CN1583139A - Preparation of dragon's blood and phospholipin composition - Google Patents
Preparation of dragon's blood and phospholipin composition Download PDFInfo
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- CN1583139A CN1583139A CN 200410046367 CN200410046367A CN1583139A CN 1583139 A CN1583139 A CN 1583139A CN 200410046367 CN200410046367 CN 200410046367 CN 200410046367 A CN200410046367 A CN 200410046367A CN 1583139 A CN1583139 A CN 1583139A
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- sanguis draxonis
- phosphatide complexes
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- phospholipid
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Abstract
A Dragon's bood-phophatide composition and its preparing process are disclosed. Its advantage is higher biological utilization rate.
Description
Technical field
This invention relates to a kind of pharmaceutical preparation and preparation thereof of blood circulation promoting and blood stasis dispelling, is specifically related to Sanguis Draxonis phosphatide complexes and preparation method.
Background technology
Cardiovascular and cerebrovascular disease all is the formidable enemy who threatens human health all the time, the raising year by year in China along with living standard, and the change of life style, and China steps into aged society gradually, the threat of cardio-cerebrovascular disorder is serious day by day.The prevalence, sickness rate, the mortality rate that show China's cardiovascular and cerebrovascular disease from EPDML statistics continue over 30 years to rise; Existing apoplexy patient 500-600 ten thousand people in the whole nation; Annual neopathy number is about 18-20 ten thousand; In recent years add up the dead population of cardiovascular and cerebrovascular disease and account for 60% of total death toll; Be 200 ten thousand people because of the cardiovascular and cerebrovascular disease death toll every year; Annual national cardiovascular and cerebrovascular vessel patient's mortality rate is about 2,00/,100,000, is higher than U.S., adds, states such as method, day.
The medicine of cardiovascular and cerebrovascular disease is based on Western medicine at present, but raising along with the dynamics of Chinese medicine development in recent years, the herbal species that some determined curative effects also occurred, as Folium Ginkgo extract, arasaponin etc., compare with the Western medicine kind, Chinese medicine has effect mitigation, few side effects, advantages such as gerontal patient's better tolerance.The Chinese medicine resource is the huge treasure-house that ancestors give us, adopts modern advanced traditional medicine exploitation to be met the requirement in reality and epoch.Therefore,, adopt modern technologies that determined curative effect, herbal species that safety is good are carried out form improvement, will produce huge social and economic implications for better exploitation Chinese medicine resource.
Sanguis Draxonis has effects such as promoting blood circulation to remove blood stasis, pain relieving, hemostasis, promoting tissue regeneration and ulcer healing, is mainly used in traumatic hemorrhage, ulcer being unable to heal, traumatic injury, the stasis of blood disease such as have a pain that stagnates, and is one of rare Chinese medicine.The Sanguis Draxonis medical material is dependence on import always in the past, and its source is the resin in babassu Sanguis Draxonis Daemonorops draco fruit and the trunk, is distributed in east, the Indian Ocean, the torrid areas is adjoined in the two sides, west.Since 1972, along with the discovery and the development and use of ground Dracaena cochinchinensis Sanguis Draxonis resource plants such as Yunnan, Guangxi, the history of the complete dependence on import of China's Sanguis Draxonis that is through with.The product of domestic Dragon Blood are called " Sanguis Draxonis ", are the resin that the resiniferous wood of Liliaceae dracaena plant Dracaena cochinchinensis Dracaena cochinchinensis, Hainan Folium Dracaenae cambodianae Dracaena combidiana obtains through extraction.Studies show that homemade Sanguis Draxonis and import Sanguis Draxonis basically identical on pharmacology and clinical efficacy, can be used as the succedaneum of import Sanguis Draxonis.The preparation of the Sanguis Draxonis of clinical practice at present has capsule, powder and conventional tablet.Aspect clinical practice, Resina Draconis preparation as one not only is used for the cardiovascular and cerebrovascular disease patient at present, and at gynecology many uses is also arranged, because of its stronger blood circulation invigorating efficacies, to menses due to the stagnation of QI smooth due to diseases such as dysmenorrhea, menoxenia therapeutical effect is all arranged.
