• 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:
    A process by means of which an increase in the particle size of a micro-ground anti-inflammatory steroid in the aerosol propellant is prevented. The increase in the particle size is prevented at the suspending stage when the solubility of the steroid into the propellant is reduced by using a low temperature and by initially mixing only a little quantity of the propellant with the steroid. If desired, the smallest and dissolved steroid particles can be removed by filtering. The particle size does not become larger even afterwards when the suspension is allowed to be stabilized for a sufficiently long time before the temperature is raised or the rest of the propellant is added.
    公开号:SU1184428A3
    申请号:SU813283353
    申请日:1981-05-18
    公开日:1985-10-07
    发明作者:Тапани Тансканен Пааво
    申请人:Орион-Ихтюмя Ой (Фирма)；
    IPC主号:
    专利说明:

    one . This invention relates to the chemical and pharmaceutical industry, namely to the preparation of beclomethasone dipropionate. The purpose of the invention is the preservation of the desired product's gens. Example 1.1.05 g of beclomethasone adipropionate is suspended in 40 g of trichlorofluoromethane at -25 ° C. The mixture is stirred with a magnesium stirrer for 3 days at -25 ° C. The suspension is mixed with 362.8 g of trichloroftermethane, previously cooled to 5 ° C, 0.12 g of oleic acid is added and the mixture is stirred for another half hour. 4.04 g of the suspension obtained in this way is metered into a can, which is closed with a metering valve and 10.36 g of dichlorodifluoromethane are introduced under pressure through the latter. Example 2. 1.05 g of beclomette zonadipropionate and 4.0 g of trichlorofluoromethane are mixed at -20 ° C. To the mixture is added trichlorofluoromethane, cooled to -20 ° C, in small portions so that 36 are added over the first 6 hours. 0 g, over the next 12h160 g and over the next 18 hours - 202.8 g. Example 3. About 5 g of beclometase nadipropionate are added to dichloro difluoromethane at -35 ° C (about 20 g). The mixture is stirred for 2 , 5 su 82 when in a tightly sealed and designed for pressure tank using a magnetic stirrer. Dichlorodifluoromethane is distilled off. 200 g of trichlorofluoromethane are added. The mixture is stirred at room temperature for 4 hours. Example 4. 3.15 g of beclomethasone adipropionate is suspended at 5 ° C in 150 ml of trichlorfluoromethane, the mixture is stirred for 1 hour and 120 ml of trichlorofluoromethane is removed by filtration using a 0.45 fi liter filter. um, after which the appropriate amount of pure trichlorofluoromethane is added. Stirring, filtration and addition are repeated three times. The last stirring was continued for 36 hours, after which trichlorofluoromethane was added to 1200 g. The temperature was kept at 5 ° C all the time. Example 5. 1.0 beclomethasone-adipropionate is suspended in 100 g of trichlorofluoromethane at -40 ° C. The mixture is stirred with a stirrer for 3 days. at -40 ° C. This suspension is added to a solution of 0.12 g of oleic acid in 300 g of trichlorofluoromethane at 5c. The suspension is stirred for another 3 hours at 5 ° C. In an aerosol canister, 4.0 g of suspension and 10.4 g of dichlorodifluoromethane are charged.
    权利要求:
    Claims (2)
    [1]
    1. Process for the preparation BEKLOMETAZONADIPROPIONATA by grinding and mixing it with a propellant - or trichlorofluoromethane, dichloro- difluoromethane, I characterized in that, in order to maintain desired product hemogenic, stirring was carried out at a temperature from +5 to -40 e C for 1-3 days in the amount of May 1-10, 2 to the total amount of propellant, which is added during or after mixing.
