CN1424042A - Crataegus leaves flavone tablets and their preparing method - Google Patents
Crataegus leaves flavone tablets and their preparing method Download PDFInfo
- Publication number
- CN1424042A CN1424042A CN 02155200 CN02155200A CN1424042A CN 1424042 A CN1424042 A CN 1424042A CN 02155200 CN02155200 CN 02155200 CN 02155200 A CN02155200 A CN 02155200A CN 1424042 A CN1424042 A CN 1424042A
- Authority
- CN
- China
- Prior art keywords
- total flavones
- folium crataegi
- crataegi total
- poloxamer
- polyethylene glycol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
A dropping pill o f the common haw-leaf flavone is prepared from common haw-leaf flavone, polyethanediol and poloxamer. Its advantages are quickly curative effect and high biological utilization rate.
Description
Technical field
The invention belongs to medical technical field, being specifically related to a kind of is the oral solid formulation and preparation method thereof of main component with the Folium Crataegi total flavones, is a kind of Folium Crataegi total flavones dropping pill formulation and preparation method thereof specifically.
Background technology
In Fructus Crataegi be Chinese medicine commonly used simply, have that removing food stagnancyization stagnates, spleen reinforcing is good for the stomach, the effect of blood circulation promoting and blood stasis dispelling.Its chemical constituent can be divided into organic acid and flavonoid, and the reach a conclusion main component of Fructus Crataegi blood circulation promoting and blood stasis dispelling of research is a total flavonoid, and in the Folium Crataegi content of total flavone than higher.Folium Crataegi total flavones has obtained lot of experiment validation as the effective ingredient of blood circulation promoting and blood stasis dispelling.Folium Crataegi total flavones has pharmacologically active widely, is mainly: hypotensive effect; Blood fat reducing prevents atherosclerosis; Increase coronary flow anti-experimental character myocardial ischemia, anti-arrhythmia; Strengthen myocardial contraction, strengthen ventricle, the motional amplitude in atrium; Synthesizing of blocking-up N-nitrosamine; Improve humoral immunization and cell immunocompetent; Bacillus proteus, escherichia coli, shigella flexneri there is antibacterial action; Vasodilator is removed the local stasis of blood state.Be mainly used in depressed blood stasis clinically, chest distress, palpitation and amnesia, vertigo and tinnitus; Coronary heart disease, angina pectoris, hyperlipemia, diseases such as cerebral arterial insufficiency.
Play the Folium Crataegi preparation seventies and just be applied to clinical treatment angina pectoris and blood fat reducing.But the Folium Crataegi preparation type is tradition relatively, and such as Yixintong sheet, the capsule of feeling at ease, multiple heart sheet etc., the variety of issue that conventional dosage forms exists is as absorbing the performance that affects the treatment slowly, and coronary heart disease, angina pectoris belong to clinical acute disease, and rapid onset needs first aid.Drop pill is a kind of spheric pill that utilizes the solid dispersion technology system of dripping to form, it utilizes water-solubility carrier to improve the dissolubility and the dissolution rate of medicine, improve the infiltration rate and the absorbtivity of medicine, thereby raising bioavailability, improve the curative effect of medicine, particularly important to cardiovascular emergency cases such as coronary heart disease, angina pectoriss.
Summary of the invention
The object of the present invention is to provide oral Folium Crataegi total flavones dropping pill formulation that a kind of drug effect is fast, bioavailability is high and preparation method thereof, and effectively control its quality.
The Folium Crataegi total flavones dropping pill formulation that the present invention proposes is a kind of oral solid formulation, it is Main Ingredients and Appearance with the Folium Crataegi total flavones, with Polyethylene Glycol (requiring its molecular weight greater than 1500) and poloxamer is that the compatibility component is formulated, the weight proportion of each component is: 1 part of Folium Crataegi total flavones, Polyethylene Glycol 2.5-5 part, poloxamer 0.5-1.5 part.
The Folium Crataegi total flavones dropping pill formulation that the present invention proposes, its preferred component weight proportion is: 1 part of Folium Crataegi total flavones, Polyethylene Glycol 3-4 part, poloxamer 0.5-1 part.
Folium Crataegi total flavones dropping pill formulation of the present invention, contain vitexin rhamnoside (5 in its main component Folium Crataegi total flavones, 7,4 '-trihydroxyflavone-8-C-β-D-glucosyl group (1 → 2)-β-D-rhamnoside) (structural formula is seen formula I) and vitexin glucoside (5,7,4 '-trihydroxyflavone-8-C-β-D-glucosyl group (1 → 4)-β-D-glucoside) (structural formula is seen formula II).
