CN105616432A - Novel application of notoginsenoside R4 to preparation of medicine for treating and/or preventing allergic rhinitis - Google Patents
Novel application of notoginsenoside R4 to preparation of medicine for treating and/or preventing allergic rhinitis Download PDFInfo
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Abstract
The invention relates to novel application of notoginsenoside R4, namely novel application of the notoginsenoside R4 to preparation of medicine for treating and/or preventing allergic rhinitis.It is proved by experiments that the notoginsenoside R4 can improve symptoms of allergic rhinitis on multiple aspects, and a quite good effect is achieved on the aspects of lowering the content of blood histamine and repairing nasal mucosa.
Description
Technical field
The present invention relates to Panax Notoginseng saponin R4A kind of new application, specifically Panax Notoginseng saponin R4New application in preparation treatment and/or Polyglucan rhinitis medicine.
Background technology
Allergic rhinitis (allergicrhinitis, AR) it is the release of the main inflammatory mediator mediated by IgE caused after a kind of susceptible body contact sensitization allergen and panimmunity competent cell, the nasal mucosa non-infectious inflammatory disease that inflammatory cytokine participates in. Allergic rhinitis prevalence worldwide is in rising trend, and in American-European countries adult, allergic rhinitis prevalence is generally 10%-25%, and China outpatient in recent years substantially rises, and has had a strong impact on the quality of life of patient. Allergic rhinitis is a kind of multi-factor disease being interacted by gene and environment and being brought out. The risk factor of allergic rhinitis is likely to be present in all age brackets. Commonly encountered diseases is because of inherited genetic factors, demodicid mite, pollen, animal scurf, fungus allergen, cockroach allergens, food allergens, free radical. Currently mainly Therapeutic Method includes: avoid contact with allergen, Drug therapy, immunization therapy, surgical intervention.
Radix Notoginseng is the dry root of araliaceae ginseng plant Radix Notoginseng (Panaxnotoginseng (Burk.) F.H.Chen), has eliminating stasis to stop pain, effect of subduing swelling and relieving pain. Modern pharmacology research shows, blood system, cardiovascular system, immune system are all had different effects by Radix Notoginseng. Radix Notoginseng total arasaponins is one of principle active component in Radix Notoginseng, has a blood vessel, increases cerebral blood flow, improves microcirculation, reduces myocardial oxygen consumption, suppresses platelet aggregation, reduces the effect such as blood viscosity, scavenging free radicals; It is widely used in the treatment of cardiovascular and cerebrovascular disease and surgery clinically. More currently for Saponins from Panax notoginseng research, but focus mostly in macroconstituent analysis, less for micro constitutent research. At present, the monomer saponin constituents that separation purification obtains from Radix Notoginseng has kind more than 70, it mostly is 20 (the S)-protopanaxadiol-type (20 (S)-Protopanaxadiol) of dammarane type, 20 (S)-PPD) and 20 (S)-Protopanaxatriol types (20 (S)-Protopanaxatriol), 20 (S)-PPT) saponin, minority is the derivant of oleanane. Panoxadiol's glycosides be represented as Rb1, panaxatriol's glycosides be represented as Rg1, ginsenoside Rg1 is the active component that arasaponin constituents content is the highest.
Do not retrieve Panax Notoginseng saponin R at present4For treating or the bibliographical information of Polyglucan rhinitis.
Summary of the invention
The present invention solves the problems of the prior art, it is provided that arasaponin R4 application in prevention and/or treatment allergic rhinitis medicine, it is for prevention and/or treatment allergic rhinitis and has significant role as related drugs exploitation.
It is an object of the invention to provide Panax Notoginseng saponin R4New application in preparation treatment and/or Polyglucan rhinitis medicine.
Preferably, described Panax Notoginseng saponin R4Purity is not less than 70%.
It is a further object of the present invention to provide Panax Notoginseng saponin R4New application in make the medicines such as treatment and/or the tablet of Polyglucan rhinitis, capsule, injection and lyophilized injectable powder with pharmaceutically acceptable carrier combination.
It is a further object of the present invention to provide a kind of Panax Notoginseng saponin R4Extracting method when preparation treatment and/or Polyglucan rhinitis new medicine use:
Described Panax Notoginseng saponin R4Prepared by following steps and obtain: take pseudo-ginseng and be ground into fine powder, extract with percent by volume 50-95% alcohol heating reflux, Radix Notoginseng extracting solution crosses HPD-100 type macroporous adsorbent resin, with percent by volume 75-95% ethanol elution, eluent concentrates, Radix Notoginseng total arasaponins concentrated solution crosses Rp-C18 silicagel column, uses methanol-water isocratic elution, Panax Notoginseng saponin R in on-line checking eluent4Content, collects right rail, concentrates, dries, to obtain final product.
