CN105582163A - Pharmaceutical composition for regulating blood lipid and preventing atherosclerosis - Google Patents

Pharmaceutical composition for regulating blood lipid and preventing atherosclerosis Download PDF

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Publication number
CN105582163A
CN105582163A CN201610107064.0A CN201610107064A CN105582163A CN 105582163 A CN105582163 A CN 105582163A CN 201610107064 A CN201610107064 A CN 201610107064A CN 105582163 A CN105582163 A CN 105582163A
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coptis
ligusticum wallichii
luffa
myrrh
cloves
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冯敏
孔淑贞
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Chongqing Technology and Business University
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Chongqing Technology and Business University
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/13Coniferophyta (gymnosperms)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/23Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A61K36/236Ligusticum (licorice-root)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/32Burseraceae (Frankincense family)
    • A61K36/328Commiphora, e.g. mecca myrrh or balm of Gilead
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/42Cucurbitaceae (Cucumber family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/54Lauraceae (Laurel family), e.g. cinnamon or sassafras
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/61Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/71Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
    • A61K36/718Coptis (goldthread)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/81Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K2236/30Extraction of the material
    • A61K2236/33Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/331Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using water, e.g. cold water, infusion, tea, steam distillation, decoction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K2236/30Extraction of the material
    • A61K2236/33Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/333Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K2236/30Extraction of the material
    • A61K2236/39Complex extraction schemes, e.g. fractionation or repeated extraction steps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K2236/51Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying

Abstract

The invention relates to a pharmaceutical composition for regulating blood lipid and preventing atherosclerosis. The pharmaceutical composition is prepared from the following raw materials in percentage by weight: 5-40% of coptis chinensis, 5-30% of loofah sponge, 1-20% of ligusticum wallichii, 5-20% of cycas recoluta flower, 5-20% of cinnamon, 1-20% of clove, 5-20% of irisensata thunb and 5-20% of myrrh. In the composition, the coptis chinensis and loofah sponge serve as monarch drugs and are in reasonable compatibility with the ligusticum wallichii, cinnamon, cycas recoluta flower, clove and irisensata thunb and then are assisted by the myrrh of proper proportion to realize synergism, the effect of regulating blood lipid is obvious, and a remarkable function of preventing atherosclerosis is realized. Moreover, the composition is small in size and convenient to prepare, carry and take; and the preparation method is simple, and the cost is low.

Description

A kind of blood fat and atherosis pharmaceutical composition of prevention of arterial of regulating
Technical field
The invention belongs to technical field of traditional Chinese medicines, relate to a kind of blood fat and atherosis pharmaceutical composition of prevention of arterial of regulating, alsoRelate to the preparation method of this Chinese medicine composition.
Background technology
Atherosclerotic (atherosclerosis, AS) is the main pathological basis of cardiovascular and cerebrovascular disease, with in large, medium sized arteryMembrane lipid calmness, atherosclerosis plaque forming, proliferation of fibrous tissue, tube wall are hardened to feature, finally cause luminal stenosis so that completeFull obstruction, causes the ischemic of the vitals such as the heart, brain, kidney, becomes the first cause of mankind's death. Inflammation and dyslipidemiaIt is the main driver that AS occurs. The abnormal cholesterol levels raising, especially LDL-C raises extremely,Thereby will be deposited on large-scalely to form atherosclerotic plaque on the arterial wall of medium-sized artery, then bring out cardiovascular relevantDisease, as diseases such as hypertension, myocardial anoxia, myocardial infarctions. Atherosclerosis is turned to the disease of a complicated reason,Be subject to the impact of several factors, the Lipid increase that wherein disorders of lipid metabolism causes is its independently hazards. The present age, doctor was manyInquire into this cause of disease from inside and outside two ends, think external cause to have a liking for food delicious food, to change raw phlegm turbid relevant, internal cause duty in spleen, kidney, liverFunctional disturbance. Statins is the fat-reducing medicament of commonly using the most clinically. But the common bad reaction of statins is liverThe abnormal rising of dirty transaminase and the pathology of muscle, its most serious bad reaction is rhabdomyolysis and peripheral nervePathology. Anti-inflammatory, blood-activating and stasis-removing can be brought into play anti-AS coronary artery by number of ways such as lipopenicillinase, antiplatelet adhesion and aggregationIt is the important means of prevention cardiovascular and cerebrovascular disease that atherosis effect effectively regulates dyslipidemia, and Chinese herbal medicine regulates the work of blood fatWith being sure, especially there is the incomparable advantage of Western medicine at prevention of arterial aspect atherosis.
