CN1428170A - Effective component of safflower, its powder injection, preparation method and medicinal application - Google Patents
Effective component of safflower, its powder injection, preparation method and medicinal application Download PDFInfo
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- CN1428170A CN1428170A CN 02144806 CN02144806A CN1428170A CN 1428170 A CN1428170 A CN 1428170A CN 02144806 CN02144806 CN 02144806 CN 02144806 A CN02144806 A CN 02144806A CN 1428170 A CN1428170 A CN 1428170A
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Abstract
The present invention relates to a Chinese medicine preparation, in particular, it is medicine for resisting cardiovascular and cerebrovascular diseases-carthamus flower effective component, its powder injection, preparation method and medicine application. Its effective component is the extract of carthamus flower which is obtained by adopting the processes of water extraction, alcohol precipitation and polyamide resin extraction, and its effective component carthamus flower HB is greater than or equal to 90%. The carthamus flower HB power injection is made by using carthamus flower HB and pharmaceutically acceplable auxiliary material as supporting agent. Its preparation method includes the following steps: dissolving carthamus flower HB in water or alcoholic water, adding auxiliary material, completely dissolving them, using active carbon or ultrafiltration to remove heat source, filling,
Description
Technical field: the present invention relates to a kind of Chinese medicine preparation, promptly as medicine---safflower effective part and its injectable powder and the preparation method and the medical usage of resisting cardiovascular disease.
Background technology: in prior art, Flos Carthami injection has been a common drug at home clinically, has the anti-cardiovascular disease effect, and its shortcoming is that effective component content is low, and preparation stability is poor.
Summary of the invention: the objective of the invention is provides a kind of effective component content height, quantitatively accurate, stay-in-grade safflower effective part and its injectable powder and preparation method and medical usage at above-mentioned deficiency.
Technical solution of the present invention is: safflower effective part is that flos carthami is precipitated through water extraction alcohol, extracts and get the effective ingredient carthamus flower HB power more than or equal to the extract more than 90 percent through polyamide again.
The preferred for preparation method of safflower effective part is to get the water that flos carthami adds 5-20 times of medical material weight, in 50-80 ℃ of heating extraction 1-4 time, and each 0.5-2.0 hour, filter, merge each extracting solution, be cooled to room temperature; Extracting solution concentrates or omits, alcohol precipitation or omission, remove alcohol, row polyamide column chromatography or anion exchange resin or macroporous resin behind the water dissolution, use less than 10% ethanol or the water elution removal of impurity, continuing goes out effective ingredient with ethanol or the ethanol elution higher than eluting impurity concentration, adds tranquilizer, decompression and solvent recovery, the row silica gel column chromatography, with organic solvent (acid that can add 0.01%-20%) gradient elution, collect the carthamus flower HB power part, reclaim solvent, the organic solvent recrystallization, that is, yield is no less than 1.0%, and carthamus flower HB power content is greater than 90%; Wherein used alcohol can also be methanol, propanol, butanols, ethylene glycol, carbochain less than 32 alkanols, carbochain less than 32 rare alcohol and phenol etc.; Wherein the big pore resin comprises various nonpolar, low poles, Semi-polarity, polar homemade or advance macroporous adsorbent resin.The used organic solvent of silica gel chromatography comprises methanol, ethanol, propanol, butanols, chloroform, ethyl acetate, acetone, dichloromethane, monochloro methane, cyclohexane extraction, petroleum ether etc., or their mixture.Used acid can be mineral acid or organic acid, as: formic acid, acetic acid, ethanedioic acid, tartaric acid, hydrochloric acid, sulphuric acid, phosphoric acid, dibasic alkaliine, dihydric phosphate, carbonic acid, nitric acid etc., or their mixture.
It is prepared from the carthamus flower HB power injectable powder by carthamus flower HB power and pharmaceutically acceptable adjuvant.
The preparation method of carthamus flower HB power injectable powder is in the pure water of carthamus flower HB power is water-soluble or arbitrary proportion, add adjuvant (mannose, dextran, various high polymer adjuvants etc.) as proppant, fully after the dissolving, active carbon or ultrafiltration desuperheating source, packing, lyophilization or spray drying, sealing, promptly.
Add the tranquilizer that prevents that the safflower effective ingredients decomposition from changing in preparation method and the preparation, the addition of tranquilizer is the 0.01%-95% of preparation total amount; Tranquilizer comprises that various water miscible antioxidants and fat-soluble antioxidant and mixing thereof use; Water miscible antioxidant such as Vc, sodium sulfite, pyrosulfite, sodium sulfite, sodium thiosulfate, formaldehyde close sodium sulfite, cysteine, methionine, thiourea, thiacetic acid., thioglycerol etc.; Fat-soluble antioxidant such as butylated hydroxyarisol (BHA), PG (PG), two fourth cresols (BHT), lecithin, tocopherol (Ve) etc.
Safflower effective part, carthamus flower HB power injectable powder are used for the treatment of and prevent cardiac and cerebral vascular diseases.
