CN101843591A - 1'-acetoxyl chavicol acetate naonparticle - Google Patents
1'-acetoxyl chavicol acetate naonparticle Download PDFInfo
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- CN101843591A CN101843591A CN201010187448A CN201010187448A CN101843591A CN 101843591 A CN101843591 A CN 101843591A CN 201010187448 A CN201010187448 A CN 201010187448A CN 201010187448 A CN201010187448 A CN 201010187448A CN 101843591 A CN101843591 A CN 101843591A
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Abstract
The invention discloses a 1'-acetoxyl chavicol acetate naonparticle consisting of 1 part by weight of 1'-acetoxyl chavicol acetate, 1-20 parts by weight of inclusion material and 0-1 part by weight of stabilizing agent and a preparation method thereof. Compared with a stake dispersion technology, the naonparticle has remarkable solubilizing effect which can reach over 200 times of the solubility of the 1'-acetoxyl chavicol acetate and has stable quality; compared with the 1'-acetoxyl chavicol acetate, the effect for resisting HIV (Human Immunodeficiency Virus) effect and the acute toxicity test result of the nanoparticle have no remarkable changes, no remarkable acrimony, sensitivity and hemolytic reactions. By adopting the known art, the nanoparticle is prepared into forms by an injected administration route or non-injected administration route.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, more particularly, relate to 1 '-'-acetoxyl chavicol acetate naonparticle and preparation method thereof.
Background technology
The English 1 '-acetoxychavicol acetate (ACA) by name of 1 '-acetoxychavicol acetate, molecular formula is C
13H
14O
4, molecular weight is 234.25, structural formula is
Chinese patent ZL031308767 report has the duplicate effect of the HIV-1 NL43 of inhibition the MT-4 cell from 1 '-acetoxychavicol acetate of the dry rhizome Rhizoma Alpiniae Galangae extraction separation purification of Zingiberaceae Zingiberaceae Alpinia plants Fructus Galangae Alpinia galanga Willd., and the MT-4 cell survival is not had influence, show the characteristics of tight security and the external migration of inhibition HIV Rev pyrenoids, have significant anti-HIV-1 infection activity as the Rev protein inhibitor.
Also have the research report show 1 '-acetoxychavicol acetate have antitumor (Moffatt J, A, etal.[J] .Carcinogenesis, 2000,21:2151-2157; Zheng Q et al.[J] .J Cancer ResClin Oncol, 2002,128:539～546), antibacterium (Janssen A M, [J] .plantaMed, 1985 (6): 507～511), antifungal (Ficker C E, et al.[J] .JEthnophamacal, 2003,85:589～593), antiulcer (Mitsuis, et al.[J] .Chem PhamBull, 1976,24:2377～2382), antioxidation (Kubota K, et al.[J] .Spec Publ R SocChem, 2001,274:601～607), antiinflammatory (Nakamura Y, [J] .Cancer Res, 1998,58:4832～4839) etc. biological activity discovers also that in recent years it has the tuberculosis activity.
The Another application of 1 '-acetoxychavicol acetate is to be used for food industry.Result of study shows that 1 '-acetoxychavicol acetate is a kind of antioxidant, and has good antioxygenic property, antioxidant effect even also better than the antioxidant of some synthetic.Because it is a kind of crude, antioxidant than synthetic is safer, reliable, and therefore, 1 '-acetoxychavicol acetate can be applied in the preservation of food, replace existing synthetic antioxidant, as a kind of safe and reliable antioxidant of meat product.
1 '-acetoxychavicol acetate still is a kind of material with pungent characteristic, so it also has another purposes in food industry---as the additive of food (as: beverage, confectionery) and personal care articles (as toothpaste).Experimental studies have found that (Matsuda, et al.Biorganic ﹠amp; MedicinalChemistry Letters, 2003,13:3197～3202), in alcoholic beverage, add a small amount of 1 '-acetoxychavicol acetate and can make drinking utensils that better mouthfeel is arranged.For example, alcohol content is when containing 1 ' of 50mg/kg-acetoxychavicol acetate in 20% the alcoholic beverage, happy equilibrated effect is made us in burning sensation formation after just obtaining just the drink burning sensation and drinking, and is that 30% beverage has better mouthfeel than alcohol content.And when 1 '-acetoxychavicol acetate content was 160mg/kg in the non-alcoholic drink, this beverage just had the mouthfeel feature of alcoholic beverage.As seen, in beverage, add 1 ' an amount of-acetoxychavicol acetate, can part even replace alcoholic content in the beverage fully.In addition, because the pungent of 1 '-acetoxychavicol acetate is purer, and shorter in the intraoral persistent period than the pungent of Fructus Capsici, so can also be applied in other food (as hard sugar and chewing gum), personal care articles (as toothpaste), make it have the sensation of pungent stimulation.