Described tablet proportioning by weight is: Panax Notoginseng saponin R420-60 part, disintegrating agent 10-100 part, lubricant 5-10 part, correctives 100-300 part; Described disintegrating agent is starch, carboxymethyl starch sodium, microcrystalline Cellulose or polyvinylpolypyrrolidone; Described lubricant is magnesium stearate, micropowder silica gel, Pulvis Talci or Polyethylene Glycol; Described correctives is lactose.
Described capsule proportioning by weight is: Panax Notoginseng saponin R420-60 part, lubricant 5-10 part, correctives 80-240 part; Described lubricant is lubricant is magnesium stearate, micropowder silica gel, Pulvis Talci or Polyethylene Glycol; Described correctives is lactose.
Described injection proportioning by weight is: Panax Notoginseng saponin R440-120 part, sodium chloride 100-300 part, water for injection 500-1500 part.
Described injectable powder proportioning by weight is: Panax Notoginseng saponin R440-120 part, water for injection 1000-3000 part.
Panax Notoginseng saponin R provided by the invention4New application for preparing treatment and/or Polyglucan rhinitis medicine aspect has the advantage that
1, Panax Notoginseng saponin R4Obtain, safety non-toxic from araliaceae ginseng plant Radix Notoginseng, can long-term taking.
2, the invention provides Panax Notoginseng saponin R4New medical application, has opened up new application; Panax Notoginseng saponin R4Prevention and treatment allergic rhinitis caused by a variety of causes to allergic rhinitis all have good effect.
3, Panax Notoginseng saponin R4Pharmacological action is obvious, test result indicate that, Panax Notoginseng saponin R4Reduction blood histamine content and nasal mucosa reparation aspect is respond well.
4, Panax Notoginseng saponin R4Raw material is easy to get, and can make various common formulations by conventional method, and such as injectable powder, injection, capsule, granule, tablet etc., preparation method is simple.
Detailed description of the invention
Further illustrate the present invention by the examples below. It should be understood that embodiments of the invention are an illustration for the present invention rather than limitation of the present invention. The simple modifications that the present invention is carried out by the essence according to the present invention broadly falls into the scope of protection of present invention.
Embodiment 1:
Take pseudo-ginseng and be ground into fine powder, extract with percent by volume 50% alcohol heating reflux, Radix Notoginseng extracting solution is with flow velocity for the 18BV/h HPD-100 type macroporous adsorbent resin by 12 times of three seven weight, with percent by volume 75% ethanol elution, eluent concentrates, Radix Notoginseng total arasaponins concentrated solution by 8 times of three seven weight Rp-C18 silicagel column, uses methanol-water isocratic elution, Panax Notoginseng saponin R in on-line checking eluent with flow velocity for 10BV/h4Content, collects right rail (on-line monitoring, the part meeting application claims is right rail), concentrates, dries, to obtain final product.
After testing, Panax Notoginseng saponin R4Content is 85%.
Embodiment 2:
Take pseudo-ginseng and be ground into fine powder, extract with percent by volume 95% alcohol heating reflux, Radix Notoginseng extracting solution is with flow velocity for the 16BV/h HPD-100 type macroporous adsorbent resin by 10 times of three seven weight, with percent by volume 95% ethanol elution, eluent concentrates, Radix Notoginseng total arasaponins concentrated solution by 8 times of three seven weight Rp-C18 silicagel column, uses methanol-water isocratic elution, Panax Notoginseng saponin R in on-line checking eluent with flow velocity for 8BV/h4Content, collects right rail (on-line monitoring, the part meeting application claims is right rail), concentrates, dries, to obtain final product.
After testing, Panax Notoginseng saponin R4Content is 70%.
Embodiment 3:
Example 1 gained Panax Notoginseng saponin R420g, microcrystalline Cellulose 10g, magnesium stearate 5g, lactose 120g; By the raw material mix homogeneously except magnesium stearate, moisten with water, cross 18 mesh sieves, dry, and then cross 20 mesh sieves, add magnesium stearate, tabletting after mix homogeneously, obtain tablet.
Embodiment 4:
Example 2 gained Panax Notoginseng saponin R420g, magnesium stearate 5g, lactose 160g; By Panax Notoginseng saponin R4, lactose mix homogeneously, moisten with water, then cross 20 mesh sieves, dry, and then cross 22 mesh sieves, add magnesium stearate, load capsule after mix homogeneously, obtain capsule.
Embodiment 5:
Example 1 gained Panax Notoginseng saponin R460g, sodium chloride 120g, water for injection 1500ml; By Panax Notoginseng saponin R4It is dissolved in water for injection, stirring and dissolving with sodium chloride, filters, aseptically filtrate is loaded in ampoule bottle, obtain injection.
