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    PROCESS FOR THE PREPARATION OF EBERCONAZOL AND INTERMEDIATES THEREOF
    1.
    发明申请
    PROCESS FOR THE PREPARATION OF EBERCONAZOL AND INTERMEDIATES THEREOF 审中-公开
    制备EB冰霜及其中间体的方法

    公开(公告)号：WO1999021838A1

    公开(公告)日：1999-05-06

    申请号：PCT/ES1997000256

    申请日：1997-10-28

    Applicant: LABORATORIOS S.A.L.V.A.T., S.A. ,  FARRERONS GALLEMI, Carles ,  MIQUEL BONO, Ignacio José ,  MONSERRAT VIDAL, Carlos

    Inventor： LABORATORIOS S.A.L.V.A.T., S.A.

    IPC: C07D233/56

    CPC classification number: C07D231/12 ,  C07C63/74 ,  C07C69/65 ,  C07D233/56 ,  C07D249/08

    Abstract: The 2-[2-(3,5-dichlorophenyl)ethyl]benzoic acid (V) which is the key intermediate for the preparation of eberconazol (I) through a known sequence of four steps is prepared by catalytic hydrogenation of 2-[2-(3,5-dichlorophenyl)ethenyl]benzoic acid (VI). The intermediate (VI) is prepared by hydrolysis of its methyl ester obtained by a Wittig reaction between 3,5-dichlorobenzaldehyde and the ylure of phosphor of the bromide of [[(2-metoxycarbonyl)phenyl]-methyl]triphenylphosphonium. The global process can be easily increased in scale since the reactions can be carried out at moderate temperature without requiring a strictly inert atmosphere and without any risk of inflammation. The carboxylic acid (VI) and its methyl ester are chemically new intermediates. The invention is useful for the industrial preparation of the antifongic agent eberconazol (I).

    Abstract translation: 2- [2-（3,5-二氯苯基）乙基]苯甲酸（V）酸，其是用于通过四个步骤的已知序列制备eberconazole（I）的关键中间体，是通过催化氢化来制备 2- [2-（3,5-二氯苯基）乙烯基]苯甲酸（VI）。 中间体（VI）是通过先前通过Wittig反应3,5-二氯苯甲醛和磷叶立德溴化物之间所获得的甲基酯的水解来制备[[（2-甲氧基羰基）苯基]甲基]三苯基鏻。 整个过程可以容易地按比例放大，因为反应可在中等温度下无炎症的风险来执行，而不estricamente惰性气氛。 羧酸（VI）及其甲酯是化学新的中间体。 本发明可用于抗真菌剂eberconazole（I）的工业制备。

    LONG TERM STABLE ORAL PHARMACEUTICAL FORMULATION OF MICROGRANULES IN SUSPENSION
    3.
    发明申请
    LONG TERM STABLE ORAL PHARMACEUTICAL FORMULATION OF MICROGRANULES IN SUSPENSION 审中-公开
    稳定的油悬浮微晶

    公开(公告)号：WO2004004682A2

    公开(公告)日：2004-01-15

    申请号：PCT/EP2003/006927

    申请日：2003-06-30

    Applicant: LABORATORIOS S.A.L.V.A.T., S.A. ,  ARTALEJO ORTEGA, Beatriz ,  BATLLORI CALBÒ, Javier ,  FERNANDEZ GARCIA, Andrés ,  JULVE RUBIO, Jordi

    Inventor： ARTALEJO ORTEGA, Beatriz ,  BATLLORI CALBÒ, Javier ,  FERNANDEZ GARCIA, Andrés ,  JULVE RUBIO, Jordi

    IPC: A61K9/00

    CPC classification number: A61K9/0095 ,  A61K9/5078 ,  A61K31/4439

    Abstract: Pharmaceutical formulation obtainable subjecting conventional microgranules to an external seal-coating layer that avoids the penetration of liquid vehicle, and selecting a hydrophobic liquid vehicle with a viscosity high enough not to wet the microgranules. The seal-coating layer may be obtained by coating the microgranules with an aqueous suspension comprising film formers and plasticizers. The liquid vehicle is comprised of oily solvents, and viscosity agents. The formulation is presented in single dose sachets ready-to-use. This formulation enables the liquid oral administration of antiulcerous microgranules of benzimidazoles (omeprazole, lansoprazole, pantoprazole, rabeprazole), with several advantages comparing to commercially available extemporaneous suspensions. The new formulation of lansoprazole microgranules has a similar bioavailability and slightly higher stability than conventional hard gelatin capsules.

    Abstract translation: 常规微粒可以将外用的密封涂层，避免液体载体渗透，并选择粘度足够高的疏水性液体载体，不会使微粒湿润。 密封涂层可以通过用包含成膜剂和增塑剂的水性悬浮液涂布微粒而获得。 液体载体由油性溶剂和粘度剂组成。 该制剂以单次剂量包装即可使用。 该配方使得能够与市售的临时悬浮液相比具有几种优点，能够液体口服苯并咪唑类抗微生物微粒（奥美拉唑，兰索拉唑，泮托拉唑，雷贝拉唑）。 兰索拉唑微粒的新制剂具有与常规硬明胶胶囊相似的生物利用度和稍高的稳定性。

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