Dissolubility is the intrinsic physicochemical property of medicine, and the medicine that dissolubility is bigger in water has dissolution rate preferably usually in gastro-intestinal Fluid, and the absorption of medicine is increased, and curative effect strengthens.Because ACA is insoluble in water, solving its solubility in water is the key point and the difficult point of its galenic pharmacy research.
According to " regulation of two notes on the use of Chinese pharmacopoeia version in 2005 is carried out the ACA dissolubility test: the ACA that took by weighing 80 mesh sieves is an amount of, be added in 25 ℃ ± 2 ℃ the distilled water, powerful jolting was 30 seconds every 5 minutes, ACA still can not dissolve fully after 30 minutes, with 0.45 μ m filtering with microporous membrane, get filtrate, measure ultraviolet absorptivity at the 218nm place, the concentration that records the ACA saturated solution is 177.5 μ g/ml.
Increasing the most frequently used method of insoluble drug dissolubility is solid dispersion technology, and solvent method and the fusion method the most frequently used method that is solid dispersion technology.
Adopt solvent method, ACA and carrier material polyethylene glycol 6000 are dissolved in 90% ethanol water jointly, ACA and carrier material are separated out simultaneously after boiling off solvent, make the coprecipitate of ACA and polyethylene glycol 6000; The dissolubility of using mass ratio that this method prepares ACA and polyethylene glycol 6000 and be 1: 5 solid dispersion is 1.15 times of crude drug, can not satisfy the requirement of preparation.
Adopt fusion method, polyethylene glycol 6000 is heated to fusion at 75 ℃, stir and add ACA down, put in-18 ℃ of refrigerators cooling curing rapidly behind the homogeneous transparent shape fluid to be formed immediately, put in the exsiccator dry 1-2 days.Use mass ratio that this method prepares ACA and polyethylene glycol 6000 respectively and be 1: 5,1: 10,1: 15,1: 20 solid dispersion, its dissolubility is respectively 1.9,1.4,1.4,1.8 times of ACA, can not satisfy the requirement of preparation.
Summary of the invention
For dissolubility and the stability problem that solves ACA, under the situation that does not influence ACA drug effect and safety, the inventor adopts the technology of the ACA enclose being made nanoparticle, and its dissolubility can reach more than 200 times of ACA, and solubilizing effect significantly is better than solid dispersion technology.The ACA nanoparticle steady quality of preparation, its anti-HIV effect and safety and ACA relatively do not have significant change.Adopt known technology, this ACA nanoparticle can be made the dosage form of drug administration by injection approach and non-injection administration approach.
Technical scheme of the present invention is, gets ACA and/or stabilizing agent, is added to and makes dissolving in the solvent, makes ACA solution; Other gets the enclose material, is added to make dissolving in the solvent, makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made ACA clathrate nanoparticle.Adopt known technology, this ACA nanoparticle can be made the dosage form of drug administration by injection approach and non-injection administration approach.
Can be used for stabilizing agent of the present invention and comprise but be not limited to sodium pyrosulfite, sodium sulfite, Sodium Ethacrynate etc. that the parts by weight proportioning of stabilizing agent and ACA is 0: 1 to 1: 1.
Can be used for enclose material of the present invention and include but not limited to cyclodextrin, for example HYDROXYPROPYL BETA-CYCLODEXTRIN, betacyclodextrin, dimethyl betacyclodextrin, sulfobutyl ether betacyclodextrin etc., the parts by weight proportioning of enclose material and ACA is 1: 1 to 20: 1.
Can be used for solvent of the present invention and include but not limited to water, 50% alcoholic solution, ethanol solution etc., the concentration of making ACA clathrate saturated solution is 10mg/ml to 100mg/ml.
Adopt known technology, ACA clathrate nanoparticle of the present invention can be made the dosage form of injection administration or non-injection administration, for example injection, peroral dosage form, powder spray, spray, aerosol, exterior-applied formulation etc.
The effect that the present invention is useful
1, the thing phase of ACA clathrate
The thing phase discrimination test of ACA clathrate proves that it is a kind of new thing phase, and its particle diameter can reach nanometer level, and therefore, the ACA clathrate can be described as the ACA nanoparticle.
2, the solubilizing effect of ACA nanoparticle
ACA nanoparticle solubilizing effect is obvious, can reach more than 200 times of ACA dissolubility, redissolves all rightly, is better than solid dispersion technology.
