• 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:

    公开号:SU959626A3
    申请号:SU792757925
    申请日:1979-04-25
    公开日:1982-09-15
    发明作者:Фельш Хорст；Хантих Герхард
    申请人:Плк Фармасьютикал Лайсенсиз Компани Лтд (Фирма)；
    IPC主号:
    专利说明:

    The invention relates to a method for stabilizing 4-methyl- 5_ (2-chloroethyl) thiazole of the formula 1 H ′ C P (G) which has a biological active, is insufficiently stable and has an unpleasant sulfurous smell and bitter taste.
    The aim of the invention is to increase storage stability.
    This goal is achieved by the fact that according to the method of stabilization of 4-methyl-5 ’(2-chloroethyl) thiazole by mixing it with a carrier, glycerol tricaprinate is used as a carrier, and is used in medicine. A known method of stabilization of 4-methyl-5 ”(2-chloroethyl) thiazole, which consists in mixing it with a non-polar carrier, which consists of one or several animal or vegetable oils or fats, or one or more fatty acids, containing 1422 carbon atoms. In this case, the decomposition of the compound of formula I is suppressed. The preparations obtained are stable during storage for some time £ ll.
    However, the compound of formula 1 stabilized in a known manner, glycerol tricaprilate, glycerol trilaurate or a neutral oil of composition, weight L:
    G lysericantricapronate Glycerol tricaprilat Glycerol tricaprinate
    Until 3
    50-65 30-45 *
    Up to 5% and mixing is carried out under conditions excluding the presence of atmospheric oxygen in an inert gas atmosphere.
    The compound of formula I, stabilized by the proposed method, can be stored for 4 years.
    PRI me R 1. The boiler with a stirrer made of special steel with a capacity of 10 l
    Until 3
    50-65
    30 - (+ 5
    Up to 5 vazapolazot отο in a vacuum version fill 4.0 kg of neutral · oil composition, wt.%:
    G glycerin trikapronate Glycerol tricaprilat Glycerol tricaprinate Glycerol trilaurate and after removal of air ’by means of - cumulation (10 min, 1 torr) are removed with technically pure nitrogen, while passing directly through the dispenser into neutral oil. Under further nitrogen aeration, with stirring, slowly (200 ml / min) 4.0 kg of freshly-transformed oxygen-free compound 1 with a chloride content of about 0.01% is fed continuously. After 10 minutes of stirring, the mixture filled the transport containers made of special steel. Then, soft gelatin capsules ... (500 mg of the mixture per capsule) are filled with a mixture without air bubbles.
    Example 2. An evacuated glass boiler (a round-bottom flask with a 5-liter stirrer) is filled with 1.5 kg of tricaprine (glycerol tricaprinate) and, after removal of air by vacuum (10 min, 1 mm Hg), is subjected to gasification with technically pure argon. Through further dispensing, directly into a solution of tricaprine. Under further aeration with argon while stirring • 1.0 kg of freshly distilled oxygen-free compound 1 with a chloride content of about 0.01% are added dropwise continuously for 10 minutes and filled with olnennye argon glass vials (bottles) with a capacity of 3 l. The mixture is then filled without air bubbles are resistant to gastric juice, soluble in the intestine, soft gelatin capsule (600 mg of mixture per capsule).
    Example 3. A boiler with a 10-liter special steel mixer in vacuum design is filled with 4.0 kg of tricaprilin (glycerol tricaprilat). The stabilization of the compounds of formula I is carried out analogously to example 1.
    Example 4. A boiler with a special steel mixer with a capacity of 10 l in a vacuum version is filled
    Order 7036/78
    VNIIIPI
    959626 4
    2.0 kg of trilaurin (glycerol trilaurate) and 2.0 kg of tricaprinate (glycerol tricaprinate) and the process is carried out analogously to example 1.
    Two mixtures of compound T of a neutral oil are prepared, wt.%: '1
    83.5
    Compound 1 Neutral Oil
    The first and second glass flasks of nitrogen are divided, 2
    68.8
    16,5 mixture was heated at 70 ° C and atmosfe100 and 170 h, mixture mixture during the expansion joint 100 hours.
