CN103877134A - Total panax notoginsenosides, preparing method thereof, preparations thereof and applications thereof - Google Patents
Total panax notoginsenosides, preparing method thereof, preparations thereof and applications thereof Download PDFInfo
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- CN103877134A CN103877134A CN201210561300.8A CN201210561300A CN103877134A CN 103877134 A CN103877134 A CN 103877134A CN 201210561300 A CN201210561300 A CN 201210561300A CN 103877134 A CN103877134 A CN 103877134A
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- total arasaponins
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Abstract
The invention discloses total panax notoginsenosides, a preparing method thereof, preparations thereof and applications thereof. The total panax notoginsenosides comprise a ginsenoside Rg 1 and a ginsenoside Rb 1, with the weight ratio of the ginsenoside Rg 1 to the ginsenoside Rb 1 being 1:0.9-1.1. The preparing method includes smashing a raw material pseudo-ginseng into coarse powder, adding 8-12 times by weight of ethanol having a concentration of 60-80%, performing reflux extraction for 2-4 times for 1-2 h in each time, performing rough filtration after each extraction step, combining the filtrates of rough filtration, performing refined filtration, concentrating the filtrate of the refined filtration until the specific density is 1.3-1.5, thus obtaining the total panax notoginsenosides. The total panax notoginsenosides can be prepared into granules, capsules, tablets, pills, oral liquids and injections. The applications relate to applications of the total panax notoginsenosides in preparation of medicines used for preventing and/or treating ischemic cerebrovascular disease. The weight ratio of the ginsenoside Rg 1 to the ginsenoside Rb 1 is controlled to be within the range of 1:0.9-1.1. The total panax notoginsenosides can reduce the area of cerebral infarction caused by cerebellar ischemia/reperfusion and can improve neurobehavioral disturbances caused by the cerebral ischemia/reperfusion.
Description
Technical field
The invention belongs to Chinese medicine extract technical field, be specifically related to a kind of Radix Notoginseng total arasaponins and preparation method thereof, preparation and application.
Background technology
Ischemic cerebrovascular, refers to due to diseases such as cerebral vasospasm that a variety of causes causes, cerebral blood supply insufficiency, cerebral thrombosis, cerebral embolism, causes cerebrovascular function obstacle, especially stops up at most with cerebrovascular.Cerebral ischemia can cause that the excessive release of ionic equilibrium forfeiture, excitatory amino acid, oxidative stress increase, apoptosis also finally causes cerebral tissue necrosis.This disease is all very high in real-life sickness rate, disability rate and fatality rate, has become one of disease of serious harm human health.
Radix Notoginseng is Araliaceae, another name Radix Notoginseng, mountain paint, Radix Stephaniae Sinicae (Radix Stephaniae Dielsianae), Herba Wedeliae Wallichii, Radix Notoginseng etc.Warm in nature, sweet in the mouth, micro-hardship; Return Liver Channel, stomach warp, heart channel, lung meridian, large intestine channel.There is hemostasis, loose blood, analgesic therapy effect.Be generally used for treatment and fall diseases such as flutterring congestive edema, thoracic obstruction angor, lump in the abdomen, blood stasis amenorrhea, dysmenorrhea, the cloudy stomachache of the stasis of blood in puerperal, sore, carbuncle and painful swelling.Modern study shows: the main active of Radix Notoginseng is Radix Notoginseng total arasaponins (PNS), Radix Notoginseng total arasaponins comprises the various active compositions such as ginsenoside Rg1, ginsenoside Rb1, arasaponin R1, wherein ginsenoside Rb1's content is the highest, and ginsenoside Rg1 takes second place.Radix Notoginseng has the blood cell of promotion metabolism, balance adjustment blood cell; Two-ways regulation nervus centralis, improves mentally, strengthens learning and memory ability; Enhancing human body immunity function, antitumor; Hemostasis, blood circulation promoting and blood stasis dispelling; Protect the liver, antiinflammatory; Slow down aging etc.The pharmacological activity of Radix Notoginseng total arasaponins in cardiovascular disease, immunity, endocrine and central nervous system has report (Ng, TB. Pharmacological activity of sanchi ginseng (Panax notoginseng). J Pharm Pharmacol, 2006,58 (8): 1007-1019.).But up to now, have no report with Radix Notoginseng total arasaponins in the effect preventing and/or treating aspect cerebral ischemia.
Summary of the invention
The first object of the present invention is to provide a kind of Radix Notoginseng total arasaponins, and the second object is to provide the preparation method of this Radix Notoginseng total arasaponins, and the 3rd object is to provide the preparation of this Radix Notoginseng total arasaponins, and the 4th object is to provide the application of this Radix Notoginseng total arasaponins.
