Chinese medicine alcohol extract with the turtle shell extract is more obvious. The macroporous resin elution method is adopted to enrich and obtain a large amount of traditional Chinese medicine effective parts with the blood fat reducing effect from the traditional Chinese medicine alcohol extract, and the effective parts and the turtle shell extract can obviously improve the blood fat reducing effect. The inventor tries other column chromatography methods, such as silica gel column chromatography, ODS column chromatography and the like, but the blood fat reducing effect is not obviously improved after the obtained effective parts of the traditional Chinese medicine are mixed with the turtle shell extract.
The invention also provides application of the pharmaceutical composition with the function of reducing blood fat as an active ingredient in preparation of medicines or health-care products with the function of reducing blood fat.
Preferably, the dosage form of the medicine or the health care product is granules, capsules, tablets, impact, oral liquid or powder.
The above granules, capsules, tablets, shocks, oral liquids or powders can be prepared by the skilled person by using the pharmaceutical composition with hypolipidemic effect as an active ingredient by conventional preparation technology.
Has the advantages that: the invention provides a drug combination with a brand-new composition and a function of reducing blood fat; firstly, giant knotweed rhizome, miracle fruit kernel, seaweed, peach kernel and turtle shell are taken as raw materials to prepare the pharmaceutical composition with the function of reducing blood fat; the pharmaceutical composition has excellent blood fat reducing effect; the composition can be used as active ingredient for preparing medicine or health product with blood lipid reducing effect.
Detailed Description
The present invention is further explained with reference to the following specific examples, which do not limit the scope of the present invention.
Example 1 preparation of a pharmaceutical composition having hypolipidemic action
The raw materials comprise: 1Kg of giant knotweed rhizome; 800g of miracle fruit kernel; 800g of seaweed; 500g of peach kernels; turtle shell 400 g.
The preparation method comprises the following steps: pulverizing rhizoma Polygoni Cuspidati, semen Synsepalum dulcificum, Sargassum, semen Persicae and carapax Trionycis, mixing, extracting with 35L water under reflux, separating extractive solution after 1.5 hr, concentrating, and drying to obtain the pharmaceutical composition with blood lipid reducing effect.
Example 2 preparation of a pharmaceutical composition having hypolipidemic action
The raw materials comprise: 1Kg of giant knotweed rhizome; 800g of miracle fruit kernel; 800g of seaweed; 500g of peach kernels; turtle shell 400 g.
The preparation method comprises the following steps:
(1) pulverizing rhizoma Polygoni Cuspidati, semen Synsepalum dulcificum, Sargassum and semen Persicae, mixing, extracting with 31L 75% ethanol under reflux under heating for 1.5 hr, separating extractive solution, concentrating, and drying to obtain Chinese medicinal ethanol extract;
(2) pulverizing carapax Trionycis, extracting with 4L water under reflux, extracting for 1.5 hr, separating extractive solution, concentrating, and drying to obtain carapax Trionycis extract;
(3) the medicinal composition is obtained by uniformly mixing the traditional Chinese medicine alcohol extract and the turtle shell extract.
Example 3 preparation of a pharmaceutical composition having hypolipidemic action
The raw materials comprise: 1Kg of giant knotweed rhizome; 800g of miracle fruit kernel; 800g of seaweed; 500g of peach kernels; turtle shell 400 g.
The preparation method comprises the following steps:
(1) pulverizing rhizoma Polygoni Cuspidati, semen Synsepalum dulcificum, Sargassum and semen Persicae, mixing, extracting with 31L 75% ethanol under reflux under heating for 1.5 hr, separating extractive solution, concentrating, and drying to obtain Chinese medicinal ethanol extract;
further, the traditional Chinese medicine alcohol extract is put on a D101 type macroporous resin column (the weight and the dosage of the filler of the macroporous resin in the macroporous resin column are 30 times of the traditional Chinese medicine alcohol extract), and ethanol with the volume fraction of 18 percent which is 5 times of the column volume is firstly used for elution (the part is discarded without use); eluting with 42% ethanol 5 times the column volume, collecting the 42% ethanol eluate, concentrating, and drying to obtain the effective components;
(2) pulverizing carapax Trionycis, extracting with 4L water under reflux, extracting for 1.5 hr, separating extractive solution, concentrating, and drying to obtain carapax Trionycis extract;
(3) mixing the effective components with carapax Trionycis extract to obtain the medicinal composition.
Comparative example 1 preparation of pharmaceutical composition having hypolipidemic effect
The raw materials comprise: 1Kg of giant knotweed rhizome; 800g of miracle fruit kernel; 800g of seaweed; 500g of peach kernels; turtle shell 400 g.