    3,5
    0.5 and op1 ° /
    I, -Ό ► h.
    170 m
    0.5 second mixture is heated t
    The first and a glass flask in an atmosphere of air at 70 ° C for 170 h and determine the decomposition of compound 1,%:
    Mixture 1 14.1
    Mixture 2 3.7
    The results of the experiments show that the addition of a neutral oil in the form of a mixture of triglycerides of saturated fatty acids reduces the decomposition of the CMT compound I. With an increase in the concentration of neutral oil, this stabilizing effect increases.
    权利要求:
    Claims (1)
    [1]
    Claim
    The method of stabilization of 4-methyl-5 “(2-chloroethyl) thiazole by mixing it with a carrier, characterized in that, in order to increase storage stability, glycerol tricaprinate, glycerol tricaprilate, glycerol trilaurate or neutral oil, wt.% Are used as a carrier:
    G litserintrikapronat Glycerin tricaprilat G glycerin tricaprinate Glycerol trilaurate mixing is carried out excluding the presence of the spirit in an inert gas atmosphere ..
    类似技术:
    公开号 | 公开日 | 专利标题
    CN1133426C|2004-01-07|Novel stable preparation use paracetamol as base and method for preparing same
    CA1168155A|1984-05-29|Acetal stabilized prostaglandin compositions
    US4328245A|1982-05-04|Carbonate diester solutions of PGE-type compounds
    ES2551680T3|2015-11-23|Conjugated Linoleic Acid Compositions
    CN1077800C|2002-01-16|Cyclosporin soft capsule composition
    CA1176567A|1984-10-23|Pharmaceutical preparation
    SU959626A3|1982-09-15|Process for stabilizing 4-methyl-5-|thiazole
    US4611008A|1986-09-09|Preparation of nitroesters for coronary artery therapy
    JPH0211698A|1990-01-16|Stable highly unsaturated fatty acid and its derivative
    RU2002108000A|2003-12-27|STABLE PHARMACEUTICAL DRUG OXALIPLATIN FOR Parenteral Administration
    AU2009224968B2|2014-01-16|Long-term stable pharmaceutical preparation having the active ingredient glycerol trinitrate
    KR100196212B1|1999-06-15|Pharmaceutically stable formulations containing nicorandil
    US20100184870A1|2010-07-22|Long-term stable pharmaceutical preparation containing the active ingredient glycerol trinitrate
    BE897721A|1984-03-09|PHARMACEUTICAL COMPOSITIONS WITH B-LACTAMIC ANTIBIOTICS OF IMPROVED STABILITY
    JP2006188474A|2006-07-20|Excellently stable fat emulsion
    CA2074726A1|1991-10-07|Oleaginous capsule of ketoprofen
    CN104140985B|2017-04-05|A kind of enzyme catalysiss non-oxidizability oils and fatss for preparing in situ and method
    FR2436991A1|1980-04-18|SOLUTIONS FOR THE QUALITY CONTROL OF BLOOD GAS ANALYZERS, COMPOSITION OF THESE SOLUTIONS AND PROCESS FOR THEIR INDUSTRIAL PREPARATION
    EP0356325A1|1990-02-28|Pharmaceutical composition containing a slightly water-soluble active substance and at least a glyceride gelled by at least a cellulose polymer
    KR930019204A|1993-10-18|Administration aerosols containing the active substance flezelastine and related structures
    EP0465550A1|1992-01-15|Pharmaceutical lipid composition for parenteral nutrition.