Embodiment 6:
Example 2 gained Panax Notoginseng saponin R460g, water for injection 2000ml; Panax Notoginseng saponin R4, inject and make dissolving with water heating, add proper amount of active carbon, stir evenly, filter, fill, lyophilization, sealing, obtain injectable powder.
Effect experiment
1, experiment material
1.1 animals
Cavia porcellus 40, cleaning grade, male and female half and half, body weight 350-400g, Guangxi Medical University's Experimental Animal Center provide. Dividing cage to feed, 4, every cage, ad lib is drunk water.
1.2 reagent
Aluminium hydroxide, ovalbumin (Sigma Co., USA); O-phthalaldehyde(OPA) (Solution on Chemical Reagents in Shanghai purchase and supply 5-linked chemical plant); Histamine diphosphate (Amresco company).
1.3 medicines
Embodiment 1, embodiment 2 (making concentration by purified water before use is 0.02g/ml). XINQIN (sic) granule (Shanghai Tong Hanchun pharmaceutical Co. Ltd), is configured to 0.67g/ml with distilled water.
1.4 instruments
ShimazuRF-5301 spectrofluorophotometer.
2, method
2.1 modeling methods
2.1.1 basis sensitization adds normal saline 1mlip Cavia porcellus with antigen ovalbumin (OVA) 0.3mg and adjuvant aluminum hydroxide 30mg, 1 time every other day, totally 7 times.
2.1.2 nasal cavity has excited after the sensitization of basis with 2%OVA collunarium, every side 50ul, every day 1 time, totally 7 times.
2.1.3 modeling effective evaluation standard is evaluated with scoring formula, observes 30min, record sneeze number, rhinocnesmus degree and nasal discharge amount, standard such as table 1 of scoring after exciting.
Table 1 allergic rhinitis symptoms scores standard
Total score reaches 5 points i.e. modeling success, continues collunarium every other day afterwards and maintains until experiment terminates.
2.2 medications and observation index
2.2.1 successful for modeling Cavia porcellus is randomly divided into 4 groups by medication: model group, embodiment 1 group, embodiment 2 groups, XINQIN (sic) granule matched group, often group 8, each medicine group is with relative medicine and dosed administration, every day gastric infusion 1 time, administration 2 weeks altogether, collunarium excites and does animal behavioral study, record every other day. Separately setting normal group (n=8), normal group every day is with normal saline gavage, every other day with normal saline collunarium.
2.2.2 animal behavioral study collunarium every other day excites, and scores by the standard of table 1.
2.2.3, after the administration of blood histamine mensuration terminates, 25% urethane anesthesia, abdominal aortic blood 5ml is to anticoagulant tube, and-20 DEG C save backup. Extract histamine, use fluorescence spectrophotometry histamine content, computing formula: histamine content (mg/ml)=[(sample value-sample blank)/(standard value-standard null white value)] �� standard substance Histamine concentrations (standard substance Histamine concentrations 50.2mg/ml) in blood.
2.3 statistical method experimental datas, through spss process, carry out One-Way variance analysis, with�� s represents. Compare between group and check with t. P 0.05 is statistically significant.
3, result
3.1 animal behavioral study results are in Table 2. After modeling, it is up to standard that the counting score of Cavia porcellus sign is respectively organized in modeling, there was no significant difference each other. After drug treatment, the sign score of 3 each medicine groups all decreases, and has significant difference (P 0.01), compare with model group and have significant difference (P 0.01) compared with normal group. There was no significant difference between 3 medicine groups.
Sign counting score before and after the treatment of table 2 allergic rhinitis in guinea-pig (N=8)
Note: with model group than * * P 0.01, * P 0.05 (lower same)
3.2 blood histamine assay results are in Table 3, and after treatment, each group blood histamine content has significant difference (P 0.01) with normal group, also has significant difference (P 0.01) with model group.
Table 3 allergic rhinitis in guinea-pig treatment front and back blood histamine content (N=8)
4, discuss
Animal behavioral study shows, embodiment 1-2 can reach the effect of mitigation symptoms by minimizing sneeze and watery nasal discharge. Histamine is to send out reaction period and late response phase respectively by a kind of important medium of mastocyte, the generation of basophilic granulocyte retting conditions in speed, local organization generation inflammatory reaction can be made, cause Marjoram Extract, tissue edema, external secretion hyperactivity, eosinophilic granulocyte is by chemotactic and swims out of in people's nasal discharge by mucosal epithelium, thus causing most of symptom of allergic rhinitis, can as one of reference index of curative effect of medication. Panax Notoginseng saponin R4Improve allergic rhinitis symptoms in many-side, and prescription is precise and appropriate, in reducing blood histamine content and nasal mucosa reparation, have good effect.
