CN101342205A - Traditional Chinese medicine preparation for decreasing blood fat - Google Patents

Traditional Chinese medicine preparation for decreasing blood fat Download PDF

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Publication number
CN101342205A
CN101342205A CNA2008101981894A CN200810198189A CN101342205A CN 101342205 A CN101342205 A CN 101342205A CN A2008101981894 A CNA2008101981894 A CN A2008101981894A CN 200810198189 A CN200810198189 A CN 200810198189A CN 101342205 A CN101342205 A CN 101342205A
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chinese medicine
extract
medicine preparation
cortex ilicis
ilicis rotundae
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CN101342205B (en
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刘国樵
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Anshi Pharmaceutical (Zhongshan) Inc.
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刘国樵
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Abstract

A Chinese medicine preparation used for decreasing blood-fat relates to the Chinese herba preparation that is prepared by extracting an effective part from ovate leaf holly bark and can decrease the blood-fat. The Chinese medicine preparation is an oral preparation prepared by an ethanol extract containing the ovate leaf holly bark and pharmaceutically acceptable auxiliary materials. The extract is the ovate leaf holly bark. The ovate leaf holly bark is extracted by the ethanol, filtered and concentrated; water is added to be mixed evenly; deposit is filtered and obtained and the extract is dried. 1 gram of the dried extract contains ilexin and ovate leaf holly bark acid with the total amount of 0.50 to 0.80g and the mass ratio of the ilexin and the ovate leaf holly bark acid is 12 to 1.5: 1. The Chinese medicine preparation has advantages that raw material are easy to be obtained; process is simple; operation is convenient; Chinese medicine can be produced in enormous quantities; product quality is easy to be controlled; toxicity is low; and adverse effect is little. Therefore, the Chinese medicine preparation can decrease the blood-fat effectively.