Summary of the invention
In view of this, the object of the present invention is to provide a kind of blood fat and atherosis pharmaceutical composition of prevention of arterial of regulating,In conjunction with the advantage of modern medicine and traditional medicine, between component, there is synergistic function, there is good adjusting blood fat and pre-Anti-atherosclerotic effect, and preparation method is simple.
For achieving the above object, the invention provides following technical scheme:
Adjusting blood fat of the present invention and the atherosis pharmaceutical composition of prevention of arterial, by weight percentage by following raw materialMake: the coptis 5~40%, luffa 5~30%, Ligusticum wallichii 1~20%, sago cycas spends 5~20%, Chinese cassia tree 5~20%, cloves 1~20%,Flagger 5~20%, myrrh 5~20%.
The optimization formula of the pharmaceutical composition that adjusting blood fat of the present invention and prevention of arterial are atherosis, described Chinese medicine composition is by heavyAmount percentage meter is made up of following raw material: the coptis 10~30%, luffa 10~25%, and Ligusticum wallichii 10~15%, sago cycas spends 10~15%,Chinese cassia tree 10~15%, cloves 5~15%, flagger 5~10%, myrrh 5~10%.
The optimization formula of the pharmaceutical composition that adjusting blood fat of the present invention and prevention of arterial are atherosis, by weight percentage byFollowing raw material is made: the coptis 20%, luffa 20%, and Ligusticum wallichii 10%, sago cycas spends 15%, Chinese cassia tree 10%, cloves 10%,Flagger 10%, myrrh 5%.
Adjusting blood fat of the present invention and the atherosis pharmaceutical composition of prevention of arterial, the processing method of the described coptis is with volumeMark is that 75% ethanol water is the solvent extraction coptis, refluxing extraction 3 times, and each solvent adding amount adds by coptis 1gSolvent 7mL meter extracts 0.5 hour at every turn, merges extract, concentrated, makes final concentration reach 1~1.5g/mL; Ligusticum wallichii bodyIntegration number is 60% ethanol water refluxing extraction 3 times, and the consumption of each ethanol water adds 6mL second by 1g Ligusticum wallichiiAlcohol solution meter extracts 0.5 hour at every turn, merges extract, reclaims solvent concentrated, makes final concentration reach 1~1.5g/mL;After luffa frying, chopping is extracted 3 times by the 1g 10mL that adds water, and each 0.5h, merges extract and be concentrated into after 1~1.5g/mLFor subsequent use; Chinese cassia tree, sago cycas flower, flagger, cloves are dried respectively and beat powder to cross 10~200 mesh sieves for subsequent use; Myrrh was smashed 100 ordersSieve; Above material is mixed by former medicine mass ratio and obtain pharmaceutical composition of the present invention.
Raw material components proterties of the present invention and effect are as follows:
1. the coptis is ranunculaceae plant coptis CoptischinensisFranch, triangle leaf coptis CoptisdeltoideaC.Y.ChengetHsiao or cloud connect the dry rhizome of CoptisteetaWall., and bitter is cold in nature, the thoughts of returning home, spleen, stomach, liver, courage,Large intestine channel, has heat-clearing and damp-drying drug, effect of purging intense heat and detonicating. Alkaloids composition is the main active of the coptis, comprises littleBark of a cork tree alkali, coptisine, epiberberine, jateorrhizine etc., modern pharmacological research discovery, jamaicin has anti-inflammatory, antibacterial, antioxygenChange, antitumor, protect the multiple physiological effects such as cardiovascular, neuroprotective system.
2. luffa is the vascular bundle of the ripening fruits of cucurbitaceous plant sponge gourd or Guangdong sponge gourd. The sponge gourd beginning is loaded in Compendium of Material Medica,List dish portion, vegetable category in. Can lead to people's train of thought internal organs, and go wind removing toxic substances, detumescence is reduced phlegm, and the pain of dispelling desinsection is controlled all blood diseases. TasteSweet, cool in nature. Return lung, liver, stomach warp. The light tonneau of body.