Formula I
Formula II
The preparation method of the crataegutt dropping pill formulation that the present invention proposes is as follows: by the component proportioning Polyethylene Glycol, poloxamer are placed in the water-bath and heat, make it fusion, add Folium Crataegi total flavones, stir, add anhydrous alcohol for medical use, stir hydrotropy, continue to stir, volatilization ethanol, 90～100 ℃ of heat preservation for standby use; Preheating DW-1 type drop pill machine, making fluid storage compartment constant temperature is fluid temperature, the coolant soybean oil is chilled to 10～12 ℃ in advance, drips system with 26～34 droplets/minute the speed of dripping; Collect drop pill at valve port, the filtering coolant ,-16～-20 ℃ of freezing processing were put in the vacuum drying oven more than 24 hours, and drying promptly gets the molding drop pill.
Adopt the content of high effective liquid chromatography for measuring molding drop pill, wherein containing vitexin rhamnoside is 6-14%, and containing the vitexin glucoside is 2-7%.
The present invention compared with prior art not only has the advantage that drug effect is fast, bioavailability is high, but also has the characteristics of process conditions advanced person, quality control strictness, suitable industrial-scale production.The Folium Crataegi total flavones drop pill is all molten loosing in 5 minutes, helps drug effect; The pharmacodynamic experiment result shows the onset time of Folium Crataegi total flavones drop pill faster than its tablet, and action intensity also is better than tablet.
The specific embodiment
The invention is further illustrated by the following examples.
Embodiment 1:
The weight proportion of Folium Crataegi total flavones drop pill each component is:
Folium Crataegi total flavones 6.40g
Polyethylene Glycol (6000) 24.02g
Poloxamer (188) 6.00g
The step of preparation Folium Crataegi total flavones drop pill is as follows:
24.02g Polyethylene Glycol (6000), 6.00g poloxamer (188) are put in the beaker, heating makes fusion in 95 ℃ of water-baths, stir, add the 6.40g Folium Crataegi total flavones, stir, add the 10ml anhydrous alcohol for medical use, fully stir, make the Folium Crataegi total flavones dissolving, continue to stir, make the ethanol volatilization, heat preservation for standby use; With the preheating of drop pill machine, fluid storage compartment temperature constant temperature is 95 ℃ ± 2 ℃, and coolant adopts soybean oil, be chilled to 10-12 ℃ in advance, regulate drip nozzle and the distance of cooling off liquid level, pour medicinal liquid into fluid storage compartment, start valve, medicinal liquid is dropwise splashed in the coolant, drip speed and be about 30 droplets/minute; In collecting a mouthful collection drop pill, absorb the surface cool agent with gauze, freezer compartment of refrigerator (18 ℃) freezing processing 24 hours is put in the vacuum drying oven, the room temperature vacuum drying, promptly.
By high effective liquid chromatography for measuring content, the result draws that wherein to contain vitexin rhamnoside be 9.37-10.31%, and containing the vitexin glucoside is 4.06-5.00%.
Embodiment 2:
Folium Crataegi total flavones drop pill each component weight proportion is:
Folium Crataegi total flavones 4.60g
Polyethylene Glycol (1500) 23.00g
Poloxamer (188) 2.50g
The embodiment of preparation Folium Crataegi total flavones drop pill method is as follows:
23.00g Polyethylene Glycol (1500), 2.50g poloxamer (188) are put in the beaker, heating makes fusion in 90 ℃ of water-baths, stir, add the 4.60g Folium Crataegi total flavones, stir, add the 9ml anhydrous alcohol for medical use, fully stir, make the Folium Crataegi total flavones dissolving, continue to stir, make the ethanol volatilization, heat preservation for standby use; With the preheating of drop pill machine, fluid storage compartment temperature constant temperature is 90 ℃ ± 2 ℃, and coolant is chilled to 10-12 ℃ in advance, regulates drip nozzle and the distance of cooling off liquid level, pours medicinal liquid into fluid storage compartment, starts valve, and medicinal liquid is dropwise splashed in the coolant, drips speed and is about 34 droplets/minute; In collecting a mouthful collection drop pill, absorb table and coolant with gauze, freezer compartment of refrigerator (16 ℃) freezing processing 24 hours is put in the vacuum drying oven, the room temperature vacuum drying, promptly.
By high effective liquid chromatography for measuring content, the result draws that wherein to contain vitexin rhamnoside be 6.15～7.12%, and containing the vitexin glucoside is 2.32～3.18%.
