CN1935167A - Water fennel total phenolic acid preparing process, and medicinal preparation using same as active component and use - Google Patents
Water fennel total phenolic acid preparing process, and medicinal preparation using same as active component and use Download PDFInfo
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- CN1935167A CN1935167A CN 200610083810 CN200610083810A CN1935167A CN 1935167 A CN1935167 A CN 1935167A CN 200610083810 CN200610083810 CN 200610083810 CN 200610083810 A CN200610083810 A CN 200610083810A CN 1935167 A CN1935167 A CN 1935167A
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Abstract
The present invention discloses an oenanthe total phenolic acid and its contained effective component hyperin, isoquercitrin, nepalin and chlorogenic acid, etc. Said invention also provides the preparation method of oenanthe total phenolic acid. Said preparation method includes the following steps: using oenanthe as medicinal raw material, adding ethyl alcohol to make extraction, recovering ethyl alcohol to obtain alcoholic extract, dissolving by using boiling water, filtering, feeding supernatant fluid into polyamide column, using water to make elution, then using ethyl alcohol to make elution, collecting eluent, recovering ethyl alcohol, vacuum drying to obtain dried extract, using colorimetry to determine total phenolic content and using said dried extract as medicinal effective component. Its total phenolic acid content is above 50%.
Description
Technical field
The invention belongs to the separation of plant amedica effective site, purification technique field, can make the total phenolic content of Herba Oenanthes Javanicae effective site, reach national 5 class Chinese medicine crude drug standards greater than 50%; And to relate to this composition be the pharmaceutical preparation of crude drug and effect, purposes.
Background technology
Extraction and separation process commonly used is: alcohol extraction-water precipitating-ethyl acetate extraction method or acid-base method, get total phenolic acid, and these methods or loss of effective components are big or composition is destroyed, make that total phenolic acid yield is low, the cost height.Therefore need a kind of new easy, extraction separation method efficiently of research, and be applicable to suitability for industrialized production.
Summary of the invention
The object of the invention is the open method for preparing total phenolic acids of water cress; Another object of the present invention is the open pharmaceutical preparation and anti-cardiovascular (blood pressure lowering, arrhythmia) disease, cerebral ischemia and the diabetes effect that are active component with this total phenolic acid.
The present invention seeks to be achieved through the following technical solutions:
Exsiccant Herba Oenanthes Javanicae herb is ground into coarse powder, extract with hydrophilic solvent heating and refluxing extraction or merceration diafiltration that 10-30 doubly measures, heat is carried 2-3 time, each 1-3 hour, then with extracting solution in being lower than the extractum that is evaporated to proportion 1.15-1.30 (70 ℃) under 60 ℃ of conditions; Add primary dose 4-6 times hot water, the gradation dissolving, left standstill 24 hours, filter, the filtrate polyamide is the column chromatography of carrier, and water flushing and water: pure ratio is 50: 50-5: 95 mixed solvent eluting, and collect water-pure lines and take off liquid, in being lower than concentrating under reduced pressure under 60 ℃ the condition, vacuum drying gets the total phenolic acids of water cress extract.
Pharmaceutical preparation of the present invention contains the total phenolic acids of water cress of 0.5%-99.5% and the excipient of 99.5%-0.5% (medicine that comprises other adapteds), preferentially contains the total phenolic acids of water cress of 1%-60% and the pharmaceutical excipient of 99%-40% (medicine that comprises other adapteds).
Press practice of pharmacy, total phenolic acids of water cress of the present invention can be prepared into the various clinical pharmaceutical dosage form as anti-cardiovascular (blood pressure lowering, arrhythmia) disease, cerebral ischemia and diabetes effect., comprise the dosage form of oral formulations or parenterai administration.Said oral formulations is selected from any in tablet, capsule, pill, granule, suspensoid, drop pill, the oral liquid; Said parenterai administration dosage form is selected from a kind of in injection, aerosol, suppository or the subcutaneous administration dosage form.
Anti-cardiovascular of the present invention (blood pressure lowering, arrhythmia) disease, cerebral ischemia and diabetes effect.Adjuvant in the medicine is meant conventional excipient, as solvent, disintegrating agent, correctives, antiseptic, coloring agent, binding agent etc.The medicine that the bright anti-cardiovascular of this law (blood pressure lowering, arrhythmia) disease, cerebral ischemia and active other compatibilities of diabetes are used, the total phenolic acids of water cress that refers to effective dose is certain medicine material, other have allowed the Chinese medicine or the chemical drugs that share compatibility.
Accompanying drawing is a total phenolic acids of water cress extract separation-extraction technology flow chart.
Following experimental example is used to further specify the present invention, but does not limit the present invention in any way.
1, pharmacological action
1 pair of heart influence total phenolic acids of water cress under 0.15% and 0.5% concentration, can make the decreased heart rate of the Bufo siccus heart that exsomatizes, contractility weakens, output reduces, and strengthen with concentration, this effect may with the blocking-up beta receptor, relevant to the effect of antiadrenergic drug excitement.Show that in the body experiment total phenolic acids of water cress injection 0.15g/kg iv has of short duration influence to the rat electrocardiogram after 30 seconds, Ventricular Rate slows to 75% of normal cardiac rate, and this results suggest total phenolic acids of water cress mainly is an inhibitory action to whole heart.
2 hypotensive activities become 50% injection with Herba Oenanthes Javanicae total phenols processed with acid, give normal Wistar rat and the different dosage of the quiet notes of spontaneous hypertensive rat (SHR) respectively, as seen blood pressure presents the dose dependent reduction, with 1-5 after the administration minute the most obvious, and compare significant difference (p＜0.01) before the administration.Total phenolic acids of water cress also can make the normal rabbits blood pressure reduce, and by 1: 1 concentration 1ml/kg, ig, blood pressure 124 ± 10.1mmHg before by administration reduced to 76 ± 30.3mmHg (p＜0.01), descends 38.7%.
The quiet water filling celery of 3 arrhythmias total phenols acid injection 3ml/kg, respectively to acetyl benzaconine, barium chloride and calcium chloride bring out rat ventricular and carry out efficacy of medicine observing.The acetyl benzaconine experimental result shows that the total phenolic acids of water cress group significantly improves and causes VP, VT, the accumulated dose of the acetyl benzaconine of VF and HS (p＜0.01).The barium chloride experimental result, none example is changeed sinus rhythm in the normal saline control rats 45min, and total phenolic acids of water cress group and lignocaine group all transfer hole in 15min.The calcium chloride experimental result, the normal saline group all chamber of appearance is quivered, and dies in the 5min.The Herba Oenanthes Javanicae group chamber incidence rate of quivering reduces by 25%, and mortality rate reduces by 50%, and quiver in verapamil group chamber and mortality rate all reduces by 25%.Above presentation of results, total phenolic acids of water cress can obviously resist the rat ventricular that acetyl benzaconine and barium chloride cause.In addition, damage has significant protective effect to total phenolic acids of water cress to myocardial reperfusion.
4 antidiabetic effects discover that total phenolic acids of water cress can make blood glucose significantly reduce (p＜0.05) for normal mouse ig20g/kg, and the blood glucose that 10g or 20g/kg prevention administration can make alloxan cause the hyperglycemia mice obviously reduces (p＜0.05).Pancreas pathological observation, visible total phenolic acids of water cress administration group islets of langerhans degree of injury and shape size thereof are light than matched group all, show the existing hypoglycemic activity of total phenolic acids of water cress, may protect the pancreas effect in addition.The blood sugar increasing that total phenolic acids of water cress 20g/kg can not cause antiadrenergic drug is also found in experiment, and prompting has blood sugar lowering and falls the blood effect.
2, the preparation of total phenolic acids of water cress crude drug
Exsiccant Herba Oenanthes Javanicae herb is ground into coarse powder, and 70% alcohol heating reflux that adds 10 times of amounts extracted 2 hours, and totally 3 times, merge extractive liquid, is put coldly, filter, then with extracting solution in being lower than the extractum that is evaporated to proportion 1.15-1.30 (70 ℃) under 60 ℃ of conditions; Add 6 times of hot water of primary dose; the gradation dissolving; left standstill 24 hours, and filtered, filtrate being added on is equivalent to 5 times of amounts of crude drug; on the polyamide column of having handled well; water wash to effluent be faint yellow after, with 70% pure eluting, collect ethanol elution to eluent and bear till the yellow; in being lower than concentrating under reduced pressure under 60 ℃ the condition, vacuum drying gets the total phenolic acids of water cress extract.
3, the preparation of capsule
Total phenolic acids of water cress raw material 100g, medical starch 100g
Total phenolic acids of water cress and medical starch are crossed 100 mesh sieves respectively, and mix homogeneously, an amount of alcohol granulation used.In 60 ℃ of dryings, granulate incapsulates.
4, the preparation of tablet
Total phenolic acids of water cress raw material 100g, medical starch 100g
Total phenolic acids of water cress and medical starch are crossed 100 mesh sieves respectively, and mix homogeneously, an amount of alcohol granulation used.In 60 ℃ of dryings, through pelletizing machine granulate, tabletting.
5, the preparation of granule
Total phenolic acids of water cress raw material 100g, medical starch 100g, Icing Sugar 40g
Total phenolic acids of water cress, medical starch and Icing Sugar are crossed 100 mesh sieves respectively, and mix homogeneously, an amount of alcohol granulation used.In 60 ℃ of dryings, granulate, packing.
6, the preparation of injection
Total phenolic acids of water cress raw material 10g, propylene glycol 20ml, Polyethylene Glycol-400 50ml, water for injection 300ml mixes heating in water bath 30min, add benzyl alcohol 50ml, reuse water for injection adds to 1000ml, handles 10min in ultrasound wave, heats 30min again in water-bath, transfer pH value 5.5-6.5, filter clear and bright, embedding, the sterilization promptly.