The chemical constituent that contains in the middle of the Sanguis Draxonis mainly is divided into 2 classes.Main active substance is flavone and Polyphenols, is broadly divided into chalcone derivative, dihydrochalcone, flavone, flavane, poly flavone and phenols according to structure, found 90 in the middle of the Sanguis Draxonis so far surplus kind of Flavonoid substances; In addition, the triterpene saponin material is also distributed more widely in the middle of Sanguis Draxonis, found 50 so far surplus kind, the aglycon of saponin is mainly diosgenin in the middle of the Sanguis Draxonis.Modern study shows that the main active site of Sanguis Draxonis is the ethyl acetate soluble substance, for low polar substances, as cochinchinenin A, cochinchinenin B.After entering in the body, well-known oral solid formulation needs to absorb through disintegrate, stripping; For hydrophobic drug, owing to deliquescent reason, bioavailability is often lower, greatly reduces the therapeutic effect of medicine.Clinical Dragonis sanguis preparation commonly used is because bioavailability is lower at present, and its therapeutic effect is often limited; In addition, cardiovascular and cerebrovascular disease patient's treatment generally needs the medicine quick acting, and common main preparation is because stripping is slow, onset has limited use slowly.Therefore, developing quick-acting Resina Draconis preparation as one will have broad application prospects.
Italy scholar Bombardelli chances in the research liposome: the natural flavone compounds has special affinity to phospholipid, the two can be in conjunction with forming complex, and show and remarkable different biological characteristics and the pharmacologically actives of parent drug, discovering afterwards, the natural component and the natural extract of a lot of types can be made phosphatide complexes, and this class phosphatide complexes is named as Phytosome or phospholipid complex.(list of references: Feng Nianping, model Guangping. natural drug transmission system-phosphatide complexes. Chinese Chinese medicine information magazine .2001,3:34-35)
Phosphatide complexes the most noticeable characteristics aspect pharmaceutics are to compare with former medicine its raising evident in efficacy, reason be phospholipid adding change in various degree the physicochemical property and the biological characteristics of medicine, effectively raise the active skull cap components absorption in vivo, significantly changed the bioavailability of active substance.As the apparent partition coefficient that studies show that the epimedium flavone phosphatide complexes can improve 3.5 times; Think that at present active skull cap components can stronger interaction partly take place with the polar group of phospholipid, suppressing single bonded in the molecule freely rotates, but 2 long-chain fat bases in the phospholipid do not participate in compound reaction, can move freely, and form a lipophilic surface; In addition, the adding of phospholipid can improve the dissolubility of Flavonoid substances in water, and the effect of two aspects finally improves the amphipathic of medicine, thereby effectively improves the bioavailability of Flavonoid substances.Research to silymarin phosphatide complexes in the flavone compound is more deep, after studies show that silymarin and phospholipid form complex, fat-soluble enhancing, bioavailability improve, and the silymarin phosphatide complexes can make the total cholesterol of liver of high fat diet rabbit, blood plasma MAD concentration reduce, and makes some metal ion such as Zn in the serum
2+And Ca
2+Concentration raise, microsome Cytochrome P450 content is raise, thereby can and remove free radical, stabilizing cell membrane anti peroxidation of lipid, the hepatic injury that high fat diet etc. is caused has good protective action.Not only can improve the principal agent bioavailability after this explanation Flavonoid substances is made phosphatide complexes, and widen the treatment target spot,, significantly improve therapeutic effect by many-sided synergism.
Summary of the invention
The technical problem that this invention solved is a kind of Resina Draconis preparation as one efficiently of preparation, and promptly the Sanguis Draxonis phosphatide complexes is compared with common Resina Draconis preparation as one, and the bioavailability of Sanguis Draxonis phosphatide complexes significantly improves, and pharmacologically active is obviously strengthened.
The Sanguis Draxonis that this invention relates to is the resin in babassu Sanguis Draxonis Daemonorops draco fruit and the trunk, Liliaceae dracaena plant Dracaena cochinchinensis Dracaena cochinchinensis, the resin that the resiniferous wood of Hainan Folium Dracaenae cambodianae Dracaena combidiana obtains through extraction; Selected phospholipid is natural or synthetic phospholipid, comprises lecithin, phosphatidylcholine, Phosphatidylserine, phosphatidyl ethanol ammonia etc.
