CN103655663A - Pharmaceutical composition containing total saponins and total alkaloids of caulophyllum robustum - Google Patents
Pharmaceutical composition containing total saponins and total alkaloids of caulophyllum robustum Download PDFInfo
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- CN103655663A CN103655663A CN201210332553.8A CN201210332553A CN103655663A CN 103655663 A CN103655663 A CN 103655663A CN 201210332553 A CN201210332553 A CN 201210332553A CN 103655663 A CN103655663 A CN 103655663A
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Abstract
The invention discloses a pharmaceutical composition containing total saponins and total alkaloids of caulophyllum robustum. The total saponins and total alkaloids of the caulophyllum robustum serve as active ingredients, and are in the mass ratio of (1:10)-(1:100). The total saponins and total alkaloids of the caulophyllum robustum are combined organically, thereby achieving the effects of dispelling wind, eliminating dampness, resisting inflammation and relieving pain. As proved by experiments, the composition has an inhibiting effect on anti-non-specific and specific inflammation models, and has a strong pain relieving effect. The apoptosis rate of RA (Rheumatoid Arthritis) rat synovial cells can be increased remarkably, thereby preventing joints from being further damaged, effectively treating rheumatoid arthritis and achieving good inflammation resisting and immunoregulation effects. Moreover, a synergistic effect is achieved by combining alkaloids with saponin compounds. Being different from a Chinese medicinal compound prepared on the basis that decoction pieces are combined, the composition is more definite in chemical ingredients of which over 50 percent can be qualified and quantified accurately, thereby easily performing quality control and meeting the requirements of the modern pharmaceuticals industry.
Description
Technical field
The present invention relates to a kind of containing the total saponins of leontice robustumDiels and the pharmaceutical composition of total alkaloids, this pharmaceutical composition contains a certain proportion of leontice robustumDiels total alkaloids and leontice robustumDiels total saponins, be mainly used in treating rheumatism and atrophic diseases, applied in any combination has synergism and attenuation simultaneously.
Background technology
Clinical practice for many years shows, certainly, Chinese medicine is alleviating patient's symptom, improves immunologic function and body condition for prevention and treatment in Chinese and western rheumatism and atrophic diseases curative effect, improves the aspect effects such as life in patients remarkable.But rheumatism in the past and rheumatoid Chinese medicine majority consist of large compound recipe, in actual production, be difficult to meet the requirement of medicine " safety, effective, steady quality "; And active Chinese drug component monomer or single medicinal substances extract have lost Chinese medicine multipath, many target spots are integrated the feature regulating, be difficult to obtain gratifying curative effect.Therefore, need to develop the relatively simple active component compatibility Chinese medicine of determined curative effect, chemical composition, enable to adapt to the requirement of modern medicine industry and drug evaluation system.
Leontice robustumDiels (Radix et Rhizoma Leonticis) is root stock and the root of Berberidaceae Radix Caulophylli platymiscium Radix Caulophylli Caulophyllum robustum Maxim., has the multiple pharmacological effect such as antiinflammatory, analgesia, antibacterial and antitumor.These species are the poisonous plants that include in Chinese Plants spectrum data storehouse, and its toxicity is water, ethanol and the ether extract 1000mg/kg of mouse peritoneal injection rhizome, and appearance activity reduces, and ataxia is fainted from fear dead.The toxicity of leontice robustumDiels mainly comprises magnoline, thaspine, methylcytisine, d-lupinine etc. from its contained alkaloids composition, and these compositions are also the main components of its anti-inflammatory and analgesic effect.In addition, also contain a large amount of saponin components in leontice robustumDiels, comprise leontin A, B, C, D, E etc., saponin component has stronger antiinflammatory action, but does not have analgesic activity.
Total saponins component and the total alkaloids component of leontice robustumDiels all have antiinflammatory action, analgesic active component is total alkaloids extract, total saponins component is used separately analgesic activity not obvious, and total saponins component is mixed the analgesic effect of using and is obviously better than using separately total alkaloids component with total alkaloids component, in prompting leontice robustumDiels, total alkaloids and total saponins may have synergism at ease pain.Also point out for analgesic drug matching, with the drug matching that contains total saponins component and total alkaloids component, may have potentiation, and can lower alkaloidal consumption, make it in safety range, reach the object of avoiding alkaloid toxic and side effects simultaneously.
Summary of the invention
The object of the present invention is to provide a kind of pharmaceutical composition containing leontice robustumDiels total alkaloids and total saponins, it is characterized in that: effective ingredient is leontice robustumDiels total alkaloids and total saponins, the mass ratio of leontice robustumDiels total alkaloids and total saponins is 1: 10～1: 100.
