• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    Allicin is stabilized as an inclusion complex with a cyclodextrin. The complex may be prepared by contacting an aqueous solution of cyclodextrin with a solution of allicin in a water miscible solvent, and the complex may be formulated into a pharmaceutical composition having antimicrobial and/or fungistatic activity in conventional manner.
    公开号:SU938732A3
    申请号:SU792854753
    申请日:1979-12-11
    公开日:1982-06-23
    发明作者:Сейтли Йожеф；Сенте Лайош；Кульчар Габор；Кермеци Дьердь
    申请人:Хиноин Дьедьсер Еш Ведьесети Термекек Дьяра Рт(Инопредприятие)；
    IPC主号:
    专利说明:

    (54) METHOD OF OBTAINING THE ALLICIN-CYCLODEXTRIN COMPLEX
    one
    The invention relates to medicine; namely, a method of producing drugs based on a cyclodextrin complex with allicin inclusion .5
    A known method of producing garlic oil containing nitrogen contains the following components: diallyl sulfide, diallyl trisulfide, diallyl tetrasulfide, dipropyl disulfide, propyllyl disulfide, dimethyl sulfide and alliin. Chemically, alliin corresponds to / + / - S-allyl-1-cystennsulfoxide and can be converted by enzymatic means into allicin, i.e. in allyl ester al-ts lilthiosulfinic acid l.
    The purpose of the invention is to obtain a new complex allicin-cyclodextrin.
    The goal is achieved by the fact that the method of obtaining the complex 20 allicin-cyclodextrin is that an aqueous solution of oi., L 7 -cyclodextrin or a solution of a mixture of these cyclodextrins is mixed with allicin in the presence of ethanol with
    then the mixture is cooled at.
    The method is carried out as follows.
    Aqueous solution d. or -dg-cyclodextrin or a solution of any mixture of these cyclodextrins in the absence of air is introduced into the allicin solution in the presence of ethanol. Mixing is carried out at 0-70 ° C, after which the complex is precipitated by cooling to. The isolation is carried out by lyophilization. When using conventional excipients, additives, and other injectors, pharmaceutical preparations are prepared in the form of tablets, capsules, dragees, suspensions, emulsions, solutions, powders, and sprayable preparations.
    权利要求:
    Claims (3)
    [1]
    - Example 1. South P) -CYCLOdextrin (water content, I), while stirring and passing nitrogen gas, is dissolved in the heated water. Slowly add 1 g of allicin in 5 ml of 9b% ethanol. The mixture is cooled at room temperature for an hour at a uniform rate and then kept at room temperature for 16 hours. The precipitate is filtered off and dried in air. 11.02 g of a white crystalline product are obtained, which according to gas chromatographic analysis contains 10.12 allicin. The output is, with respect to cyclodextrin 99.1, based on allicin - 76. The product has the following physical data: grain size 8-10 microns, solubility in water of 0.82 g (100 ml) at 25 ° C, solubility in ethanol 0,080 g (100 ml) at. The product is unlimited soluble in dimethylformamide and dimethyl sulfoxide. Example
    [2]
    2. The method is carried out analogously to example 1, but the crystalline complex-inclusion is separated from the reaction mixture by lyophilization. The lyophilized product is a very fine-grained material that has only a very slight smell of garlic, because only a little absorbed allicin remains on the surface of the complex. Example
    [3]
    3. Tablets with 150 mg of biologically active substance: allicin complex with 150 g of jb-cyclodextrin, 80 g of starch, 18 mg of lactose, 2 mg of magnesium stearate. Tablets are prepared by a known method. The mixture containing the above components is granulated in a dry state before tabletting. Example k. Enterosolvent Dragus. The tablets prepared according to Example 3 are coated with a coating dissolving in the intestine. The coating may also contain various colorants to indicate the amount of biologically active substance. Example 5 - Powder. Ingredients: Allicin complex with 0.5 g of α-cyclodextrin, 98.0 g of talc. The mixture is filled into spray cans. The proposed method provides a new complex allicin-cyclode | Strings for drugs. The method of obtaining the allicin-cyclodextrin complex, which consists in the fact that an aqueous solution of p, y-cyclodextrin or a solution of a mixture of these cyclodextrins is mixed with allicin in the presence of ethanol, then the mixture is cooled at. Sources of information taken into account during the examination 1. Heiv Chim Acta 31,189,. The proposed method in the patent literature is not described.