The disclosed Sanguis Draxonis phosphatide complexes of this invention can prepare by following technical proposals:
According to the percentage by weight Sanguis Draxonis: phospholipid=5: 1-1: 5 take by weighing sample, add suitable low polarity solvent, stir or heating is phospholipid and the dissolving of Sanguis Draxonis composition, treat the solution clarification after, concentrating under reduced pressure is flung to most of low polarity solvent, and vacuum drying promptly obtains phosphatide complexes.
The solvent that this invention relates to comprises ethyl acetate, chloroform, ether, acetone, methanol, ethanol etc. for Sanguis Draxonis and phospholipid all being had the low polar solvent of better dissolubility.
The pharmacological action of Sanguis Draxonis phosphatide complexes significantly improves directly related with the raising of its formation phosphatide complexes artifact availability, because the research to the Chinese medicine bioavailability is relatively more difficult, chief reason is that active component is many, content is low, and is bigger to the detection difficulty of intravital micro constitutent.The research data of comprehensive Sanguis Draxonis, lourerin A (loureirin A) and lourerin B (loureirinB) are the sign composition in the Sanguis Draxonis, content is higher relatively and have clear and definite biological activity, and it is stronger to adopt these 2 materials to carry out bioavailability test operability.
loureirin?A
loureirin?B
We obtain lourerin A 10.2g, lourerin B 9.7g respectively by the silica gel column chromatography preparation in the middle of Sanguis Draxonis; Take by weighing each 6.0g of lourerin A and lourerin B respectively, add the 12.0g soybean phospholipid, prepare phosphatide complexes according to the preparation method of above-mentioned Sanguis Draxonis phosphatide complexes.
Get 20 of rats, the mixture of the above-mentioned phosphatide complexes of orally give, lourerin A and lourerin B was put to death animal after 2 hours, got blood, measured the content of central lourerin A of blood and lourerin B, and the result is as follows:
| Dosage | ??C Lourerin A(mg/ml) | ????C Lourerin B(mg/ml) | |
| Phosphatide complexes dosage | ????5.0g/Kg | ??1.032±0.12 | ????1.125±0.09 |
| Lourerin A, B mixture | ????2.5g/Kg | ??0.645±0.11 | ????0.665±0.10 |
Can see that from last table phosphatide complexes can significantly improve the bioavailability of lourerin A and lourerin B, can infer the Sanguis Draxonis phosphatide complexes owing to the systemic improvement of body, its therapeutic effect of the raising of bioavailability will obtain remarkable reinforcement.
The specific embodiment
Embodiment 1
Take by weighing Sanguis Draxonis 100g and refining oral soybean phospholipid 100g, add ethyl acetate 500mL, room temperature is the excusing from death dissolving down, and to forming settled solution, 60 ℃ of reclaim under reduced pressure are flung to organic solvent, and vacuum drying obtains the Sanguis Draxonis phosphatide complexes.
Embodiment 2
Get Sanguis Draxonis and add 5 times of volume of ethanol, supersound extraction, each 30min, extract 2 this, merge extractive liquid,, reclaim under reduced pressure obtains Sanguis Draxonis extract; Take by weighing Sanguis Draxonis extract 100g and lecithin 500g, add ethanol 1000mL, room temperature stirs fully dissolving down, filters, and obtains settled solution, and solvent is flung in decompression, and vacuum drying obtains phosphatide complexes.
Embodiment 3
Get the acetone that Sanguis Draxonis adds 5 times of volumes, supersound extraction, each 30min, extract 2 this, merge extractive liquid,, reclaim under reduced pressure obtains Sanguis Draxonis extract; Take by weighing Sanguis Draxonis extract 100g and lecithin 500g, add ethanol 1000mL, room temperature stirs fully dissolving down, filters, and obtains settled solution, and solvent is flung in decompression, and vacuum drying obtains phosphatide complexes.