3. Ligusticum wallichii is the dry rhizome of samphire Ligusticum wallichii LigusticumchuanxiongHort., and " legendary god of farming's book on Chinese herbal medicine begins to be loaded inThrough ". It is warm in nature, pungent, the micro-hardship of taste; There is effect of blood-activating and qi-promoting, wind-expelling pain-stopping. Clinically be mainly used in treating heart and brain bloodThe aspects such as pipe, breathing, urinary system.
4. the medicinal beginning of Chinese cassia tree is loaded in Shennong's Herbal, classify as top grade, " the pungent temperature of taste, main all kinds of diseases and ailments are supported spirit, and color,Profit joint, tonifying middle-Jiao and Qi. For all medicines are first engaged logical making, the logical god of clothes, makes light of one's life by commiting suicide not old for a long time. " Chinese cassia tree lists in wood in Compendium of Material MedicaPortion's the 34 volume: " hard muscles and bones, promoting blood circulation should be led hundred medicines, clothes for a long time, and angle, not old ".
5. cloves begins to be loaded in " property of medicine opinion ", and taste is pungent, extremely hot in nature. Return spleen, stomach, lung, kidney, in Chinese pharmacology, belong to drugs for dispelling internal cold,Warm stomach, warm kidney, can treat deficiency-cold in spleen and stomach. Modern pharmacology studies have shown that it has the free radical of removing, the antipyretic effect such as antibacterial.
6. myrrh begin to be loaded in the Tang Dynasty " Kaibao Bencao ", is the conventional important drugs simply in China's summary, inDoctor thinks, myrrh bitter is pungent, property flat, has promoting blood circulation and stopping pain, effect of detumescence and promoting granulation. Pharmacological research shows: myrrh has and moves backHeat, anti-inflammatory, analgesia, adjusting blood fat, anti parasitic, the multiple pharmacologically active such as antimicrobial, antitumor, and safer, nothingObvious toxic-side effects.
7. flagger IrisensataThunb: taste is salty, sour, bitter, slightly cool in nature. Clearing heat and detoxicating, hemostasis, diuresis. It is nontoxic,Enter kidney, the heart channel of Hang-Shaoyin. Compendium of Material Medica is recorded: " calabash shell serving as a dipper grass virgin soil Yezhong, grows thickly on the spot, one two, 30 stems, height of seedling three, fourChi, puts forth in leaf, blossoms and bears fruit. Suffer from the glutted person of chest abdomen, get horse chinaberry and beat cold water clothes, let out number and go and heal. "
8. sago cycas flower, calls as cycad, is the flower of cycad sago cycas (Cycasrevoluta), and property is flat, heat-clearing,Hemostasis, the loose stasis of blood. Control dysentery, spit blood, have blood in stool, stomachache, hematuria, menorrhalgia, treating swelling and pain by traumatic injury. " property of medicine is examined " recordedIt " controls convulsive seizure due to phlegm-fire "; " south of the Five Ridges gather medicinal herbs record " records its " hemostasis, lower phlegm. Control convulsive seizure due to phlegm-fire. " sago cycas is containing sago cycas element (Cyasine) and new ironSet plain first, second, there is active anticancer.
The pharmaceutical composition that adjusting blood fat of the present invention and prevention of arterial are atherosis can be further according to the routine side of pharmaceutical preparationMethod is made the various formulations that are applicable to clinical use, include but not limited to powder, granule, capsule, pill (plain ball orCoated pellet) etc.
Single medicine action effect is clinically limited, and beneficial effect of the present invention is: in said composition, with the coptis,Luffa is monarch drug in a prescription altogether, by itself and Ligusticum wallichii, Chinese cassia tree, sago cycas flower, cloves, flagger reasonable compatibility, then is aided with proper proportionMyrrh, Synergistic, regulates blood fat successful, and has the effect that remarkable prevention of arterial is atherosis. Remove this groupArbitrary composition in closing, does not all have their synergistic lipopenicillinases and study of anti-atherogenic effect effective. And coptis bitter cold,Chinese cassia tree extremely hot in nature, Ligusticum wallichii is warm in nature, cloves extremely hot in nature, with certain proportion compatibility, the cold temperature of mending that can disappear, long-term taking, does not hinderTaste. Meanwhile, with the alcohol extract of the coptis and Ligusticum wallichii for and other several drugs compatibility, be not only conducive to the coptis and Ligusticum wallichiiThe absorption of active component, onset speed is fast, and bioavilability is high, reduces blood fat and antiatherogenic effective. ThisOutward, said composition volume is little, is beneficial to preparation, carries and takes; And method for making is easy, cost is low.