    [2]
    2. The method according to π. 1, characterized in that in the case of stirring at a temperature of +5 to -10¾, the mixture is filtered during mixing through a membrane filter with pores of 0.2-0.5 microns. g sl ro>
    1 1184428 2
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    同族专利:
    公开号 | 公开日
    FI63672C|1983-08-10|
    FR2482457A1|1981-11-20|
    FI801610A|1981-11-20|
    CS221831B2|1983-04-29|
    SE437766B|1985-03-18|
    PL127872B1|1983-12-31|
    BE888822A|1981-11-16|
    HU188093B|1986-03-28|
    ES502286A0|1982-04-01|
    JPS5716820A|1982-01-28|
    CA1162852A|1984-02-28|
    FR2482457B1|1985-01-04|
    ES8203606A1|1982-04-01|
    US4347236A|1982-08-31|
    AT380791B|1986-07-10|
    DD158856A5|1983-02-09|
    NO155429C|1987-04-01|
    NL8102457A|1981-12-16|
    FI63672B|1983-04-29|
    DE3119745A1|1982-02-11|
    PT72989A|1981-06-01|
    GB2076422B|1983-12-14|
    NO811686L|1981-11-20|
    ATA179181A|1985-12-15|
    PL231220A1|1982-01-18|
    GB2076422A|1981-12-02|
    DK218481A|1981-11-20|
    SE8103143L|1981-11-20|
    NO155429B|1986-12-22|
    CH647408A5|1985-01-31|
    PT72989B|1983-07-06|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    BE629985A|1962-11-29|
    GB1429184A|1972-04-20|1976-03-24|Allen & Hanburys Ltd|Physically anti-inflammatory steroids for use in aerosols|
    JPS5632879B2|1976-06-28|1981-07-30|
    US4225597A|1976-10-01|1980-09-30|Schering Corporation|Beclomethasone dipropionate-hexane solvate and aerosols prepared therefrom|
    IT1121513B|1979-05-28|1986-04-02|Chiesi Farma Spa|PROCESS FOR THE CONVERSION OF ANTI-INFLAMMATORY STEROID UMO IN A SUSCEPTIBLE FORM OF BEING ADMINISTERED AS AN AEROSOL|KR890000664B1|1981-10-19|1989-03-22|바리 안소니 뉴우샘|Preparation method for micronised be clomethasone dispropionate mono-hydrate|
    AU601176B2|1986-03-10|1990-09-06|Kurt Burghart|Benzodiazepine aerosols|
    JPH01156916A|1987-09-25|1989-06-20|Ss Pharmaceut Co Ltd|Remedy for hepatic disease|
    US5744123A|1991-12-12|1998-04-28|Glaxo Group Limited|Aerosol formulations containing P134a and particulate medicaments|
    US5674471A|1991-12-12|1997-10-07|Glaxo Group Limited|Aerosol formulations containing P134a and salbutamol|
    US5658549A|1991-12-12|1997-08-19|Glaxo Group Limited|Aerosol formulations containing propellant 134a and fluticasone propionate|
    US5683676A|1991-12-12|1997-11-04|Glaxo Group Limited|Canister containing aerosol formulations containing P134a and particulate medicaments|
    US5736124A|1991-12-12|1998-04-07|Glaxo Group Limited|Aerosol formulations containing P134a and particulate medicament|
    IL104068A|1991-12-12|1998-10-30|Glaxo Group Ltd|Surfactant-free pharmaceutical aerosol formulation comprising 1,1,1,2-tetrafluoroethane or 1,1,1,2,3,3,3-heptafluoro-n- propane as propellant|
    CA2421976C|1991-12-12|2004-04-20|Glaxo Group Limited|Medicaments|
    US5916540A|1994-10-24|1999-06-29|Glaxo Group Limited|Aerosol formulations containing P134A and/or P227 and particulate medicament|
    CA2126244C|1991-12-18|2000-09-26|Robert K. Schultz|Suspension aerosol formulations|
    US7105152B1|1991-12-18|2006-09-12|3M Innovative Properties Company|Suspension aerosol formulations|
    US7101534B1|1991-12-18|2006-09-05|3M Innovative Properties Company|Suspension aerosol formulations|
    GB9202519D0|1992-02-06|1992-03-25|Glaxo Group Ltd|Medicaments|
    US5376359A|1992-07-07|1994-12-27|Glaxo, Inc.|Method of stabilizing aerosol formulations|
    MX9304585A|1992-07-31|1994-03-31|Glaxo Group Ltd|PHARMACEUTICAL FORMULATION IN AEROSOL, CAN SUITABLE TO RELEASE THE FORMULATION AND INHALER OF DOSE DOSE THAT COMPRISES THE CAN.|
    US7582284B2|2002-04-17|2009-09-01|Nektar Therapeutics|Particulate materials|
    GB0208742D0|2002-04-17|2002-05-29|Bradford Particle Design Ltd|Particulate materials|
    WO2008097664A1|2007-02-11|2008-08-14|Map Pharmaceuticals, Inc.|Method of therapeutic administration of dhe to enable rapid relief of migraine while minimizing side effect profile|
    US9394314B2|2012-12-21|2016-07-19|Map Pharmaceuticals, Inc.|8′-hydroxy-dihydroergotamine compounds and compositions|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    FI801610A|FI63672C|1980-05-19|1980-05-19|FOERFARANDE FOER FRAMSTAELLNING AV EN BLANDNING AV BEKLOMETASONDIPROPIONAT OCH TRIKLORFLUORMETAN ELLER DIKLORDIFLUORMETAN|
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