Excipient or dressing that pharmaceutical composition provided by the invention and medicine allow are prepared into pharmaceutical preparation, and dosage form is liquid preparation or solid preparation.
The whole bag of tricks that leontice robustumDiels total saponins and total alkaloids can adopt various equivalent modifications to understand prepares, and comprises chemosynthesis and bioconversion method.
Described pharmaceutical composition, contains magnoline, thaspine and methylcytisine, and its content range is 5-20%, these compounds also can obtain by the approach of chemosynthesis or biotransformation; contain leontin A, leontin B, leontin C, leontin D, leontin G, 3-O-α-L-arabopyranose-Hederagenin-28-O-β-D-Glucopyranose .-(1 → 6)-β-D-pyranglucoside, helexin-28-O-α-L-pyrans rhamnose-(1 → 4)--β-D-Glucopyranose. (1 → 6)-β-D-pyranglucoside, helexin-3-O-β-D-Glucopyranose .-(1 → 3)-α-L-arabopyranose glycosides, 3-O-β-D-Glucopyranose .-(1 → 3)-α-L-arabopyranose-helexin--28-O-α-L-pyrans rhamnose-(1 → 4)--β-D-pyranglucoside, 3-O-β-D-Glucopyranose .-(1 → 2) [β-D-Glucopyranose .-(1 → 3)]-α-L-arabopyranose-helexin--28-O-α-L-pyrans rhamnose-(1 → 4)--β-D-Glucopyranose .-(1 → 6)-β-D-pyranglucoside), 3-O-β-D-Glucopyranose .-(1 → 2)-α-L-arabopyranose-helexin-28-O-α-L-pyrans rhamnose-(1 → 4)--β-D-Glucopyranose .-(1 → 6)-β-D-Glucopyranose .-(1 → 4)-α-L-pyrans rhamnose-(1 → 4)--β-D-Glucopyranose .-(1 → 6)-β-D-pyranglucoside, oleanolic acid-3-O-β-D-Glucopyranose .-(1 → 2)-α-L-arabopyranose glycosides, 3-O-β-D-Glucopyranose .-(1 → 2)-α-L-arabopyranose-oleanolic acid saponin unit-28-O-α-L-pyrans rhamnose-(1 → 4)--β-D-Glucopyranose. (1 → 6)-β-D-pyranglucoside, 3-O-β-D-Glucopyranose .-(1 → 3)-α-L-arabopyranose-oleanolic acid saponin unit-28-O-α-L-pyrans rhamnose-(1 → 4)--β-D-Glucopyranose. (1 → 6)-β-D-pyranglucoside, echinocystic acid-3-O-β-D-Glucopyranose .-(1 → 2)-α-L-arabopyranose glycosides, 3-O-β-D-Glucopyranose .-(1 → 2)-α-L-arabopyranose-echinocystic acid soap-28-O-α-L-pyrans rhamnose-(1 → 4)--β-D-Glucopyranose .-(1 → 6)-β-D-pyranglucoside, 3-O-β-D-Glucopyranose .-(1 → 2)-β-D-Glucopyranose .-(1 → 6)-β-D-pyranglucoside,-α-L-arabopyranose-echinocystic acid sapogenin-28-O-α-L-pyrans rhamnose-(1 → 4), 3-O-β-D-Glucopyranose .-(1 → 2) [β-D-Glucopyranose .-(1 → 3)]--β-D-Glucopyranose .-(1 → 6)-β-D-pyranglucoside etc., its content range is 10-70%, these compounds also can obtain by the approach of chemosynthesis or biotransformation.
Another object of the present invention is to provide the application of said composition in treatment rheumatism or atrophic diseases medicine.Said composition also can combine with other drug, the application in preparation treatment rheumatism or atrophic diseases ancillary drug.
The present invention organically combines the total saponins constituents of leontice robustumDiels and total alkaloids constituents, the effect of common performance " expelling wind and removing dampness, anti-inflammatory and antalgic ".Experiment showed, that said composition antagonism is non-specific and specificity inflammation model is inhibited, and there is stronger analgesic activity.Can significantly improve the apoptosis rate of RA lymphocyte of adjurant arthritis rat cell, thereby stop the further destruction in joint, effectively treat rheumatoid arthritis, there is good antiinflammatory and immunoregulation effect.And alkaloid and saponins compound share and have synergistic function.Different with take decoction pieces compatibility as basic Chinese medicine compound, the chemical composition of said composition is clearer and more definite, surpasses 50% chemical composition and can obtain quantitative and qualitative analysis accurately, is therefore easy to carry out quality control, can meet the requirement of modern pharmaceutical industry.
