CN102349938A - Saussurea involucrate extractive carrier compound and preparation method thereof - Google Patents
Saussurea involucrate extractive carrier compound and preparation method thereof Download PDFInfo
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- CN102349938A CN102349938A CN2011103217026A CN201110321702A CN102349938A CN 102349938 A CN102349938 A CN 102349938A CN 2011103217026 A CN2011103217026 A CN 2011103217026A CN 201110321702 A CN201110321702 A CN 201110321702A CN 102349938 A CN102349938 A CN 102349938A
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Abstract
The invention relates to a saussurea involucrate extractive carrier compound and a preparation method thereof. The compound comprises 1-20 parts of saussurea involucrate extractive and 10-90 parts of auxiliary material which contains phospholipid and 1-20 parts of surfactant. The preparation method includes the following steps: dissolving the saussurea involucrate extractive, the auxiliary material and the surfactant, at the mass-to-volume ratio of 6:1-3:1, in 95% ethanol or absolute ethyl alcohol to form an organic phase; selecting phosphate buffer with pH value of 6.8, 7.0, 7.4, 7.8 or 8.0 to form a water phase, wherein the volume ratio of the organic phase to the water phase is 1:2-1:8; and injecting the organic phase to the water phase and blending under the rotating speed of 300-700r/min for 20-80 minutes. A transparent system, i.e. a saussurea involucrate carrier, can be formed while blending. The preparation method of the saussurea involucrate carrier is simple, the encapsulating efficiency is high, the encapsulating efficiency of flavonoid components in the saussurea involucrate extractive, based on calculation of rutin, is 75-96%, and the encapsulating efficiency of phenylpropanoid components in the saussurea involucrate extractive, based on calculation of chlorogenic acid, is 70-95%.
Description
Technical field
The present invention relates to a kind of Herba Saussureae Involueratae extract carrier composition and method of making the same.
Background technology
Herba Saussureae Involueratae is the geographic important medicinal plants of the western high mountain of China; It is Tibetan medicine Mongolian medicine Uygur medicine a kind of ethnic drug commonly used; Its " function of warm in nature, little hardship, expelling wind and dampness " beginning is shown in Tibetan medicine document " month king's medicine is precious ", and is also on the books at Qing Dynasty's supplementary Amplifications of the Compendium of Materia Medica and " Xinjiang Chinese herbal medicine ".Mainly be distributed in Xinjiang of China Tianshan Mountains and Kun Lun Mountain one band, be grown in more than the snow line.Among the people with all herbal medicine, warm in nature, mildly bitter flavor is gone into liver,spleen,kidney three warps, and function such as have warming the kidney to activate YANG, expelling wind and dampness, restore menstrual flow and invigorate blood circulation is used to treat rheumatism numbness pain, rheumatoid arthritis, cold and pain in the lower abdomen, diseases such as menoxenia.Because its important medical value becomes the object that people pay close attention to and study for many years always.
Herba Saussureae Involueratae has been carried out deep research both at home and abroad, mainly contained phenylpropyl alcohol element, flavone, alkaloid, terpenoid, lactone, polysaccharide, volatile oil chemical constituent in the Herba Saussureae Involueratae, the modern pharmacology experiment shows that flavone, phenylpropyl alcohol element are main active in the Herba Saussureae Involueratae.
Preparation capable of permeating skin is meant in the skin surface administration, makes medicine pass through the novel form that skin produces whole body or local therapeutic effects.Transdermal absorption formulation and the administration of traditional Chinese medical science acupuncture point have play the same tune on different musical instruments wonderful, all are to utilize skin as medicine input body circulation door, the effect of performance Drug therapy.After occurring the eighties in 20th century, cause the very big interest of medical market, become domestic and international medical worker's research focus in recent years.
Therefore, be foundation with Herba Saussureae Involueratae clinical practice basis, in conjunction with the pharmacological effect effect of Herba Saussureae Involueratae, the high new formulation of preparation compliance is the important channel of Herba Saussureae Involueratae being processed a kind of new-type traditional Chinese anti-inflammatory preparation.
Carrier (transfersomes; TF) be a kind of self aggregation vesicle; Its main constituent is phospholipid and surfactant (like sodium cholate, sodium deoxycholate etc.); Also being called flexible nano liposome (ultradeformable liposomes), is the newtype drug transdermal penetration carrier that a kind of transdermal effect more is better than liposome.
The Chinese patent Granted publication is number for CN101209274B discloses a kind of Herba Saussureae Involueratae extract and production method thereof, but this patent does not provide a kind of dosage form that supplies the Herba Saussureae Involueratae extract transdermal administration to the drug action of active component in the Herba Saussureae Involueratae extract; The Chinese patent notification number is that CN101890067A discloses a kind of anti-inflammatory and analgesic snow lotus gel and preparation method thereof; Be that the direct dispersing and mixing of Herba Saussureae Involueratae extract is prepared from the substrate of gel; Do not adopt pharmaceutical preparations to learn the processed that the transdermal technology is carried out Herba Saussureae Involueratae extract; Very limited because of the transdermal of medicine simultaneously, need in the gel prescription to realize transdermal through adding penetration enhancer.The Chinese patent notification number is the production method that CN101209274A discloses a kind of saussurea involucrata catablasm, is Herba Saussureae Involueratae extract to be dispersed in molding is prepared from the catablasm base material, is to realize transdermal, has also added Percutaneous absorption enhancer in the molding prescription.
