CN1475490A - Valerian extract and its preparation method and use - Google Patents
Valerian extract and its preparation method and use Download PDFInfo
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- CN1475490A CN1475490A CNA031499260A CN03149926A CN1475490A CN 1475490 A CN1475490 A CN 1475490A CN A031499260 A CNA031499260 A CN A031499260A CN 03149926 A CN03149926 A CN 03149926A CN 1475490 A CN1475490 A CN 1475490A
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Abstract
A valerian extract with calming and anti-spasm activity, its medicines for treating the spasm of cardiac blood vessel, respiratory tract and enterogastric tract and increasing the acidity of gall, and its preparing process are disclosed. Said extract contains valerian oil and valerianine (10-90%).
Description
Technical field
The present invention relates to a kind of calm pharmaceutical preparation that ends the active Rhizoma et radix valerianae extract of convulsion and contain this extract that has, also comprise this preparation method of extract and medical treatment or health caring use.
Background technology
Valerian is a Valerianaceae valeriana per nnial herb, mainly contain compositions such as monoterpenes (iridoid), sesquiterpenoids, alkaloids, lignanoids, flavonoid, it is a kind of tranquilizer of gentleness, effect with good improvement sleep, its function also comprise safely keeping tensions down, anxiety, be overexcited and be used as bring high blood pressure down, spasmolytic and neuroleprics.Among the peoplely in Europe drink valerian and simmer tea and being used to help to fall asleep the history of existing at least centuries.
Because people observe the drug dependence and the habituation of coming out to some synthetic drugs at present commonly used as 2,3 benzodiazines (benzodiazepines) in clinical, show the worry that more and more weighs.As the selection of plant amedica treatment (phytotherapy), gentle tranquilizer valerian has just been stood increasing pharmacologically active and clinical trial under this trend, and the valerian valerian is very popular as the calming soporific medicine in western countries in recent years.But the preparation that the valerian extract that yet there are no use technology extraction of the present invention is made.
The patent retrieval situation relevant with the present invention is as follows: Chinese patent CN1396166A novel method for preparing general valerianin, introduced method with the Petroleum ether extraction general valerianin, and this extracting method has lost the activeconstituents valerian naphtha.The preparation method of a Chinese patent CN1337255A Rhizoma et radix valerianae extract only adopts the method for traditional ethanol percolation, and impurity is many in the extract.The medicinal use of Chinese patent CN1370586A north valerian extractive with organic solvent has been introduced methanol extract and as the purposes of calming soporific class medicine.The method that adopts supercritical extraction and organic solvent extraction to combine is extracted the method for activeconstituents valerian naphtha and valerianin and is still initiated.Clear and definite by the valerian extract activeconstituents that the present invention obtains, the purity height, taking dose is little, and pharmacological action is remarkable, is expected to be developed to the calm convulsion of ending, and eliminates the specific medicament of calculus in the courage.
Summary of the invention
The present invention relates to a kind of have calm end the active valerian extract of convulsion and contain the preparation that this extract is made, also comprise this preparation method of extract.This extract is mainly become to be grouped into general valerianin etc. by valerian naphtha, and wherein general valerianin (valtrate) (in valeric acid) content is 10-90%.Its preparation method is through CO
2Technology such as supercritical extraction and organic solvent extraction is refining to form.
Concrete extracting method is as follows:
1, valerian is ground into meal, crosses 20 mesh sieves, place extraction kettle to extract, extracting pressure is 7.0-45Mpa, again through heat exchanger heats to extraction temperature 32-80 ℃, extraction time 2-8h is dissolved with the supercritical CO of extract
2Enter through reducing valve and to resolve separation in the separating still, resolve pressure 4.0-7.0Mpa, resolution temperature 20-80 ℃, resolve time 2-8h, valerian naphtha.
2, the alcohol solution dipping 4-12h of the 50-95% that doubly measures with 4-10 of the dregs of a decoction after will extracting, add ethanol percolation, detect when not having valerianin in the percolate (detecting) with high performance liquid chromatography, collect percolate, decompression recycling ethanol concentrates percolate 1-4 times to medicinal material weight, concentrated solution adds isopyknic organic solvent extraction, extract 2-5 time, combining extraction liquid, reclaim under reduced pressure gets the valerianin extract.
