CN1313111C - Chinese medicinal extract for resisting osteoporosis and its preparation - Google Patents
Chinese medicinal extract for resisting osteoporosis and its preparation Download PDFInfo
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- CN1313111C CN1313111C CNB2004100183174A CN200410018317A CN1313111C CN 1313111 C CN1313111 C CN 1313111C CN B2004100183174 A CNB2004100183174 A CN B2004100183174A CN 200410018317 A CN200410018317 A CN 200410018317A CN 1313111 C CN1313111 C CN 1313111C
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Abstract
The present invention relates to the technical field of medicines, particularly to a traditional Chinese medicine extract prepared from cuscuta seed, Chinese magnoliavine fruit and common cnidium fruit. The extract can be prepared in a way that the three traditional Chinese medicines are mixed and then together extracted or in a way that the three traditional Chinese medicines are respectively extracted and then mixed together, and is rich in flavonoids components, lignans components and coumarins components. The present invention has the characteristics of simple and convenient preparation technology, low cost, high effective component content and easily controlled quality. Animal experiments show that the present invention has obviously preventive and curative effects on osteoporosis so that the present invention can be used for preparing medicines or foods for preventing and curing osteoporosis.
Description
Technical field
The present invention relates to medical technical field, system is the Chinese medicine extract of feedstock production with Semen Cuscutae, Fructus Schisandrae Chinensis, Fructus Cnidii, promptly adopt all medicines to close and carry or the blended process preparation in single medicinal material extraction back, and the purposes of using it for preparation osteoporotic medicine of control or food.
Background technology
Osteoporosis is old people and postmenopausal women's commonly encountered diseases and a frequently-occurring disease, has medicines such as estrogen, calcium preparation and bis phosphoric acid salt available at present clinically, but because side effect is serious, late result is not good enough, has restricted its extensive use to a great extent.
Semen Cuscutae, Fructus Schisandrae Chinensis, Fructus Cnidii are conventional Chinese medicine, record in the many editions Pharmacopoeias of the People's Republic of China.Semen Cuscutae mainly contains flavones ingredients such as Quercetin, Herba Astragali Melilotoidis (Herba Astragali Sinici) glycosides, and tool nourishing the liver and kidney, controlling nocturnal emission with astringent drugs reducing urination are antiabortive, makes eye bright, the antidiarrheal effect.Fructus Schisandrae Chinensis mainly contains lignan components such as deoxyschizandrin, schisandrin B, schisandrin C, and Bearberry Extract is astringent or styptic treatment for spontaneous sweating, the effect of supplementing QI for promoting the production of body fluid, kidney calming.Fructus Cnidii mainly contains Coumarins compositions such as osthole, bergapten, imperatorin, tool warming the kidney to invigorate YANG, dampness, dispel the wind, insecticidal action.Prescriptions Worth Thousand Gold for Emergencies only records with these 3 flavor Chinese medicine equal portions and is used for the treatment of sexual impotence, or only with 2 parts of Semen Cuscutae, and it is unable that 2 parts of Fructus Schisandrae Chinensis, 1 part of Fructus Cnidii are used for the treatment of the five kinds of strain and seven kinds of impairment weakness with emaciation.Compendium of Material Medica is also recorded and only is used for the treatment of sexual impotence with these 3 flavor Chinese medicine equal portions.And, all raw material pulverizing is mixed and made into the simple and easy watered pill in Prescriptions Worth Thousand Gold for Emergencies and the Compendium of Material Medica, the coarse and crude backwardness of technology, range of application is very limited.Modern also do not see with this 3 flavor medicine prescription compatibility be used for clinical report, more do not see with the medicinal report of making osteosporosis resistant medicament of this three flavor.
Summary of the invention
The present invention is that the feedstock production extract is used for preparation control medicine for treating osteoporosis with Semen Cuscutae, Fructus Schisandrae Chinensis, Fructus Cnidii.Its extract can adopt three flavor medicines to close to carry or the single prescription is proposed back blended method preparation, and it can be prepared into any common drug dosage form with acceptable accessories.Prove that through zoopery it has significant preventive and therapeutic effect to osteoporosis.Extract of the present invention can adopt following two kinds of methods preparation:
Method one, close lifting manipulation:
(1) prescription and proportioning: 1～5 part of Semen Cuscutae, 1～5 part of Fructus Schisandrae Chinensis, 1～5 part of Fructus Cnidii;
(2) preparation extracting solution: take by weighing each crude drug coarse powder respectively in proportion, mix, the above-mentioned raw materials coarse powder is soaked in an amount of extraction solvent, extracting solvent is 0～95% ethanol or methanol aqueous solution, till percolation to flavonoid, lignanoids and Coumarins composition assay reactions is negative routinely, collect percolate, get extracting solution.This step also can adopt 5～10 times to extract solvent refluxing extraction one to repeatedly, gets extracting solution.