The preparation method comprises the following steps:
(1) pulverizing rhizoma Polygoni Cuspidati, semen Synsepalum dulcificum, Sargassum and semen Persicae, mixing, extracting with 31L 75% ethanol under reflux under heating for 1.5 hr, separating extractive solution, concentrating, and drying to obtain Chinese medicinal ethanol extract;
further, the traditional Chinese medicine alcohol extract is put on a D101 type macroporous resin column (the weight of the filler of the macroporous resin in the macroporous resin column is 30 times of that of the traditional Chinese medicine alcohol extract), and is eluted by water with the volume of 5 times of the column (the part is discarded without use); eluting with 20% ethanol 5 times the column volume, collecting the effective components eluted with 20% ethanol, concentrating, and drying to obtain the effective components;
(2) pulverizing carapax Trionycis, extracting with 4L water under reflux, extracting for 1.5 hr, separating extractive solution, concentrating, and drying to obtain carapax Trionycis extract;
(3) mixing the effective components with carapax Trionycis extract to obtain the medicinal composition.
Comparative example 1 is different from example 3 in the elution conditions of the macroporous resin.
Comparative example 2 preparation of pharmaceutical composition having hypolipidemic effect
The raw materials comprise: 1Kg of giant knotweed rhizome; 800g of miracle fruit kernel; 800g of seaweed; 500g of peach kernels; turtle shell 400 g.
The preparation method comprises the following steps:
(1) pulverizing rhizoma Polygoni Cuspidati, semen Synsepalum dulcificum, Sargassum and semen Persicae, mixing, extracting with 31L 75% ethanol under reflux under heating for 1.5 hr, separating extractive solution, concentrating, and drying to obtain Chinese medicinal ethanol extract;
further, the traditional Chinese medicine alcohol extract is put on a D101 type macroporous resin column (the weight and the dosage of the filler of the macroporous resin in the macroporous resin column are 30 times of the traditional Chinese medicine alcohol extract), and ethanol with the volume fraction of 40 percent which is 5 times of the column volume is firstly used for elution (the part is discarded without use); eluting with 60% ethanol 5 times the column volume, collecting the 60% ethanol eluate, concentrating, and drying to obtain the effective components;
(2) pulverizing carapax Trionycis, extracting with 4L water under reflux, extracting for 1.5 hr, separating extractive solution, concentrating, and drying to obtain carapax Trionycis extract;
(3) mixing the effective components with carapax Trionycis extract to obtain the medicinal composition.
Comparative example 2 differs from example 3 in the elution conditions of the macroporous resin.
Examples of the experiments
Dividing 70 male and female half SD rats into 6 groups on average, and each group comprises 10 rats; the test groups are respectively a normal group, a high fat control group and test groups 1-5. The normal group is fed with common feed every day, the high-fat control group and the experimental group are fed with high-fat feed every day in a range of 1-5, and SD rats in each group drink water freely. In the experimental groups 1 to 5, the pharmaceutical compositions with the hypolipidemic effect prepared in the examples 1 to 3 and the comparative examples 1 to 2 were added to a daily high-fat feed in an amount of 5 mg/kg. The SD rats are sacrificed after being continuously fed for 30 days, and the total cholesterol TC and the triglyceride TG content of the serum of each group of SD rats are measured after the blood is collected by the abdominal veins; the test results are shown in Table 1.
TABLE 1 results of the hypolipidemic test
Feeding medicine TC content (mmol/L) TG content (mmol/L)
Normal group Is free of 1.55±0.39 1.48±0.33
High fat control group Is free of 8.41±0.67 2.62±0.49
Experimental group 1 EXAMPLE 1 pharmaceutical composition 5.92±0.54 2.21±0.41
Experimental group 2 EXAMPLE 2 pharmaceutical composition 5.17±0.47 2.01±0.45
Experimental group 3 EXAMPLE 3 pharmaceutical composition 3.05±0.43 1.44±0.38
Experimental group 4 Comparative example 1 pharmaceutical composition 6.08±0.51 2.30±0.35
Experimental group 5 Comparative example 2 pharmaceutical composition 6.71±0.66 2.42±0.42
As can be seen from the experimental data in table 1, the SD rats of experimental groups 1 to 3 fed with the pharmaceutical composition with hypolipidemic effect prepared in examples 1 to 3 had significantly lower contents of total serum cholesterol TC and triglyceride TG than those of the SD rats of the high-fat control group. This shows that the pharmaceutical composition of the present invention has excellent hypolipidemic effect. In addition, it can be seen that the reduction degree of the total serum cholesterol TC and triglyceride TG of the SD rats in experimental groups 1 to 3 is different; this indicates that: the pharmaceutical compositions prepared by different preparation methods by using giant knotweed rhizome, miracle fruit kernel, seaweed, peach kernel and turtle shell as raw materials have different hypolipidemic activities. In example 3, the blood lipid reducing effect of the pharmaceutical composition is further improved and is most significant in the blood lipid reducing effect by using the pharmaceutical composition obtained by enriching the active ingredients of the alcoholic extract of the traditional Chinese medicine by using a macroporous resin column and then mixing the alcoholic extract of the traditional Chinese medicine with the turtle shell extract.