The preparation that contains the Rhizoma et radix valerianae extract of being made by above-mentioned preparation method comprises with this Rhizoma et radix valerianae extract being the single preparations of ephedrine of activeconstituents, also comprises the pharmaceutical composition that contains the said extracted thing.Its preparation type comprises: tablet, slow releasing tablet, capsule, slow releasing capsule, soft capsule, pellet, aqueous injection, powder injection, infusion solution and fat milk injection.Various formulations are to make with ordinary method, and wherein the Rhizoma et radix valerianae extract existence is a solid state or liquid, and administering mode is oral, intravenously or intramuscular injection.Its purposes can be as medicine, also can be used as the food with nourishing function.
Wherein extracting the solution that valerian uses is ethanol or methanol solution, and its PH scope is 3-9.The solvent that the extraction crude extract is used is a kind of or any two kinds combination in propyl carbinol, hexanaphthene, sherwood oil, ethyl acetate, methylene dichloride and the primary isoamyl alcohol equal solvent.
The plant that wherein is used for extracting Rhizoma et radix valerianae extract is a valerian, is meant all plants that contain valerian naphtha and valerianin.
With following embodiment and test example foregoing invention is described better.
Embodiment 1
Get valerian valerian 500g and be ground into meal, cross 20 mesh sieves, place extraction kettle to extract, extracting pressure is 25Mpa, again through heat exchanger heats to 50 ℃ of extraction temperature, extraction time 6h, the supercritical CO 2 that is dissolved with extract enters through reducing valve resolves separation in the separating still, resolve pressure 7.0Mpa, 30 ℃ of resolution temperatures, parsing time 4h gets valerian naphtha 20ml.
With 85% the alcohol solution dipping immersion 6h of the dregs of a decoction after the extraction with 8 times of amounts, add ethanol percolation, detect when not having valerianin in the percolate with high performance liquid chromatography, collect percolate, decompression recycling ethanol concentrates percolate 2 times to medicinal material weight, add isopyknic organic solvent extraction, extract 2-5 time, combining extraction liquid, decompression and solvent recovery get general valerianin extract 12g.
Embodiment 2
Preparation contains the solid preparation of Rhizoma et radix valerianae extract.
Its preparation method is that Rhizoma et radix valerianae extract and pharmaceutical excipient are comprised that vehicle, weighting agent, disintegrating agent, Drug coating, sustained release dosage, solubility promoter, dispersion agent, sanitas etc. mix, granulate, adopt conventional pharmaceutical technology to make tablet, capsule, soft capsule, slow releasing tablet, slow releasing capsule, pellet etc.
Embodiment 3
Preparation Rhizoma et radix valerianae extract aqueous injection, powder injection, infusion solution and fat milk injection.
(1) preparation figured silk fabrics leather extract aqueous injection, with Rhizoma et radix valerianae extract 30g, adding 1L contains the injection liquid aqueous solution of tween 80, and regulator solution PH to 5.0-7.0 is after the millipore filtration ultrafiltration, add the injection water and add to specified amount, be sub-packed in the ampoule every 2ml, sealing by fusing, after the assay was approved, packing promptly.
(2) preparation Rhizoma et radix valerianae extract infusion solution, with Rhizoma et radix valerianae extract 10g, adding 1L contains the injection liquid aqueous solution of tween 80, regulator solution PH to 5.0-7.0 after the millipore filtration ultrafiltration, adds the injection water and adds to specified amount, be sub-packed in 100ml, 150ml, the corresponding infusion bottle of 200ml, roll lid, after the assay was approved, packing promptly.
(3) preparation Rhizoma et radix valerianae extract powder injection after the water for injection dissolving of Rhizoma et radix valerianae extract with 10 times of amounts, after the injection liquid of adding metering fully dissolves with water-soluble pharmaceutical excipient, is transferred PH to 5.0, ultrafiltration, vacuum-drying, aseptic subpackaged in the 5ml cillin bottle, roll lid, after the assay was approved, packing promptly.
(4) preparation Rhizoma et radix valerianae extract lyophilized injectable powder, with Rhizoma et radix valerianae extract 30g, adding 500ml contains the injection liquid aqueous solution of tween 80, and regulator solution PH to 5.0-7.0 is after the millipore filtration ultrafiltration, add the injection water and add to specified amount, be sub-packed in the ampoule lyophilize, sealing by fusing, after the assay was approved, packing promptly.