3, anti-HIV effect of ACA nanoparticle and safety
Results of pharmacodynamic test shows, with ACA relatively, ACA nanoparticle of the present invention to the C8166 cytotoxicity, induce the C8166 cell to form the inhibitory action that syncytium and p24 antigen produces to HIV-1 not have significant change.
The acute toxicity tests shows, compares with ACA, and ACA nanoparticle of the present invention safety does not have significant change.
Zest, anaphylaxis, hemolytic result of the test show that ACA nanoparticle of the present invention does not have obvious irritation, anaphylaxis and hemolytic reaction.
4, the stability of ACA nanoparticle
Get the ACA nanoparticle, at illumination (4500LX ± 500LX), high temperature (40 ℃, 60 ℃, 80 ℃), high humidity (25 ℃, RH95% ± 5%, 25 ℃, RH75% ± 5%) test 10 days under the condition, investigate appearance character, moisture absorption weightening finish and ACA content respectively at sampling in the 0th, 5,10 day.The result shows that the ACA nanoparticle increases weight all more than 5%, and explanation should be preserved at the drying place.High temperature, illumination all have certain influence to the ACA content in the ACA nanoparticle, and explanation should be preserved at shading, shady and cool place.
5, stabilizing agent is to the influence of ACA clathrate aqueous stability
The ACA compound aqueous solution that adds stabilizing agent boils sampling detection ACA content after 30 minutes.The result shows, adds stabilizing agent and can not make the stability of ACA clathrate aqueous solution satisfy the requirement of galenic pharmacy.
6, adopt known technology, ACA nanoparticle of the present invention can be made the dosage form of drug administration by injection approach and non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol, exterior-applied formulation etc.
The specific embodiment
Embodiment 1
Get 1 weight portion ACA and be added to and make dissolving in the water, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in the water and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 2
Get 1 weight portion ACA and be added in 50% alcoholic solution and make dissolving, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in 50% alcoholic solution and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 3
Get 1 weight portion ACA and be added to and make dissolving in the dehydrated alcohol, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in the dehydrated alcohol and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 4
Get 1 weight portion ACA and be added to and make dissolving in the water, make ACA solution; Other gets 1 to 20 weight portion betacyclodextrin and is added in the water and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 5
Get 1 weight portion ACA and be added in 50% alcoholic solution and make dissolving, make ACA solution; Other gets 1 to 20 weight portion betacyclodextrin and is added in 50% alcoholic solution and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 6
Get 1 weight portion ACA and be added to and make dissolving in the dehydrated alcohol, make ACA solution; Other gets 1 to 20 weight portion betacyclodextrin and is added in the dehydrated alcohol and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 7
Get 1 weight portion ACA and be added to and make dissolving in the water, make ACA solution; Other gets 1 to 20 weight portion dimethyl betacyclodextrin and is added in the water and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 8
Get 1 weight portion ACA and be added in 50% alcoholic solution and make dissolving, make ACA solution; Other gets 1 to 20 weight portion dimethyl betacyclodextrin and is added in 50% alcoholic solution and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 9
Get 1 weight portion ACA and be added to and make dissolving in the dehydrated alcohol, make ACA solution; Other gets 1 to 20 weight portion dimethyl betacyclodextrin and is added in the dehydrated alcohol and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Embodiment 10
Get 1 weight portion ACA and be added to and make dissolving in the water, make ACA solution; Other gets 1 to 20 weight portion sulfobutyl ether betacyclodextrin and is added in the water and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 11
Get 1 weight portion ACA and be added in 50% alcoholic solution and make dissolving, make ACA solution; Other gets 1 to 20 weight portion sulfobutyl ether betacyclodextrin and is added in 50% alcoholic solution and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 12
Get 1 weight portion ACA and be added to and make dissolving in the dehydrated alcohol, make ACA solution; Other gets 1 to 20 weight portion sulfobutyl ether betacyclodextrin and is added in the dehydrated alcohol and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 13
Get 1 weight portion ACA and sodium pyrosulfite and be added to and make dissolving in the water, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in the water and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution that contains 1mg to 50mg sodium pyrosulfite among every 1ml, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 14
Get 1 weight portion ACA and sodium pyrosulfite and be added in 50% alcoholic solution and make dissolving, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in 50% alcoholic solution and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution that contains 1mg to 50mg sodium pyrosulfite among every 1ml, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 15
