CN101214252B - Antiviral antibacterial medicinal composition and preparation thereof - Google Patents
Antiviral antibacterial medicinal composition and preparation thereof Download PDFInfo
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- CN101214252B CN101214252B CN200810013610XA CN200810013610A CN101214252B CN 101214252 B CN101214252 B CN 101214252B CN 200810013610X A CN200810013610X A CN 200810013610XA CN 200810013610 A CN200810013610 A CN 200810013610A CN 101214252 B CN101214252 B CN 101214252B
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Abstract
The present invention discloses an antiviral antibacterial medicine combination which contains the high-purity baicalin with the weight percentage of 2 percent to 10 percent of the high-purity baicalin , 0.1 percent to 5 percent of scutellarin and the pharmic acceptable auxiliary material with the rest quantity. The high-purity baicalin and the high-purity scutellarin are obtained by processing crude baicalin or scutellarin extract mainly by enzymolysis, absorption chromatography and crystallization technology. The baicalin and the scutellarin in the medicine combination of the present invention have high purity and low dosage and take effect fast; the medicine combination of the present invention has long effective plasma concentration lasting time, does not have non-drug-induced bad reaction and does not have drug resistance; LD50 dosage is improved by 1.5 times. The preparation has obvious curative effect at the aspects of antivirus, bacteriostasis and diminishing inflammation and also has good effect at the aspects of removing oxygen free radical and resisting biological oxygenation.
Description
Technical field
The present invention relates to antiviral and antibacterial class pharmaceutical composition and preparation method thereof, relate in particular to a kind of antiviral of high-purity baicalin and baicalin, antibiotic, anti-inflammation drugs composition and method of making the same of containing.
Background technology
Baicalin is one of medicinal ingredient in the Chinese crude drug Radix Scutellariae, mainly be present in the root, stem, leaf of Radix Scutellariae, has pharmacological action widely, as heat-clearing and toxic substances removing, antibacterial, antiinflammatory, antiviral, infection, antioxidation, antitumor, blood sugar lowering, blood pressure lowering etc., the clinical diseases such as treatment hepatitis B, viral influenza, infection, hypertension, diabetes, acquired immune deficiency syndrome (AIDS) that are mainly used in.Because the pharmacological action of baicalin is outstanding, thereby all contains this composition in many compound Chinese medicinal preparation, as oral formulations: Qingkailing granule agent, SHUANGHUANGLIAN oral liquid, YINHUANG HANPIAN etc.
Baicalin is the aglycon part of baicalin after hydrolysis, discovers that its pharmacological action is better than baicalin, and is more outstanding at aspects such as antiviral, AIDS virus resisting especially, yet because the water insoluble and poor stability of baicalin, so be difficult to effectively be utilized.
Though baicalin and baicalin are widely adopted in pharmacy at present, but the baicalin of crude drug, baicalin do not pass a test owing to production technology, ubiquity purity difference (injection stage content is only about 90%), product quality problem not up to standard, therefore often cause the injection of the flavone compound preparation of resources of Chinese medicinal herb to be prone to the property untoward reaction of many non-medicines source clinically, as phenomenons such as allergy, measles even shocks.Given this, study highly purified crude drug and preparation thereof and become the problem that the world of medicine pays much attention to.
China is the hotspot of hepatitis B disease, acquired immune deficiency syndrome (AIDS) is also rising year by year, therefore the research and development of antiviral class medicine are very urgent, add common clinically diseases such as bacterial infection, the research and development effect is fast, good effect, side effect are low has antiviral concurrently, antibiotic, anti-inflammation drugs has realistic meaning more.Test confirms that highly purified baicalin, baicalin are having its distinctive feature aspect the above-mentioned disease of treatment, though it derives from Chinese medicine, but not the Chinese medicine of general concept, the Medicine Act management aspect should belong to Western medicine in China, this Western medicine can compare favourably with antibiotics on clinical treatment, and have no drug resistance, antiviral effect is remarkable, therefore research and development contain the antiviral of high-purity baicalin and baicalin, antibiotic, anti-inflammation drugs composite preparation more helps excavating China's natural resources of Chinese medicinal materials, bring benefit to the mankind, promote the clinical value of Chinese medicine.