    KR20200005110A|2020-01-15|Methods for improving stability of pharmaceutical products containing a taxane-containing pharmaceutical composition
    JPH01175943A|1989-07-12|Composition for promoting absorption of lipid substance in intestine
    SU1090404A1|1984-05-07|Method of preparing sibasone solution for injections
    JP3550176B2|2004-08-04|Tocopherol-enriched refined sesame oil, fat infusion containing it and oral preparation
    同族专利:
    公开号 | 公开日
    HU179741B|1982-12-28|
    CS208779B2|1981-09-15|
    AU523518B2|1982-07-29|
    AU4637379A|1979-11-01|
    AT358530B|1980-09-10|
    IE48778B1|1985-05-15|
    NO150317B|1984-06-18|
    CA1113941A|1981-12-08|
    NZ190240A|1980-10-24|
    DD142962A5|1980-07-23|
    DE2916573C2|1982-09-02|
    FI66120C|1984-09-10|
    PT69532A|1979-05-01|
    IE790836L|1979-10-25|
    FI791324A|1979-10-26|
    YU91079A|1984-10-31|
    JPS6337791B2|1988-07-27|
    FI66120B|1984-05-31|
    EP0005121A3|1979-11-28|
    EP0005121A2|1979-10-31|
    EP0005121B1|1982-10-13|
    YU42302B|1988-08-31|
    JPS54147914A|1979-11-19|
    IL57292A|1982-11-30|
    UA5545A1|1994-12-28|
    DE2963835D1|1982-11-18|
    NO791339L|1979-10-26|
    DK155978C|1989-10-30|
    US4247702A|1981-01-27|
    ES480590A1|1980-08-16|
    ZA791661B|1980-04-30|
    ATA296178A|1980-02-15|
    DK155978B|1989-06-12|
    DK167879A|1979-10-26|
    DE2916573A1|1979-10-31|
    GR66987B|1981-05-15|
    NO150317C|1984-09-26|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    US2844512A|1954-11-05|1958-07-22|Upjohn Co|Fumagillin enveloped in fatty or waxy substance and enclosed in ultraviolet opaque container|
    US3265629A|1958-12-22|1966-08-09|Ncr Co|Coating by phase separation|
    US3146167A|1961-10-05|1964-08-25|Smith Kline French Lab|Method of preparing sustained release pellets and products thereof|
    FR1416304A|1961-10-10|1965-11-05|Smith Kline French Lab|Improvements to tablets and tablets containing a large amount of active ingredient released over a prolonged period of time, and to processes for their preparation|
    FR1536904A|1962-12-19|1968-09-02|Smith Kline French Lab|Process for preparing pharmaceutical pills with progressive release of their active principle|
    SE319577B|1966-03-08|1970-01-19|Astra Ab|
    JPS4971127A|1972-11-18|1974-07-10|
    NL189235C|1974-02-28|1993-02-16|Akzo Nv|METHOD FOR THE PREPARATION OF AN ORAL PHARMACEUTICAL PREPARATION WITH ANDROGENIC ACTION|
    NL7510104A|1975-08-27|1977-03-01|Akzo Nv|PROCESS FOR THE PREPARATION OF AN ORAL ACTIVE PHARMACEUTICAL PREPARATION.|
    DE2631281A1|1976-07-12|1978-01-19|Kali Chemie Pharma Gmbh|Increasing solubility of pharmaceuticals for use in gelatin capsules - by dissolving in fatty acid mono:glyceride and opt. di:glyceride cpds.|
    US4202888A|1976-07-12|1980-05-13|Kali-Chemie Pharma Gmbh.|Readily enterally absorbable pharmaceutical compositions of cardiac glycosides and preparation thereof|JPS58159425A|1982-03-18|1983-09-21|Fujisawa Pharmaceut Co Ltd|Gel base|
    SE9303281D0|1993-10-07|1993-10-07|Astra Ab|New formulation|
    AT267189T|1999-10-15|2004-06-15|Sucampo Ag|BIZYCLIC COMPOSITIONS AND METHOD FOR THEIR STABILIZATION|
    US9884024B2|2005-12-27|2018-02-06|Hemant N Joshi|Physically dispersed, molecularly dissolved and/or chemically bound drug in an empty, hard capsule shell composition|
    JP2013032289A|2009-10-28|2013-02-14|Daiichi Sankyo Co Ltd|Wax stable formulation|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    AT296178A|AT358530B|1978-04-25|1978-04-25|STABILIZATION PROCEDURE|LV930686A| LV5492A3|1978-04-25|1993-06-28|Panemiens for the stabilization of 4-methyl-5-thiazole|
    LTRP949A| LT2255B|1978-04-25|1993-09-06|4-METHYL-5-THIAZOL STABILIZATION BUDGET|
    [返回顶部]