CN1615995A - Cyclodextrin super molecular composition of Chinese medicine giant knutweed rhizome and its preparing method - Google Patents
Cyclodextrin super molecular composition of Chinese medicine giant knutweed rhizome and its preparing method Download PDFInfo
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- CN1615995A CN1615995A CN200410064797.8A CN200410064797A CN1615995A CN 1615995 A CN1615995 A CN 1615995A CN 200410064797 A CN200410064797 A CN 200410064797A CN 1615995 A CN1615995 A CN 1615995A
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Abstract
The super-molecular cyclodextrin-giant knotweed composition is inclusion compound or 5-15 kinds of de-clathrated effective giant knotweed components. The ratio between Chinese medicine giant knotweed and cyclodextrin is 1 to 3-20. The composition is prepared through mixing water solution or suspension of cyclodextrin with medicine powder or coarse extractive in the amount of 1/20-1/3 cyclodextrin weight, filtering, water washing or extracting, evaporating to eliminate solvent and drying. The coarse extractive is obtained with giant knotweed powder and through refluxing in non-toxic organic solvent, filtering and evaporating to eliminate solvent. The present invention has purified active component and raised medicine component content.
Description
Technical Field
The invention relates to a traditional Chinese medicine preparation, in particular to a cyclodextrin supermolecule composition of a traditional Chinese medicine giant knotweed and a preparation method of the composition.
Background
Rhizoma Polygoni Cuspidati, also known as herba Hedyotidis Diffusae, radix Dactylicapni, radix Sophorae Flavescentis, herba Swertiae Bimaculatae, and herba Polygoni Cuspidati. Is dried rhizome and root of Polygonum cuspidatum of Polygonaceae. Is a perennial herb. The stem is upright and hollow, red or purple-red spots are scattered on the surface, and the node is slightly enlarged. Alternate leaves, oval or ovoid. Evaluation of plum-season: "cane for its stem, tiger for its macula". It mostly occurs in the groves, sides of rivers and under-forest yin-temperature areas. Is distributed in the southern part of the Yangtze river in China and in the provinces of Shaanxi, Henan, Shandong, etc.
Hu Zhang is slightly cold in nature and slightly bitter in taste. The traditional functions are clearing heat and promoting diuresis, promoting blood circulation and relieving pain, relaxing bowels and detoxifying, relieving cough and reducing sputum. As recorded in the famous physicians' bibliographic record, Hu Zhang is named as Shu Li Yue Shu and breaks the blood stagnation. Modern pharmacological research shows that giant knotweed contains mainly free anthraquinone derivatives including emodin, physcion, chrysophanol, etc., emodin-8-glucoside, physcion-8-glucoside, polydatin, condensed tannin, several kinds of polysaccharide, etc.
In vitro tests prove that the giant knotweed decoction (25 percent) and the polydatin have the inhibition effect on staphylococcus aureus, proteus, pseudomonas aeruginosa, typhoid bacillus, shigella flexneri and the like; the 10% water decoction of rhizoma Polygoni Cuspidati has inhibitory effect on influenza virus, orphan virus, and herpes simplex virus. In recent years, researches on giant knotweed rhizome show that the giant knotweed rhizome has unique effects on diminishing inflammation and resisting infection and is widely applied to various inflammatory diseases. Modern researches and developments of a single Chinese patent medicine of giant knotweed: the detoxifying lipid-lowering tablet (pharmacopoeia standard number: WS3-B-2812-97) has the functions of clearing away heat and toxic material, removing dampness by diuresis, raising white blood cells and lowering blood fat. Can be used for treating acute and chronic hepatitis, chronic bronchitis and rheumatic arthritis; can be used for treating hyperlipidemia, and leukopenia caused by chemotherapy and radiotherapy. However, the medicinal components are crude extracts, the content is low, the composition is complex, the quality is difficult to control, and the medicinal effect is unstable.
The experimental research on the anti-endotoxin of giant knotweed and various decoctions thereof and the anti-inflammation of mice has not been reported.