The first object of the present invention is achieved in that described Radix Notoginseng total arasaponins comprises ginsenoside Rg1, ginsenoside Rb1, and described ginsenoside Rg1 and ginsenoside Rb1's weight ratio are 1:0.9 ~ 1.1.
As optimal technical scheme, described ginsenoside Rg1 and ginsenoside Rb1's weight ratio are 1:1.
The second object of the present invention is achieved in that and comprises raw material processing, reflux, extract,, filtering and concentrating step, is specially:
A, raw material processing: raw material Radix Notoginseng powder is broken into coarse powder;
B, reflux, extract: add the ethanol of 8 ~ 12 times of amounts 60 ~ 80% of weight ratio, reflux, extract, 2 ~ 4 times, each 1 ~ 2h;
C, filtering and concentrating are dried: coarse filtration after each extraction, merge coarse filtration liquid, and then carry out fine straining; Fine straining liquid is concentrated into the density 1.3～1.5 that compares, and obtains described Radix Notoginseng total arasaponins.
The 3rd object of the present invention is achieved in that described Radix Notoginseng total arasaponins is prepared into powder, or in described Radix Notoginseng total arasaponins, adds the adjuvant of pharmaceutically accepting to be prepared into granule, capsule, tablet, pill, oral liquid or injection.
The 4th object of the present invention is achieved in that described Radix Notoginseng total arasaponins prevents and/or treats the application in ischemic cerebrovascular medicine in preparation.
The present invention adopts the core composition of new method control Radix Notoginseng total arasaponins, and ginsenoside Rg1 and ginsenoside Rb1's weight ratio is controlled in the scope of 1:0.9 ~ 1.1.Test with this Radix Notoginseng total arasaponins, find that Radix Notoginseng total arasaponins can reduce the brain infarction area that Cerebral Ischemia/Reperfusion causes, and improve the neurobehavioral obstacle that cerebral ischemia re-pouring causes, that is, work for preventing and/or treating ischemic cerebrovascular.
Brief description of the drawings
Fig. 1 is the Radix Notoginseng total arasaponins neurobehavioral obstacle that improves cerebral ischemia-reperfusion in mice (compared with Sham group, # < 0.001, compared with MCAO group, * < 0.01);
Fig. 2 is that Radix Notoginseng total arasaponins reduces the brain infarction area that ischemia-reperfusion causes.
Detailed description of the invention
Below in conjunction with embodiment and accompanying drawing, the present invention is further illustrated, but never in any form the present invention is limited, and any conversion or the improvement done based on training centre of the present invention, all fall into protection scope of the present invention.
Radix Notoginseng total arasaponins of the present invention, comprises ginsenoside Rg1, ginsenoside Rb1, and described ginsenoside Rg1 and ginsenoside Rb1's weight ratio are 1:0.9 ~ 1.1.
As preferred implementation, described ginsenoside Rg1 and ginsenoside Rb1's weight ratio are 1:1.
The preparation method of Radix Notoginseng total arasaponins of the present invention, comprises raw material processing, reflux, extract,, filtering and concentrating step, is specially:
A, raw material processing: raw material Radix Notoginseng powder is broken into coarse powder;
B, reflux, extract: add the ethanol of 8 ~ 12 times of amounts 60 ~ 80% of weight ratio, reflux, extract, 2 ~ 4 times, each 1 ~ 2h;
C, filtering and concentrating are dried: coarse filtration after each extraction, merge coarse filtration liquid, and then carry out fine straining; Fine straining liquid is concentrated into the density 1.3～1.5 that compares, and obtains described Radix Notoginseng total arasaponins.
As preferred implementation:
Coarse powder described in A step is 20 ~ 80 orders.
The amount that adds ethanol in B step is 70% ethanol of 10 times of amounts of weight ratio.
Reflux, extract, described in B step 3 times, each 1.5h.
Fine straining described in C step is that embrane method is filtered, and the aperture of filter membrane is 0.1 ~ 10 μ m; Described simmer down to normal pressure concentrates or concentrating under reduced pressure, takes the methods such as lyophilization, thin film concentration or spraying are dried to concentrate.
Radix Notoginseng total arasaponins of the present invention is prepared into powder, or described Radix Notoginseng total arasaponins adds the adjuvant of pharmaceutically accepting to be prepared into granule, capsule, tablet, pill, oral liquid or injection.
Described adjuvant comprises filler, diluent, binding agent, excipient, absorption enhancer, filler, surfactant and the stabilizing agent etc. of pharmaceutical field routine, also can add if desired flavouring agent, pigment and sweeting agent etc.Can add one or more pharmaceutically acceptable adjuvants.
Radix Notoginseng total arasaponins of the present invention prevents and/or treats the application in ischemic cerebrovascular in preparation.