Preferred 30～95% ethanol of the used extraction solvent of this step or methanol, preferred especially 95% ethanol.Preferred 8 times are extracted solvent during reflux, extract,, reflux each 2 hours 3 times.
(3) concentrate drying
Said extracted liquid decompression and solvent recovery to there not being the alcohol flavor, is filtered to get filtrate.With the filtrate crushed after being dried, promptly get powder of the present invention.
(4) tabletting
Adjuvant mixes, tabletting if extract obtained powder and tablet used always, promptly gets tablet, also can make different dosage forms such as pill, unguentum, mixture routinely.
Method two, singly carry the back and mix:
(1) prescription and proportioning: 1～5 part of Semen Cuscutae, 1～5 part of Fructus Schisandrae Chinensis, 1～5 part of Fructus Cnidii;
(2) preparation extracting solution: take by weighing each crude drug coarse powder respectively in proportion, respectively above-mentioned each raw material coarse powder is soaked in an amount of extraction solvent, extracting solvent is 0～95% ethanol or methanol aqueous solution, difference is percolation routinely, Semen Cuscutae, Fructus Schisandrae Chinensis, Fructus Cnidii are till percolation to flavonoid, lignanoids, Coumarins composition assay reactions is negative respectively, collect each percolate, get each single medicinal material extracting solution; This step also can adopt 5～10 times to extract solvent refluxing extraction one to repeatedly respectively, gets each single medicinal material extracting solution.
This step is extracted preferred 30～95% ethanol of solvent or methanol.Preferred especially: it is 95% ethanol that Semen Cuscutae extracts solvent; It is 90% ethanol that Fructus Schisandrae Chinensis extracts solvent; It is 95% ethanol that Fructus Cnidii extracts solvent.
(3) concentrate drying:
Respectively above-mentioned Semen Cuscutae, Fructus Schisandrae Chinensis, each single medicinal material extracting solution reclaim under reduced pressure of Fructus Cnidii are not distinguished the flavor of to there being alcohol, filter to get filtrate, filtrate crushed after being dried respectively gets powders A, B, C.
(4) mix
Gained powders A, B, C are mixed, promptly get extract of the present invention;
(5) tabletting
With extract obtained powder and tablet adjuvant commonly used mix, tabletting, can get tablet, also can make different dosage forms such as pill, unguentum, mixture routinely.
Extract of the present invention has the osteoporotic effect of significant control through the zoopery proof, so can be used for preparation osteoporotic medicine of control or food.
The specific embodiment
Now in conjunction with the embodiments the present invention is described in detail.
Embodiment 1 closes lifting manipulation and prepares extract of the present invention
(1) preparation extracting solution
Get Semen Cuscutae coarse powder 1kg, Fructus Schisandrae Chinensis coarse powder 1kg, Fructus Cnidii coarse powder 1kg, be soaked in 3000ml 95% ethanol, placement is spent the night, percolation routinely, control percolation speed 3～5ml/ minute is added solvent, till percolation to flavonoid, lignanoids, Coumarins composition assay reactions is negative at any time in the percolation process, collect percolate, be extracting solution.
(2) preparation extract: said extracted liquid decompression and solvent recovery is not distinguished the flavor of to there being alcohol, remove by filter float and insoluble impurities, again with the filtrate crushed after being dried, promptly get extract powder 165.0g, the TLC calibrating contains flavonoid, lignanoid and Coumarins composition, with total coumarins content is index, measures total coumarins content 23.55% with the HPLC method.
