盐酸达泊西汀的合成及其制剂工艺研究

发布时间：2018-01-19 05:28

本文关键词： 盐酸达泊西汀合成制剂工艺研究　出处：《吉林大学》2017年硕士论文　论文类型：学位论文

【摘要】：盐酸达泊西汀是一种选择性5-羟色胺再摄取抑制剂(SSRIs),是目前唯一被批准用于治疗男性早泄的药物,其最先由美国礼来制药公司(Elililly)研制用于治疗抑郁,后来由强生公司在芬兰及瑞典作为治疗早泄的药物获得批准上市。本文研究了盐酸达泊西汀的合成工艺,并进行了工艺优化,以价格相对便宜的苯甲醛、丙二酸等为起始原料合成盐酸达泊西汀,合成工艺具有路线简单、易于操作、成本较低等优点,适合工业化生产。对盐酸达泊西汀原料药的质量标准进行了研究,建立了含量测定分析方法和有关物质分析方法,均为高效液相色谱法,并进行了方法学考察;对自制三批样品进行了质量评价,均符合标准要求。对盐酸达泊西汀片进行了制备及评价,首先建立了盐酸达泊西汀片的溶出度测定方法;其次对其制剂工艺进行了研究,筛选了制剂处方,并对制剂工艺稳定性进行了考察;最后对盐酸达泊西汀片进行了溶出度评价,通过比较发现自制片剂与原研片剂溶出行为相似,可以初步判定两种制剂具有生物等效性。
[Abstract]:Dapoxetine Hydrochloride is a selective serotonin reuptake inhibitor, SSRIsa, and is the only drug currently approved for the treatment of premature ejaculation in men. It was first developed by Elililly, an American pharmaceutical company, to treat depression. Johnson has been approved for the treatment of premature ejaculation in Finland and Sweden. The synthetic process of dapoxetine hydrochloride was studied and optimized for relatively cheap benzaldehyde. Dapoxetine hydrochloride was synthesized from malonic acid and so on. The synthetic process has the advantages of simple route, easy operation and low cost. The quality standard of dapoxetine hydrochloride was studied, and the method of content determination and analysis of related substances was established, both of which were HPLC, and the methodology was investigated. The quality evaluation of three batches of dapoxetine hydrochloride tablets was carried out, which met the standard requirements. The preparation and evaluation of dapoxetine hydrochloride tablets were carried out. Firstly, a method for the determination of dissolution of dapoxetine hydrochloride tablets was established. Secondly, the preparation process was studied, the formulation of the preparation was screened, and the stability of the preparation was investigated. Finally, the dissolution of dapoxetine hydrochloride tablets was evaluated. It was found that the dissolution behavior of the two tablets was similar to that of the original tablets, and the bioequivalence of the two preparations could be preliminarily determined.
【学位授予单位】：吉林大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：R914;R943

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