Raw material Radix Notoginseng powder is broken into 20 object coarse powder, gets coarse powder 10kg, wherein add 60% ethanol 80kg; Reflux, extract, 2 times, each 1h; After each extraction, use filter screen coarse filtration, merge coarse filtration liquid; With the film fine straining of 0.1 μ m, the fine straining liquid obtaining adopts atmosphere pressure desiccation to be concentrated under condition of normal pressure, is concentrated into the density 1.3 that compares, and obtains described Radix Notoginseng total arasaponins.
After measured, in the Radix Notoginseng total arasaponins of preparation, ginsenoside Rg1 and ginsenoside Rb1's weight ratio is 1:0.9.
Raw material Radix Notoginseng powder is broken into 80 object coarse powder, gets coarse powder 15kg, wherein add 80% ethanol 180kg; Reflux, extract, 4 times, each 2h; After each extraction, use filter bag coarse filtration, merge coarse filtration liquid; With the film fine straining of 10 μ m, the fine straining liquid obtaining adopts hypobaric drying method to be concentrated under reduced pressure, is concentrated into the density 1.5 that compares, and obtains described Radix Notoginseng total arasaponins.
After measured, in the Radix Notoginseng total arasaponins of preparation, ginsenoside Rg1 and ginsenoside Rb1's weight ratio is 1:1.1.
Embodiment 3
Raw material Radix Notoginseng powder is broken into 50 object coarse powder, gets coarse powder 10kg, wherein add 70% ethanol 100kg; Reflux, extract, 3 times, each 1.5h; After each extraction, use filter bag coarse filtration, merge coarse filtration liquid; With the film fine straining of 10 μ m, the fine straining liquid obtaining adopts freeze-drying to be concentrated under reduced pressure, is concentrated into the density 1.5 that compares, and obtains described Radix Notoginseng total arasaponins.
After measured, in the Radix Notoginseng total arasaponins of preparation, ginsenoside Rg1 and ginsenoside Rb1's weight ratio is 1:1.
Embodiment 4
Get Radix Notoginseng total arasaponins prepared by embodiment 1 and pack, be prepared into powder.
Embodiment 5
Getting Radix Notoginseng total arasaponins prepared by embodiment 2 adds the adjuvant of pharmaceutically accepting to be prepared into granule.
Embodiment 6
Getting Radix Notoginseng total arasaponins prepared by embodiment 3 adds the adjuvant of pharmaceutically accepting to be prepared into capsule.
Embodiment 7
Getting Radix Notoginseng total arasaponins prepared by embodiment 1 adds the adjuvant of pharmaceutically accepting to be prepared into tablet.
Embodiment 8
Getting Radix Notoginseng total arasaponins prepared by embodiment 2 adds the adjuvant of pharmaceutically accepting to be prepared into pill.
Embodiment 9
Getting Radix Notoginseng total arasaponins prepared by embodiment 3 adds the adjuvant of pharmaceutically accepting to be prepared into oral liquid.
Embodiment 10
Getting Radix Notoginseng total arasaponins prepared by embodiment 1 adds the adjuvant of pharmaceutically accepting to be prepared into injection.
Embodiment 11
1. materials and methods
1.1 laboratory animal
Male C57BL/6 mice, body weight 25-30g(is purchased from Medical University Of Chongqing).
1.2 reagent
The Radix Notoginseng total arasaponins that adopts embodiment 3 to prepare, with physiological saline solution, 40mg/kg lumbar injection two days.2,3,5-triphenyltetrazolium chloride (TTC) is purchased from Sigma.
1.3 method
Brain Middle cerebral artery occlusion (MCAO) method for filling again: lumbar injection pentobarbital sodium (50mg/kg) is by mouse anesthesia.Dorsal position is fixed mice extremity with adhesive tape, cut off skin at cervical region along center line, blunt separation subcutaneous tissue, is separated to after the front flesh of trachea, along the downward separating muscle of right side sternocleidomastoid and fascia, isolate right carotid (CCA), external carotid artery (ECA) and internal carotid artery (ICA).Respectively hang single line at CCA proximal part and ECA distal end, by vascular ligation.Hang single line at CCA again, prepare against static line bolt below and use.Cut the otch (eye scissors approximately becomes miter angle with blood vessel) of an inclination at CCA with eye scissors, the blood vessel otch turning on still seeing like this in the time that blood just flows out.Insert from CCA with ophthalmic tweezers clamping bolt line, and inject ICA, stop gim peg line to bolt wire tag to crotch.Sew up wound, is placed in the environment of 20-25 DEG C and raises, and after two hours, line bolt is extracted, then is poured into 24 hours.After carrying out neuroethology scoring, cervical vertebra dislocation is put to death, and gets brain and carries out TTC dyeing.