Summary of the invention
Of poor quality at existing baicalin, baicalin crude drug, purity is low, and its preparation easily produces the problem of untoward reaction.The purpose of this invention is to provide a kind of antiviral of high-purity baicalin and baicalin, antibiotic, anti-inflammation drugs composition and method of making the same of containing.
Antiviral antibacterial combination of the present invention is characterized in that containing the high-purity baicalin that percentage by weight is 2%-10%, the high-purity baicalin of 0.1%-5% and the acceptable accessories of surplus;
Wherein: described high-purity baicalin and high-purity baicalin are made by following step separation and purification:
Get Radix Scutellariae extract or baicalin crude product, add the distilled water of 12～20 times of its weight, add glycosidase, glycuronidase, baicalin enzyme or the flavone enzyme of its weight 0.01%～0.2% or the mixture of its any ratio again under 25 ℃～50 ℃; The pH of fully stirring and dissolving, and accent solution is 5～8; Conventional filtration removes slag, and contained in the chromatographic column of adsorbent filtrate adding, with the mixing eluent eluting of pH6～10, indicates as chromatography with baicalin and baicalin reference substance, collects baicalin and baicalin component eluent respectively; With the baicalin collected and baicalin eluent respectively the pH of regulator solution 1～4 be heated to 70 ℃～100 ℃, place, natural sedimentation is more than 24 hours, conventional filtration, the collecting precipitation thing, oven dry promptly obtains high-purity baicalin and high-purity baicalin respectively.
Wherein: described adsorbent is granularity 10～120 purpose silica gel, permutite or macroporous adsorbent resin.Described mixing eluent is that volume ratio is 1: 1～5 water: alcohol mixeding liquid or volume ratio are 1: 1～10 water: methyl alcohol mixed liquor.
Antiviral antibacterial combination of the present invention is characterized in that being prepared into said dosage form on any pharmaceutics.
Wherein: described dosage form is an injection, its preparation method is: take by weighing the high-purity baicalin of recipe quantity and the antioxidative stabilizer of baicalin and baicalin and baicalin gross weight 0.1%～8% respectively, be dissolved in the distilled water altogether, adding sodium chloride again makes solution become isosmotic solution, transferring the pH value of solution is 4～9, adopts the ultrafilter membrane ultrafiltration of 4000～10000 molecular weight, packing, sterilization promptly gets the antiviral anti-biotic injection.
Wherein: described dosage form is an oral formulations, its preparation method is: take by weighing the high-purity baicalin of recipe quantity and the antioxidative stabilizer of baicalin and baicalin and baicalin gross weight 0.1%～8% respectively, the pharmaceutically acceptable excipient that adds surplus again, mix homogeneously, make oral liquid, or make one of capsule, powder, granule, or pelletize, tabletting is made tablet.
Wherein: described dosage form is an eye drop, its preparation method is: take by weighing the high-purity baicalin of recipe quantity and the antioxidative stabilizer of baicalin and baicalin and baicalin gross weight 0.1%～8% respectively, be dissolved in the distilled water altogether, adding sodium chloride again makes solution become isosmotic solution, transferring the pH value of solution is 6～8, adopts the ultrafilter membrane ultrafiltration of 4000～10000 molecular weight, packing, sterilization promptly gets the antibiotic eye drop of antiviral.
Wherein: described dosage form is a membrane, its preparation method is: the high-purity baicalin and the baicalin that take by weighing recipe quantity respectively, the medicinal polylactic acid, carbomer, hyaluronic acid, the glycerol that add surplus are made the film material, film, cut apart, packing, sterilization promptly get antiviral antibacterial film agent medicine.
In the preparation of above-mentioned antiviral antibacterial combination preparation, described antioxidative stabilizer is one of vitamin C, sodium sulfite, sodium sulfite, vitamin E.
