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    ETHYLIDENE DERIVATIVES OF TRICYCLIC CARBAPENEMS
    1.
    发明公开
    ETHYLIDENE DERIVATIVES OF TRICYCLIC CARBAPENEMS 失效
    乙二醇衍生物碳酸钙

    公开(公告)号：EP0946558A1

    公开(公告)日：1999-10-06

    申请号：EP97947251.0

    申请日：1997-12-18

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

    发明人： COPAR, Anton ,  SOLMAJER, Tomaz ,  ANZIC, Borut ,  KUZMAN, Tadeja ,  MESAR, Tomaz ,  KOCJAN, Darko

    IPC分类号： A61K31 ,  A61P31 ,  C07D477 ,  C07D495

    CPC分类号： C07D477/00 ,  C07D495/14

    摘要： Disclosed are novel ethylidene derivatives of tricyclic carbapenems of formula (I), wherein the ring marked C and X have the meaning as in the description, in the form of pure diastereoisomers and in the form of pure geometric isomers. Novel ethylidene derivatives of tricyclic carbapenems of formula (I) are used as inhibitors of the action of the enzyme β-lactamase and/or as antibiotics in human and veterinary medicine. Also disclosed are pharmaceutical formulations for the treatment of bacterial infections of human and animal organisms comprising as an active ingredient a therapeutically effective amount of an ethylidene derivative of tricyclic carbapenems of formula (I) in the form of an acid, a pharmaceutically acceptable salt or ester thereof and optionally in a combination with a β-lactam antibiotic, and usual pharmaceutically acceptable carriers and auxiliary substances. Also disclosed is a process for the preparation of novel ethylidene derivatives of tricyclic carbapenems of formula (I).

    Animal feed and an additive thereto or to drinking water containing an antibiotic mixture of gentamicin with lincomycin or clindamycin
    4.
    发明公开
    Animal feed and an additive thereto or to drinking water containing an antibiotic mixture of gentamicin with lincomycin or clindamycin 失效
    动物饲料，含有庆大霉素的林可霉素或克林霉素抗生素混合物的饲料添加剂或饮用水。

    公开(公告)号：EP0585514A1

    公开(公告)日：1994-03-09

    申请号：EP93100072.3

    申请日：1993-01-05

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

    发明人： Sever, Bojan

    IPC分类号： A23K1/17

    CPC分类号： A23K50/75 ,  A23K20/195

    摘要： Described is novel animal feed and an additive thereto or to drinking water containing an antibiotic combination of 1 part by weight of gentamicin and 5 to 60 parts by weight of lincomycin or clindamycin, preferably in the form of pharmacologically acceptable acid addition salts thereof, for the prophylaxis and the therapy of infections and, consequently, for the increase of the gain in body weight in fattening animals.
    For the increase of the gain in body weight in poultry, the combination of gentamicin sulfate and lincomycin hydrochloride is very effective.

    摘要翻译： 描述的是新颖的动物饲料和添加剂于此或重量林可霉素或克林霉素的重量的庆大霉素和5至60份饮用水1份的抗生素组合的含，优选药理学上可接受的酸加成盐的形式，其用于在 预防和感染的治疗，因此，在育肥动物体重增益的增加。 用于家禽体重的增益的增加，硫酸庆大霉素和盐酸林可霉素的组合是非常有效的。

    Inclusion complexes of clavulanic acid and of alkali salts thereof with beta-cyclodextrines
    5.
    发明公开
    Inclusion complexes of clavulanic acid and of alkali salts thereof with beta-cyclodextrines 失效
    β-环糊精 - Inklusionskomplexen vonClavulansäureund ihren Alkalisalzen。

    公开(公告)号：EP0578231A1

    公开(公告)日：1994-01-12

    申请号：EP93110883.1

    申请日：1993-07-07

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

    发明人： Zmitek, Janko, Dr. ,  Fercej-Temeljotov, Darja, Mag. ,  Verhnjak, Katarina ,  Kotnik, Sonja ,  Kovacic, Mateja

    IPC分类号： A61K47/48 ,  A61K31/42

    CPC分类号： B82Y5/00 ,  A61K31/42 ,  A61K31/424 ,  A61K47/6951

    摘要： Described is a new process for the preparation of alkali clavulanate from an aqueous solution of crude clavulanic acid, which is obtained in a conventional manner after the fermentation with a clavulanic-acid-producing microorganism, extracted with an ethyl acetate solution of a hydrophobic β-CD derivative such as heptakis-(2,3,6-tri-O-acetyl)-β-CD in at least equimolar ratio with regard to clavulanic acid. The resulting novel inclusion complexes of clavulanic acid and hydrophobic β-CD derivative in a molar ratio about 1:1 are isolated, purified and then converted with an alkali base or alkali alkanoate to the desired alkali clavulanate, which is isolated. Furthermore, there are described new inclusion complexes of clavulanic acid and of its pharmaceutically acceptable alkali salts both with hydrophilic β-CD derivatives and with hydrophobic β-CD derivatives, processes for the preparation thereof and the use thereof for the preparation of galenic forms with immediate as well as with sustained action, in combination with amoxicillin trihydrate, which are valuable medicaments in the therapy of infectious diseases.