Description

The Chinese medicine preparation that is used for blood fat reducing
Technical field
The present invention relates to field of medicaments, be specifically related to after Cortex Ilicis Rotundae extraction effective site, prepare the Chinese medicine preparation of blood fat reducing.
Background technology
Chinese crude drug " Cortex Ilicis Rotundae " is the dry bark of holly plant Ilex rotunda Thunb. (Ilex rotunda Thunb.), be distributed widely in the southern china each province, main product in Guangxi, Guangdong Province, the heat-clearing and toxic substances removing that is usually used among the people, reducing swelling and alleviating pain, heating cures cold, acute, chronic hepatitis, acute gastroenteritis, gastric and duodenal ulcers, rheumatic arthritis.Have at present and use Cortex Ilicis Rotundae and other medical materials together, extracting in water, the treatment gastroenteritis of making, the medicine of dyspepsia etc., as compound recipe Cortex Ilicis Rotundae capsule, fukean tablet, the suitable capsule of the intestines and stomach etc.
Cortex Ilicis Rotundae is the medical material that extensive use is arranged, and at present its Pharmacological action study is mainly concentrated on cardiovascular system, secondly is some researchs of vitro antibacterial activity.
At present, global hyperlipemic patients constantly increases, and is the major disease of harm humans health.Effectively the medicine of control blood fat and few side effects is few on the market, and the Western medicine commonly used such as the simvastatin of his class D have lipid-lowering effect preferably, but muscle, kidney and liver are had in various degree infringement.[adverse effect magazine, 2002 (5), 306-308].The Chinese medicine class is many based on compound recipe, but because unknown effective ingredient, quality is restive.Therefore develop natural drug safe, really effective blood fat reducing and have great importance, vast market prospect is arranged.
Summary of the invention
The effective site that the objective of the invention is extraction blood fat reducing from the Cortex Ilicis Rotundae medical material is made Chinese medicine preparation.
The Chinese medicine preparation of blood fat reducing provided by the present invention, it is the oral formulations that a kind of adjuvant that contains the ethanol extraction of Cortex Ilicis Rotundae medical material and pharmaceutically allow is made, said extract is the dry bark with Aquifoliaceae Ilex rotunda Thunb. (Ilexrotunda Thunb.) plant, extract with the 85-95% alcoholic solution, filter, extracting solution is concentrated into 0.1-0.8 times of Cortex Ilicis Rotundae inventory, after the water that adds 2-5 times of extracting solution weight stirs evenly, the leaching precipitate, the dry extract that gets, containing Peltatin glucoside and rotundicacid total amount in the 1g extract dry product is 0.50~0.80g, and wherein Peltatin glucoside and rotundicacid mass ratio are 12~1.5: 1.
The method that Cortex Ilicis Rotundae extracts with alcoholic solution, the technology of the heat reflow method of available routine or infusion process or percolation.
The convenience of taking for the patient and according to the characteristic of extract, the present invention can add the adjuvant that pharmaceutically allows with extract, process of Chinese medicine preparation is routinely made pill, tablet, capsule, as add Mel, cane sugar powder is made pill, or concentrated pill is made tablet, capsule as adding starch, dextrin etc., or adding Oleum Arachidis hypogaeae semen, gelatin, glycerol etc. are made soft capsule etc., also do not get rid of other peroral dosage form.
Beneficial effect of the present invention: 1, the extraction of active constituents of medicine, raw material is easy to get, and technology is simple, easy to operate, can put into production in enormous quantities; 2, product quality is easy to control; 3, be the Chinese medicine preparation of effective blood fat reducing, toxicity is low, and side effect is little.
Below by evidence beneficial effect of the present invention
One, the preparation of Cortex Ilicis Rotundae extract
Get Cortex Ilicis Rotundae medical material 20Kg, be ground into coarse powder, add 95% ethanol warm macerating and extract secondary, each 24 hours, filter, merge extractive liquid, is concentrated into 5.6Kg, adds 16Kg water, stir evenly, the leaching precipitate, drying gets Cortex Ilicis Rotundae extract, lot number 040408
Assay: liquid chromatography (HPLC)
Chromatographic condition and system suitability test are filler with octadecylsilane chemically bonded silica; Acetonitrile: 0.1% glacial acetic acid (50: 50) is made mobile phase; The detection wavelength is 210nm.
The Peltatin glucoside reference substance is got in the preparation of reference substance solution respectively, the rotundicacid reference substance is an amount of, and accurate the title decides, and adds acetonitrile and makes the solution that every 1ml contains Peltatin glucoside 150 μ g, rotundicacid 50 μ g respectively, promptly.
Above-mentioned Cortex Ilicis Rotundae extract is got in the preparation of need testing solution, and porphyrize is got about 0.025g, accurate claims surely, puts in the 100ml measuring bottle, and it is an amount of to add acetonitrile, and at power 250W, supersound process is 10 minutes under the frequency 50KHz, puts coldly, adds dilution in acetonitrile to scale, shakes up, promptly.
Accurate respectively reference substance solution and each the 20 μ l of need testing solution of drawing of algoscopy inject chromatograph of liquid, measure, promptly.
Recording the weight content that contains Peltatin glucoside in 040408 batch of Cortex Ilicis Rotundae extract by above method is 52.59%, and the weight content of rotundicacid is 15.55%.
Two, the blood fat reducing of extract test
1 materials and methods
1.1 medicine is subjected to the reagent thing: Cortex Ilicis Rotundae extract.Lot number 040408
Positive drug: the simvastatin sheet, Shanghai Xinyi Wanxiang Pharmaceutical Co., Ltd., lot number is 071101.
1.2 instrument and reagent automatic clinical chemistry analyzer, centrifuge; 1% sodium carboxymethyl cellulose (autogamy).
1.3 the preparation of lipomul takes by weighing 15g Adeps Sus domestica and puts in the 200mL beaker, is heated to make its dissolving about 100 ℃, slowly adds the 6g cholesterol, is stirred to dissolving fully; Add 0.2g propylthiouracil and 20mL Tween 80 again, fully stir evenly.In another beaker, add the 65mL distilled water simultaneously, be placed on and be heated to 60 ℃ on the electric furnace, add the 2g cholate then No. 3, fully stir up to dissolving fully.With two kinds of solution, fully mixing is promptly made lipomul then.