(3) preparation tablet:
Prescription and proportioning:
Extract powder 100g
Starch 40g
Lactose 30g
Microcrystalline Cellulose 30g
7% starch slurry is an amount of
Magnesium stearate 1%
By said ratio extract powder, starch, lactose, microcrystalline Cellulose are crossed 80 mesh sieves respectively, mixing, after 40 mesh sieves 3 times, above-mentioned mixed powder with 7% starch slurry system soft material, is crossed 24 mesh sieve grains, 50 ℃ of dryings 2 hours, dried particles is crossed 30 mesh sieve granulate, adds magnesium stearate, mixing, tabletting gets 1000 in tablet.
Embodiment 2 closes lifting manipulation and prepares extract of the present invention
Extract solvent and select water for use, all the other get extract powder 180.40g with embodiment 1, and the TLC calibrating contains flavonoid, lignanoid, Coumarins composition, and the HPLC method is measured total coumarins content 2.20%.
Have and studies show that the Coumarins composition has clear and definite function of resisting osteoporosis, embodiment 2 and embodiment 1 compare, although the extract powder yield is high slightly, but wherein the Coumarins component content is far below embodiment 1, second-rate, The pharmacological results has also fully proved this point, so embodiment 1 is best preparation method.
Embodiment 3 closes lifting manipulation and prepares extract of the present invention
With 8 times of amount 95% alcohol reflux 3 times, each 2 hours, all the other were with embodiment 1, extract powder 216.0g.The TLC calibrating contains flavonoid, lignanoid and Coumarins composition, and the HPLC method is measured total coumarins content 19.54%.
Embodiment 4 single lifting manipulations prepare extract of the present invention
Take by weighing Semen Cuscutae coarse powder 1kg, Fructus Schisandrae Chinensis coarse powder 1kg, Fructus Cnidii coarse powder 1kg respectively, respectively be soaked in 1000ml 95% ethanol, till percolation to flavonoid, lignanoids, Coumarins composition assay reactions is negative routinely respectively, collect percolate, get each single medicinal material extracting solution; Respectively each single medicinal material extracting solution reclaim under reduced pressure is not distinguished the flavor of to there being alcohol, filter to get filtrate.With Semen Cuscutae filtrate crushed after being dried, get powders A 123.33g; With Fructus Schisandrae Chinensis filtrate crushed after being dried, get powder B 147.15g.With Fructus Cnidii filtrate crushed after being dried, get powder C 92.40g.A, B, C are mixed, promptly get extract powder of the present invention, the TLC calibrating contains flavonoid, lignanoid and Coumarins composition, and the HPLC method is measured total coumarins content 12.68%.
Pharmacological evaluation
Retinoic acid can cause osteoporosis, and the ethoxy Alendronate is to be used to prevent and treat osteoporotic medicine at present clinically.By pharmacological evaluation, observe Chinese medicine extract of the present invention and prevent and treat the osteoporosis effect.
1 experiment material
1.1 animal
SD rat The 2nd Army Medical College Experimental Animal Center provides
1.2 medicine
Pharmaceutical college of ethoxy Alendronate The 2nd Army Medical College new drug assessment centers provides with 0.5%CMC and is made into 2.0% suspension
Retinoic acid Shanghai No.6 Pharmaceutical Factory lot number 200106012 usefulness 0.5%CMC are made into 1.5% suspension
Extract 1 is made into 0.5%CMC by embodiment 1 preparation and is equivalent to crude drug 2g/ml suspension
Extract 2 is made into 0.5%CMC by embodiment 2 preparations and is equivalent to crude drug 2g/ml suspension
CMC Shanghai chemical reagents corporation
1.3 instrument
QCT-bone density analytical system U.S. LACA company
2 methods and result
2.1 to experimental osteoporosis prevention effect
50 of rats, be divided into 5 groups at random, every group 10, be normal control group (group of solvents), model control group, positive controls (ethoxy Alendronate group), 1 group of extract, 2 groups of extracts, except that the normal control group, all the other are respectively organized rat and all irritate stomach and give retinoic acid 0.5ml/kg, every day 1 time, continuous 14 days, when giving retinoic acid, each medication group was pressed the dosage gastric infusion of table 1, every day 1 time, continuous 28 days, normal control group and model group gave 0.5%CMC, and dose is per kilogram of body weight 0.5ml, weigh weekly therebetween 1 time, and adjust the administration consumption in view of the above.The 29th day sacrificed by decapitation got rat bilateral femur, peels meat and other tissue off, and wherein a side femur is done rat femur scanning on dual intensity X line borne densitometers, measures bone density (g/cm
2), then in 120 ℃ of oven dry one hour, place interior 200 ℃, 400 ℃, 600 ℃, 800 ℃ each ashing of mnffer stove 2 hours again, after ashing finishes to cool off, claim ash to weigh (Washg), with measuring bone ash calcium, bone ash phosphorus content behind 6N HCL extraction calcium, the phosphorus.
