CN101849918A - Vitexin-2''-O-rhamnoside pill and preparation method - Google Patents
Vitexin-2''-O-rhamnoside pill and preparation method Download PDFInfo
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- CN101849918A CN101849918A CN 201010184455 CN201010184455A CN101849918A CN 101849918 A CN101849918 A CN 101849918A CN 201010184455 CN201010184455 CN 201010184455 CN 201010184455 A CN201010184455 A CN 201010184455A CN 101849918 A CN101849918 A CN 101849918A
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Abstract
The invention provides a preparation method of vitexin-2''-O-rhamnoside pills, which comprises the following steps: heating hawthorn leaf activated monomer component vitexin-2''-O-rhamnoside and matrix, fusing and stirring evenly; and pouring into a condenser at a certain speed and shrinking the solid solution to prepare into the vitexin-2''-O-rhamnoside pills. The vitexin-2''-O-rhamnoside pills prepared by the invention can be solely or jointly applied to treatment of chest obstruction and heart ache with high efficacy.
Description
Technical field
The present invention relates to the vitexin-2 ''-O-rhamnoside drop pill, particularly relating to Folium Crataegi active monomer component vitexin-2 ''-O-rhamnoside is ingredient, with Polyethylene Glycol, sodium stearate or its mixture is substrate, with liquid paraffin, dimethicone or vegetable oil is condensing agent, the drop pill and the preparation method of treatment obstruction of qi in the chest and cardialgia.
Background technology
Show according to the health ministry statistics: in recent years, population of China cardiovascular death number has accounted for more than 1/3rd of total death toll, classifies the first place of the city and the rural population ten big causes of death as
[1]Cardiovascular disease incidence rate, disability rate and mortality rate just are being ascendant trend year by year, and in view of the hazardness of cardiovascular disease, World Health Organization (WHO) has classified it as one of current full scope of organization overall work emphasis
[2]The chronic disease that with the cardiovascular disease is representative has become the major issue of serious threat human health, and becomes the main cause of medical expense excessive increase
[3]Therefore treat this type of disease new drug and demand exploitation urgently.
Folium Crataegi is the dried leaves of rosaceous plant Fructus Pyri Pashiae (Crataegus pinnatifida Bge.var major), Fructus Crataegi (C.pinnatifida Bge.), records in Chinese Pharmacopoeia.The sweet acid of Folium Crataegi, warm in nature, go into the conscience taste, can blood stasis dispelling regulate the flow of vital energy, restore menstrual flow and invigorate blood circulation strengthening the spleen to promote digestion, dispersing the stagnated live-QI to relieve the stagnation of QI, free from worry chest and diaphragm.Modern study thinks that it has expanding cardiovascular, sends the supply of blood oxygen, and the blood fat reducing level is regulated lipid metabolism, reduces peripheral vascular resistance, the effect of microcirculation improvement
[4]At present, utilize the preparation of the Folium Crataegi extract exploitation kinds such as capsule, Yixintong sheet and injection, Ao Shaen injection of feeling at ease.But be developed to new drug with its active monomer component and still do not have further investigation.
Summary of the invention
Purpose of the present invention, providing a kind of is the Sublingual drop pill of the treatment obstruction of qi in the chest and cardialgia of feedstock production with the monomeric compound vitexin-2 ''-O-rhamnoside that extracts in the Folium Crataegi.
Another object of the present invention provides a kind of preparation method of vitexin-2 ''-O-rhamnoside drop pill.
The object of the present invention is achieved like this:
The vitexin-2 ''-O-rhamnoside drop pill is characterized in that with the vitexin-2 ''-O-rhamnoside being that medicine material is prepared into, and every drop pill contains vitexin-2 ''-O-rhamnoside 5-25mg, is the Sublingual dropping pill formulation of treatment obstruction of qi in the chest and cardialgia.
Medicine material in the vitexin-2 ''-O-rhamnoside drop pill is the monomeric compound that extraction separation obtains from Folium Crataegi.
The preparation method of vitexin-2 ''-O-rhamnoside drop pill, be that vitexin-2 ''-O-rhamnoside is added in the middle of the molten matrix, constantly stir, make uniform fusion medicinal liquid, the fusion medicinal liquid that makes is transferred in the reservoir, regulate drop pill machine temperature control system, make the drop pill temperature remain on 70 ℃～95 ℃, fused material splashes in the condensing agent with suitable speed by the dropping-pill machine head, with 50 ℃～-15 ℃ condensing agent coolings, drop pill with drop pill machine exit takes out again, remove the surface condensation agent, drying, promptly;
Described substrate is Polyethylene Glycol or stearic acid sodium, and the weight proportion of vitexin-2 ''-O-rhamnoside and substrate is 1: 0.5-10;
Described condensing agent is liquid paraffin, dimethicone or vegetable oil.
Described Polyethylene Glycol is one or more mixture in cetomacrogol 1000, polyethylene glycol 1500, Macrogol 4000, the polyethylene glycol 6000.