Detailed description of the invention
In order to make object of the present invention, technical scheme and beneficial effect clearer, below the preferred embodiments of the present invention are enteredThe description that row is detailed.
The preparation of embodiment 1, pharmaceutical composition and adjusting blood fat compliance test result
1) preparation method is as follows:
The ethanol water refluxing extraction that is 70% by volume fraction after coptis section 3 times, the consumption of each ethanol water is pressedThe 1g coptis adds 7mL ethanol water meter, extracts 0.5 hour at every turn, merges extract, reclaims solvent and is concentrated into concentrationFor 1g/mL, for subsequent use; The ethanol water refluxing extraction that Ligusticum wallichii section is 60% by volume fraction 3 times, each ethanol is water-solubleThe consumption of liquid adds 6mL ethanol water by 1g Ligusticum wallichii, extracts 0.5 hour at every turn, merges extract, reclaims solvent alsoBe concentrated into concentration and be 1g/mL, for subsequent use; After luffa frying, chopping is extracted 3 times by the 1g 10mL that adds water, and each 0.5h, closesAnd extract is concentrated into after 1g/mL for subsequent use; Chinese cassia tree, sago cycas flower, flagger, cloves are dried respectively and beat powder to cross 100 mesh sieves standbyWith; It is for subsequent use that myrrh was smashed 100 mesh sieves.
According to formula ratio: 1. the coptis 20%, luffa 20%, Ligusticum wallichii 10%, sago cycas spends 15%, Chinese cassia tree 10%, cloves 10%,Flagger 10%, myrrh 5%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g) obtain serum regulating drug composition group 1.
2. the coptis 40%, luffa 10%, Ligusticum wallichii 10%, sago cycas spends 10%, Chinese cassia tree 10%, cloves 10%, flagger 5%,Myrrh 5%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containing crude drug 0.2g)Obtain serum regulating drug composition group 2.
3. the coptis 5%, luffa 30%, Ligusticum wallichii 20%, sago cycas spends 10%, Chinese cassia tree 15%, cloves 5%, flagger 10%,Myrrh 5%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containing crude drug 0.2g)Obtain serum regulating drug composition group 3.
4. the coptis 30%, luffa 10%, Ligusticum wallichii 15%, sago cycas spends 10%, Chinese cassia tree 10%, cloves 15%, flagger 5%,Myrrh 5%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containing crude drug 0.2g)Obtain serum regulating drug composition group 4.
5. the coptis 10%, luffa 25%, Ligusticum wallichii 10%, sago cycas spends 15%, Chinese cassia tree 10%, cloves 10%, flagger 10%,Myrrh 10%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containing crude drug 0.2g)Obtain serum regulating drug composition group 5.
2) separately prepare control drug 1~14 by following formula:
Control drug 1: according to formula ratio mass ratio: the coptis 21%, luffa 21%, Ligusticum wallichii 11%, sago cycas spends 16%,Chinese cassia tree 11%, cloves 10%, flagger 10%, mixes ready extraction concentrate liquid or powder, and addsWater is made liquid (every mL is containing crude drug 0.2g)
Control drug 2: according to formula ratio: the coptis 22%, luffa 22%, sago cycas spends 17%, Chinese cassia tree 11%, cloves 11%,Flagger 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 3: according to formula ratio: the coptis 22%, luffa 22%, Ligusticum wallichii 11%, sago cycas spends 17%, cloves 11%,Flagger 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 4: according to formula ratio: the coptis 22%, luffa 22%, Ligusticum wallichii 11%, sago cycas spends 17%, Chinese cassia tree 11%,Flagger 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 5: according to formula ratio: the coptis 22%, luffa 22%, Ligusticum wallichii 11%, sago cycas spends 17%, Chinese cassia tree 11%,Cloves 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containsCrude drug 0.2g).
Control drug 6: according to formula ratio: the coptis 25%, luffa 25%, Ligusticum wallichii 11%, Chinese cassia tree 11%, cloves 11%,Flagger 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 7: according to formula ratio: luffa 25%, Ligusticum wallichii 12%, sago cycas spends 20%, Chinese cassia tree 12%, cloves 12%,Flagger 12%, myrrh 7%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 8: according to formula ratio: the coptis 25%, Ligusticum wallichii 12%, sago cycas spends 20%, Chinese cassia tree 12%, cloves 12%,Flagger 12%, myrrh 7%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 9: according to formula ratio: the coptis 23%, luffa 23%, Ligusticum wallichii 13%, sago cycas spends 18%, Chinese cassia tree 13%,Cloves 10%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containing crude drug 0.2g).