Embodiment 4
The preparation of Sanguis Draxonis phosphatide complexes capsule:
Prescription:
Sanguis Draxonis phosphatide complexes (making) 300g by embodiment 2 methods
Pregelatinized Starch 80g
95% ethanol q.s.
Crosslinked CMC-Na 12g
Micropowder silica gel 3g
Make 1000
Method for making: get the Sanguis Draxonis phosphatide complexes, pulverized 80 mesh sieves; Add pregelatinized Starch, as adhesive, cross 20 mesh sieve system soft materials, 60 ℃ of dryings, granulate with 95% ethanol; Dried granule added crosslinked CMC-Na of 100 purposes and micropowder silica gel mixing, measured the content of index composition in the granule, and was encapsulated, the about 0.4g of loading amount; Packing promptly.
Embodiment 5
The preparation of Sanguis Draxonis phosphatide complexes tablet:
Prescription:
Sanguis Draxonis phosphatide complexes (making) 400g by embodiment 1 method
Microcrystalline Cellulose 95g
Hyprolose 25g
95% ethanol q.s.
Cross-linking sodium carboxymethyl cellulose 25g
Magnesium stearate 4.5g
Make 1000
Method for making: the Sanguis Draxonis phosphatide complexes, add microcrystalline Cellulose, hyprolose,, cross 20 mesh sieves and granulate as binding agent with 95% ethanol, 60 ℃ of dryings, granulate adds tabletting behind cross-linking sodium carboxymethyl cellulose and the magnesium stearate mixing, makes 1000; LE film coating powder coating with 7.6%, promptly.
Embodiment 6
Sanguis Draxonis phosphatide complexes preparation of soft capsule:
Prescription:
Sanguis Draxonis phosphatide complexes (making) 400g by embodiment 1 method
Vegetable oil 95g
Cera Flava 25g
Make 1000
Method for making: take by weighing Sanguis Draxonis phosphatide complexes, vegetable oil, Cera Flava according to preparation prescription, place colloid mill to be ground into ointment shape suspended matter, be pressed into 1000, promptly.
Embodiment 7
Sanguis Draxonis phosphatide complexes preparation of soft capsule:
Prescription:
Sanguis Draxonis phosphatide complexes (making) 50g by embodiment 2 methods
Hydrogenated vegetable oil 300g
Cera Flava 50g
Make 1000
Method for making: take by weighing Sanguis Draxonis phosphatide complexes, vegetable oil, Cera Flava according to preparation prescription, place colloid mill to be ground into ointment shape suspended matter, be pressed into 1000, promptly.
Embodiment 8
Sanguis Draxonis phosphatide complexes preparation of soft capsule:
Prescription:
Sanguis Draxonis phosphatide complexes (making) 200g by embodiment 3 methods
PEG400?????????????????????????????????????????????50g
Cera Flava 70g
Make 1000
Method for making: take by weighing Sanguis Draxonis phosphatide complexes, PEG400, Cera Flava according to preparation prescription, place colloid mill to be ground into ointment shape suspended matter, be pressed into 1000, promptly.
Embodiment 8
Sanguis Draxonis phosphatide complexes preparation of soft capsule:
Prescription:
Sanguis Draxonis phosphatide complexes (making) 300g by embodiment 3 methods
PEG6000????????????????????????????????????????????100g
Cera Flava 75g
Make 1000
Method for making: take by weighing Sanguis Draxonis phosphatide complexes, PEG6000, Cera Flava according to preparation prescription, place colloid mill to be ground into ointment shape suspended matter, be pressed into 1000, promptly.
Claims (9)
1, a kind of Sanguis Draxonis phosphatide complexes is characterized in that containing Sanguis Draxonis or the Sanguis Draxonis extract of 20-80%, and remaining component is a phospholipid.
2, complex according to claim 1 is characterised in that phospholipid is natural or synthetic phospholipid, comprises lecithin, phosphatidylcholine, Phosphatidylserine, phosphatidyl ethanol ammonia.
3, Sanguis Draxonis phosphatide complexes according to claim 1, being characterized as described phospholipid is phosphatidylcholine.