Embodiment 3:
The weight proportion of Folium Crataegi total flavones drop pill each component is:
Folium Crataegi total flavones 7.00g
Polyethylene Glycol (4000) 17.50g
Poloxamer (188) 10.50g
The step of preparation Folium Crataegi total flavones drop pill is as follows:
17.50g Polyethylene Glycol (4000), 10.50g poloxamer (188) are put in the beaker, heating makes fusion in 98 ℃ of water-baths, stir, add the 7.00g Folium Crataegi total flavones, stir, add the 12ml anhydrous alcohol for medical use, fully stir, make the Folium Crataegi total flavones dissolving, continue to stir, make the ethanol volatilization, heat preservation for standby use; With the preheating of drop pill machine, fluid storage compartment temperature constant temperature is 98 ℃ ± 2 ℃, and coolant is chilled to 10 ~ 12 ℃ in advance, regulates drip nozzle and the distance of cooling off liquid level, pours medicinal liquid into fluid storage compartment, starts valve, and medicinal liquid is dropwise splashed in the coolant, drips speed and is about 26 droplets/minute; In collecting a mouthful collection drop pill, absorb the surface cool agent with gauze, freezer compartment of refrigerator (20 ℃) freezing processing 36 hours is put in the vacuum drying oven, the room temperature vacuum drying, promptly.
By high effective liquid chromatography for measuring content, the result draws that wherein to contain vitexin rhamnoside be 9.31～10.09%, and containing the vitexin glucoside is 5.18～6.82%.
Embodiment 4:
The weight proportion of Folium Crataegi total flavones drop pill each component is:
Folium Crataegi total flavones 6.25g
Polyethylene Glycol (6000) 23.46g
Poloxamer (188) 6.20g
The step of preparation Folium Crataegi total flavones drop pill is as follows:
23.46g Polyethylene Glycol (6000), 6.20g poloxamer (188) are put in the beaker, heating makes fusion in 90 ℃ of water-baths, stir, add the 6.25g Folium Crataegi total flavones, stir, add the 10ml anhydrous alcohol for medical use, fully stir, make the Folium Crataegi total flavones dissolving, continue to stir, make the ethanol volatilization, heat preservation for standby use; With the preheating of drop pill machine, fluid storage compartment temperature constant temperature is 92 ℃ ± 2 ℃, and coolant is chilled to 10 ~ 12 ℃ in advance, regulates drip nozzle and the distance of cooling off liquid level, pours medicinal liquid into fluid storage compartment, starts valve, and medicinal liquid is dropwise splashed in the coolant, drips speed and is about 28 droplets/minute; In collecting a mouthful collection drop pill, absorb the surface cool agent with gauze, freezer compartment of refrigerator (18 ℃) freezing processing 28 hours is put in the vacuum drying oven, the room temperature vacuum drying, promptly.
By high effective liquid chromatography for measuring content, the result draws that wherein to contain vitexin rhamnoside be 10.82～11.56%, and containing the vitexin glucoside is 4.78～5.11%.
Claims (4)
1, a kind of Folium Crataegi total flavones dropping pill formulation, it is characterized in that with the Folium Crataegi total flavones being Main Ingredients and Appearance, is that the compatibility component is formulated with molecular weight greater than 1500 Polyethylene Glycol and poloxamer, and the weight proportion of each component is: 1 part of Folium Crataegi total flavones, 2.5～5 parts of Polyethylene Glycol, 0.5～1.5 part of poloxamer.
2, Folium Crataegi total flavones dropping pill formulation according to claim 1 is characterized in that the weight proportion of each component is: 1 part of Folium Crataegi total flavones, Polyethylene Glycol 3-4 part, poloxamer 0.5-1 part.
3, Folium Crataegi total flavones dropping pill formulation according to claim 1 is characterized in that wherein containing vitexin rhamnoside 6-14%, vitexin glucoside 2-7%.
