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    THREE-PHASE PHARMACEUTICAL FORM WITH CONSTANT AND CONTROLLED RELEASE OF AMORPHOUS ACTIVE INGREDIENT FOR SINGLE DAILY APPLICATION
    26.
    发明公开
    THREE-PHASE PHARMACEUTICAL FORM WITH CONSTANT AND CONTROLLED RELEASE OF AMORPHOUS ACTIVE INGREDIENT FOR SINGLE DAILY APPLICATION 失效
    三相药物剂型常数和一次性日无定形物质形式的控释

    公开(公告)号：EP0827397A2

    公开(公告)日：1998-03-11

    申请号：EP96915292.0

    申请日：1996-05-17

    申请人： Lek, Tovarna Farmacevtskih in Kemicnih Izdelkov, D.D.

    发明人： KERC, Janez ,  REBIC, Ljubomira, Barbara ,  KOFLER, Bojan

    IPC分类号： A61K9 ,  A61K31 ,  A61K45 ,  A61K47 ,  A61P9

    CPC分类号： A61K9/2077 ,  A61K9/2846 ,  A61K9/2866 ,  A61K9/2886

    摘要： Described is a novel three-phase pharmaceutical form with constant and controlled release of an amorphous active ingredient stabilized with polymers for a single daily peroral application, which is especially suitable for active ingredients existing in amorphous form or in one or more polymorphous forms, which exhibit poor solubility in crystal form depending on the polymorphous form, particle size and the specific surface area of the active ingredient. The active ingredient can be used in its amorphous or any polymorphous form, which in the process of the preparation of the three-phase pharmaceutical form according to the invention is converted into the amorphous form. The three-phase pharmaceutical form with constant and controlled release of an amorphous active ingredient for a single daily peroral application contains a core consisting of a first and a second phase and a coating representing the third phase. In the first phase the three-phase pharmaceutical form contains an amorphous active ingredient, the water-soluble polymer polyvinylpyrrolidone and a cellulose ether as carriers of the amorphous active ingredient and simultaneously as inhibitors of its crystallization, a surfactant that improves the solubility of the active ingredient and promotes the absorption of the amorphous active ingredient from gastrointestinal tract, in the second phase it contains a cellulose ether and a mixture of mono-, di- and triglycerides as sustained release agents and the third phase is represented by a poorly soluble or gastro-resistant film coating, which in the first few hours after the application controls the release of the active ingredient and can consist of an ester of hydroxypropylmethylcellulose with phthalic anhydride or of a copolymerizate based on methacrylic acid and ethyl acrylate. Described is also a process for the preparation of this pharmaceutical form.

    NEW COMBINED PROCESS FOR THE PURIFICATION OF VANCOMYCIN HYDROCHLORIDE
    27.
    发明公开
    NEW COMBINED PROCESS FOR THE PURIFICATION OF VANCOMYCIN HYDROCHLORIDE 失效
    组合工艺清洁盐酸万古霉素

    公开(公告)号：EP0809652A1

    公开(公告)日：1997-12-03

    申请号：EP96901183.0

    申请日：1996-02-06

    申请人： LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d., Ljubljana

    发明人： PFLAUM, Zlatko ,  TURKALJ, Robert

    IPC分类号： C07K1 ,  C07K9

    CPC分类号： C07K9/008

    摘要： The present invention discloses a new process for the purification of vancomycin hydrochloride by combining preparative chromatography on a silica gel column and the precipitation with ethanol from a salt-water-ethanolic solution without intermediary filtering, whereby the chromatographic purity of the product is improved. The chromatography is carried out on a column containing a silica gel stationary phase and a water mobile phase at defined pH, mobile phase flow and temperature as well as the amount and concentration of vancomycin hydrochloride. The process is distinguished by the yield and chromatographic purity of the obtained product of about 93 % area. Vancomycin hydrochloride purified according to the present invention is useful for peroral as well as parenteral administration since the portion of impurities it contains is for one third smaller than in hitherto available products.

    A process for the preparation of amlodipine benzenesulphonate
    29.
    发明公开
    A process for the preparation of amlodipine benzenesulphonate 失效
    Verfahren zur Herstellung von amlodipin-Benzolsulfonat。

    公开(公告)号：EP0599220A1

    公开(公告)日：1994-06-01

    申请号：EP93118661.3

    申请日：1993-11-19

    申请人： LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d.

    发明人： Furlan, Borut ,  Copar, Anton, Dr. ,  Jeriha, Alenka

    IPC分类号： C07D211/90

    CPC分类号： C07D211/90

    摘要： There is disclosed a process for the preparation of 3-ethyl 5-methyl (±) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridine-dicarboxylate monobenzenesulphonate (amlodipine benzenesulphonate) of formula

    wherein 3-ethyl 5-methyl (±) 2-[2-(N-tritylamino)-ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate is reacted with benzenesulphonic acid in a methanolic or an aqueous methanolic medium at a temperature from 20 °C to the reflux temperature and the title compound is isolated and purified.
    Amlodipine benzene sulphonate is a valuable anti-ischaemic and anti-hypertensive agent.