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    同族专利:
    公开号 | 公开日
    DK526779A|1980-06-13|
    YU299079A|1983-06-30|
    FR2444060A1|1980-07-11|
    HU177081B|1981-07-28|
    AT363492B|1981-08-10|
    JPS55115866A|1980-09-06|
    JPS642105B2|1989-01-13|
    CH642347A5|1984-04-13|
    GB2061987A|1981-05-20|
    GB2061987B|1983-05-18|
    DE2948869C2|1992-07-09|
    FR2444060B1|1984-06-29|
    NO794044L|1980-06-13|
    ATA782979A|1981-01-15|
    DE2948869A1|1980-07-03|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    US3061444A|1960-10-07|1962-10-30|Gen Foods Corp|Inclusion compounds incorporating edible juice constituents|
    HU174699B|1977-07-01|1980-03-28|Chinoin Gyogyszer Es Vegyeszet|Process for preparing cyclodextrin inclusion complexes of natural and synthetic spices, aromatic and flavoring materials|HU184066B|1979-12-28|1984-06-28|Chinoin Gyogyszer Es Vegyeszet|Plant growth regulating substance and process for preparing such compound|
    JPS5920230A|1982-07-19|1984-02-01|Ciba Geigy Ag|Drug containing piruprophen|
    FR2550193A1|1983-08-05|1985-02-08|Sal Fine Chemicals Internation|Inclusion complexes of methyl and allyl trisulphide with cyclodextrins, process for preparing them and pharmaceutical compositions containing them|
    HU196230B|1983-12-29|1988-10-28|Chinoin Gyogyszer Es Vegyeszet|Process for producing water-soluble forms of polyene antibiotics and pharmaceutics comprising such active ingredient and plant protective with antifungal effect|
    EP0211392B1|1985-08-06|1991-03-27|Kao Corporation|Liquid shampoo composition|
    DE3638290A1|1986-11-07|1988-05-19|Herbe Wirkstoffe Gmbh|Pharmaceutical composition|
    US4774329A|1987-08-04|1988-09-27|American Maize-Products Company|Controlled release agent for cetylpyridinium chloride|
    EP0392608B1|1989-04-12|1995-06-28|The Procter & Gamble Company|Solid consumer product compositions containing small particle cyclodextrin complexes|
    SE8902235D0|1989-06-20|1989-06-20|Haessle Ab|NOVEL CYCLODEXTRIN INCLUSION COMPLEXES|
    CA2013485C|1990-03-06|1997-04-22|John Michael Gardlik|Solid consumer product compositions containing small particle cyclodextrin complexes|
    DE4024155C2|1990-07-30|1995-12-07|Marcela Dipl Ing Holzhey|Use of an "Allicin-Urotropin" product for the area of internal treatmentof humans and animals for fungal diseases|
    DE4338508A1|1993-11-11|1995-05-18|Asta Medica Ag|Pharmaceutical preparations containing thioctic acid or dihydroliponic acid in the form of inclusion compounds with cyclodextrins or cyclodextrin derivatives and in the form of granules, chewable or effervescent tablets|
    DE19500863A1|1995-01-13|1996-07-18|Consortium Elektrochem Ind|Method of making ajoes|
    GB0120887D0|2001-08-29|2001-10-17|Sahajanand Biotech Private Ltd|Local drug delivery system in coronary stents|
    GB0122793D0|2001-09-21|2001-11-14|Stone Island Holdings Ltd|Allicin|
    US20070160725A1|2004-03-03|2007-07-12|Mousala, S., L.|Use of extracts and compounds of allium-genus plants as preservatives in the food and agri-food industries|
    GB0422582D0|2004-10-11|2004-11-10|Nasaleze Patents Ltd|Pharmaceutical compositions|
    CN107802842A|2016-09-07|2018-03-16|汤臣倍健股份有限公司|Allicin flavoring preparation and preparation method thereof|
    CN107789345A|2016-09-07|2018-03-13|汤臣倍健股份有限公司|Flavoring allicin cyclodextrin complexes and preparation method thereof|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    HU78CI1871A|HU177081B|1978-12-12|1978-12-12|Process for preparing the occlusion complex of allicin with cyclodextrin|
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