4, Sanguis Draxonis phosphatide complexes according to claim 1, the source that it is characterized in that Sanguis Draxonis are the resin of babassu Sanguis Draxonis, the natural resin of Liliaceae Dracaena cochinchinensis, the natural resin of Liliaceae Hainan Folium Dracaenae cambodianae.
5, Sanguis Draxonis phosphatide complexes according to claim 1 is characterized in that stating Sanguis Draxonis extract and refers to the extract that obtains after Sanguis Draxonis extracts with following solvent, and extraction solvent is selected from methanol, ethanol, propanol, butanols, ethyl acetate and acetone.
6, according to the described Sanguis Draxonis phosphatide complexes of claim 1, its peroral dosage form is selected from tablet, soft capsule, hard capsule.
7, Sanguis Draxonis phosphatide complexes according to claim 6 is characterized in that described oral formulations dosage form is a soft capsule, and this soft capsule content is formed according to following ratio, Sanguis Draxonis phosphatide complexes: dispersant: stabilizing agent=1-10: 2-20: 0.1-5.
8, according to the described Sanguis Draxonis phosphatide complexes of claim 7, the dispersant that it is characterized in that the soft capsule made by the Sanguis Draxonis phosphatide complexes is selected from vegetable oil, hydrogenated vegetable oil or polyethylene glycols, and vegetable oil is selected from one or more in soybean oil, Oleum Arachidis hypogaeae semen, Petiolus Trachycarpi oil, Oleum Cocois, Semen Maydis oil, Oleum Camelliae, Oleum sesami, olive oil, the Oleum Camelliae; Hydrogenated vegetable oil is selected from one or more in oil with hydrogenated soybean, hydrogenated groundnut, hydrogenated palm oil, hydrogenated coconut oil, hydrogenated corn oil, hydrogenation Oleum Camelliae, hydrogenation Oleum sesami, hydrogenation olive oil, the hydrogenation Oleum Camelliae; Polyethylene Glycol is selected from PEG-400 or PEG-6000.
9, Sanguis Draxonis phosphatide complexes according to claim 7 is characterized in that the stabilizing agent of the soft capsule made by the Sanguis Draxonis phosphatide complexes is a Cera Flava.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410046367 CN1583139A (en) | 2004-06-08 | 2004-06-08 | Preparation of dragon's blood and phospholipin composition |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410046367 CN1583139A (en) | 2004-06-08 | 2004-06-08 | Preparation of dragon's blood and phospholipin composition |
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| CN1583139A true CN1583139A (en) | 2005-02-23 |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579737A (en) * | 2012-02-29 | 2012-07-18 | 泰山医学院 | Dragon blood nano medicament crystallized preparation and preparation method thereof |
| CN103751798A (en) * | 2014-01-27 | 2014-04-30 | 江苏健佳药业有限公司 | Silybin-phospholipid complex and preparation method thereof |
| CN103751785A (en) * | 2014-01-27 | 2014-04-30 | 江苏健佳药业有限公司 | Silymarin-phospholipid complex and preparation method thereof |
| CN103751799A (en) * | 2014-01-27 | 2014-04-30 | 江苏健佳药业有限公司 | Phospholipid complex of silybum marianum extract and preparation method for phospholipid complex |
-
2004
- 2004-06-08 CN CN 200410046367 patent/CN1583139A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579737A (en) * | 2012-02-29 | 2012-07-18 | 泰山医学院 | Dragon blood nano medicament crystallized preparation and preparation method thereof |
| CN102579737B (en) * | 2012-02-29 | 2014-12-10 | 泰山医学院 | Dragon blood nano medicament crystallized preparation and preparation method thereof |
| CN103751798A (en) * | 2014-01-27 | 2014-04-30 | 江苏健佳药业有限公司 | Silybin-phospholipid complex and preparation method thereof |
| CN103751785A (en) * | 2014-01-27 | 2014-04-30 | 江苏健佳药业有限公司 | Silymarin-phospholipid complex and preparation method thereof |
| CN103751799A (en) * | 2014-01-27 | 2014-04-30 | 江苏健佳药业有限公司 | Phospholipid complex of silybum marianum extract and preparation method for phospholipid complex |
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