Disclosure of Invention
The invention belongs to a novel technical method for modernization of traditional Chinese medicine technology. The method adopts a supermolecule preparation method of the inclusion compound to obtain the composition with stable components, and achieves the purposes of purifying the active ingredients of the traditional Chinese medicine and improving the content of the medicinal ingredients by a simple technical process. The novel Chinese patent medicine with good curative effect, controllable quality, simple preparation and convenient taking is created. Meanwhile, the purpose of improving the quality of the existing giant knotweed Chinese patent medicine preparation and the analysis method thereof can be achieved.
Cyclodextrins and their derivatives are new pharmaceutical materials that have developed relatively rapidly in recent years and are widely used to improve pharmaceutical formulations. The separation and extraction of the traditional Chinese medicine components is not reported in documents at present.
The invention adopts novel molecular microcapsule material beta-cyclodextrin (beta-CD) or hydroxypropyl-beta-cyclodextrin (HP-beta-CD) or sulfobutylether-beta-cyclodextrin (SBE-beta-CD) to react with giant knotweed medicinal material, and extracts and separates giant knotweed effective components from a plurality of complex components by generating a supermolecule inclusion compound to prepare the medicinal composition containing a plurality of active components.
The giant knotweed rhizome single traditional Chinese medicinal material is respectively mixed with beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin or sulfobutylether-beta-cyclodextrin and other medicinal cyclodextrin derivatives in a certain proportion under specific conditions, or water, alcohol extract or water extraction and alcohol precipitation extract of the medicinal material is mixed with the cyclodextrin and the derivatives, the cyclodextrin and the derivatives and partial components thereof form super molecular bodies, and the cyclodextrin-medicinal component compound is obtained through separation and purification treatment. The composition contains about 5-15 different compounds, has stable content and composition, and has strong activity in resisting endotoxin, bacteria, inflammation and other diseases. The supermolecule composition obtained by the method can be directly administrated, can be used for creating a novel Chinese medicinal preparation, and can also be used for analyzing specific components of a Chinese patent medicament containing the giant knotweed rhizome and improving the quality standard of the existing Chinese patent medicament.
The specific scheme of the invention is as follows.
A cyclodextrin supermolecule composition of a traditional Chinese medicine giant knotweed comprises the traditional Chinese medicine giant knotweed and cyclodextrin, the ratio of the traditional Chinese medicine giant knotweed and the cyclodextrin is 1: 20-1: 3, the composition is obtained by adding medicinal material powder or crude extract with the mass ratio of 1/20-1/3 into aqueous solution or suspension of the cyclodextrin, mixing, stirring, filtering, washing or extracting with water, evaporating to remove a solvent and drying; wherein the crude extract is obtained by refluxing the medicinal powder of the traditional Chinese medicine giant knotweed with a nontoxic or low-toxic organic solvent, filtering and evaporating the organic solvent.
The cyclodextrin supermolecule composition of the traditional Chinese medicine giant knotweed rhizome is in the form of an inclusion compound (the composition comprises 5-15 effective components of the traditional Chinese medicine giant knotweed rhizome and cyclodextrin) or 5-15 effective components of the traditional Chinese medicine giant knotweed rhizome after the inclusion compound is removed.
The cyclodextrin in the above composition is preferably beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin or sulfobutylether-beta-cyclodextrin.
The nontoxic or low toxic organic solvent is preferably ethanol, ethyl acetate, propanol or a mixture of two or more of the above.
The composition can be used alone as medicine, or used as raw material to make into tablet, capsule, etc., and various adjuvants can be added according to the existing pharmaceutical technology.
Through separation and identification, the supermolecule composition is proved to mainly contain compounds such as emodin, physcion, chrysophanol, emodin-8-glucoside, physcion-8-glucoside and resveratrol, and the content of the compounds with determined structures is more than 95%.
The preparation method of the cyclodextrin supramolecular composition of the traditional Chinese medicine giant knotweed comprises the following steps:
supermolecule of giant knotweed medicinal materials: pulverizing rhizoma Polygoni Cuspidati, and sieving to obtain medicinal powder; or,
refluxing the medicinal powder with nontoxic or low-toxic organic solvent, filtering, and evaporating to remove organic solvent to obtain crude extract;
mixing cyclodextrin with 1-20 times of pure water to obtain suspension or solution, adding 1/20-1/3 weight parts of medicinal powder or crude extract, mixing, stirring, filtering, washing with water or extracting, evaporating to remove solvent, and drying to obtain light-colored solid (composition).