    摘要翻译： 公开了制备3-乙基5-甲基（+/-）2 - [（2-氨基乙氧基）甲基] -4-（2-氯苯基）-1,4-二氢-6-甲基-3 ，其中3-乙基5-甲基（+/-）2- [2-（N-三苯甲基氨基） - 乙氧基甲基] -4-（2-氯苯基） - 苯并噻唑-5-磺酸盐（氨氯地平苯磺酸盐） 1,4-二氢-6-甲基-3,5-吡啶二羧酸酯与苯磺酸在甲醇或甲醇水溶液中在20℃至回流温度下反应，分离和纯化标题化合物。 氨氯地平苯磺酸盐是有价值的抗缺血和抗高血压药物。

    Neue Alkylendiammonium-diclavulanat-Derivate, Verfahren zu deren Herstellung sowie deren Verwendung
    30.
    发明公开
    Neue Alkylendiammonium-diclavulanat-Derivate, Verfahren zu deren Herstellung sowie deren Verwendung 失效
    新Alkylendiammonium棒酸盐的衍生物，其制备方法及其用途。

    公开(公告)号：EP0562583A1

    公开(公告)日：1993-09-29

    申请号：EP93104890.4

    申请日：1993-03-24

    申请人： LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d.

    发明人： Copar, Anton, Dr. Ing.

    IPC分类号： C07D498/047

    CPC分类号： C07D503/00

    摘要： Es wird ein neues Verfahren zur Herstellung von Clavulansäure und deren pharmazeutisch annehmbaren Salzen wie Kalium-clavulanat beschrieben. Demgemäss wird rohe Clavulansäure, die in der Form eines Extraktes in einem organischen Lösungsmittel wie Ethylacetat vorliegt, welcher Extrakt auf bekannte Weise nach der Fermentation mit einem Clavulansäure produzierenden Mikroorganismus erhalten wurde, mit substituierten Alkylendiaminen der Formel II

    worin die Substituenten R₁, R₂, R₃, R₄ und R₅ sowie n die im Anspruch 1 genannten Bedeutungen besitzen, z.B. mit N,N'-Diisopropylethylendiamin, zu neuen Alkylendiammonium-clavulanaten der Formel I

    worin die Substituenten R₁, R₂, R₃, R₄ und R₅ sowie n die im Anspruch 1 genannten Bedeutungen besitzen, z.B. zu N,N'-Diisopropylethylendiammonium-diclavulanat, umgesetzt. Die erhaltenen Verbindungen der Formel I werden gegebenenfalls isoliert und mti Alkalisalzen von Alkansäuren, z.B. mit Kalium-2-ethyl-hexanoat in Isopropanol, zu Kalium-clavulanat umgesetzt.
    Wegen der hemmenden Wirkung auf β-Lactamasen und einer signifikanten synergistischen Wirkung in Kombination mit β-Lactam-Antibiotika aus der Reihe der Penicilline und Cephalosporine sind die Clavulansäure und deren pharmazeutisch annehmbare Salze wertvolle Verbindungen zur Herstellung von galenischen Präparaten, die gegen durch zahlreiche Gram-positive und Gram-negative Mikroorganismen verursachte Infektionskrankheiten wirksam sind.

    摘要翻译： 它是用于制备棒酸及其药学如克拉维酸钾描述上可接受的盐的新方法。 因此，粗克拉维酸，这是一种提取物的形式在有机溶剂如乙酸乙酯，将其以已知的方式与克拉维酸的微生物发酵后得到的提取物，与式II 其中取代基R1，R2的取代的亚烷基二胺 ，R3，R4和R5和n具有权利要求1中给出的含义，包括 与N，N'-二异丙基乙二胺，式新Alkylendiammonium-clavulanaten I 其中取代基R1，R2，R3，R4和R5和n具有权利要求1中，例如在给定的含义 到N，N'- diisopropylethylenediammonium二棒酸盐实现。 我所得到的式I的化合物是任选地分离和MTI的链烷酸，例如碱金属盐 用氢-2-乙基 - 己酸于异丙醇中以克拉维酸钾反应。 因为β内酰胺酶的抑制活性，并结合β内酰胺抗生素从系列青霉素和头孢菌素的显著协同作用的是克拉维酸及其药学上可接受的盐是用于制备药物制剂的针对多种革兰氏有价值的化合物 阳性和革兰氏阴性微生物引起的感染性疾病是有效的。