    摘要翻译： 描述了从使用产生克拉维酸的微生物发酵后以常规方式获得的粗克拉维酸水溶液制备克拉维酸碱的新方法，用疏水性β-葡聚糖的乙酸乙酯溶液萃取， CD衍生物，如克拉维酸至少等摩尔比例的七（ - ） - （2,3,6-三-O-乙酰基）-β-CD。 所得到的克拉维酸和疏水性β-CD衍生物的新型包合物以约1:1的摩尔比分离，纯化，然后用碱碱金属碱式碱金属转化成所需的克拉维酸碱盐，将其分离。 此外，还描述了克拉维酸及其药学上可接受的碱金属盐与亲水性β-CD衍生物和疏水性β-CD衍生物的新型包合配合物，其制备方法及其用于立即制备盖仑制剂的用途 以及持续的作用，与阿莫西林三水合物组合，这是治疗感染性疾病的有价值的药物。

    NOVEL PHARMACEUTICAL FORMULATION WITH CONTROLLED RELEASE OF ACTIVE SUBSTANCES
    7.
    发明公开
    NOVEL PHARMACEUTICAL FORMULATION WITH CONTROLLED RELEASE OF ACTIVE SUBSTANCES 失效
    药物制剂中活性成分的控释

    公开(公告)号：EP1003487A1

    公开(公告)日：2000-05-31

    申请号：EP98932706.9

    申请日：1998-07-13

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

    发明人： KOFLER, Bojan ,  REBIC, Ljubomira, Barbara ,  SIRCA, Judita ,  VENTURINI, Peter

    IPC分类号： A61K9/50 ,  A61K9/16 ,  A61K9/20 ,  A61K31/415 ,  A61K31/44 ,  A61K31/435

    CPC分类号： A61K9/1652 ,  A61K9/2095 ,  A61K9/5073

    摘要： There is disclosed a method for stabilizing active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, by means of anhydrous granulation of active substances and dried pharmaceutically acceptable auxiliary substances for the preparation of pellet cores or granules. All pharamceutically acceptable auxiliary substances employed are dried before use so that their weight loss at drying is less than 1.0 % of the total weight of the pharmaceutically acceptable auxiliary substance, preferably less than 0.5 % Organic solvents used in process of anhydrous granulation should contain less than 0.2 % of water. A novel pharmaceutical formulation with controlled release of active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, is disclosed as well.

    Dispersable dihydroergotoxin tablets
    9.
    发明公开
    Dispersable dihydroergotoxin tablets 失效
    可分散的双氢麦角新碱片剂

    公开(公告)号：EP0361354A1

    公开(公告)日：1990-04-04

    申请号：EP89117650.5

    申请日：1989-09-25

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

    发明人： Milovac, Jenny ,  Kovacic, Mateja ,  Kopitar, Zdravko ,  Urbancic-Smerkolj, Janja ,  Lenardic, Andrej ,  Zorz, Mirjan ,  Kofler, Bojan ,  Vene-Mozina, Angela ,  Nikolic, Vida ,  Lampret, Marija ,  Meden, Breda

    IPC分类号： A61K31/48 ,  A61K9/20

    CPC分类号： A61K9/2059 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K31/48

    摘要： There are described novel dispersible tablets of dihydroergotoxine or of acid addition salts thereof, containing 0.1 to 4 % by weight of dihydroergotoxine or its acid addition salts, 4 to 60 % by weight of one or more disintegrating agents, 0.8 to 10 % by weight of an organic acid and, optionally, 0.2 to 2 % by weight of an antioxidizing agent together with other common adjuvants.
    The process for the manufacture of dispersible tablets of dihydroergotoxine and of acid addition salts thereof is carried out on the basis of known methods by granulating the ingredients and by compressing the granulate to tablets.
    Dispersible tablets disintegrate within less than 1 minute when brought in contact with water at room temperature to yield a fine dispersion, which facilitates the oral applica­tion. Therefore such tablets are particulary suitable for the aged. Dispersible tablets containing dihydroergotoxine or acid addition salts thereof excell by their improved rate of dissolution and good bioavailability.

    摘要翻译： 描述了二氢麦角新碱或其酸加成盐的新型分散片剂，其含有0.1至4重量％的二氢麦角碱或其酸加成盐，4至60重量％的一种或多种崩解剂，0.8至10重量％ 有机酸和任选地0.2至2重量％的抗氧化剂以及其它常见助剂。 制备二氢麦角碱分散片及其酸加成盐的方法是在已知方法的基础上通过将各成分造粒并将颗粒压制成片剂来进行的。 当分散片在室温下与水接触时，在不到1分钟的时间内崩解，产生精细分散体，便于口服。 因此这种片剂特别适合老年人。 含有二氢麦角碱或其酸加成盐的分散片优于其溶解速率和良好的生物利用度。