In the preparation of above-mentioned antiviral antibacterial combination preparation, described excipient is a filler: arbitrary proportion mixes between one of lactose, mannitol, sorbitol, starch, modified starch, dextrin, calcium sulfate, microcrystalline Cellulose or its both or the many persons; And/or binding agent: arbitrary proportion mixes between one of polyvinylpyrrolidone, hypromellose, methylcellulose, sodium carboxymethyl cellulose, starch slurry, syrup, rubber cement or its both or the many persons; And/or disintegrating agent: arbitrary proportion mixes between one of hydroxypropyl starch, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, crosslinked carboxymethyl fecula sodium, carboxymethylcellulose calcium, sodium carboxymethyl cellulose, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, soluble starch or its both or the many persons; And/or lubricant: arbitrary proportion mixes between one of magnesium stearate, calcium stearate, Polyethylene Glycol, micropowder silica gel, Pulvis Talci or its both or the many persons.
The present invention adopts adsorption technology that Radix Scutellariae extract or baicalin crude product are carried out purification, has obtained highly purified baicalin (content is 98% ± 2) and baicalin (98% ± 2) crude drug, at first from source control product quality.In preparation, add stabilizing agent and adjuvant and check on, thoroughly solved clinical application safety and effectiveness through hyperfiltration technique.For making various pharmaceutical dosage forms and laying the foundation for clinical a kind of antiviral safely and effectively, antibiotic, the anti-inflammation drugs of providing.
The ingenious homology of baicalin source baicalin and the difference of curative effect utilized of the present invention is made preparation with the various dose ratio, brings into play its two kinds of compositions advantage separately, makes few, the instant effect of its consumption.
Injection of the present invention and tablet, basis that premenstruum is a large amount of and pharmacological effect experimentation show, its distinctive feature in treatment is: the baicalin in the compositions absorbs fast, at first play a role, constantly brought into play persistent effect thereupon baicalin by the body enzyme hydrolysis, the characteristics that preparation presents are that consumption is few, produce effects is fast, the prolongation of effective blood drug concentration persistent period, median lethal dose(LD 50) doubles above, nonirritant, have no drug resistance and immunogen reaction, and good bioavailability is arranged, and pharmacological action is definite, clinical characteristics such as safe and convenient to use.
The specific embodiment
Embodiment 1
Get Radix Scutellariae extract or baicalin crude product 100 grams, 1500 milliliters of adding distil waters, add glycosidase 1 gram stirring and dissolving under 50 ℃, transferring the pH of solution is 5, filter and remove residue, contained in the chromatographic column of granularity 40 purpose permutites filtrate adding,, collect baicalin and baicalin component (indicating as the permutite chromatography) respectively with baicalin and baicalin reference substance with 1: 1 water and the alcohol mixed solution eluting of pH6; With the baicalin collected and baicalin eluent respectively the pH of regulator solution be 1.5, be heated to 70 ℃, place 24h, natural sedimentation is filtered, the collecting precipitation thing, oven dry promptly obtains high-purity baicalin and high-purity baicalin respectively.
Take by weighing high-purity baicalin 100 grams and high-purity baicalin 1 gram respectively, add injection vitamin C 3.5 grams, add 1000 milliliters of dissolvings of water, adding sodium chloride again makes solution become isosmotic solution, transferring the pH value of solution is 6, adopts the ultrafilter membrane ultrafiltration of 5000 molecular weight, the filtrate packing, sterilization promptly gets the injection of antiviral, antibiotic, antiinflammatory.
Embodiment 2
Get Radix Scutellariae extract or baicalin crude product 200 grams, 4000 milliliters of adding distil waters, add baicalin enzyme 2 gram stirring and dissolving under 40 ℃, transferring the pH of solution is 6, filter and remove residue contains filtrate adding in the chromatographic column of granularity 60 purpose silica gel, with 1: 3 water and the alcohol mixed solution eluting of pH7, collect baicalin and baicalin component respectively, indicate as silica gel column chromatography with baicalin and baicalin reference substance; With the baicalin collected and baicalin eluent respectively the pH of regulator solution be 2, be heated to 80 ℃, place 36h, natural sedimentation is filtered, the collecting precipitation thing, oven dry promptly obtains high-purity baicalin and high-purity baicalin respectively.
