CN1463700A - Silymarin nano granular preparation and process for preparing the same - Google Patents
Silymarin nano granular preparation and process for preparing the same Download PDFInfo
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- CN1463700A CN1463700A CN 02121452 CN02121452A CN1463700A CN 1463700 A CN1463700 A CN 1463700A CN 02121452 CN02121452 CN 02121452 CN 02121452 A CN02121452 A CN 02121452A CN 1463700 A CN1463700 A CN 1463700A
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Abstract
The present invention is one kind of nano silybin preparation and its preparation process. The preparation has silybin extracted from Chinese medicine material silybum mariamum as effective component, stearic acid as carrier and lecithin as emulsifying agent, and is prepared via combined process of stirring emulsification and high pressure emulsification to coat silybin inside nano solid liposome particle. The nano particle has size of about 200 nm.
Description
Technical field
The present invention relates to a kind of Chinese medicine solid nano grain preparation and preparation method thereof, particularly a kind of silymarin nano particle preparations and preparation method.
Background technology
Oral medicine in the instructions of taking of Chinese medicine, generally all be to be brewed into decoction by Chinese medicine preparation, so-called Chinese medicine preparation generally also is through decoct extracting the gained main component, adds the liquid preparation that excipient substance is made into tablet, pill and various water base or organic group then.The administrated method that these are traditional makes the Effective Components of Chinese Herb utilization rate low, and the drug effect performance is more casual.
The nanotechnology that rise recent years is to utilize various technology that material is carried out nanoscale processing, reduces the diameter of material grains, increases specific surface area, thereby improves the activity of material greatly.Nanotechnology has all obtained certain utilization in various fields, but because Chinese medicine had not also set foot in field of nanometer technology.
As utilize the processing method of Western medicine, the main effective ingredient bag of Chinese medicine is stated from the solid lipid nanometer granule, make nano level Chinese medicinal granule preparation, improve the oral administration bioavailability of insoluble drug, realize the passive targeting of the drug-supplying system of nanoparticle by the control nanometer particle size, increase the selectivity to the lesions position treatment of Chinese medicine, Chinese medicine is played a role on molecular level, drug effect has rapid raising.
Summary of the invention
The object of the present invention is to provide a kind of Chinese medicine silymarin nano particle preparations, it can play a role on nanometer level.The present invention also provides a kind of preparation method of above-mentioned silymarin nano particle preparations.
Silymarin nano particle preparations of the present invention, as effective ingredient, is carrier with the stearic acid with the silymarin that extracts in the medicine Herba Silybi mariani therefrom, is emulsifying agent with lecithin, employing stirring and emulsifying and high pressure breast are spared the method that combines, and the silymarin bag are stated from the solid lipid nanoparticle make.
The particle diameter of above-mentioned nanoparticle is about 200nm.
The preparation method of silymarin nano particle preparations of the present invention may further comprise the steps:
(1) a certain amount of stearic acid heating and melting in water-bath is standby;
(2) take by weighing a certain amount of silymarin, fully be dissolved under the ultrasound wave condition in the organic solvent, add above-mentioned fusion stearic acid, slight fever makes it be dissolved into organic facies;
(3) get a certain amount of lecithin and glycerol and be scattered in the water, form water;
(4) organic facies that (2) are made is at the water that injects about 80 degrees centigrade under 1500 rev/mins the stirring condition, and continues to stir 4 hours, makes colostrum;
(5) colostrum that (4) are made is scattered in the water under 1000 rev/mins stirring condition fast;
(6) disperse system that (5) are made high pressure breast under the pressure of 1400Bar is spared 5 times, is cooled to room temperature again, can make the silymarin solid lipid nanoparticle of 200nm.
This method can also be used to prepare the nano particle preparations of other Chinese medicines.
Silymarin nano particle preparations of the present invention with the effective ingredient silymarin of Chinese medicine Herba Silybi mariani, is stated from the lipid nanometer solid particle by above-mentioned method bag, and the drug effect of silymarin can be brought into play on nanometer level.
The specific embodiment
The present invention is that the effective ingredient silymarin bag with the Chinese medicine Herba Silybi mariani is stated from the lipid solid nano grain, makes nano particle preparations.Silymarin is a flavonoid compound, is made up of a plurality of components, is characterized in being soluble in organic solvent and water insoluble, therefore can be dispersed in the method for aqueous phase with organic facies, is made into tiny granule.