Test example 1: the sedative-hypnotic property of Rhizoma et radix valerianae extract
1, kunming mice is 60, body weight 22 ± 2g (S), and with the Rhizoma et radix valerianae extract gastric infusion for preparing among the embodiment, every group is irritated gastric capacity is 20mg/kg.The 0.9%NaCI solution of the same dosage of control group is irritated stomach, respectively the record active situation of irritating before and after the stomach at once, regularly observing mouse in 15,30,45,60,90 minutes.Adopt open field method, at an about 100m
2Open space, evenly divide 19 lattice, observe the lattice number that mouse creeps in 3 minutes.
Table 1 Rhizoma et radix valerianae extract influences the mouse active
Movable number of times
After the medication of group number of animals (minute)
Before the medication
At once 15 30 45 60 90
0.9％NaCI 30 73.35±5.90 30.00±4.61 35.78±3.78 35.25±4.89 29.67±6.34 28.45±6.80 23±3.90
Rhizoma et radix valerianae extract 30 74.78 ± 3.56 18.67 ± 3.98 13.70 ± 1.80 10.60 ± 1.84 7.89 ± 3.80 8.70 ± 3.65 10.60 ± 8.00
The result shows: administration group and control group have significant difference (P＜0.01).
Test example 2: Rhizoma et radix valerianae extract is eliminated the effect of cholelithiasis
1, animal model is set up and the technology path: experimental rabbit is with 3% vetanarcol 30mg/kg intravenous anesthesia, and the abdominal cavity is opened in strict aseptic technique, cuts gall-bladder after taking out most bile, implants disinfectant calculosis, the purse string suture gall-bladder.Perform the operation after 1 week, get 16 good rabbit of recovery and be divided into 2 groups at random.Experimental group is irritated and is raised Rhizoma et radix valerianae extract 30mg/kg, every day 1 time; Control group irritate raise etc. appearance, etc. ooze aquae destillata solution, every day 1 time.After 56 days, the ear vein blood sampling is equipped with inspection.Cut the abdominal cavity, expose gall-bladder and common bile duct, put to death then, calculus in the taking-up gall-bladder rinses and 60 ℃ of oven dry are weighed.
2, statistical method: measurement data represents that with x ± s statistical inference is checked with t check and x2.
Table 2 gall-bladder is implanted into calculus and changes (x ± s)
Group n weight (mg) calculus is counted the on average amount of alleviating (mg) of niter rate calculus
Control group experiment preceding 8 38.80 ± 2.38 8
Experiment back 35.61 ± 5.15 8 0% 2.20 ± 5.69
Experimental group experiment preceding 8 38.80 ± 2.38 8
Experiment back 10.13 ± 4.52 2 75% 29.58 ± 2.82
The result shows: administration group and control group have significant difference (P＜0.01).
Conclusion: experimental group calculus disappearance rate is 75%.Control group calculus disappearance rate is 0%, two group relatively utmost point significant difference (P＜0.01).The experimental group calculus on average amount of alleviating has utmost point significant difference (P＜0.01) obviously greater than control group between group.
Claims (8)
1, the present invention relates to a kind of calm active valerian extract of convulsion and preparation of making of extract thus thereof of ending that have, also comprise this preparation method of extract and medical application.It is characterized in that this extract is mainly become to be grouped into general valerianin etc. by valerian naphtha, wherein general valerianin content is 10-90%.
2, according to the valerian method for preparing extractive in the claim 1, it is characterized in that: form through technologies such as CO2 supercritical extraction and organic solvent extraction are refining.
3, according to the preparation method in the claim 2.It is characterized in that:
(1) with any meal that is ground in the valerian, cross 20 mesh sieves, place extraction kettle to extract, extracting pressure is 7.0-45Mpa, again through heat exchanger heats to extraction temperature 32-80 ℃, extraction time 2-8h is dissolved with the supercritical CO of extract
2Enter through reducing valve and to resolve separation in the separating still, resolve pressure 4.0-7.0Mpa, resolution temperature 20-80 ℃, resolve time 2-8h, valerian naphtha.
