IMPROVED PROCESS FOR THE PRODUCTION OF HIGH-PURITY SULFATED HA
    1.
    发明申请
    IMPROVED PROCESS FOR THE PRODUCTION OF HIGH-PURITY SULFATED HA 审中-公开
    改进的生产高纯度硫化氢的方法

    公开(公告)号:WO2017085622A1

    公开(公告)日:2017-05-26

    申请号:PCT/IB2016/056868

    申请日:2016-11-15

    CPC classification number: C08B37/0072 A61K31/737

    Abstract: The present invention relates to an improved process for the production of sulfated hyaluronic acid (HA), sulfated HA-derivatives and/or mixtures thereof, having a high purity and a sulfation degree ranging from 1 to 3, which comprises the following steps: a) solubilization of HA-Na or HA-derivative-Na, in an aprotic solvent in the presence of an organic sulfonic acid; b) sulfation of the solution obtained by the addition of an excess of sulfating agents; c) precipitation in ethanol until a precipitate is obtained; d) solubilization of the precipitate thus obtained in a mixture of water and the aprotic solvent used in step a), in the presence of an excess of NaCl, with a pH adjustment within a range of 3 to 4; e) further precipitation with ethanol until a powder is obtained; f) washings of the powder coming from step e) and drying the product thus obtained under vacuum. The present invention also relates to sulfated HA, sulfated HA derivatives and/or mixtures thereof, having a high purity and sulfation degree ranging from 1 to 3, thus prepared, and the relative pharmaceutical mixtures.

    Abstract translation: 本发明涉及用于生产硫酸化透明质酸(HA),硫酸化HA-衍生物和/或其混合物的改进方法,其具有高纯度和1至3范围内的硫酸化度 其包括以下步骤:a)在有机磺酸存在下,在非质子传递溶剂中溶解HA-Na或HA-衍生物-Na; b)通过加入过量的硫酸化剂获得的溶液的硫酸化; c)在乙醇中沉淀直至获得沉淀; d)将如此获得的沉淀物在步骤a)中使用的水和非质子溶剂的混合物中,在过量的NaCl存在下溶解,其中pH调节在3至4的范围内; e)用乙醇进一步沉淀,直至获得粉末; f)洗涤来自步骤e)的粉末,并在真空下干燥由此获得的产物。 本发明还涉及如此制备的具有1至3的高纯度和硫酸化度的硫酸化HA,硫酸化HA衍生物和/或其混合物,以及相关的药物混合物。

    CONJUGATES OF HYALURONIC ACID AND AMINOBISPHOSPHONATES AND THE THERAPEUTIC USE THEREOF

    公开(公告)号:WO2020079551A1

    公开(公告)日:2020-04-23

    申请号:PCT/IB2019/058698

    申请日:2019-10-11

    Abstract: The present invention describes conjugates of hyaluronic acid (HA) and an amino-bisphosphonate (N-BP) of general formula (I): Formula (I) wherein L, m, n and x are as defined in claim 1, and the salts thereof. Said conjugates and the pharmaceutical compositions thereof are useful in the intra-articular and/or locoregional treatment of osteoarthrosis and its repercussions at cartilage and subchondral level; in the treatment of post-menopausal or drug-induced osteoporosis; in the treatment of bone fragility due to trauma or disease; and in the intraosseous and/or locoregional treatment of disorders characterised by altered metabolic bone turnover, in particular Paget's disease. They are also useful to improve the osseointegration of prostheses.

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