The more optimized and more specific steps of the preparation method are as follows:
supermolecule of giant knotweed medicinal materials:
pulverizing the raw materials according to conventional method, and sieving to obtain medicinal powder; or,
refluxing the medicinal powder with nontoxic or low-toxic organic solvent such as ethanol, ethyl acetate, propanol, etc., filtering, and evaporating to remove organic solvent to obtain crude extract;
mixing beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin or sulfobutyl ether-beta-cyclodextrin with 1-20 times of pure water to form suspension or solution, adding 1/20-1/3 mass percent of medicinal powder or crude extract, fully mixing, stirring for 0.5-15 hours, filtering, washing or extracting with water, evaporating to remove solvent, and drying to obtain light-colored solid (composition).
The method can also be added with the following steps:
and (4) separating the inclusion compound and removing the cyclodextrin.
The invention has the advantages that:
the medicine components and contents are stable: the beta-cyclodextrin or the derivative of the inclusion material and specific chemical components in the Chinese medicinal materials form a super molecular body (inclusion compound), the number of the included chemical components is basically constant, and the relative content of each component is basically stable. The components of the obtained composition are clear and the quality of the composition is controllable.
The supramolecular composition has strong activity: in vitro endotoxin test demonstrated that the composition samples had strong endotoxin-destroying and antibacterial activity, with 95% endotoxin destruction at doses lower than the positive control polymyxin B. Anti-inflammatory experiments in mice prove that the composition sample is superior to the anti-inflammatory effects of the detoxification lipid-lowering tablet (giant knotweed rhizome standard prescription) and the Shuanghuanglian oral liquid. The detoxicating lipid-lowering tablet is the crude extract of single-ingredient giant knotweed rhizome water extraction.
Anti-inflammatory test results in mice (P < 0.05)
| Sample | Inhibition rate |
| Shuanghuanglian oral liquid (contrast) | 26.6％ |
| Composition comprising a metal oxide and a metal oxide | 28.1％ |
| Detoxicating hypolipemic tablet (contrast) | 26.3％ |
The working principle and the working process are as follows: the key of the technology of the invention is the inclusion compound and the preparation of the inclusion compound.
The inclusion principle is as follows:
the molecular microcapsule material beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin or sulfobutylether-beta-cyclodextrin and specific molecules of the traditional Chinese medicine giant knotweed form stable super molecular bodies (inclusion compounds), the inclusion compounds and other non-included molecules have different physical properties, and the inclusion compounds and other non-included molecules can be separated by adopting other simple methods, thereby achieving the purpose of purifying the effective components of the giant knotweed.
Molecules of active ingredients that can be included into cyclodextrins must possess the appropriate spatial dimensions (into the cyclodextrin) and weak forces that can form hydrophobic bonds with the cyclodextrin, FDW forces, hydrogen bonds, etc. Thereby enabling stable binding with cyclodextrin.
The apparent stability constant of the clathrate of active ingredient of rhizoma Polygoni Cuspidati combined with cyclodextrin is about 102-103M-1It is usually not dissociated by a solvent under the conditions, and is not dissociated by heating under a solid. And thus can be separated from other non-included molecules.
The generated inclusion compound is verified by UV, X-ray and DSC spectra; the energy advantage of the inclusion compound is verified by a computer MM + calculation program; apparent inclusion constants were determined by electron spectroscopy; the inclusion compound has a specific composition formed by further separating into monomer compounds after dissociation, and the structure of each compound is formed by1The HNMR, IR, MS and control methods were validated. The content of each compound in the composition was determined by HPLC.
The invention points of the invention:
the giant knotweed rhizome traditional Chinese medicine material is directly prepared into the super molecular body (inclusion compound) with the cyclodextrin.
The giant knotweed rhizome is extracted by organic solvent, reacts with cyclodextrin, and is purified to prepare the super molecular body (inclusion compound).
The composition in the clathrate contains 5-15 components of rhizoma Polygoni Cuspidati, such as emodin.