Take by weighing high-purity baicalin 150 grams and high-purity baicalin 1.5 grams respectively, add injection vitamin C 6.5 grams, add 1000 milliliters of dissolvings of water, adding sodium chloride again makes solution become isosmotic solution, transferring the pH value of solution is 6.5, adopts the ultrafilter membrane ultrafiltration of 6000 molecular weight, the filtrate packing, sterilization promptly gets the injection of antiviral, antibiotic, antiinflammatory.
Embodiment 3
Get Radix Scutellariae extract or baicalin crude product 150 grams, 3000 milliliters of adding distil waters, add glycuronidase 2 gram stirring and dissolving under 30 ℃, transferring the pH of solution is 7, filter and remove residue contains filtrate adding in the chromatographic column of granularity 60 purpose macroporous adsorbent resins, with 1: 4 water and the alcohol mixed solution eluting of pH 8, collect baicalin and baicalin component respectively, indicate as macroporous adsorption resin chromatography with baicalin and baicalin reference substance; With the baicalin collected and baicalin eluent respectively the pH of regulator solution be 3, be heated to 90 ℃, place 50h, natural sedimentation is filtered, the collecting precipitation thing, oven dry promptly obtains high-purity baicalin and high-purity baicalin respectively.
Take by weighing high-purity baicalin 80 grams and high-purity baicalin 50 grams respectively, add injection vitamin C 2 grams, add 1000 milliliters of dissolvings of water, adding sodium chloride again makes solution become isosmotic solution, transferring the pH value of solution is 7, adopts the ultrafilter membrane ultrafiltration of 8000 molecular weight, the filtrate packing, sterilization promptly gets the eye drop of antiviral, antibiotic, antiinflammatory.
Embodiment 4
Get Radix Scutellariae extract or baicalin crude product 150 grams, 3000 milliliters of adding distil waters, add flavone enzyme 3 gram stirring and dissolving under 45 ℃, transferring the pH of solution is 8, filter and remove residue contains filtrate adding in the chromatographic column of granularity 100 purpose permutites, with 1: 6 water and the methanol mixed eluant solution of pH 9, collect baicalin and baicalin component respectively, indicate as the permutite chromatography with baicalin and baicalin reference substance; With the baicalin collected and baicalin eluent respectively the pH of regulator solution be 5, be heated to 100 ℃, place 40h, natural sedimentation is filtered, the collecting precipitation thing, oven dry promptly obtains high-purity baicalin and high-purity baicalin respectively.
Take by weighing baicalin 80 grams and baicalin 20 respectively and restrain, add medicinal sodium sulfite 6 grams, glucose 70 grams, starch 570 grams, magnesium stearate 54 grams, mixed powder, pelletizing press sheet promptly get antiviral, antibiotic, anti-inflammation drugs tablet.
Perhaps, take by weighing baicalin 80 grams and baicalin 20 grams respectively, add medicinal sodium sulfite 2 grams, glucose 40 grams, syrup 324 grams, distilled water to 1000 gram fully mixes, packing, and sterilization makes antiviral, antimicrobial oral liquid.
Embodiment 5
Get Radix Scutellariae extract or baicalin crude product 100 grams, 2000 milliliters of adding distil waters, add baicalin enzyme 2 gram stirring and dissolving under 35 ℃, transferring the pH of solution is 5, filter and remove residue contains filtrate adding in the chromatographic column of granularity 60 purpose silica gel, with 1: 3 water and the methanol mixed eluant solution of pH 10, indicate as silica gel column chromatography with baicalin and baicalin reference substance, collect baicalin and baicalin component respectively; With the baicalin collected and baicalin eluent respectively the pH of regulator solution be 4, be heated to 90 ℃, place 30h, natural sedimentation is filtered, the collecting precipitation thing, oven dry promptly obtains high-purity baicalin and high-purity baicalin respectively.