The opposite side femur is made the decalcification paraffin section, and microscopically is observed bone structure.(seeing Xu Shuyun chief editor " pharmacological experimental methodology " third edition for details, People's Health Publisher, 1561～1568 pages) the results are shown in Table 1.By table 1 as seen, the femur thigh density of 1 group of extract of the present invention, 2 groups of rats of extract, bone ash weight, calcium content of bone and bone phosphorus content are all apparently higher than model group, near normal control group and positive controls, show that extract of the present invention has significant preventive effect to osteoporosis.
From pathological section as seen, the cortical bone of model group all has the pathological change that loose, attenuation and bone trabecula loosen, attenuate and even disappear.Each administration group and positive controls only have the cortical bone attenuation of individual animal and the change that bone trabecula attenuates, and routine number is few, pathological changes is light, also show that extract of the present invention has significant preventive effect to osteoporosis.
2, the therapeutical effect of 2 pairs of experimental osteoporosis
50 of rats, be divided into 5 groups at random, every group 10, be normal control group (group of solvents), model control group, positive controls (ethoxy Alendronate group), 1 group of extract, 2 groups of extracts, except that the normal control group, each is organized rat and all irritates stomach retinoic acid 0.5ml/kg, every day 1 time, continuous 14 days, each medication group was pressed dosage gastric infusion in the table 2 in the 15th day, every day 1 time, continuous 28 days, normal control group and model group give 0.5%CMC, dose is 0.5ml/kg, weighs weekly therebetween 1 time, and adjusts the administration consumption in view of the above.Observation index the results are shown in Table 2 with experiment 2.1.
By table 2 as seen, 1 group of extract, 2 groups of rat femur bone densities of extract, bone ash weight, calcium content of bone and bone phosphorus content are all apparently higher than model group, more also be in same level with the normal control group, show that extract of the present invention has significant therapeutical effect to osteoporosis
From pathological section as seen, the cortical bone of model group all has the pathological change that loose, attenuation and bone trabecula loosen, attenuate and disappear.Each administration group and positive controls only have the cortical bone attenuation of individual animal and the change that bone trabecula attenuates, and pathological changes is lighter, also show that extract of the present invention has significant therapeutical effect to osteoporosis.
Preparation method of extract of the present invention is simple, and is with low cost, and the protect against osteoporosis effect is remarkable, has no side effect, thereby can be used for preparing the medicine or the food of protect against osteoporosis.
Table 1 Chinese medicine extract of the present invention is to experimental osteoporosis prevention effect
| Group | Dosage | Femoral bmd g/cm 2 | The heavy wash (g) of femur bone ash | Femur bone ash calcium g/100g bone ash | Femur bone ash phosphorus g/100g bone ash |
| 2 groups of 1 group of extracts of normal control group model matched group ethoxy Alendronate group extract | 0.5％CMC 0.5％CMC 50mg/kg 2.0g/kg 2.0g/kg | 0.224±0.009 0.208±0.006* 0.219±0.015** 0.225±0.008** 0.221±0.006** | 0.250±0.006 0.214±0.003* 0.264±0.005** 0.240±0.009** 0.251±0.005** | 31.03±0.72 29.08±0.50* 30.90±0.42** 30.09±0.66** 31.50±0.50** | 18.06±0.45 17.23±0.40* 18.27±0.410** 17.84±0.32** 18.09±0.17** |
Annotate: 1. 3. 2. x ± SD relatively compare * * P＜0.05 with model control group in * P＜0.05 with the normal control group
Table 2 Chinese medicine extract of the present invention is to the therapeutical effect of experimental osteoporosis
| Group | Dosage | Femoral bmd g/cm2 | The heavy wash (g) of femur bone ash | Femur bone ash Ca Ca g/100g bone ash | Femur bone ash P P g/100g bone ash |
| 2 groups of 1 group of extracts of normal control group model matched group ethoxy Alendronate group extract | 0.5％CMC 0.5％CMC 50mg/kg 2.0g/kg 2.0g/kg | 0.210±0.007 0.189±0.009* 0.212±0.013** 0.214±0.003** 0.217±0.005** | 0.248±0.007 0.210±0.004* 0.242±0.007** 0.245±0.010** 0.251±0.004** | 31.89±0.90 30.23±0.33* 30.90±0.42** 31.30±0.50** 31.49±0.40** | 17.96±0.56 17.23±0.33* 17.67±0.30** 17.76±0.20** 17.88±0.42** |