The specific embodiment
In order to understand better the present invention, be further described with the following Examples.
Embodiment 1
Get leontice robustumDiels medicinal material coarse powder, the alcohol heating reflux with appropriate 50% extracts medical material, after extracting solution cool overnight, filters, the concentrated upper D101 macroporous adsorbent resin of filtrate, first water rinses, and then uses the alcohol flushing of 30-70%, and eluate is concentrated, lyophilization and get final product.Adopt HPLC-ELSD method to detect extract, analysis condition is Agilent Extend-C18, and mobile phase is H
2o-CH
3cN, water is reduced to 10% from 70% linearity in 30min; ELSD parameter: 105 ℃ of drift tube temperatures, flow rate of carrier gas 2.7L/min; Respectively with leontin B, D, G, lonticinD, leontice robustumDiels glycosides D, thaspine, methylcytisine, for detecting composition, adopt its content of external standard method.Leontin B wherein, D, the content that the content of G is respectively 1%, 9%, 27%, lonticin D is 5%, the content of leontice robustumDiels glycosides D is 8%.Thaspine, methylcytisine content are respectively 0.2%, 0.3%.
Embodiment 2 compositionss 1 (leontice robustumDiels total alkali: leontice robustumDiels total saponins=1: 40) analgesic activity experiment is screened qualified female mice by pain thresholding, random packet, after fasting 6h, 3 groups of total extracts of gavage various dose respectively wherein, the normal saline of one group of gavage equivalent, one group of gavage somedon, the mixture dosage of another three groups of difference gavage 1 ‰ total alkaloidss, 4% total saponins, 0.5 ‰ total alkaloidss and 2% total saponins.Measure before administration, after administration 0.5,1,2,3 and the pain threshold of 4h mice, surpass 60s and press 60s calculating.Experimental result is in Table 1.
The impact of table 1 leontice robustumDiels test sample on the experiment of mice hot-plate analgesia
Note: compare with matched group
*p < 0.05
*p < 0.01, with the comparison of total alkaloids group
△p < 0.05
Embodiment 3 compositionss 2 (leontice robustumDiels total alkali: leontice robustumDiels total saponins=1: 30) antiinflammatory action experiment
Get the male rat that body weight is 140～160g, by body weight random group, 10 every group, adopt gastric infusion, before administration, every Mus gavages normal saline by 30ml/kg, 30min after administration, every subcutaneous inserting needle of Rat Right metapedes sole of the foot portion causes inflammation near the clear solution 0.1ml of 10% Fresh Egg of subcutaneous injection ankle joint, respectively at causing scorching rear 0.5h, 1h, 2h, 4h, 6h, measures and causes scorching sufficient volume, calculates each rat and causes the right back sufficient sole of the foot volume-variation value in scorching front and back.Experimental result is in Table 2.
The impact (X ± s.n=10) of table 2 leontice robustumDiels test sample on foot swelling due to Ovum Gallus domesticus album
Note: compare with matched group
*p < 0.05,
*p < 0.01
Embodiment 4 compositionss 3 (leontice robustumDiels total alkali: leontice robustumDiels total saponins=1: the 30) impact on adjuvant arthritis rats serum cytokines
Rat random packet, except blank group injecting normal saline, by the CIA (1mg/ml) of 5 intradermal injection 0.5ml of every rat root of the tail part.After 7 days, use the same method intradermal injection CIA (1mg/ml) as booster immunization again.Every group starts administration, continuous 3 weeks for the 10th day after the 1st immunity.The therapeutical effect of observation group's composite medicine to rheumatoid arthritis.Measure rat blood serum cytokine IL-β, IL-4, TNF-alpha levels
The impact of table 3 compositions 3 on adjuvant arthritis rats serum cytokines
With model group comparison
*p < 0.01,
*p < 0.05 compares #p < 0.01, ##p < 0.05 with blank group
Embodiment 5 tablet preparations
Get compositions 120g (ratio of leontice robustumDiels total alkali and leontice robustumDiels total saponins is 1: 40), starch 180g, dextrin 10g are mixed evenly, bonding with 10% pregelatinized Starch slurry, wet granulation, dry, add appropriate magnesium stearate mixed, be pressed into 1000, tablet, coating and get final product.
Embodiment 6 capsules
200g compositions (ratio of leontice robustumDiels total alkali and leontice robustumDiels total saponins is 1: 10) is mixed with hydroxypropyl cellulose 60g and micropowder silica gel 30g, with appropriate 70% ethanol, make wetting agent, wet granulation, adds magnesium stearate after the oven dry of sieving, mix rear encapsulatedly, make 1000.
Embodiment 7 granules
The compositions 120g (ratio of leontice robustumDiels total alkali and leontice robustumDiels total saponins is 1: 10) that gets it filled, adds dextrin 200g, and sucrose 700g, adds appropriate ethanol and mix, and crosses 10 mesh sieve granulating, 60-70 ℃ of vacuum drying, granulate subpackage and get final product.The heavy Sgo of every bag
Embodiment 8 drop pill
200g pharmaceutical composition (ratio of leontice robustumDiels total alkali and leontice robustumDiels total saponins is 1: 20) is ground to sieve (100 order), add polyethylene glycol 6000 350g and stearic acid 25g mixes, be heated to 90 ℃, be stirred to fusing, remain on 80-85 ℃, control speed splashes into methyl-silicone oil and is cooled to ball, makes 1000.
Embodiment 9 oral liquids
Get 12g pharmaceutical composition (ratio of leontice robustumDiels total alkali and leontice robustumDiels total saponins is 1: 20), add heated and stirred in appropriate distilled water to dissolve.In warm water, add in addition sucrose 200g, after appropriate antiseptic dissolves, merge, add water to 1000mI, mix, filter fill after cold preservation, sterilizing obtains 1000ml oral liquid.In water, heated and stirred is dissolved.In warm water, add in addition sucrose 200g, after appropriate antiseptic dissolves, merge, add water to 1000mI and mix, filter fill after cold preservation, sterilizing obtains 1000ml oral liquid.
Embodiment 10 injections
The compositions 12g (ratio of leontice robustumDiels total alkali and leontice robustumDiels total saponins is 1: 30) that gets it filled, is dissolved in water for injection, and adds 4% Tween 80, fully stirs evenly, and adjusts pH to 6.8, injects water to fine straining after 1000mI ultrafiltration after filtration, fill sterilizing and get final product.
Embodiment 11 injectable powder
The compositions 120g (ratio of leontice robustumDiels total alkali and leontice robustumDiels total saponins is 1: 30) that gets it filled, injects water to 950ml, stirring and dissolving, adjust pH6.8, inject water to 1000ml, drop into 0.02% active carbon and stir 10min, filter then ultrafiltration, fine straining.Subpackage postlyophilization, aseptic sealing by fusing and get final product.Every 100g 500mI normal saline dilution before using.
Claims (6)
1. containing a pharmaceutical composition for leontice robustumDiels total alkaloids and total saponins, it is characterized in that: effective ingredient is leontice robustumDiels total alkaloids and total saponins, the mass ratio of leontice robustumDiels total alkaloids and total saponins is 1: 10～1: 100.
2. the pharmaceutical composition of a kind of leontice robustumDiels total alkaloids according to claim 1 and total saponins, is characterized in that: the mass ratio of leontice robustumDiels total alkaloids and total saponins is 1: 10～1: 40.
3. a kind of pharmaceutical composition containing leontice robustumDiels total alkaloids and total saponins according to claim 1 and 2, is characterized in that: excipient or dressing that said composition and medicine allow are prepared into pharmaceutical preparation, and dosage form is liquid preparation or solid preparation.
4. a kind of pharmaceutical composition containing leontice robustumDiels total alkaloids and total saponins according to claim 3 is characterized in that: the form of medication of described pharmaceutical preparation is oral administration or drug administration by injection.
5. the application of a kind of pharmaceutical composition containing leontice robustumDiels total alkaloids and total saponins according to claim 1 in the medicine of preparation treatment rheumatism and atrophic diseases.
6. the pharmaceutical composition of a kind of leontice robustumDiels total alkaloids according to claim 1 and total saponins, is characterized in that: said composition and other drug combination, the application in the medicine of preparation treatment rheumatism and atrophic diseases.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN106860623A (en) * | 2017-01-15 | 2017-06-20 | 匡海学 | A kind of compound leontice robustumDiels composition and its production and use |
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Non-Patent Citations (1)
| Title |
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| 李国玉: "类叶牡丹抗风湿有效部位的化学成分研究", 《中国博士学位论文全文数据库 医药卫生科技辑》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106860623A (en) * | 2017-01-15 | 2017-06-20 | 匡海学 | A kind of compound leontice robustumDiels composition and its production and use |
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Application publication date: 20140326 |