(" be main active in the Folium Crataegi O-rhamnoside), content reaches more than 2% vitexin-2 above-mentioned vitexin-2 ''-O-rhamnoside, and its water solublity is strong, and pharmacologically active is strong, and acellular poison is fit to be developed to new drug.
The cultured cell in vitro result of study shows that vitexin-2 ''-O-rhamnoside influences transmembrane potential and calcium ion concentration stabilizing cell membrane by regulating cell membrane calcium ion gated channel; Enzyme such as LDH is produced and expose minimizing; Regulate obviously protecting myocardial cell anoxia oxygen supply damages again of aspect such as myocardial cell activity material output and activity; protection ischemical reperfusion injury myocardial cell; and can in physiological range, reduce the myocardial cell frequency of beating; this chemical compound can make endotheliocyte vascular relaxing factor NO output obviously increase in addition, and the blood vessel factor that contracts ET-1mRNA expresses and ET-1 obviously reduces.Other discovers
[11]Vitexin rhamnoside has concentration dependent diastole effect to the arterial ring that exsomatizes, and this effect produces by the mode of endothelium-dependent relaxation and the non-dependence of endothelium, and has the pharmacological action characteristics of part calcium antagonist.Therefore, find that vitexin rhamnoside has the new pharmacological action of direct expansion artery blood vessel, can be used for the preparation of cardiovascular and cerebrovascular diseases medicine.
Studies show that flavones ingredient oral administration administration artifact availability is low, may be for due to the gastrointestinal tract bacterial decomposition, disintegrate fast behind the sublingual administration, the medicine stripping is released into the Sublingual mucosa, can fast and effeciently see through the Sublingual mucosa and enter the systemic blood circulation.And drop pill can absorb soon through sublingual administration, and dosage is little, when clinical application, can accurately adjust dosage, and be easy to carry, so vitexin-2 ''-O-rhamnoside is developed to dropping pill formulation by the ball number that increase and decrease is taken, the treatment obstruction of qi in the chest and cardialgia will have vast market prospect.
The specific embodiment
Embodiment one
A kind of preparation method of vitexin-2 ''-O-rhamnoside drop pill, be that vitexin-2 ''-O-rhamnoside crude drug and substrate are added fused PEG1500 and PEG4000 (PEG1500: PEG4000=1: 1) by 1: 1 proportioning, constantly stir, make uniform fusion medicinal liquid.Be transferred in the reservoir, regulate drop pill machine temperature control system, make the drop pill temperature remain on 80 ℃～90 ℃.Fused material splashes in the liquid paraffin with suitable speed by the dropping-pill machine head.The liquid paraffin temperature is controlled at 5 ℃～-5 ℃.The oil ball separates, and with the drop pill taking-up in drop pill machine exit, removes the surface condensation agent, and is dry under preference temperature, damp condition, promptly.
Embodiment two
A kind of preparation method of vitexin-2 ''-O-rhamnoside drop pill, be that vitexin-2 ''-O-rhamnoside crude drug and substrate are added fused PEG1000 and PEG6000 (PEG1000: PEG6000=1: 1) by 1: 1 proportioning, constantly stir, make uniform fusion medicinal liquid.Be transferred in the reservoir, regulate drop pill machine temperature control system, make the drop pill temperature remain on 80 ℃～90 ℃.Fused material splashes in the liquid paraffin with suitable speed by the dropping-pill machine head.The liquid paraffin temperature is controlled at 5 ℃～-5 ℃.The oil ball separates, and with the drop pill taking-up in drop pill machine exit, removes the surface condensation agent, and is dry under preference temperature, damp condition, promptly.
Embodiment three
A kind of preparation method of vitexin-2 ''-O-rhamnoside drop pill is that vitexin-2 ''-O-rhamnoside crude drug and substrate are added among the fused PEG4000 by 1: 2 proportioning, constantly stirs, and makes uniform fusion medicinal liquid.Be transferred in the reservoir, regulate drop pill machine temperature control system, make the drop pill temperature remain on 85 ℃～95 ℃.Fused material splashes in the dimethicone with suitable speed by the dropping-pill machine head.The dimethyl-silicon oil temperature is controlled at 10 ℃～-5 ℃.The oil ball separates, and with the drop pill taking-up in drop pill machine exit, removes the surface condensation agent, and is dry under preference temperature, damp condition, promptly.
Embodiment four
A kind of preparation method of vitexin-2 ''-O-rhamnoside drop pill, be that vitexin-2 ''-O-rhamnoside crude drug and substrate are added fused PEG4000 and PEG6000 (PEG4000: PEG6000=1: 1) by 1: 5 proportioning, constantly stir, make uniform fusion medicinal liquid.Be transferred in the reservoir, regulate drop pill machine temperature control system, make the drop pill temperature remain on 80 ℃～95 ℃.Fused material splashes in the dimethicone with suitable speed by the dropping-pill machine head.The dimethyl-silicon oil temperature is controlled at 20 ℃～-5 ℃.The oil ball separates, and with the drop pill taking-up in drop pill machine exit, removes the surface condensation agent, and is dry under preference temperature, damp condition, promptly.
