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    • 2. 发明申请
    • Nasallly applicable pharmaceutical preparation and the production thereof
    • 适用于药物制剂及其生产
    • US20060127317A1
    • 2006-06-15
    • US10530969
    • 2003-10-09
    • Ernst HesseGerhard Hantichwolfgang NitschmannHelmut Scheidl
    • Ernst HesseGerhard Hantichwolfgang NitschmannHelmut Scheidl
    • A61L9/04
    • A61K9/0043
    • The invention relates to a novel pharmaceutical preparation which can be administered nasally and is based on an aqueous solution, emulsion or the like which comprises at least one mucosally absorbable and/or locally acting active pharmaceutical ingredient, at least one preservative formed by benzalkonium chloride alone or together with other preservative substances, at least one buffer which keeps the pH at 4 to 6, and in addition at least one osmotic agent and/or at least one wetting agent and which is characterized in that the preparation has a substantially improved ciliary tolerability owing to the fact that in the preparation a buffer based on malic acid is present instead of a buffer which has been employed to date in the pharmaceutical preparation and is based on citrate(s), phosphate(s) and/or acetate(s)—partly or completely replacing it (them)—while retaining the composition, concentration and amount ratios, intended in each case for the pharmaceutical preparation, of active ingredient(s), preservative(s), osmotic agent(s) and wetting agent(s). It further relates to a process for producing the preparation and to the use of a malic acid buffer in the preparation.
    • 本发明涉及一种可以鼻腔给药并且基于水溶液,乳液等的新型药物制剂,其包含至少一种粘膜可吸收和/或局部作用的活性药物成分,至少一种由单独的苯扎氯铵形成的防腐剂 或与其它防腐物质一起,至少一种将pH保持在4至6的缓冲液,另外还含有至少一种渗透剂和/或至少一种润湿剂,其特征在于所述制剂具有显着改善的纤毛耐受性 由于在制备中存在基于苹果酸的缓冲液而不是已经在药物制剂中使用的基于柠檬酸盐,磷酸盐和/或乙酸盐的缓冲液, 一方面或完全替代它们(它们),同时保留用于药物制剂的每种情况下的组合物,浓度和量比例为活性物质 成分,防腐剂,渗透剂和润湿剂。 本发明还涉及制备该制剂的方法和该制剂中苹果酸缓冲液的使用。