The obtained composition has strong antibacterial and anti-inflammatory activity.
Simple operation and high efficiency: the invention uses beta-cyclodextrin or derivatives as basic materials, is supplemented with common low-toxicity or nontoxic organic solvents, has low requirements on separation operation conditions and equipment, and has good separation effect.
The supermolecule prepared traditional Chinese medicine composition has stable composition and content, high purity, less impurities and good appearance.
Detailed Description
Example 1, the preparation of the present composition was carried out following the procedure:
giant knotweed rhizome medicinal powder and cyclodextrin → inclusion compound
Pulverizing the raw materials, and sieving to obtain medicinal powder.
Mixing beta-cyclodextrin with pure water of 20 times to obtain suspension or solution, adding medicinal powder of 1/3 weight parts, mixing thoroughly, stirring for 0.5-15 hours, filtering, washing with water or extracting, evaporating to remove solvent, and drying to obtain light-colored solid (composition).
Example 2 substantially the same as example 1, except that hydroxypropyl- β -cyclodextrin was mixed with 1-fold amount of pure water to form a suspension or solution, and 1/20 mass ratio of the medicinal powder was added.
Example 3, basically the same as example 1, but the sulfobutyl ether-beta-cyclodextrin was mixed with 10 times the amount of pure water to form a suspension or solution, and the amount of the medicinal material powder was added in a mass ratio of 1/10.
Example 4, the preparation of the present composition was carried out following the procedure described below,
giant knotweed rhizome medicinal material powder and solvent → extract → cyclodextrin → inclusion compound ═ composition
Pulverizing the raw materials, sieving to obtain medicinal powder, refluxing the medicinal powder with ethanol, filtering, and steaming to remove ethanol to obtain crude extract.
Mixing beta-cyclodextrin with 10 times of pure water to form suspension or solution, adding 1/20 mass percent of medicinal powder or crude extract, fully mixing, stirring for 0.5-15 hours, filtering, washing with water or extracting, evaporating to remove solvent, and drying to obtain light-colored solid (composition).
Example 5, essentially the same as example 4, but employing ethyl acetate as the non-toxic or low-toxic organic solvent to reflux the drug powder. The cyclodextrin is hydroxypropyl-beta-cyclodextrin mixed with 1 time of pure water.
Example 6, essentially the same as example 4, but employing propanol as the non-toxic or low-toxic organic solvent for the refluxing powder. The cyclodextrin is prepared by mixing sulfobutyl ether-beta-cyclodextrin with 10 times of pure water.
Example 7, basically the same as example 4, but the nontoxic or low toxic organic solvent used to reflux the powder was a mixture of ethanol and ethyl acetate.
Example 8, basically the same as example 4, but the nontoxic or low toxic organic solvent of the reflux medicinal powder is a mixture of ethyl acetate and propanol.
Example 9 is substantially the same as example 4, except that the nontoxic or low toxic organic solvent for refluxing the medicinal powder is a mixture of ethanol, ethyl acetate and propanol.
Example 10, essentially the same as the above example, but with the addition of the following steps:
and (4) separating the inclusion compound and removing the cyclodextrin. To obtain 5-15 effective components of Chinese medicine giant knotweed rhizome.
Claims (7)
1. A cyclodextrin supermolecule composition of a traditional Chinese medicine giant knotweed rhizome comprises the traditional Chinese medicine giant knotweed rhizome and cyclodextrin, the ratio of the traditional Chinese medicine giant knotweed rhizome to the cyclodextrin is 1: 20-1: 3, the composition is obtained by adding medicinal material powder or crude extract with the mass ratio of 1/20-1/3 into aqueous solution or suspension of the cyclodextrin, mixing, stirring, filtering, washing or extracting with water, evaporating to remove a solvent and drying; wherein the crude extract is obtained by refluxing the medicinal powder of the traditional Chinese medicine giant knotweed with a nontoxic or low-toxic organic solvent, filtering and evaporating the organic solvent.
2. The cyclodextrin supramolecular composition of the traditional Chinese medicine giant knotweed rhizome according to claim 1, which is characterized in that: the cyclodextrin is beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin or sulfobutylether-beta-cyclodextrin.