Embodiment:
(1) take by weighing the stearic acids of 1.0 grams, stearic acid heated in 90 degrees centigrade of water-baths make its fusion, standby;
(2) take by weighing the silymarin of 50mg, fully be dissolved under the condition in 5 minutes in the ethyl acetate of 20ml at the ultrasonic echography of 50Hz, add above-mentioned fusion stearic acid, slight fever (50 degrees centigrade of water-baths) makes it fully be dissolved into organic facies, and is standby;
(3) get in the 50ml water that is scattered in 80 degrees centigrade under injection soybean phospholipid 0.5g and the glycerol 1.0g normal pressure, it is standby to form water;
(4) organic facies that makes in the above-mentioned steps (2) is injected 80 degrees centigrade of left and right sides 50ml and, has been annotated back continuation stirring 4 hours, make colostrum with the water that 1500 rev/mins speed stirs;
(5) colostrum that step (4) is made be scattered in 200ml and the water that stirs with 1000 rev/mins speed in condition, stirred 5 minutes under the room temperature;
(6) disperse system that step (5) is made is being spared 5 times (under the room temperature with M110s type high pressure dispersing emulsification machine (U.S. Microfuidics company product) high pressure breast under the pressure of 1400Bar, every next circulation), be cooled to room temperature again, can make the silymarin solid lipid nano-particle preparation 240ml of 200nm, the moisture silibin 0.5mg that flies of wherein every ml preparation.
The silymarin solid lipid nano-particle preparation that the inventive method makes can be made lyophilized preparation with freeze-drying, also can directly adopt aqueous injection technology to make aqueous injection, is used for clinical by oral or two kinds of route of administration of intravenous injection.
This product belongs to the nanoparticle drug-delivery preparation, can be used for the treatment of hepatic disease such as hepatic fibrosis, acute, chronic hepatitis.The administration nano-drug administration system of particle diameter about 200nm can improve the bioavailability of oral administration.Nanoparticle enters after the systemic circulation, be easy to by macrophage phagocytic in the lymphatic organs such as liver, spleen and discharge medicine, make the medicine passive target in liver and spleen, improve the drug level of medicine at diseased region, improve the curative effect of medicine, reduce the toxic and side effects of medicine simultaneously at other position.
Claims (4)
1. silymarin nano particle preparations, it is characterized in that: using the silymarin that extracts from Herba Silybi mariani is effective ingredient, with the stearic acid is carrier, with lecithin is emulsifying agent, employing stirring and emulsifying and high pressure breast are spared the method that combines, and the silymarin bag are stated from the solid lipid nanoparticle make.
2. silymarin nano particle preparations according to claim 1 is characterized in that: the particle diameter of this nanoparticle is about 200nm.
3. the preparation method of a silymarin nano particle preparations is characterized in that: may further comprise the steps:
(1) stearic acid heating and melting in water-bath is standby;
(2) take by weighing a certain amount of silymarin, fully be dissolved under the ultrasound wave condition in the organic solvent, add above-mentioned fusion stearic acid, slight fever makes it be dissolved into organic facies;
(3) get a certain amount of lecithin and glycerol and be scattered in the water, form water;
(4) organic facies that (2) are made is at the water that injects about 80 degrees centigrade under 1500 rev/mins the stirring condition, and continues to stir 4 hours, makes colostrum;
(5) colostrum that (4) are made is scattered in the water under 1000 rev/mins stirring condition fast;
(6) disperse system that (5) are made high pressure breast under the pressure of 1400Bar is spared 5 times, is cooled to room temperature again, can make the silymarin solid lipid nanoparticle of 200nm.