Claims (9)
1, a kind of total phenolic acids of water cress crude drug is characterized in that this crude drug contains total phenolic acid 55-80%.
2, a kind of preparation method of total phenolic acids of water cress crude drug as claimed in claim 1 is characterized in that this preparation method is:
Exsiccant Herba Oenanthes Javanicae herb is ground into coarse powder, extract with hydrophilic solvent heating and refluxing extraction or merceration diafiltration that 10-30 doubly measures, heat is carried 2-3 time, each 1-3 hour, then with extracting solution in being lower than the extractum that is evaporated to proportion 1.15-1.30 (70 ℃) under 60 ℃ of conditions; Add primary dose 4-6 times hot water, the gradation dissolving, left standstill 24 hours, filter, polyamide is the column chromatography of carrier on the filtrate, and water flushing and water: pure ratio is 50: 50-5: 95 mixed solvent eluting, collect water-alcohol eluen, in being lower than concentrating under reduced pressure under 60 ℃ the condition, vacuum drying gets the total phenolic acids of water cress extract.
3, the preparation method of total phenolic acids of water cress crude drug as claimed in claim 2 is characterized in that this preparation method is:
Exsiccant Herba Oenanthes Javanicae herb is ground into coarse powder, and 70% alcohol heating reflux that adds 10 times of amounts extracted 2 hours, and totally 3 times, merge extractive liquid, is put coldly, filter, then with extracting solution in being lower than the extractum that is evaporated to proportion 1.15-1.30 (70 ℃) under 60 ℃ of conditions; Add 6 times of hot water of primary dose; the gradation dissolving; left standstill 24 hours, and filtered, filtrate being added on is equivalent to 5 times of amounts of crude drug; on the polyamide column of having handled well; water wash to effluent be faint yellow after, with 70% pure eluting, collect ethanol elution to eluent and bear till the yellow; in being lower than concentrating under reduced pressure under 60 ℃ the condition, vacuum drying gets the total phenolic acids of water cress extract.
4, a kind ofly contain the pharmaceutical preparation of crude drug according to claim 1, in order to improve its dissolubility and bioavailability, can adopt and add cosolvent such as tween 80, or adopt can be miscible with water propylene glycol, Polyethylene Glycol-400 dissolving, or methods such as employing and organic base formation salt are made water soluble preparation.
5, a kind of containing just like claim 1 and the described pharmaceutical preparation of claim 4, it is characterized in that containing the crude drug of the present invention of 0.5%-99.5% and the drug excipient of 99.5%-0.5%, the crude drug of the present invention of preferred 1%-60% and the drug excipient of 99%-40%.
6, pharmaceutical preparation as claimed in claim 5 is characterized in that said medicine is oral formulations or parenterai administration dosage form.
7, pharmaceutical preparation as claimed in claim 6 is characterized in that said oral formulations is selected from any in the middle of the tablet, pill, capsule, granule, suspensoid, drop pill, oral liquid.
8, pharmaceutical preparation as claimed in claim 7 is characterized in that described parenterai administration dosage form is selected from any in the middle of injection, aerosol, suppository or the subcutaneous administration dosage form.
9, total phenolic acids of water cress crude drug of the present invention is in preparation anti-cardiovascular (blood pressure lowering, arrhythmia) disease, cerebral ischemia and the active application of diabetes.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100838103A CN100548318C (en) | 2006-06-02 | 2006-06-02 | A kind of preparation technology of total phenolic acids of water cress and the pharmaceutical preparation and the application that are active component with this total phenolic acid |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100838103A CN100548318C (en) | 2006-06-02 | 2006-06-02 | A kind of preparation technology of total phenolic acids of water cress and the pharmaceutical preparation and the application that are active component with this total phenolic acid |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1935167A true CN1935167A (en) | 2007-03-28 |
| CN100548318C CN100548318C (en) | 2009-10-14 |
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| CNB2006100838103A Active CN100548318C (en) | 2006-06-02 | 2006-06-02 | A kind of preparation technology of total phenolic acids of water cress and the pharmaceutical preparation and the application that are active component with this total phenolic acid |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108186700A (en) * | 2018-03-22 | 2018-06-22 | 黄正明 | A kind of purposes that anti-hiv drug preparation is used to prepare using total phenolic acids of water cress as bulk pharmaceutical chemicals |
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2006
- 2006-06-02 CN CNB2006100838103A patent/CN100548318C/en active Active
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108186700A (en) * | 2018-03-22 | 2018-06-22 | 黄正明 | A kind of purposes that anti-hiv drug preparation is used to prepare using total phenolic acids of water cress as bulk pharmaceutical chemicals |
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| Publication number | Publication date |
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| CN100548318C (en) | 2009-10-14 |
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