Therefore, adopt carrier pharmaceutics technology, through the research of carrier preparation technology and prescription, preparation Herba Saussureae Involueratae carrier can reach the purpose that realizes effective transdermal, and need not realize transdermal through adding Percutaneous absorption enhancer.
Summary of the invention
The objective of the invention is to, a kind of Herba Saussureae Involueratae extract carrier composition and method of making the same is provided.
The objective of the invention is to realize like this:
It is that 1～20 part Herba Saussureae Involueratae extract and weight portion is the adjuvant of 0～90 part of phosphatidase 11 that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 1～20 part surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: soybean lecithin, Ovum Gallus domesticus Flavus lecithin at least a; Surfactant is: sodium cholate, sodium deoxycholate at least a.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant were dissolved in 95% ethanol or the dehydrated alcohol by the feed liquid mass volume ratio in 6: 1～3: 1 constitute organic facies; It is a kind of formation water in 6.8,7.0,7.4,7.8 and 8.0 the phosphate buffer that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 2～1: 8, organic facies is injected aqueous phase stir, and speed of agitator is 300～700 rev/mins, and mixing time is 20～80 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Herba Saussureae Involueratae extract carrier provided by the invention is a kind of preparation technique of Herba Saussureae Involueratae extract processing; With this Herba Saussureae Involueratae carrier during through the external administration; Can effectively promote the transdermal of effective ingredient in the extract; Show in the experiment of Herba Saussureae Involueratae carrier transdermal test in vitro; Flavones ingredient in rutin is 50%～80% in 24 hours accumulation of rat skin in vitro through percentage rate, and seeing through percentage rate in the plain constituents of the phenylpropyl alcohol of chlorogenic acid in 24 hours accumulation of rat skin in vitro is 40%～70%.Can also be prepared into cataplasma, gel or ointment with Herba Saussureae Involueratae extract carrier compositions through known method.
The method for preparing of Herba Saussureae Involueratae carrier involved in the present invention is simple, particle size distribution is 10～1000nm; And has higher entrapment; Envelop rate in the flavones ingredient of rutin in the Herba Saussureae Involueratae extract is 75～96%, is 70～95% in the envelop rate of the plain constituents of phenylpropyl alcohol of chlorogenic acid.
The specific embodiment
Embodiment 1: it is that 1 part Herba Saussureae Involueratae extract and weight portion is the adjuvant of 0 part of phosphatidase 11 that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 1 part surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: soybean lecithin; Surfactant is: sodium cholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in 95% ethanol by the feed liquid mass volume ratio at 6: 1 constitute organic facies; It is 6.8 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 2, organic facies is injected aqueous phase stir, and speed of agitator is 300 rev/mins, and mixing time is 20 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 2: it is that 20 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 90 parts in phospholipid that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 20 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: Ovum Gallus domesticus Flavus lecithin; Surfactant is: sodium deoxycholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in by the feed liquid mass volume ratio at 3: 1 constitute organic facies in the dehydrated alcohol; Phosphate buffer is selected from pH 8.0 and constitutes water; Organic facies and water volume ratio are 1: 8, organic facies is injected aqueous phase stir, and speed of agitator is 700 rev/mins, and mixing time is 80 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 3: it is that 10 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 0 part of phosphatidase 15 that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 10 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: soybean lecithin; Surfactant is: sodium cholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in 95% ethanol by the feed liquid mass volume ratio at 5: 1 constitute organic facies; It is 7.4 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 5, organic facies is injected aqueous phase stir, and speed of agitator is 500 rev/mins, and mixing time is 50 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 4: it is that 5 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 0 part of phosphatidase 13 that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 5 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: Ovum Gallus domesticus Flavus lecithin; Surfactant is: sodium deoxycholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in by the feed liquid mass volume ratio at 5: 1 constitute organic facies in the dehydrated alcohol; It is 7.0 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 4, organic facies is injected aqueous phase stir, and speed of agitator is 400 rev/mins, and mixing time is 30 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 5: it is that 15 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 80 parts in phospholipid that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 15 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: soybean lecithin; Surfactant is: sodium cholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in 95% ethanol by the feed liquid mass volume ratio at 4: 1 constitute organic facies; It is 7.4 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 7, organic facies is injected aqueous phase stir, and speed of agitator is 600 rev/mins, and mixing time is 70 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 6: it is that 12 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 0 part of phosphatidase 16 that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 12 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: Ovum Gallus domesticus Flavus lecithin; Surfactant is: sodium deoxycholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in 95% ethanol by the feed liquid mass volume ratio at 4: 1 constitute organic facies; It is 7.4 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 6, organic facies is injected aqueous phase stir, and speed of agitator is 400 rev/mins, and mixing time is 40 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 7: it is that 8 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 0 part