Control drug 10: the coptis 25%, luffa 25%, Ligusticum wallichii 15%, sago cycas spends 20%, flagger 10%, myrrh 5%,Ready extraction concentrate or powder are mixed, and add water and make liquid (every mL containing crude drug 0.2g).
Control drug 11: the coptis 25%, luffa 25%, Chinese cassia tree 15%, cloves 15%, flagger 10%, myrrh 10%,Ready extraction concentrate or powder are mixed, and add water and make liquid (every mL containing crude drug 0.2g).
Control drug 12: Ligusticum wallichii 20%, sago cycas spends 25%, Chinese cassia tree 15%, cloves 15%, flagger 15%, myrrh 10%,Ready extraction concentrate or powder are mixed, and add water and make liquid (every mL containing crude drug 0.2g).
Control drug 13: the coptis 100%, directly adds water the concentrate of extraction and make liquid (every mL is containing crude drug 0.2g).
Control drug 14: luffa 100%, directly adds water luffa vegetable sponge and make liquid (every mL is containing crude drug 0.2g).3) 160 of male golden yellow gophers, normally raised after one week, and Golden Hamster is divided into 8 of blank normal group and high fat at random152 of model group. Normal group continues to raise with normal diet, and high fat group all changes feeds high lipid food, after 4 weeks by use capillary fromVena ophthalmica clump sample of blood, drawn. Gained blood sample is the centrifugal 10min of centrifugal 3000r/min at 4 DEG C, after separation obtainsMeasure blood lipid level in serum, if blood fat raises, modeling success is described. High fat component is become to 19 groups, i.e. control group 1~14With 1~5 group of Experimental agents group; Definite method of dosage is to convert the dosage into animal used as test by clinical dosage,Each group gavage every day is treated 4 weeks by human body 15g every day drug intervention, the isopyknic physiological saline of normal group gavage. Medicine connectsContinuous therapeutic intervention 4 weeks, fasting 12h after last administration. After fasting 12h, gather blood from Golden Hamster vena ophthalmica clumpFluid samples, gained blood sample is the centrifugal 10min of centrifugal 3000r/min at 4 DEG C, again measures blood lipid level in serum, knotFruit is as shown in table 1.
Blood lipid level before and after table 1 administration
(with ratio before administration,P<0.05,△△P<0.01;n=8)
As shown in Table 1: (1), from experimental result, the lipid-lowering effect of Experimental agents group 1~5 is better than control group, particularlyThe lipid-lowering effect of Experimental agents group is best, not only can extremely significantly reduce TC and LDL-C level (p < 0.01), also canExtremely significantly reduce the level (p < 0.01) of TG; From reducing the amplitude of blood lipid level, Experimental agents group 1 is golden yellowThe TC level of suslik is from being reduced to higher than 12% of normal group higher than 109% of normal group; LDL-C level is from higher than just79% of normal group is reduced to higher than 13% of normal group; The level of TG also from be reduced to higher than 213% of normal group higher thanNormal 87%; Reduce the amplitude maximum of blood lipid level; Effect is best. (2) reduce any medicine in drug regimen,Capital reduces lipid-lowering effect (control group 1~8), and they may reduce TC, part or all of index in TG and LDL-C, butThe level reducing and amplitude are all not as good as Experimental agents group; Particularly in control group, remove the control group 7 of the coptis and remove luffaThe lipid-lowering effect of control group 8 poorer; The visible coptis and the luffa important function in this drug regimen. (3) reduce medicineAfter two kinds of medicines in thing combination, when the effect of lipopenicillinase is more a kind of than minimizing poorer (control group 9~12), particularly removing the coptisAfter two kinds of monarchs drug in a prescription of luffa, from the experimental results, there is the trend that reduces serum lipids, but there is no statistical significance; Enter oneStep has proved the coptis and luffa critical role in the present invention. (4) from the result of control group 13 and 14, use separatelyThe coptis also has certain reduction TC and the effect of LDL-C, but effect is not as drug regimen; Luffa has certain falling separatelyThe effect of low TG. Show that by the experimental result of control group other medicines in this combination add the work of rear mutual SynergisticWith. Shown by above-mentioned experimental result, drug regimen of the present invention and optimization formula have more significant result for the treatment of.