Although, above use generality explanation, detailed description of the invention and test, the present invention is described in detail, but on basis of the present invention, it is possible to it is made some modifications or improvements, and this will be apparent to those skilled in the art. Therefore, these modifications or improvements without departing from theon the basis of the spirit of the present invention, belong to the scope of protection of present invention.
Claims (8)
1. Panax Notoginseng saponin R4New application in preparation treatment and/or Polyglucan rhinitis medicine.
2. new application according to claim 1, described Panax Notoginseng saponin R4Purity is not less than 70%.
3. new application according to claim 1, it is characterised in that described Panax Notoginseng saponin R4Prepared by following steps and obtain: take pseudo-ginseng and be ground into fine powder, extract with percent by volume 50-95% alcohol heating reflux, Radix Notoginseng extracting solution crosses HPD-100 type macroporous adsorbent resin, with percent by volume 75-95% ethanol elution, eluent concentrates, Radix Notoginseng total arasaponins concentrated solution crosses Rp-C18 silicagel column, uses methanol-water isocratic elution, Panax Notoginseng saponin R in on-line checking eluent4Content, collects right rail, concentrates, dries, to obtain final product.
4. new application according to claim 1 and 2, it is characterised in that described Panax Notoginseng saponin R4Tablet, capsule, injection and lyophilized injectable powder is made with pharmaceutically acceptable carrier combination.
5. new application according to claim 5, it is characterised in that described tablet proportioning by weight is: Panax Notoginseng saponin R420-60 part, disintegrating agent 10-100 part, lubricant 5-10 part, correctives 100-300 part; Described disintegrating agent is starch, carboxymethyl starch sodium, microcrystalline Cellulose or polyvinylpolypyrrolidone; Described lubricant is magnesium stearate, micropowder silica gel, Pulvis Talci or Polyethylene Glycol; Described correctives is lactose.
6. new application according to claim 5, it is characterised in that described capsule proportioning by weight is: Panax Notoginseng saponin R420-60 part, lubricant 5-10 part, correctives 80-240 part; Described lubricant is lubricant is magnesium stearate, micropowder silica gel, Pulvis Talci or Polyethylene Glycol; Described correctives is lactose.
7. new application according to claim 5, it is characterised in that described injection proportioning by weight is: Panax Notoginseng saponin R440-120 part, sodium chloride 100-300 part, water for injection 500-1500 part.
8. new application according to claim 5, it is characterised in that described injectable powder proportioning by weight is: Panax Notoginseng saponin R440-120 part, water for injection 1000-3000 part.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110179843A (en) * | 2019-04-23 | 2019-08-30 | 昆明医科大学 | External-use pharmaceutical composition for treating non-allergic rhinitis |
| CN115487275A (en) * | 2022-10-25 | 2022-12-20 | 湖南祥民制药有限公司 | A Chinese medicinal granule containing Notoginseng radix extract and its preparation method |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1539493A (en) * | 2003-11-01 | 2004-10-27 | 任秀云 | Combination of Chinese traditional medicine for curing disease of respiratory system and preparing method |
| CN1886156A (en) * | 2003-09-30 | 2006-12-27 | 特莱索恩儿童健康研究院 | Immunotherapy method |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1886156A (en) * | 2003-09-30 | 2006-12-27 | 特莱索恩儿童健康研究院 | Immunotherapy method |
| CN1539493A (en) * | 2003-11-01 | 2004-10-27 | 任秀云 | Combination of Chinese traditional medicine for curing disease of respiratory system and preparing method |
Non-Patent Citations (2)
| Title |
|---|
| OH, HYUN-A等: "Ginsenoside Rg1 inhibits the TSLP production in allergic rhinitis mice", 《IMMUNOPHARMACOLOGY AND IMMUNOTOXICOLOGY》 * |
| 杨志刚: "三七中皂苷的抗肿瘤及免疫佐剂活性研究", 《中国优秀博硕士学位论文全文数据库（博士）医药卫生科技辑》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110179843A (en) * | 2019-04-23 | 2019-08-30 | 昆明医科大学 | External-use pharmaceutical composition for treating non-allergic rhinitis |
| CN110179843B (en) * | 2019-04-23 | 2021-02-05 | 昆明医科大学 | External-use pharmaceutical composition for treating non-allergic rhinitis |
| CN115487275A (en) * | 2022-10-25 | 2022-12-20 | 湖南祥民制药有限公司 | A Chinese medicinal granule containing Notoginseng radix extract and its preparation method |
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