Mice is divided into 6 groups at random, i.e. sham-operation Sham group, MCAO model group, Rg1 administration group, Rb1 administration group, Rg1/Rb1 administration group and Radix Notoginseng total arasaponins (PNS) administration group, 6 every group.Medicine lumbar injection two days, every day twice, performs the operation and is administered once for first 1 hour again, Sham group and MCAO model group intraperitoneal injection of saline at one time.
1.4 neuroethology scorings
Pour into again after 24 hours, by Longa point system, cerebral ischemic model is marked.This scoring method divides 5 grades, as following:
0 point: normal, impassivity functional impairment;
1 point: offside (i.e. left side) fore paw can not full extension, slight neurologic impairment;
2 points: when walking, mice turn-takes to offside, moderate neurologic impairment;
3 points: when walking, mice health is toppled over to offside, severe neurologic impairment;
4 points: can not spontaneously walk, lose consciously.
1.5 TTC dyeing
Mice cervical vertebra dislocation is put to death, get brain, remove after olfactory bulb, cerebellum and brain stem, be crownly cut into 6 and carry out TTC dyeing, 37 DEG C of lucifuges are hatched 30 min, and infarct size is white in color.
2. result
2.1 Radix Notoginseng total arasaponinss have improved the neurological behavior disorder that MCAO causes;
2.2 Radix Notoginseng total arasaponinss have reduced the brain infarction area that MCAO causes, but effect degree differs.
3. conclusion
Radix Notoginseng total arasaponins has the effect that prevents and/or treats ischemic cerebrovascular.
Claims (10)
1. a Radix Notoginseng total arasaponins, comprises ginsenoside Rg1, ginsenoside Rb1, it is characterized in that described ginsenoside Rg1 and ginsenoside Rb1's weight ratio are 1:0.9 ~ 1.1.
2. Radix Notoginseng total arasaponins according to claim 1, is characterized in that described ginsenoside Rg1 and ginsenoside Rb1's weight ratio are 1:1.
3. a preparation method for Radix Notoginseng total arasaponins described in claim 1 or 2, is characterized in that comprising raw material processing, reflux, extract,, filtering and concentrating step, specifically comprises:
A, raw material processing: raw material Radix Notoginseng powder is broken into coarse powder;
B, reflux, extract: add the ethanol of 8 ~ 12 times of amounts 60 ~ 80% of weight ratio, reflux, extract, 2 ~ 4 times, each 1 ~ 2h;
C, filtering and concentrating are dried: coarse filtration after each extraction, merge coarse filtration liquid, and then carry out fine straining; Fine straining liquid is concentrated into relative density 1.3 ~ 1.5, obtains described Radix Notoginseng total arasaponins.
4. Radix Notoginseng total arasaponins preparation method according to claim 3, is characterized in that the coarse powder described in A step is 20 ~ 80 orders.
5. Radix Notoginseng total arasaponins preparation method according to claim 3, is characterized in that in B step, adding the amount of ethanol is 70% ethanol of 10 times of amounts of weight ratio.
6. Radix Notoginseng total arasaponins preparation method according to claim 3, is characterized in that reflux, extract, described in B step 3 times, each 1.5h.
7. Radix Notoginseng total arasaponins preparation method according to claim 3, is characterized in that being filtered into embrane method fine straining described in C step, and the aperture of filter membrane is 0.1 ~ 10 μ m; Described simmer down to normal pressure concentrates or concentrating under reduced pressure, takes the methods such as lyophilization, thin film concentration or spraying are dried to concentrate.
8. the Radix Notoginseng total arasaponins preparation described in claim 1 or 2, is characterized in that described Radix Notoginseng total arasaponins to be prepared into powder.
9. the Radix Notoginseng total arasaponins preparation described in claim 1 or 2, is characterized in that adding the adjuvant of pharmaceutically accepting to be prepared into granule, capsule, tablet, pill, oral liquid or injection in described Radix Notoginseng total arasaponins.
10. the Radix Notoginseng total arasaponins described in a claim 1 or 2 prevents and/or treats the application in ischemic cerebrovascular in preparation.
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| CN201210561300.8A CN103877134A (en) | 2012-12-21 | 2012-12-21 | Total panax notoginsenosides, preparing method thereof, preparations thereof and applications thereof |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1387854A (en) * | 2002-07-10 | 2003-01-01 | 云南植物药业有限公司 | Dispersed general arasaponin tablet and its prepn and application |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1387854A (en) * | 2002-07-10 | 2003-01-01 | 云南植物药业有限公司 | Dispersed general arasaponin tablet and its prepn and application |
Non-Patent Citations (1)
| Title |
|---|
| 许重阳等: "三七地下部位皂甙成分的HPLC测定及含量比较", 《中国实用医药》 * |
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Application publication date: 20140625 |
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