Pharmaceutical cyclosporin formulation with improved biopharmaceutical properties, improved physical quality and greater stability, and method for producing said formulation
    41.
    发明授权
    Pharmaceutical cyclosporin formulation with improved biopharmaceutical properties, improved physical quality and greater stability, and method for producing said formulation 失效
    具有改善的生物药物性质,改善的物理质量和更大的稳定性的药物环孢菌素制剂以及用于生产所述制剂的方法

    公开(公告)号:US06551619B1

    公开(公告)日:2003-04-22

    申请号:US09674417

    申请日:2001-01-22

    Abstract: The invention relates to solid, particulate lipid-based excipients which are loaded with cyclosporine. Said excipients have improved biopharmaceutical properties for cyclosporines in vivo, are of a better quality (in terms of fineness, homogeneity of the particles, inclusion of the medicament) and are more physically stable in the particulate formulation (no aggregation or gel formation). The invention also relates to a therapeutic treatment with cyclosporine formulations which produce an average blood level concentration in the steady state range of 300 ng/ml to over 1000 ng/ml, preferably over 800 ng/ml, especially up to 900 ng/ml, preferably 400 ng/ml to 800 ng/ml in the absence of high initial blood level concentrations essentially over 1500 ng/ml, especially over 1200 ng/ml. This blood level concentration is preferably maintained for an extended period of at least 5 hours, preferably at least 7 hours.

    Abstract translation: 本发明涉及负载有环孢菌素的固体颗粒状基于脂质的赋形剂。 所述赋形剂在体内具有改善的环孢菌素的生物药物性质,具有更好的质量(在细度,颗粒的均匀性,药物的包合性方面),并且在颗粒制剂中更具物理稳定性(无聚集或凝胶形成)。 本发明还涉及使用环孢菌素制剂的治疗性治疗,其在300ng / ml至超过1000ng / ml,优选超过800ng / ml,特别是至多900ng / ml的稳态范围内产生平均血液浓度, 优选400ng / ml至800ng / ml,在不存在高的初始血液浓度基本上超过1500ng / ml,特别是超过1200ng / ml的情况下。 该血液浓度优选保持至少5小时,优选至少7小时的延长时间。

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