The atherosis compliance test result of prevention of arterial of embodiment 2, pharmaceutical composition
1) preparation method is as follows:
The ethanol water refluxing extraction that is 70% by volume fraction after coptis section 3 times, the consumption of each ethanol water is pressedThe 1g coptis adds 7mL ethanol water meter, extracts 0.5 hour at every turn, merges extract, reclaims solvent and is concentrated into concentrationFor 1g/mL, for subsequent use; The ethanol water refluxing extraction that Ligusticum wallichii section is 60% by volume fraction 3 times, each ethanol is water-solubleThe consumption of liquid adds 6mL ethanol water by 1g Ligusticum wallichii, extracts 0.5 hour at every turn, merges extract, reclaims solvent alsoBe concentrated into concentration and be 1g/mL, for subsequent use; After luffa frying, chopping is extracted 3 times by the 1g 10mL that adds water, and each 0.5h, closesAnd extract is concentrated into after 1g/mL for subsequent use; Chinese cassia tree, sago cycas flower, flagger, cloves are dried respectively and beat powder to cross 100 mesh sieves standbyWith; It is for subsequent use that myrrh was smashed 100 mesh sieves.
According to formula ratio: 1. the coptis 20%, luffa 20%, Ligusticum wallichii 10%, sago cycas spends 15%, Chinese cassia tree 10%, cloves 10%,Flagger 10%, myrrh 5%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g) obtain pharmaceutical composition group 1.
2. the coptis 40%, luffa 10%, Ligusticum wallichii 10%, sago cycas spends 10%, Chinese cassia tree 10%, cloves 10%, flagger 5%,Myrrh 5%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containing crude drug 0.2g)Obtain pharmaceutical composition group 2.
3. the coptis 5%, luffa 30%, Ligusticum wallichii 20%, sago cycas spends 10%, Chinese cassia tree 15%, cloves 5%, flagger 10%,Myrrh 5%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containing crude drug 0.2g)Obtain pharmaceutical composition group 3.
4. the coptis 30%, luffa 10%, Ligusticum wallichii 15%, sago cycas spends 10%, Chinese cassia tree 10%, cloves 15%, flagger 5%,Myrrh 5%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containing crude drug 0.2g)Obtain pharmaceutical composition group 4.
5. the coptis 10%, luffa 25%, Ligusticum wallichii 10%, sago cycas spends 15%, Chinese cassia tree 10%, cloves 10%, flagger 10%,Myrrh 10%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containing crude drug 0.2g)Obtain pharmaceutical composition group 5.
2) separately prepare control drug 1~8 by following formula:
Control drug 1: according to formula ratio mass ratio: the coptis 21%, luffa 21%, Ligusticum wallichii 11%, sago cycas spends 16%,Chinese cassia tree 11%, cloves 10%, flagger 10%, mixes ready extraction concentrate liquid or powder, and addsWater is made liquid (every mL is containing crude drug 0.2g)
Control drug 2: according to formula ratio: the coptis 22%, luffa 22%, sago cycas spends 17%, Chinese cassia tree 11%, cloves 11%,Flagger 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 3: according to formula ratio: the coptis 22%, luffa 22%, Ligusticum wallichii 11%, sago cycas spends 17%, cloves 11%,Flagger 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 4: according to formula ratio: the coptis 22%, luffa 22%, Ligusticum wallichii 11%, sago cycas spends 17%, Chinese cassia tree 11%,Flagger 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 5: according to formula ratio: the coptis 22%, luffa 22%, Ligusticum wallichii 11%, sago cycas spends 17%, Chinese cassia tree 11%,Cloves 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mL containsCrude drug 0.2g).
Control drug 6: according to formula ratio: the coptis 25%, luffa 25%, Ligusticum wallichii 11%, Chinese cassia tree 11%, cloves 11%,Flagger 11%, myrrh 6%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 7: according to formula ratio: luffa 25%, Ligusticum wallichii 12%, sago cycas spends 20%, Chinese cassia tree 12%, cloves 12%,Flagger 12%, myrrh 7%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
Control drug 8: according to formula ratio: the coptis 25%, Ligusticum wallichii 12%, sago cycas spends 20%, Chinese cassia tree 12%, cloves 12%,Flagger 12%, myrrh 7%, mixes ready extraction concentrate or powder, and adds water and make liquid (every mLContaining crude drug 0.2g).