3. The cyclodextrin supramolecular composition of the traditional Chinese medicine giant knotweed rhizome according to claim 1 or 2, which is characterized in that: the composition also contains emodin, physcion, chrysophanol, emodin-8-glucoside, physcion-8-glucoside, resveratrol, polydatin, etc. which are unique to Chinese medicine giant knotweed.
4. The cyclodextrin supramolecular composition of the traditional Chinese medicine giant knotweed rhizome according to claim 1, 2 or 3, which is characterized in that: the nontoxic or low toxic organic solvent is ethanol, ethyl acetate, propanol, or a mixture of two or more of them.
5. A method for preparing cyclodextrin supramolecular composition of the traditional Chinese medicine giant knotweed rhizome in claim 1 comprises the following steps: supermolecule of giant knotweed medicinal materials: pulverizing rhizoma Polygoni Cuspidati, and sieving to obtain medicinal powder; or,
refluxing the medicinal powder with nontoxic or low-toxic organic solvent, filtering, and evaporating to remove organic solvent to obtain crude extract;
and mixing the cyclodextrin or the cyclodextrin and 1-20 times of pure water to form suspension or solution, adding 1/20-1/3 mass percent of medicinal powder or crude extract, mixing, stirring, filtering, washing or extracting with water, evaporating to remove the solvent, and drying to obtain the light-colored solid composition.
6. The method for preparing the cyclodextrin supramolecular composition of the traditional Chinese medicine giant knotweed rhizome according to claim 5, which is characterized in that the specific operations of the steps are as follows:
supermolecule of giant knotweed medicinal materials:
pulverizing the raw materials according to conventional method, and sieving to obtain medicinal powder; or,
refluxing the medicinal powder with nontoxic or low-toxic organic solvent such as ethanol, ethyl acetate, propanol, etc., filtering, and evaporating to remove organic solvent to obtain crude extract;
mixing beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin or sulfobutyl ether-beta-cyclodextrin with 1-20 times of pure water to form suspension or solution, adding 1/20-1/3 mass percent of medicinal material powder or crude extract, fully mixing, stirring for 0.5-15 hours, filtering, washing or extracting with water, evaporating to remove a solvent, and drying to obtain the light-colored solid composition.
7. The method for preparing the cyclodextrin supramolecular composition of the traditional Chinese medicine giant knotweed rhizome according to claim 5 or 6, which is characterized by further comprising the following steps:
and (3) performing de-clathration, and removing cyclodextrin to obtain 5-15 effective components of rhizoma Polygoni Cuspidati.
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| CN105561327A (en) * | 2016-01-21 | 2016-05-11 | 南京师范大学 | Beta-cyclodextrin-panax notoginseng micro powder composition and preparing method and preparation thereof |
| CN105561328A (en) * | 2016-01-21 | 2016-05-11 | 南京呈鼎生物科技有限公司 | Cyclodextrin containing marigold flower micro powder and preparation method and application thereof |
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| CN1513822A (en) * | 2002-12-31 | 2004-07-21 | 庸 曹 | Technology of extracting high purity resveratrol from polygonoum cuspidatum |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105561327A (en) * | 2016-01-21 | 2016-05-11 | 南京师范大学 | Beta-cyclodextrin-panax notoginseng micro powder composition and preparing method and preparation thereof |
| CN105561328A (en) * | 2016-01-21 | 2016-05-11 | 南京呈鼎生物科技有限公司 | Cyclodextrin containing marigold flower micro powder and preparation method and application thereof |
| CN105903033A (en) * | 2016-06-21 | 2016-08-31 | 重庆医科大学 | Resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound and preparing method thereof |
| CN107637593A (en) * | 2016-07-22 | 2018-01-30 | 四川利尔作物科学有限公司 | The bactericidal composition of controlling plant diseases and its application |
| CN107468771A (en) * | 2017-10-11 | 2017-12-15 | 南京仙草堂生物科技有限公司 | It is a kind of to treat Traditional Chinese medicine lozenge of chill and preparation method thereof |
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| CN100344300C (en) | 2007-10-24 |
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