As can be seen from the decrease in serum total cholesterol TC and triglyceride TG levels in the SD rats of experimental groups 4 and 5, the decrease was much smaller than that in the SD rat of experimental group 3. This indicates that: the macroporous resin elution method plays a decisive role in determining whether effective parts with the function of reducing blood fat can be enriched from the alcohol extracts of giant knotweed rhizome, miracle fruit kernel, seaweed and peach kernel; only under the condition of macroporous resin elution, a large amount of effective parts of the traditional Chinese medicine with the function of reducing blood fat can be enriched from the alcohol extracts of giant knotweed rhizome, miracle fruit kernel, seaweed and peach kernel; other macroporous resin elution conditions cannot enrich a large amount of effective parts of the traditional Chinese medicine with the function of reducing blood fat from the alcohol extracts of giant knotweed rhizome, miracle fruit kernel, seaweed and peach kernel; therefore, the effect of reducing blood fat is not obvious after the effective parts of the traditional Chinese medicine obtained by enrichment by the macroporous resin method in the comparative examples 1 and 2 are mixed with the turtle shell extract.

Claims (6)

1. A pharmaceutical composition with a function of reducing blood fat is characterized by being prepared from the following raw materials in parts by weight:
10-15 parts of giant knotweed; 5-10 parts of miracle fruit kernels; 5-10 parts of seaweed; 3-8 parts of peach kernels; 3-6 parts of turtle shell;
the pharmaceutical composition is prepared by the following method:
mixing giant knotweed rhizome, miracle fruit kernel, seaweed and peach kernel, heating and refluxing the mixture by using 50 to 95 volume percent of ethanol, and concentrating an extracting solution to obtain a traditional Chinese medicine ethanol extract; further enriching the effective components of the Chinese medicinal alcohol extract by using a macroporous resin column to obtain the effective parts of the Chinese medicinal materials;
extracting carapax Trionycis with water under reflux, concentrating the extractive solution, and drying to obtain carapax Trionycis extract;
mixing the effective parts of the traditional Chinese medicines with the turtle shell extract to obtain the pharmaceutical composition;
the specific method for further enriching the active ingredients of the traditional Chinese medicine alcohol extract by using the macroporous resin column comprises the following steps: loading the traditional Chinese medicine alcohol extract to a macroporous resin column, and eluting by using ethanol with the volume fraction of 18% and 3-6 times of the column volume; eluting with 42% ethanol (3-6 times column volume), collecting 42% ethanol-eluted effective components, concentrating, and drying to obtain the effective components;
the macroporous resin column is a D101 type macroporous resin column.
2. The pharmaceutical composition with the effect of reducing blood fat according to claim 1, which is prepared from the following raw materials in parts by weight:
10-12 parts of giant knotweed; 6-8 parts of miracle fruit kernels; 6-8 parts of seaweed; 5-6 parts of peach kernels; and 4-5 parts of turtle shell.
3. The pharmaceutical composition with the effect of reducing blood fat according to claim 1, which is prepared from the following raw materials in parts by weight:
10 parts of giant knotweed; 8 parts of miracle fruit kernels; 8 parts of seaweed; 5 parts of peach kernel; and 4 parts of turtle shell.
4. The pharmaceutical composition with hypolipidemic effect according to claim 1, wherein:
the specific method for further enriching the active ingredients of the traditional Chinese medicine alcohol extract by using the macroporous resin column comprises the following steps: loading the Chinese medicinal alcohol extract on macroporous resin column, eluting with ethanol with volume fraction of 18% 5 times of column volume; then eluting with 42% ethanol with 5 times column volume, collecting 42% ethanol eluted effective components, concentrating and drying to obtain the Chinese medicinal effective components.
5. The use of the pharmaceutical composition with hypolipidemic effect of any one of claims 1 to 4 as an active ingredient in the preparation of a medicament or health product with hypolipidemic effect.
6. The use of claim 5, wherein the pharmaceutical or nutraceutical formulation is a granule, capsule, tablet, granule, oral liquid or powder.
CN202010670432.9A 2020-07-13 2020-07-13 Pharmaceutical composition with blood fat reducing effect and preparation method and application thereof Active CN111870626B (en)

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基于现代文献探讨干预血脂异常的药食同源类药物用药特点及其病机分析;葛肖波等;《世界中西医结合杂志》;20200531;第15卷(第5期);845-849 *
神秘果对高脂模型小鼠的降血脂效应;卢申姣等;《中药药理与临床》;20180430;第34卷(第2期);75-79 *

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