3) get wild type under 88 ApoE gene knockout mices in 6 week age (ApoEKO mouse) and 8 identical genetic backgroundsC57BL/6 (widetype, WT) mouse, adaptability was fed after 2 weeks, ApoEKO mouse was divided into 11 groups at random, every group8. The grouping situation of 11 groups is respectively model group, Simvastatin group, control group (1~8) and Experimental agents group. Wild typeMouse, as Normal group, gives normal diet and feeds. ApoE gene knockout mice all adopts high lipid food to feed. RealTest drug regimen and control group by each group every day gavage after being converted into Mouse Weight by per day for adults 15g medicine, intervene 12 weeks, pungent cutting downAfter being converted into Mouse Weight by per day for adults 20mg medicine, his spit of fland group intervenes 12 weeks; Normal group and the isopyknic life of model group gavageReason salt solution. With a 3% amobarbital 0.3ml/ anesthetized mice, open the parallel heart extracting blood 1mL in thoracic cavity, then row left ventricle perfusion,Maintain 20 to 30min, to reach the object of rinsing blood vessel. Gained blood sample 3500rpm, 4 DEG C of centrifugal 15min, separate bloodSlurry ,-20 DEG C of preservations, after for detection of experiments such as serum lipid metabolic index. Under disecting microscope is observed, light along backbone leading edgeSoft separation aortic tissue, uses micro-surgical instrument carefully to peel off circumvascular adipose tissue, isolates afterwards whole masterArtery (from heart junction to bilateral arteria iliaca communis bifurcation). Under disecting microscope, isolate aorta vessel, OCT bagBury and in freezing microtome (20 DEG C) section, from the aortic root freezing serial section of cross section of leaveing, in from aorta petal1000 μ m places start to collect, and 10 one of μ m thickness get 1,10 histotomies of every mouse collection, capture range bag every 20Draw together aortic root and play 2000 μ m length. All sections are placed in aqueous isopropanol 5min, and proceed in oil red O dye liquor and hatch 10min,Use afterwards 85% isopropyl alcohol differentiation, after washing, haematoxylin is redyed 2min, and water-based mountant mounting is placed on micro-Microscopic observation bloodInside pipe wall lipid Infiltrating, account for red plaque area sustainer tube chamber cross section area (recurrence standard circular) hundredDivide the relative size that recently represents atherosclerotic (AS) pathology, detect the average thickness of blood vessel and evaluate atheroscleroticThe situation that thickens of rear vascular wall.
Table 2 Experimental agents and each control group are to ApoE(-/-)The impact of knock out mice blood lipid level
(with normal group ratio,##P < 0.01; With model group ratio,*P<0.05,**P<0.01,n=8)
Table 3 Experimental agents and each control group are to ApoE(-/-)The impact of knock out mice atherosclerotic plaque pathology
(with normal group ratio,##P < 0.01; With model group ratio,*P<0.05,**P<0.01,n=8)
Can find out from the result of table 2 and table 3, no matter model group and normal group contrast, be serum lipid metabolic index or chest masterRed plaque area after the average thickness of arterial blood tube wall or the oil red O stain of aorta slice, model group is all extremely significantly highIn normal group; Atherosclerotic modeling success is described. The visible Experimental agents group of serum matter metaboilic level result of table 2 can the utmost pointSignificantly reduce TC in ApoE gene knockout mice serum, TG and LDL-C level, and the effect of its reduction is better than conventional lipopenicillinaseThe effect of antiatherosclerosis Western medicine Simvastatin, control group 1~8 also can reduce the lipid-metabolism level of serum in various degree,But effect is not as Experimental agents group. By the result of table 2, further confirm on effect for reducing blood fat, appoint and remove drug regimenIn a kind of composition, the effect of lipopenicillinase is had to impact, particularly remove larger (control group 7 Hes of impact after the coptis or luffaControl group 8), there is the trend that prevention of arterial is atherosis, but do not there is statistical significance (p > 0.05). The result of table 2 and realityThe result of executing lipopenicillinase experiment in example 1 is similar. The result of table 3 has further proved that drug regimen of the present invention is at prevention of arterial congee sampleIn sclerosis, have unique advantage, its action effect is better than the conventional antiatherogenic Western medicine Simvastatin of lipopenicillinase.