1.4 60 of animal and grouping cleaning level SD rats, female, body weight 210 ± 10g is provided by Yangzhou University comparative medicine center, the quality certification number: SYXK (Soviet Union) 2002-0045.Be divided into 6 groups at random, 10 every group, that is: 1. normal control group, 2. hyperlipidemia model group, 3. simvastatin group (1.5mg/kg), 4. Cortex Ilicis Rotundae extract low dose group (150mg/kg), 5. Cortex Ilicis Rotundae extract high dose group (450mg/kg).
After 1.5 each group of experimental technique is freely absorbed the normal diet adaptability and is fed a week, model group, simvastatin group, Cortex Ilicis Rotundae extract low dose group, high dose group on this basis every morning irritate stomach by 10ml/kg amount and give lipomul, last till that experiment finishes.After one week of modeling, give corresponding medicine every afternoon: normal group and model group are given 1% sodium carboxymethyl cellulose (1ml/100g body weight), the simvastatin group is given simvastatin 1% sodium carboxymethyl cellulose suspension (1ml/100g body weight), the Cortex Ilicis Rotundae extract 1% sodium carboxymethyl cellulose suspension (1ml/100g body weight) that Cortex Ilicis Rotundae extract is low, high dose group is given variable concentrations respectively, successive administration 21 days, claimed 1 body weight in per three days, to adjust dosage.Each treated animal in administration after 21 days fasting can't help water 16h, pluck eyeball and get blood, separation of serum is measured serum total cholesterol (TC), serum triglycerides (TG), serum high-density LP cholesterol (HDL-C) and serum low-density LP cholesterol (LDL-C).
1.6 statistical disposition detects The data SPSS software and handles, enumeration data is all represented with X ± S.
2 results
Influence to hyperlipidemia model rat fat index: the results are shown in Table 1
Table 1 Cortex Ilicis Rotundae extract is to the influence of hyperlipidemia model rat fat index (X ± S)
Figure A20081019818900061
Annotate: compare with model group, *There were significant differences in P<0.05; *There are highly significant difference and normal group in P<0.01 relatively, and there were significant differences in △ P<0.05; There is highly significant difference △ △ P<0.01
Conclusion: as can be seen from Table 1, to the rat of hyperlipemia, Cortex Ilicis Rotundae extract can significantly reduce serum total cholesterol (TC) and serum triglycerides (TG) content; Significantly reduce serum low-density LP cholesterol level (LDL-C), serum high-density LP cholesterol (HDL-C) content significantly raises.
Three, the acute toxicity test in mice of Cortex Ilicis Rotundae extract
Mouse stomach Cortex Ilicis Rotundae extract 1.25,2.5,5,10g/kg do not see in two weeks that death and other abnormal response take place, and can't measure the LD50 that is subjected to reagent thing mouse stomach.Mice is with Cmax, maximum volume, and no overt toxicity reaction does not also have dead behind interior three gastric infusions of 24h in one week.The maximum dosage-feeding that records the administration of Ilex rotunda Thunb. saponin mouse stomach is 60g/kg.
It is lower that more than the test poison that tentatively shows Cortex Ilicis Rotundae extract is paid effect.
Further set forth technical scheme of the present invention below by embodiment
The specific embodiment
The preparation of embodiment 1 Cortex Ilicis Rotundae extract
Get Cortex Ilicis Rotundae medical material 20Kg, be ground into coarse powder, add 95% ethanol percolate extraction, carry out percolation by 11 pages of methods of Pharmacopoeia of People's Republic of China appendix of version in 2005, not obvious to the liebermann-Burchard test until percolate, extracting solution is concentrated into 3Kg, adds 6Kg water, stir evenly, the leaching precipitate, drying gets Cortex Ilicis Rotundae extract 1.2Kg, measure to such an extent that the weight content of Peltatin glucoside is 42.51% with high-efficient liquid phase technique, rotundic acid is 21.02%.
The preparation of embodiment 2 Cortex Ilicis Rotundae extracts
Get Cortex Ilicis Rotundae medical material 2Kg, be ground into coarse powder, add 85% ethanol 12Kg, the heating and refluxing extraction secondary, each 2 hours, filter, merge the filtrate of second extraction, be concentrated into 1.6Kg, add 8Kg water, stir evenly, leaching precipitate, drying, this precipitate reuse 70% alcohol heating reflux dissolving is filtered, and solution concentration adds water 0.6Kg to 0.2Kg, stir evenly leaching precipitate, drying, Cortex Ilicis Rotundae extract 82g, measure to such an extent that to contain Peltatin glucoside be 65.22% with high-efficient liquid phase technique, rotundic acid is 6.08%.
The preparation of embodiment 3 Cortex Ilicis Rotundae extracts
Get Cortex Ilicis Rotundae medical material 2Kg, be ground into coarse powder, add 85% soak with ethanol and extract secondary, each 24 hours, filter, extracting solution is concentrated into 0.8Kg, adds 1.6Kg water, stir evenly, the leaching precipitate, drying gets Cortex Ilicis Rotundae extract 102g, measure to such an extent that to contain Peltatin glucoside be 42.02% with high-efficient liquid phase technique, rotundic acid is 9.08%.
Embodiment 4 tablets
Get the Cortex Ilicis Rotundae extract 400g of the foregoing description 1, be ground into fine powder, add the about 250g of 10% gelatinized corn starch, mix, 14 mesh sieves are granulated, and in 100 ℃ of dryings, granulate adds magnesium stearate 2.5g mixing, is pressed into 1000, promptly.Every heavy 0.42g, containing Peltatin glucoside and rotundicacid total amount is 250 ± 5mg.
Embodiment 5 capsules
Get the Cortex Ilicis Rotundae extract 320g of the foregoing description 1, be ground into fine powder, add the about 200g of 10% gelatinized corn starch, mix, 20 mesh sieves are granulated, and in 100 ℃ of dryings, granulate incapsulates, promptly.Every capsules contains content 0.32g, and containing Peltatin glucoside and rotundicacid total amount is 200 ± 5mg.
Embodiment 6 pills
Get the Cortex Ilicis Rotundae extract 320g of the foregoing description 1, be ground into fine powder, add refined honey 20g and an amount of water pill, drying, polishing, that is, 10 balls are equivalent to 2g, and containing Peltatin glucoside and rotundicacid total amount is 1250 ± 5mg.