Get 1 weight portion ACA and sodium pyrosulfite and be added to and make dissolving in the dehydrated alcohol, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in the dehydrated alcohol and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution that contains 1mg to 50mg sodium pyrosulfite among every 1ml, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 16
Get 1 weight portion ACA and sodium sulfite and be added to and make dissolving in the water, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in the water and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution that contains 1mg to 50mg sodium sulfite among every 1ml, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 17
Get 1 weight portion ACA and sodium sulfite and be added in 50% alcoholic solution and make dissolving, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in 50% alcoholic solution and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution that contains 1mg to 50mg sodium sulfite among every 1ml, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 18
Get 1 weight portion ACA and sodium sulfite and be added to and make dissolving in the dehydrated alcohol, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in the dehydrated alcohol and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution that contains 1mg to 50mg sodium sulfite among every 1ml, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 19
Get 1 weight portion ACA and edetate sodium and be added to and make dissolving in the water, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in the water and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution that contains 1mg to 50mg edetate sodium among every 1ml, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 20
Get 1 weight portion ACA and edetate sodium and be added in 50% alcoholic solution and make dissolving, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in 50% alcoholic solution and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution that contains 1mg to 50mg edetate sodium among every 1ml, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Embodiment 21
Get 1 weight portion ACA and edetate sodium and be added to and make dissolving in the dehydrated alcohol, make ACA solution; Other gets 1 to 20 weight portion HYDROXYPROPYL BETA-CYCLODEXTRIN and is added in the dehydrated alcohol and dissolves, and makes the enclose material solution; Under agitation, ACA solution is added in the enclose material solution, makes the ACA inclusion complex in solution that contains 1mg to 50mg edetate sodium among every 1ml, solvent evaporated is crossed 80 mesh sieves, and drying is made the ACA nanoparticle.
Adopt known technology, the ACA nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach, for example injection, peroral dosage form, powder spray, spray, aerosol exterior-applied formulation etc.
Claims (2)
1.1 '-'-acetoxyl chavicol acetate naonparticle is characterized in that it is made up of 1 '-acetoxychavicol acetate, enclose material and/or stabilizing agent; The English of described 1 '-acetoxychavicol acetate is called 1 '-acetoxychavicolacetate, and molecular formula is C
13H
14O
4, molecular weight is 234.25, structural formula is
Described enclose material is HYDROXYPROPYL BETA-CYCLODEXTRIN, betacyclodextrin, dimethyl betacyclodextrin or sulfobutyl ether betacyclodextrin, and the parts by weight proportioning of enclose material and 1 '-acetoxychavicol acetate is 1: 1 to 20: 1; Described stabilizing agent is sodium pyrosulfite, sodium sulfite or edetate sodium, and the parts by weight proportioning of stabilizing agent and 1 '-acetoxychavicol acetate is 0: 1 to 1: 1.
2. the described 1 '-'-acetoxyl chavicol acetate naonparticle of claim 1, the preparation method that it is characterized in that it is to get 1 '-acetoxychavicol acetate and/or stabilizing agent, be added to and make dissolving in the solvent, make 1 '-acetoxychavicol acetate solution; Other gets the enclose material, is added to make dissolving in the solvent, makes the enclose material solution; Under agitation, 1 '-acetoxychavicol acetate solution is added in the enclose material solution, makes 1 '-acetoxychavicol acetate inclusion complex in solution, solvent evaporated, sieve, drying is made particle diameter and can be reached 1 ' of nanometer level-'-acetoxyl chavicol acetate naonparticle; Described solvent is water, 50% alcoholic solution or ethanol solution; Adopt known technology, this nanoparticle can be made the dosage form of drug administration by injection approach or non-injection administration approach.
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| CN201010187448A CN101843591A (en) | 2010-05-31 | 2010-05-31 | 1'-acetoxyl chavicol acetate naonparticle |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1879612A (en) * | 2005-06-17 | 2006-12-20 | 上海艾力斯医药科技有限公司 | Nano particles of taxane cyclodextrin inclusion compound and preparation method thereof |
| CN101134724A (en) * | 2007-10-16 | 2008-03-05 | 南昌弘益科技有限公司 | 1'-acetoxy chavicol acetate |
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- 2010-05-31 CN CN201010187448A patent/CN101843591A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1879612A (en) * | 2005-06-17 | 2006-12-20 | 上海艾力斯医药科技有限公司 | Nano particles of taxane cyclodextrin inclusion compound and preparation method thereof |
| CN101134724A (en) * | 2007-10-16 | 2008-03-05 | 南昌弘益科技有限公司 | 1'-acetoxy chavicol acetate |
Non-Patent Citations (1)
| Title |
|---|
| 20050131 R.C.罗,等 药用辅料手册 264,654-656 , 1 * |
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