D6-四苯喹嗪固体口服剂型、化合物、及其药物组合物、制备及治疗方法

文档序号:1118749 发布日期:2020-10-02 浏览:13次 >En<

阅读说明:本技术 D6-四苯喹嗪固体口服剂型、化合物、及其药物组合物、制备及治疗方法 (D6Solid oral dosage forms of (E) -tetrabenazine, compounds, and pharmaceutical compositions, preparation and treatment methods thereof ) 是由 A·萨默 C·张 J·卡特 J·阿瑟 M·布雷德伯里 T·甘特 M·沙赫巴兹 于 2013-09-18 设计创作,主要内容包括:本发明涉及一种固体口服剂型,所述固体口服制剂包括6毫克的d&lt;Sub&gt;6&lt;/Sub&gt;-四苯喹嗪和剂型重量的约5%至约30%的聚合物,所述聚合物为聚(环氧乙烷)聚合物、科利当聚合物、羟丙基甲基纤维素聚合物、羟丙基纤维素聚合物、卡波普聚合物或它们的组合,其中如果所述口服剂型以进食状态口服给予人,则其给药结果为:约132hr*ng/mL的血浆中总组合量的氘化二氢四苯喹嗪的AUC&lt;Sub&gt;inf&lt;/Sub&gt;;或者约15.5ng/mL的血浆中总组合量的氘化二氢四苯喹嗪的C&lt;Sub&gt;max&lt;/Sub&gt;。本发明还涉及有关结晶型体包括该结晶型体的药物组合物,以及施用其的治疗方法。本发明的技术方案使得四苯喹嗪的药代动力学参数表现优异。(The present invention relates to a solid oral dosage form, said solid oral dosage formThe preparation comprises d 6mg 6 -tetrabenazine and from about 5% to about 30% by weight of the dosage form of a polymer which is a poly (ethylene oxide) polymer, a colestyrol polymer, a hydroxypropyl methylcellulose polymer, a hydroxypropyl cellulose polymer, a carbopol polymer, or a combination thereof, wherein if the oral dosage form is administered orally to a human in the fed state, the result of administration is: AUC of total combined amount of deuterated dihydrotetrabenazine in plasma of about 132hr ng/mL inf (ii) a Or about 15.5ng/mL of the total combined amount of deuterated dihydrotetrabenazine C in plasma max . The invention also relates to related crystalline forms, pharmaceutical compositions comprising the crystalline forms, and methods of treatment using the same. The technical scheme of the invention ensures that the pharmacokinetic parameters of the tetrabenazine are excellent.)

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