Usage and dosage: consumption every day 1-3 time, at every turn in carthamus flower HB power 1-500mg, intravenous injection or instillation.
Carthamus flower HB power freeze-dried powder pharmacodynamic study shows: 1, the influence that mice is closed trachea electrocardio extinction time of carthamus flower HB power freeze-dried powder studies show that, the carthamus flower HB power freeze-dried powder is the same with Flos Carthami injection to have obvious prolongation and close trachea mouse core electrograph extinction time.2, the carthamus flower HB power freeze-dried powder studies show that the effect of the rabbit ear blood vessel that exsomatizes, the carthamus flower HB power freeze-dried powder has the effect of more intense expansion rabbit ear blood vessel, each time point after the administration is compared with normal discharge before the administration, the effect of the increase rabbit ear vascular flow that equal tool is apparent in view.3, the carthamus flower HB power freeze-dried powder causes that to pituitrin the protective effect of rat heart muscle ischemia ECG studies show that; the carthamus flower HB power freeze-dried powder has the electrocardio that rat heart muscle ischemia place electrocardiogram that tangible antagonism causes by pituitrin shows to be changed; can significantly correct the rising of T ripple and low flat, the rising of ST section.4, the carthamus flower HB power freeze-dried powder studies show that the influence of rabbit thrombus in vivo, and the carthamus flower HB power freeze-dried powder has the formation that makes the effect that the rabbit thrombus in vivo reduces and suppress thrombus in vivo.
In a word, the carthamus flower HB power freeze-dried powder can improve the supply of ischemic myocardium oxygen and blood, can significantly improve the little mousetrap die electrograph extinction time of holding one's breath, and can resist the myocardial ischemia that is caused by pituitrin.But the carthamus flower HB power freeze-dried powder also anticoagulant and rabbit thrombus in vivo formation, improve blood stasis animal blood rheology index.It is the good medicine of a treatment myocardial ischemia that the carthamus flower HB power freeze-dried powder does not lose.
Advantage of the present invention is: 1, adopt injectable powder to replace traditional aqueous injection, steady quality, taking convenience, be convenient to storage and transportation.2, adopt of the active ingredient of the Flos Carthami extract of carthamus flower HB power content more than 90 percent as injectable powder, the purity height, composition is clear, and drug effect is remarkable.3, on extracting, the advanced technologies that adopts polyamide to extract at a high speed, efficient, pollution-free, has guaranteed that to greatest extent the Flos Carthami active ingredient separates out the yield height.4, the effect that has very strong treatment and prevention cardiovascular and cerebrovascular disease.
Below in conjunction with embodiment the present invention is described in further detail:
The specific embodiment: embodiment 1: the preparation of safflower effective ingredients
Get flos carthami and be ground into coarse powder, add the water of 10 times of medical material weight, in 80 ℃ of extracting in waters 3 times, each 1.0 hours, filter, merge 3 times extracting solution, be cooled to room temperature.Row macroporous resin HPD100 adsorpting column chromatogram eliminates with 5% ethanol elution to impurity, continues and cleans with 20% ethanol elution to effective ingredient, 20% ethanol elution part adds tranquilizer, decompression and solvent recovery, the type silica gel column chromatography, be eluted to impurity with chloroform-methanol-formic acid (20: 1: 0.1) and eliminate, continuing is eluted to effective ingredient with chloroform-methanol-formic acid (20: 5: 0.1) and cleans, and reclaims solvent, ethyl alcohol recrystallization, that is, yield is no less than 1.0%, and carthamus flower HB power content is greater than 90%.
Embodiment 2: the carthamus flower HB power lyophilized injectable powder
Get safflower effective ingredients 20g, Vc 0.5g, mannose 100g, make 1000 by aforementioned technology.
Claims (6)
1, a kind of safflower effective part is characterized in that flos carthami is precipitated through water extraction alcohol, extracts and get the effective ingredient carthamus flower HB power more than or equal to the extract more than 90 percent through polyamide again.
2, a kind of preferred for preparation method for preparing the described safflower effective part of claim 1 is characterized in that getting the water that flos carthami adds 5-20 times of medical material weight, in 50-80 ℃ of heating extraction 1-4 time, each 0.5-2.0 hour, filter, merge each extracting solution, be cooled to room temperature; Extracting solution concentrates or omits, and alcohol is removed in alcohol precipitation or omission, row polyamide column chromatography or anion exchange resin or macroporous resin are used less than 10% ethanol or the water elution removal of impurity behind the water dissolution, and continuing goes out effective ingredient with ethanol or the ethanol elution higher than eluting impurity concentration, add tranquilizer, decompression and solvent recovery, row silica gel column chromatography, with the organic solvent gradient elution, collect the carthamus flower HB power part, reclaim solvent, the organic solvent recrystallization, that is, yield is no less than 1.0%, and carthamus flower HB power content is greater than 90%; Wherein used alcohol can also be methanol, propanol, butanols, ethylene glycol, carbochain less than 32 alkanols, carbochain less than 32 rare alcohol and phenol etc.; Wherein the big pore resin comprises various nonpolar, low poles, Semi-polarity, polar homemade or advance macroporous adsorbent resin; The used organic solvent of silica gel chromatography comprises methanol, ethanol, propanol, butanols, chloroform, ethyl acetate, acetone, dichloromethane, monochloro methane, cyclohexane extraction, petroleum ether etc., or their mixture; Used acid can be mineral acid or organic acid, as: formic acid, acetic acid, ethanedioic acid, tartaric acid, hydrochloric acid, sulphuric acid, phosphoric acid, dibasic alkaliine, dihydric phosphate, carbonic acid, nitric acid etc., or their mixture.