Annotate: 1. 3. 2. x ± SD relatively compare * * P＜0.05 with model control group in * P＜0.05 with the normal control group
Claims (6)
1, a kind of Chinese medicine extract is in preparation protect against osteoporosis medicine or Application in Food, said Chinese medicine extract is by 1～5 part of Semen Cuscutae extract, 1～5 part of Fructus Schisandrae Chinensis extrat, 1～5 part of Fructus cnidii extract is formed, by closing lifting manipulation or the branch lifting manipulation makes, the said lifting manipulation of closing is: each crude drug coarse powder is mixed in proportion, with extracting solvent percolation or backflow, get extracting solution, said extraction solvent is 0～95% ethanol or methanol aqueous solution, then said extracted liquid decompression and solvent recovery is not distinguished the flavor of to there being alcohol, filter to get filtrate, will get extract of the present invention after the filtrate drying; Lifting manipulation was in said minute: Semen Cuscutae, Fructus Schisandrae Chinensis, Fructus Cnidii raw material coarse powder are used extracted solvent percolation or backflow respectively, get each single medicinal material extracting solution, said extraction solvent is 0～95% ethanol or methanol aqueous solution, again each single medicinal material extracting solution difference decompression and solvent recovery is not distinguished the flavor of to there being alcohol, filter to get filtrate, get each single medicinal material extract after the filtrate drying, each single medicinal material extract is mixed by a certain percentage, be Chinese medicine extract of the present invention.
2,, it is characterized in that said is 30～95% ethanol or methanol by closing the used extraction solvent of Chinese medicine extract that lifting manipulation makes by the application of the described Chinese medicine extract of claim 1.
3,, it is characterized in that said is 95% ethanol by closing the used extraction solvent of Chinese medicine extract that lifting manipulation makes by the application of the described Chinese medicine extract of claim 2.
4, by the application of the described Chinese medicine extract of claim 1, it is characterized in that the said used extraction solvent of each single medicinal material extract that is made by minute lifting manipulation is 30～95% ethanol or methanol.
5, press the application of the described Chinese medicine extract of claim 4, it is characterized in that the said used extraction solvent of Semen Cuscutae extract that is made by minute lifting manipulation is 95% ethanol, the used extraction solvent of Fructus Schisandrae Chinensis extrat is 90% ethanol, and the used extraction solvent of Fructus Cnidii is 95% ethanol.
6,, it is characterized in that Semen Cuscutae, the Fructus Schisandrae Chinensis of Chinese medicine extract, the ratio of Fructus Cnidii are 1: 1: 1 by the application of the described any Chinese medicine extract of claim 1 to 5.
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|---|---|---|---|
| CNB2004100183174A CN1313111C (en) | 2004-05-13 | 2004-05-13 | Chinese medicinal extract for resisting osteoporosis and its preparation |
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| CNB2004100183174A CN1313111C (en) | 2004-05-13 | 2004-05-13 | Chinese medicinal extract for resisting osteoporosis and its preparation |
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| CN1313111C true CN1313111C (en) | 2007-05-02 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102178911B (en) * | 2011-04-21 | 2012-08-29 | 北京身心康国际中医研究院 | Chinese medicine preparation used for dispelling wind and eliminating dampness, dredging collaterals and stopping pains for people with deficiency of yang and phlegm dampness constitution, and preparation method and application of preparation |
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Patent Citations (2)
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| CN1121810A (en) * | 1993-12-25 | 1996-05-08 | 广东医学院医药科技开发中心 | Compound Chinese medicine preparation for treatment of osteoporosis and preparing process thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102178911B (en) * | 2011-04-21 | 2012-08-29 | 北京身心康国际中医研究院 | Chinese medicine preparation used for dispelling wind and eliminating dampness, dredging collaterals and stopping pains for people with deficiency of yang and phlegm dampness constitution, and preparation method and application of preparation |
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