Take by weighing baicalin 90 grams and baicalin 30 grams respectively, add medicinal polylactic acid 1 gram, carbomer 1 gram or hyaluronic acid 1.5 grams, glycerol 1 gram, the dissolving of adding distil water to 1000 gram, make the film material, film, cut apart, packing, sterilization promptly get antiviral, antibiotic, antiinflammatory membrane medicine.
Claims (1)
1. an antiviral antibacterial combination is characterized in that containing the high-purity baicalin that percentage by weight is 2%-10%, the high-purity baicalin of 0.1%-5% and the acceptable accessories of surplus;
Wherein: described high-purity baicalin and high-purity baicalin are made by following step separation and purification:
Get Radix Scutellariae extract or baicalin crude product, add the distilled water of 12～20 times of its weight, add glycosidase, glycuronidase, baicalin enzyme or the flavone enzyme of its weight 0.01%～0.2% or the mixture of its any ratio again under 25 ℃～50 ℃; The pH of fully stirring and dissolving, and accent solution is 5～8; Conventional filtration removes slag, and contained in the chromatographic column of adsorbent filtrate adding, with the mixing eluent eluting of pH6～10, indicates as chromatography with baicalin and baicalin reference substance, collects baicalin and baicalin component eluent respectively; With the baicalin collected and baicalin eluent respectively regulator solution pH 1～4 be heated to 70 ℃～100 ℃, place, natural sedimentation is more than 24 hours, conventional filtration, the collecting precipitation thing, oven dry promptly obtains high-purity baicalin and high-purity baicalin respectively;
Above-mentioned adsorbent is granularity 10～120 purpose silica gel, permutite or macroporous adsorbent resin;
Above-mentioned mixing eluent is that volume ratio is 1: 1～5 water: alcohol mixeding liquid or volume ratio are 1: 1～10 water: methyl alcohol mixed liquor.
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| CN200810013610XA CN101214252B (en) | 2008-01-08 | 2008-01-08 | Antiviral antibacterial medicinal composition and preparation thereof |
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| CN101214252B true CN101214252B (en) | 2011-03-16 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2014052621A1 (en) * | 2012-09-28 | 2014-04-03 | Kline Ellis | Glycosidase regimen for treatment of infectious disease |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103308541B (en) * | 2012-03-08 | 2016-03-02 | 中国医药大学 | The quantitative analysis method of roxburgh anoectochilus terminal bud candy glycosides and separation method |
| CN112593307A (en) * | 2020-12-26 | 2021-04-02 | 江西浣星谷科技有限公司 | Nano biological anti-RNA virus fabric and preparation method thereof |
| CN112806394A (en) * | 2021-02-24 | 2021-05-18 | 江西浣星谷科技有限公司 | anti-RNA virus nano-film and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1961888A (en) * | 2005-11-11 | 2007-05-16 | 杭州华东医药集团生物工程研究所有限公司 | Lyophilized powder injection of baikal skullcap root extract and preparation method thereof |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1961888A (en) * | 2005-11-11 | 2007-05-16 | 杭州华东医药集团生物工程研究所有限公司 | Lyophilized powder injection of baikal skullcap root extract and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 薛慧玲.微生物发酵转化黄芩的研究.中国优秀博硕士学位论文全文数据库(硕士)工程科技Ⅰ辑2007年 第03期.2007,2007年(第03期),摘要，第二、三章. |
| 薛慧玲.微生物发酵转化黄芩的研究.中国优秀博硕士学位论文全文数据库(硕士)工程科技Ⅰ辑2007年 第03期.2007,2007年(第03期),摘要,第二、三章. * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014052621A1 (en) * | 2012-09-28 | 2014-04-03 | Kline Ellis | Glycosidase regimen for treatment of infectious disease |
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| CN101214252A (en) | 2008-07-09 |
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