3, the carthamus flower HB power injectable powder that contains the described safflower effective part of claim 1 is characterized in that it is prepared from by carthamus flower HB power and pharmaceutically acceptable adjuvant.
4, a kind of preparation method for preparing the described carthamus flower HB power injectable powder of claim 3, it is characterized in that in the pure water of carthamus flower HB power is water-soluble or arbitrary proportion, add adjuvant as proppant, fully after the dissolving, active carbon or ultrafiltration desuperheating source, packing, lyophilization or spray drying, sealing, promptly.
5, according to described safflower effective part of claim 1 to 4 and preparation method, it is characterized in that in preparation method and preparation, adding the tranquilizer that prevents that the safflower effective ingredients decomposition from changing, the addition of tranquilizer is the 0.01%-95% of preparation total amount; Tranquilizer comprises that various water miscible antioxidants and fat-soluble antioxidant and mixing thereof use; Water miscible antioxidant such as Vc, sodium sulfite, pyrosulfite, sodium sulfite, sodium thiosulfate, formaldehyde close sodium sulfite, cysteine, methionine, thiourea, thiacetic acid., thioglycerol etc.; Fat-soluble antioxidant such as butylated hydroxyarisol (BHA), PG (PG), two fourth cresols (BHT), lecithin, tocopherol (Ve) etc.
6, safflower effective part, carthamus flower HB power injectable powder are used for the treatment of and prevent cardiac and cerebral vascular diseases.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 02144806 CN1428170A (en) | 2002-11-10 | 2002-11-10 | Effective component of safflower, its powder injection, preparation method and medicinal application |
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| CN 02144806 CN1428170A (en) | 2002-11-10 | 2002-11-10 | Effective component of safflower, its powder injection, preparation method and medicinal application |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102119984A (en) * | 2011-03-13 | 2011-07-13 | 浙江大学 | Preparation method and application of carthamus tinctorius L. active ingredient containing hydroxysafflor yellow A |
| CN102119948A (en) * | 2011-03-13 | 2011-07-13 | 浙江大学 | Carthamus tinctorius L. active ingredient with myocardial protection function and preparation method and application |
| CN102119947A (en) * | 2011-03-13 | 2011-07-13 | 浙江大学 | Preparation method and application of carthamus tinctorius L. active ingredient |
| CN104288201A (en) * | 2014-10-30 | 2015-01-21 | 王江泉 | Safflower soft capsule and preparation method thereof |
| CN113514595A (en) * | 2021-04-27 | 2021-10-19 | 云南省农业科学院经济作物研究所 | Rapid detection method for semi-quantitatively determining hydroxysafflor yellow A |
-
2002
- 2002-11-10 CN CN 02144806 patent/CN1428170A/en active Pending
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102119984A (en) * | 2011-03-13 | 2011-07-13 | 浙江大学 | Preparation method and application of carthamus tinctorius L. active ingredient containing hydroxysafflor yellow A |
| CN102119948A (en) * | 2011-03-13 | 2011-07-13 | 浙江大学 | Carthamus tinctorius L. active ingredient with myocardial protection function and preparation method and application |
| CN102119947A (en) * | 2011-03-13 | 2011-07-13 | 浙江大学 | Preparation method and application of carthamus tinctorius L. active ingredient |
| CN102119948B (en) * | 2011-03-13 | 2012-11-21 | 浙江大学 | Carthamus tinctorius L. active ingredient with myocardial protection function and preparation method and application |
| CN102119947B (en) * | 2011-03-13 | 2012-11-21 | 浙江大学 | Preparation method and application of carthamus tinctorius L. active ingredient |
| CN102119984B (en) * | 2011-03-13 | 2013-03-13 | 浙江大学 | Preparation method and application of carthamus tinctorius L. active ingredient containing hydroxysafflor yellow A |
| CN104288201A (en) * | 2014-10-30 | 2015-01-21 | 王江泉 | Safflower soft capsule and preparation method thereof |
| CN113514595A (en) * | 2021-04-27 | 2021-10-19 | 云南省农业科学院经济作物研究所 | Rapid detection method for semi-quantitatively determining hydroxysafflor yellow A |
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