4, a kind of preparation method of Folium Crataegi total flavones dropping pill formulation as claimed in claim 1 is characterized in that concrete steps are as follows:
(1) by the component proportioning Polyethylene Glycol, poloxamer are placed in the water-bath and heat, make it fusion, add Folium Crataegi total flavones, stir, add anhydrous alcohol for medical use, stir hydrotropy, continue to stir, volatilization ethanol, 90～100 ℃ of heat preservation for standby use;
(2) preheating DW-1 type drop pill machine, making fluid storage compartment constant temperature is fluid temperature, the coolant soybean oil is chilled to 10～12 ℃ in advance, drips system with 26～34 droplets/minute the speed of dripping;
(3) collect drop pill at valve port, the filtering coolant ,-16～-20 ℃ of freezing processing were put in the vacuum drying oven more than 24 hours, and drying promptly gets the molding drop pill.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02155200 CN1424042A (en) | 2002-12-19 | 2002-12-19 | Crataegus leaves flavone tablets and their preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02155200 CN1424042A (en) | 2002-12-19 | 2002-12-19 | Crataegus leaves flavone tablets and their preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1424042A true CN1424042A (en) | 2003-06-18 |
Family
ID=4752579
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02155200 Pending CN1424042A (en) | 2002-12-19 | 2002-12-19 | Crataegus leaves flavone tablets and their preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1424042A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1323694C (en) * | 2005-07-13 | 2007-07-04 | 天津大学 | Compound dripping pills contg. fruit of Chinese haw-thorn, and its prepn. method |
| CN100376231C (en) * | 2005-12-13 | 2008-03-26 | 江苏大学 | Compound grease-reducing drop pills preparation method |
| CN100453072C (en) * | 2005-01-28 | 2009-01-21 | 北京正大绿洲医药科技有限公司 | Isatis root drops and preparation thereof |
| CN101849918A (en) * | 2010-05-27 | 2010-10-06 | 辽宁中医药大学 | Vitexin-2''-O-rhamnoside pill and preparation method |
-
2002
- 2002-12-19 CN CN 02155200 patent/CN1424042A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100453072C (en) * | 2005-01-28 | 2009-01-21 | 北京正大绿洲医药科技有限公司 | Isatis root drops and preparation thereof |
| CN1323694C (en) * | 2005-07-13 | 2007-07-04 | 天津大学 | Compound dripping pills contg. fruit of Chinese haw-thorn, and its prepn. method |
| CN100376231C (en) * | 2005-12-13 | 2008-03-26 | 江苏大学 | Compound grease-reducing drop pills preparation method |
| CN101849918A (en) * | 2010-05-27 | 2010-10-06 | 辽宁中医药大学 | Vitexin-2''-O-rhamnoside pill and preparation method |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1256954C (en) | Blumea oil dripping pills and its preparation process | |
| CN1424042A (en) | Crataegus leaves flavone tablets and their preparing method | |
| CN1679676A (en) | Six-component saf-flower drops and preparation thereof | |
| CN1686389A (en) | Danhong drip pill prepared from salvia root and carthamus and its preparation method | |
| CN1424041A (en) | Kakonein preparations and their production | |
| CN1634431A (en) | Drop pills containing honeysuckle flower and radix Scutellariae extract for treating upper respiratory tract infection | |
| CN1919255A (en) | Aim Naoluotong drop pill and its preparation method | |
| CN1593584A (en) | Novel formulation of 'Xiaoyan Lidan' and its preparation method | |
| CN1297255C (en) | Dripping pills for treating high blood fat and its preparing method | |
| CN1299714C (en) | Method for preparing traditional Chinese compound ointment | |
| CN1634427A (en) | Soft capsule containing rhubarb, goldthread root and scutellaria root and preparation technique thereof | |
| CN1258364C (en) | Formula of calebassine dripping pills and its preparation method | |
| CN1562095A (en) | Hawthorn essence defatting dripping pill and preparing method and its use | |
| CN1307976C (en) | Thorax comforting drop pills for treating cardiopathy and preparation method thereof | |
| CN1634452A (en) | Yin-nourishing lung-heat clearing drop pills | |
| CN1634508A (en) | Saussurea involucrata drop pill and its preparation method | |
| CN1634478A (en) | Tendril-leaved fritillary bulb loquat drop pills and preparation method thereof | |
| CN1915301A (en) | Drop pills of corydalis tuber, and preparation method | |
| CN1759862A (en) | Prescription of arenobufagin drop pills and preparation method | |
| CN1294901C (en) | Embolism eliminatinging drop pills with qi invigorating, blood flow promoting and collateral dredging function | |
| CN1762424A (en) | Sutellaria root pills formula and its preparation method | |
| CN101623306A (en) | Bracken pill and preparation method thereof | |
| CN1613485A (en) | Iron-sheet dendrobe compound drop pellets and their preparation | |
| CN1695670A (en) | refrigerant buccal drop pills and preparation method | |
| CN1762408A (en) | Honey suckle pill formula and its preparation method |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |