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SLOWLY RELEASING TRANILAST PREPARATION AND LONG-ACTING TRANILAST PREPARATION CONTAINING SAME

机译:缓释曲尼司特的制备和长效包含相同的长效曲尼司特的制备

摘要

PURPOSE:To provide a long-acting drug preparation for oral administration, composed of a slowly releasing component containing toranylast treated with an enteric substance as an active component and a quickly releasing tranilast component, capable of maintaining high drug concentration in blood for a long period and expected to exhibit sufficient clinical effect. CONSTITUTION:A slowly releasing tranilast preparation is prepared by coating (A) tranilast [N-(3,4-dimethoxycinnamoyl)anthranylic acid] known as a remedy for allergic diseases with (B) an enteric substance (a substance soluble at a critical pH of =5.0, preferably =5.5) such as cellulose acetate phthalate, methacrylic acid/methyl methacrylate copolymer, etc., by spraying, centrifugal flow coating, etc. The slowly releasing component is compounded with a quickly releasing component containing tranilast free from treatment with the enteric substance at a ratio to give a tranilast content ratio in both components of 2:8-8:2 by weight to obtain the objective long-acting preparation.
机译:目的:提供一种口服的长效药物制剂,该制剂由缓释组分和速释曲尼司特组分组成,该缓释组分含有以肠溶性物质作为活性成分处理的托拉司特,能够长期保持血液中的高药物浓度并有望表现出足够的临床效果。组成:缓释曲尼司特制剂的制备方法是,将(A)曲尼司特[N-(3,4-二甲氧基肉桂酰基)邻氨基苯甲酸]涂在已知为过敏性疾病的药物上,并以(B)肠溶性物质(在临界pH下可溶的物质) ≥5.0,优选≥5.5),例如邻苯二甲酸乙酸纤维素,甲基丙烯酸/甲基丙烯酸甲酯共​​聚物等,通过喷涂,离心流涂等。将缓慢释放的组分与不含不含曲尼司特的快速释放组分混合。以肠溶物质的比例处理,使两种成分中曲尼司特的含量比为2:8-8:2,以获得目标的长效制剂。

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