Finally explanation, above preferred embodiment is only unrestricted in order to technical scheme of the present invention to be described, although by upperState preferred embodiment and the present invention is described in detail, but it will be appreciated by those skilled in the art that can be in formAbove and in details it is made to various changes, and do not depart from the claims in the present invention book limited range.

Claims (5)

1. regulate the pharmaceutical composition that blood fat and prevention of arterial are atherosis, by weight percentage by following raw material systemBecome: the coptis 5~40%, luffa 5~30%, Ligusticum wallichii 1~20%, sago cycas spends 5~20%, Chinese cassia tree 5~20%, cloves 1~20%,Flagger 5~20%, myrrh 5~20%.
2. composition according to claim 1, is characterized in that, is made up by weight percentage: the coptis of following raw material10~30%, luffa 10~25%, Ligusticum wallichii 10~15%, sago cycas spends 10~15%, Chinese cassia tree 10~15%, cloves 5~15%,Flagger 5~10%, myrrh 5~10%.
3. composition according to claim 1, is characterized in that, is made up by weight percentage: the coptis of following raw material20%, luffa 20%, Ligusticum wallichii 10%, sago cycas spends 15%, Chinese cassia tree 10%, cloves 10%, flagger 10%, does not haveMedicine 5%.
4. according to the adjusting blood fat described in claim 1-3 any one and the atherosis pharmaceutical composition of prevention of arterial, its featureBe, the processing method of the described coptis be ethanol water taking volume fraction as 75% as the solvent extraction coptis, refluxExtract 3 times, each solvent adding amount adds solvent 7mL by coptis 1g, extracts 0.5 hour at every turn, merges and extractsLiquid, concentrated, make final concentration reach 1~1.5g/mL; The ethanol water refluxing extraction 3 that Ligusticum wallichii is 60% by volume fractionInferior, the consumption of each ethanol water adds 6mL ethanol water by 1g Ligusticum wallichii, extracts 0.5 hour at every turn, closesAnd extract, reclaim solvent concentrated, make final concentration reach 1~1.5g/mL; After luffa frying, chopping adds water by 1g10mL extracts 3 times, and each 0.5h merges extract and is concentrated into after 1~1.5g/mL for subsequent use; Chinese cassia tree, sago cycas flower, fourthPerfume (or spice) is dried respectively and is beaten powder to cross 10~200 mesh sieves for subsequent use; Myrrh is smashed; Above material is mixed and be get final product by former medicine mass ratioPharmaceutical composition of the present invention.
5. according to the adjusting blood fat described in claim 1-4 any one and the atherosis pharmaceutical composition of prevention of arterial, this medicineComposition can be made the various formulations that are applicable to clinical use according to the conventional method of pharmaceutical preparation, includes but not limited to fall apartAgent, granule, capsule, pill.
CN201610107064.0A 2016-02-26 2016-02-26 Pharmaceutical composition for regulating blood lipid and preventing atherosclerosis Pending CN105582163A (en)

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* Cited by examiner, † Cited by third party
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CN106053187A (en) * 2016-05-20 2016-10-26 北京九州柏林生物科技有限公司 Liquid set for dyeing biological tissue sample slices
CN107095092A (en) * 2017-05-11 2017-08-29 王长山 A kind of wintercherry fruit or calyx health drink and preparation method thereof

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CN101288726A (en) * 2008-05-15 2008-10-22 天科仁祥技术(北京)有限责任公司 Medicine composition for adjusting blood fat and its preparation method

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CN101288726A (en) * 2008-05-15 2008-10-22 天科仁祥技术(北京)有限责任公司 Medicine composition for adjusting blood fat and its preparation method

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郑琼莉等: ""清热燥湿化瘀法对高脂血症患者血脂及动脉弹性指数的影响"", 《上海中医药杂志》 *

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Publication number Priority date Publication date Assignee Title
CN106053187A (en) * 2016-05-20 2016-10-26 北京九州柏林生物科技有限公司 Liquid set for dyeing biological tissue sample slices
CN107095092A (en) * 2017-05-11 2017-08-29 王长山 A kind of wintercherry fruit or calyx health drink and preparation method thereof

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