Embodiment five
A kind of preparation method of vitexin-2 ''-O-rhamnoside drop pill, be that vitexin-2 ''-O-rhamnoside crude drug and substrate are added fused PEG4000 and PEG6000 (PEG4000: PEG6000=1: 1) by 1: 3 proportioning, constantly stir, make uniform fusion medicinal liquid.Be transferred in the reservoir, regulate drop pill machine temperature control system, make the drop pill temperature remain on 80 ℃～95 ℃.Fused material splashes in the liquid paraffin with suitable speed by the dropping-pill machine head.The liquid paraffin temperature is controlled at 20 ℃～-5 ℃.The oil ball separates, and with the drop pill taking-up in drop pill liquid machine exit, removes the surface condensation agent, and is dry under preference temperature, damp condition, promptly.
Embodiment six
A kind of preparation method of vitexin-2 ''-O-rhamnoside drop pill is that vitexin-2 ''-O-rhamnoside crude drug and substrate are added in the stearic acid fusing sodium by 1: 1 proportioning, constantly stirs, and makes uniform fusion medicinal liquid.Be transferred in the reservoir, regulate drop pill machine temperature control system, make the drop pill temperature remain on 80 ℃～95 ℃.Fused material splashes in the vegetable oil with suitable speed by the dropping-pill machine head.The vegetable oil temperature is controlled at 10 ℃～0 ℃.The oil ball separates, and with the drop pill taking-up in drop pill liquid machine exit, removes the surface condensation agent, and is dry under preference temperature, damp condition, promptly.
Claims (4)
1. the vitexin-2 ''-O-rhamnoside drop pill is characterized in that with the vitexin-2 ''-O-rhamnoside being that medicine material is prepared into, and every drop pill contains vitexin-2 ''-O-rhamnoside 5-25mg, is the Sublingual dropping pill formulation of treatment obstruction of qi in the chest and cardialgia.
2. vitexin-2 ''-O-rhamnoside drop pill according to claim 1 is characterized in that the medicine material in the vitexin-2 ''-O-rhamnoside drop pill is the monomeric compound that extraction separation obtains from Folium Crataegi.
3. the preparation method of vitexin-2 ''-O-rhamnoside drop pill according to claim 1, it is characterized in that: vitexin-2 ''-O-rhamnoside is added in the middle of the molten matrix, constantly stir, make uniform fusion medicinal liquid, the fusion medicinal liquid that makes is transferred in the reservoir, regulate drop pill machine temperature control system, make the drop pill temperature remain on 70 ℃～95 ℃, fused material splashes in the condensing agent with suitable speed by the dropping-pill machine head, with 50 ℃～-15 ℃ condensing agent coolings, drop pill with drop pill machine exit takes out again, remove the surface condensation agent, drying, promptly;
Described substrate is Polyethylene Glycol or stearic acid sodium, and the weight proportion of vitexin-2 ''-O-rhamnoside and substrate is 1: 0.5-10;
Described condensing agent is liquid paraffin, dimethicone or vegetable oil.
4. the preparation method of vitexin-2 ''-O-rhamnoside drop pill according to claim 3 is characterized in that described Polyethylene Glycol is one or more mixture in cetomacrogol 1000, polyethylene glycol 1500, Macrogol 4000, the polyethylene glycol 6000.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 201010184455 CN101849918A (en) | 2010-05-27 | 2010-05-27 | Vitexin-2''-O-rhamnoside pill and preparation method |
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| CN 201010184455 CN101849918A (en) | 2010-05-27 | 2010-05-27 | Vitexin-2''-O-rhamnoside pill and preparation method |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104958311A (en) * | 2015-06-10 | 2015-10-07 | 广西中医药大学 | New use of vitexin xyloside |
| CN106265706A (en) * | 2015-05-20 | 2017-01-04 | 辽宁中医药大学 | A kind of male ice drop pill treating acute myocardial ischemia and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1424042A (en) * | 2002-12-19 | 2003-06-18 | 中国人民解放军第二军医大学 | Crataegus leaves flavone tablets and their preparing method |
| CN101050226A (en) * | 2007-05-10 | 2007-10-10 | 辽宁中医药大学 | Method for separating derivative of vitexin |
-
2010
- 2010-05-27 CN CN 201010184455 patent/CN101849918A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1424042A (en) * | 2002-12-19 | 2003-06-18 | 中国人民解放军第二军医大学 | Crataegus leaves flavone tablets and their preparing method |
| CN101050226A (en) * | 2007-05-10 | 2007-10-10 | 辽宁中医药大学 | Method for separating derivative of vitexin |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106265706A (en) * | 2015-05-20 | 2017-01-04 | 辽宁中医药大学 | A kind of male ice drop pill treating acute myocardial ischemia and preparation method thereof |
| CN104958311A (en) * | 2015-06-10 | 2015-10-07 | 广西中医药大学 | New use of vitexin xyloside |
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Application publication date: 20101006 |