4. the preparation method of a Chinese medicine nano particle preparations is characterized in that: may further comprise the steps:
(1) stearic acid heating and melting in water-bath is standby;
(2) take by weighing a certain amount of Chinese medicine effective component extracts, fully be dissolved under the ultrasound wave condition in the organic solvent, add above-mentioned fusion stearic acid, slight fever makes it be dissolved into organic facies;
(3) get a certain amount of lecithin and glycerol and be scattered in the water, form water;
(4) organic facies that (2) are made is at the water that injects about 80 degrees centigrade under 1500 rev/mins the stirring condition, and continues to stir 4 hours, makes colostrum;
(5) colostrum that (4) are made is scattered in the water under 1000 rev/mins stirring condition fast;
(6) disperse system that (5) are made high pressure breast under the pressure of 1400Bar is spared 5 times, is cooled to room temperature again, can make the silymarin solid lipid nanoparticle of 200nm.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02121452 CN1463700A (en) | 2002-06-21 | 2002-06-21 | Silymarin nano granular preparation and process for preparing the same |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 02121452 CN1463700A (en) | 2002-06-21 | 2002-06-21 | Silymarin nano granular preparation and process for preparing the same |
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| CN1463700A true CN1463700A (en) | 2003-12-31 |
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| CN 02121452 Pending CN1463700A (en) | 2002-06-21 | 2002-06-21 | Silymarin nano granular preparation and process for preparing the same |
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Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1327835C (en) * | 2004-07-08 | 2007-07-25 | 北京科信必成医药科技发展有限公司 | Hepedestal oral disintegration tablet and its preparing method |
| CN100349565C (en) * | 2005-09-30 | 2007-11-21 | 南京工业大学 | Curcumenol solid lipid nanoparticle and preparation method thereof |
| CN100356915C (en) * | 2005-08-25 | 2007-12-26 | 江苏大学 | Nanometer preparation of silybin and preparation method thereof |
| CN100386080C (en) * | 2005-12-01 | 2008-05-07 | 西安交通大学 | Tetrandrine solid lipide nano particle and its preparing method |
| CN101129336B (en) * | 2007-07-24 | 2010-04-14 | 浙江大学 | Method of preparing lipid nano granule |
| CN101224194B (en) * | 2007-01-18 | 2011-06-15 | 重庆太极医药研究院 | Silybin guest nanometer particle and preparing method thereof |
| CN102614239A (en) * | 2012-04-25 | 2012-08-01 | 晨光生物科技集团天津有限公司 | Silymarin compound nanoparticle and preparation method thereof |
| CN105477040A (en) * | 2016-01-04 | 2016-04-13 | 重庆医药高等专科学校 | Silymarin PLGA enteric nanoparticles and preparation method thereof |
| CN108524364A (en) * | 2018-06-14 | 2018-09-14 | 上海棠美生物科技有限公司 | A kind of cosmetic active object nano-carrier package and preparation method thereof |
| CN109198182A (en) * | 2018-10-25 | 2019-01-15 | 杨凌金石牧业有限责任公司 | A kind of Chinese medicine compound prescription additive for animal and fowl fodder |
| CN109260261A (en) * | 2018-11-21 | 2019-01-25 | 温州医科大学附属第医院 | The Chinese medicine and method of triple embrane method preparation treatment primary biliary cirrhosis |
-
2002
- 2002-06-21 CN CN 02121452 patent/CN1463700A/en active Pending
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1327835C (en) * | 2004-07-08 | 2007-07-25 | 北京科信必成医药科技发展有限公司 | Hepedestal oral disintegration tablet and its preparing method |
| CN100356915C (en) * | 2005-08-25 | 2007-12-26 | 江苏大学 | Nanometer preparation of silybin and preparation method thereof |
| CN100349565C (en) * | 2005-09-30 | 2007-11-21 | 南京工业大学 | Curcumenol solid lipid nanoparticle and preparation method thereof |
| CN100386080C (en) * | 2005-12-01 | 2008-05-07 | 西安交通大学 | Tetrandrine solid lipide nano particle and its preparing method |
| CN101224194B (en) * | 2007-01-18 | 2011-06-15 | 重庆太极医药研究院 | Silybin guest nanometer particle and preparing method thereof |
| CN101129336B (en) * | 2007-07-24 | 2010-04-14 | 浙江大学 | Method of preparing lipid nano granule |
| CN102614239A (en) * | 2012-04-25 | 2012-08-01 | 晨光生物科技集团天津有限公司 | Silymarin compound nanoparticle and preparation method thereof |
| CN105477040A (en) * | 2016-01-04 | 2016-04-13 | 重庆医药高等专科学校 | Silymarin PLGA enteric nanoparticles and preparation method thereof |
| CN108524364A (en) * | 2018-06-14 | 2018-09-14 | 上海棠美生物科技有限公司 | A kind of cosmetic active object nano-carrier package and preparation method thereof |
| CN109198182A (en) * | 2018-10-25 | 2019-01-15 | 杨凌金石牧业有限责任公司 | A kind of Chinese medicine compound prescription additive for animal and fowl fodder |
| CN109260261A (en) * | 2018-11-21 | 2019-01-25 | 温州医科大学附属第医院 | The Chinese medicine and method of triple embrane method preparation treatment primary biliary cirrhosis |
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