(2) the alcohol solution dipping 4-12h of the 50-95% that doubly measures with 4-10 of the dregs of a decoction after will extracting, adding ethanol percolation does not have valerianin to end to detecting in the percolate, collect percolate, decompression recycling ethanol, concentrate percolate 1-4 times to medicinal material weight, concentrated solution adds isopyknic organic solvent extraction, extracts 2-5 time, combining extraction liquid, reclaim under reduced pressure get the valerianin extract.
4, the preparation type that contains this Rhizoma et radix valerianae extract according to claim 1 comprises tablet, slow releasing tablet, capsule, slow releasing capsule, soft capsule and pellet etc., and its formulation can also be injection, powder injection, infusion solution and fat milk injection.Various formulations are to make with ordinary method, and wherein the Rhizoma et radix valerianae extract existence is a solid state or liquid, and administering mode is oral, intravenously or intramuscular injection.
5,,, also comprise the pharmaceutical composition that contains the said extracted thing comprising being the single preparations of ephedrine of activeconstituents with this Rhizoma et radix valerianae extract according to the preparation in the claim 1.
6, the solution of using according to extraction valerian in the claim 2 is ethanol or methanol solution, and its PH scope is 3-9.The solvent that the extraction crude extract is used is one or both in propyl carbinol, hexanaphthene, sherwood oil, ethyl acetate, methylene dichloride and the primary isoamyl alcohol equal solvent.
7, according to the preparation in the claim 4, can be used as medicine, also can be used as food with nourishing function.
8,, be meant all plants that contain valerian naphtha and valerianin according to the valerian in the claim 1.
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| Application Number | Priority Date | Filing Date | Title |
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| CNA031499260A CN1475490A (en) | 2003-07-31 | 2003-07-31 | Valerian extract and its preparation method and use |
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| CNA031499260A CN1475490A (en) | 2003-07-31 | 2003-07-31 | Valerian extract and its preparation method and use |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1321649C (en) * | 2005-06-09 | 2007-06-20 | 武汉联绎生物科技有限公司 | Composition for treating female algomenorrhea and its preparing method |
| CN101396381B (en) * | 2007-09-29 | 2011-09-07 | 北京北大维信生物科技有限公司 | Valerian extract and preparation method and use thereof |
| CN102526135A (en) * | 2011-11-23 | 2012-07-04 | 武汉联合药业有限责任公司 | Valerian preparation and preparation method thereof |
| CN105112296A (en) * | 2015-07-29 | 2015-12-02 | 中南林业科技大学 | Rhizoctonia oryzae-sativae bacterial strain and its application in preparing Valerenic acid and sedative hypnotic Chinese patent medicine |
| CN112889912A (en) * | 2021-03-11 | 2021-06-04 | 西南大学 | Application of valeric acid in storage and preservation of fruits and vegetables and method for delaying senescence in postharvest treatment of fruits |
-
2003
- 2003-07-31 CN CNA031499260A patent/CN1475490A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1321649C (en) * | 2005-06-09 | 2007-06-20 | 武汉联绎生物科技有限公司 | Composition for treating female algomenorrhea and its preparing method |
| CN101396381B (en) * | 2007-09-29 | 2011-09-07 | 北京北大维信生物科技有限公司 | Valerian extract and preparation method and use thereof |
| CN102526135A (en) * | 2011-11-23 | 2012-07-04 | 武汉联合药业有限责任公司 | Valerian preparation and preparation method thereof |
| CN105112296A (en) * | 2015-07-29 | 2015-12-02 | 中南林业科技大学 | Rhizoctonia oryzae-sativae bacterial strain and its application in preparing Valerenic acid and sedative hypnotic Chinese patent medicine |
| CN105112296B (en) * | 2015-07-29 | 2018-07-06 | 中南林业科技大学 | One plant of angle load bacteria strain and its application in valepotriate, calming soporific class Chinese patent drug is prepared |
| CN112889912A (en) * | 2021-03-11 | 2021-06-04 | 西南大学 | Application of valeric acid in storage and preservation of fruits and vegetables and method for delaying senescence in postharvest treatment of fruits |
| CN112889912B (en) * | 2021-03-11 | 2022-07-12 | 西南大学 | Application of valeric acid in storage and preservation of fruits and vegetables and method for delaying senescence in postharvest treatment of fruits |
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