Claims (3)

1, a kind of Chinese medicine preparation that is used for blood fat reducing, it is characterized in that: contain the ethanol extraction of Cortex Ilicis Rotundae medical material and oral formulations that the adjuvant that pharmaceutically allows is made, said extract is the dry bark with Aquifoliaceae Ilex rotunda Thunb. (Ilex rotunda Thunb.) plant, extract with the 85-95% alcoholic solution, filter, extracting solution is concentrated into 0.1-0.8 times of Cortex Ilicis Rotundae inventory, after the water that adds 2-5 times of extracting solution weight stirs evenly, the leaching precipitate, the dry extract that gets, containing Peltatin glucoside and rotundicacid total amount in the 1g extract dry product is 0.50~0.80g, and wherein Peltatin glucoside and rotundicacid mass ratio are 12~1.5: 1.
2, the Chinese medicine preparation of blood fat reducing according to claim 1 is characterized in that said Cortex Ilicis Rotundae extracts with alcoholic solution, its method available heat circumfluence method or infusion process or percolation.
3, the Chinese medicine preparation of blood fat reducing according to claim 1 is characterized in that said oral formulations is pill, tablet, capsule.
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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101849950A (en) * 2010-06-22 2010-10-06 赵全成 Application of rotundic acid in preparing blood lipid regulating medicines
CN101856357A (en) * 2010-06-22 2010-10-13 赵全成 Application of rotundic acid in preparing medicines for preventing and treating cardiovascular and cerebrovascular diseases
CN102058632A (en) * 2010-12-28 2011-05-18 赵全成 Application of medicinal composition to preparation of medicament for preventing and treating alcoholic liver damage and fatty liver and lowering blood fat
CN102078346A (en) * 2011-01-14 2011-06-01 刘国樵 Chinese medicinal preparation for relieving heat, resisting inflammation and easing pain
CN102210724A (en) * 2011-05-09 2011-10-12 刘国樵 Comprehensive use of ovateleaf holly bark medicinal material
CN102579525A (en) * 2012-03-28 2012-07-18 广东南方洁灵科技实业有限公司 Ilex rotunda thunb extract and preparation method and application thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101099754A (en) * 2006-07-07 2008-01-09 李超生 Preparation method and application for pedunculoside II

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101849950A (en) * 2010-06-22 2010-10-06 赵全成 Application of rotundic acid in preparing blood lipid regulating medicines
CN101856357A (en) * 2010-06-22 2010-10-13 赵全成 Application of rotundic acid in preparing medicines for preventing and treating cardiovascular and cerebrovascular diseases
CN101856357B (en) * 2010-06-22 2012-07-04 赵全成 Application of rotundic acid in preparing medicines for preventing and treating cardiovascular and cerebrovascular diseases
CN102058632A (en) * 2010-12-28 2011-05-18 赵全成 Application of medicinal composition to preparation of medicament for preventing and treating alcoholic liver damage and fatty liver and lowering blood fat
CN102058632B (en) * 2010-12-28 2012-05-30 吉林修正药业新药开发有限公司 Application of medicinal composition to preparation of medicament for preventing and treating alcoholic liver damage and fatty liver and lowering blood fat
CN102078346A (en) * 2011-01-14 2011-06-01 刘国樵 Chinese medicinal preparation for relieving heat, resisting inflammation and easing pain
CN102078346B (en) * 2011-01-14 2014-01-01 刘国樵 Chinese medicinal preparation for relieving heat, resisting inflammation and easing pain
CN102210724A (en) * 2011-05-09 2011-10-12 刘国樵 Comprehensive use of ovateleaf holly bark medicinal material
CN102210724B (en) * 2011-05-09 2012-11-14 安士制药(中山)有限公司 Comprehensive utilization of ovate leaf holly bark medicinal material
CN102579525A (en) * 2012-03-28 2012-07-18 广东南方洁灵科技实业有限公司 Ilex rotunda thunb extract and preparation method and application thereof

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