of phosphatidase 16 that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 8 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: soybean lecithin; Surfactant is: sodium deoxycholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in by the feed liquid mass volume ratio at 3: 1 constitute organic facies in the dehydrated alcohol; It is 7.0 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 6, organic facies is injected aqueous phase stir, and speed of agitator is 500 rev/mins, and mixing time is 50 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 8: it is that 18 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 70 parts in phospholipid that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 18 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: Ovum Gallus domesticus Flavus lecithin; Surfactant is: sodium cholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in 95% ethanol by the feed liquid mass volume ratio at 6: 1 constitute organic facies; It is 8.0 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 7, organic facies is injected aqueous phase stir, and speed of agitator is 600 rev/mins, and mixing time is 70 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 9: it is that 2 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 0 part of phosphatidase 12 that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 2 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: soybean lecithin; Surfactant is: sodium deoxycholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in by the feed liquid mass volume ratio at 4: 1 constitute organic facies in the dehydrated alcohol; It is 6.8 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 3, organic facies is injected aqueous phase stir, and speed of agitator is 400 rev/mins, and mixing time is 30 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 10: it is that 11 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 5 parts of phosphatidase 11s that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 11 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: Ovum Gallus domesticus Flavus lecithin; Surfactant is: sodium cholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in 95% ethanol by the feed liquid mass volume ratio at 5: 1 constitute organic facies; It is 7.4 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 6, organic facies is injected aqueous phase stir, and speed of agitator is 500 rev/mins, and mixing time is 50 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 11: it is that 19 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 80 parts in phospholipid that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 19 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: soybean lecithin; Surfactant is: sodium cholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in 95% ethanol by the feed liquid mass volume ratio at 4: 1 constitute organic facies; It is 8.0 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 7, organic facies is injected aqueous phase stir, and speed of agitator is 600 rev/mins, and mixing time is 60 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 12: it is that 3 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 0 part of phosphatidase 13 that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 3 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: soybean lecithin; Surfactant is: sodium cholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in by the feed liquid mass volume ratio at 4: 1 constitute organic facies in the dehydrated alcohol; It is 7.4 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 4, organic facies is injected aqueous phase stir, and speed of agitator is 400 rev/mins, and mixing time is 40 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Embodiment 13: it is that 14 parts Herba Saussureae Involueratae extract and weight portion is the adjuvant of 0 part of phosphatidase 16 that the Herba Saussureae Involueratae carrier comprises weight portion; Adjuvant is that 13 parts surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: Ovum Gallus domesticus Flavus lecithin; Surfactant is: sodium deoxycholate.
Herba Saussureae Involueratae carrier preparation method of composition may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant are dissolved in 95% ethanol by the feed liquid mass volume ratio at 6: 1 constitute organic facies; It is 7.0 formation waters that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 4, organic facies is injected aqueous phase stir, and speed of agitator is 600 rev/mins, and mixing time is 80 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
Claims (2)
1. Herba Saussureae Involueratae extract carrier compositions, the Herba Saussureae Involueratae extract and the weight portion that it is characterized in that comprising weight portion and be 1～20 part are the adjuvant of 0～90 part of phosphatidase 11; Adjuvant is that 1～20 part surfactant is formed by phospholipid and weight portion; Said Herba Saussureae Involueratae extract is: the material that contains rutin and chlorogenic acid; Phospholipid in the carrier adjuvant is: soybean lecithin, Ovum Gallus domesticus Flavus lecithin at least a; Surfactant is: sodium cholate, sodium deoxycholate at least a.
2. Herba Saussureae Involueratae extract carrier preparation of compositions method according to claim 1 is characterized in that may further comprise the steps: Herba Saussureae Involueratae extract, phospholipid, surfactant were dissolved in 95% ethanol or the dehydrated alcohol by the feed liquid mass volume ratio in 6: 1～3: 1 constitute organic facies; It is a kind of formation water in 6.8,7.0,7.4,7.8 and 8.0 the phosphate buffer that phosphate buffer is selected from pH; Organic facies and water volume ratio are 1: 2～1: 8, organic facies is injected aqueous phase stir, and speed of agitator is 300～700 rev/mins, and mixing time is 20～80 minutes, stirs to form transparent system, promptly gets Herba Saussureae Involueratae carrier suspension.
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101209274A (en) * | 2007-12-25 | 2008-07-02 | 新疆维吾尔自治区药物研究所 | Saussurea involucrata extract and saussurea involucrata catablasm and producing method thereof |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101209274A (en) * | 2007-12-25 | 2008-07-02 | 新疆维吾尔自治区药物研究所 | Saussurea involucrata extract and saussurea involucrata catablasm and producing method thereof |
Non-Patent Citations (3)
| Title |
|---|
| 《中国新药杂志》 20060308 王弘等 新型透皮给药载体__传递体研究进展 341-344 1-2 第15卷, 第05期 * |
| 尚北城等: "传递体研究进展", 《西南国防医药》 * |
| 王弘等: "新型透皮给药载体――传递体研究进展", 《中国新药杂志》 * |
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Application publication date: 20120215 |