浅析国产琥乙红霉素组分及有关物质分析.docVIP

浅析国产琥乙红霉素组分及有关物质分析 　论文联盟编辑。 【摘要】 目的 考察国产琥乙红霉素原料和制剂的组分和有关物质，为修订中国药典2005年版琥乙红霉素质量标准提供依据。方法 采用美国药典30版收载的HPLC法测定6个厂家的红霉素原料、琥乙红霉素原料和制剂共16批样品的组分和有关物质，并采用欧洲药典5.0版收载的方法测定琥乙红霉素样品中游离红霉素的含量。结果 国产红霉素以红霉素A为主组分，含有少量的红霉素B、红霉素C和红霉素E组分，有关物质主要为脱水红霉素A，其它有关物质含量较少。以红霉素为原料合成的琥乙红霉素中的主要有关物质为游离红霉素。结论 建议将中国药典2005版琥乙红霉素有关物质的薄层色谱法修订为高效液相色谱法，便于更好地控制产品质量。 【关键词】 琥乙红霉素； HPLC； 组分和有关物质； 游离红霉素 ABSTRACT Objective To investigate the related substances profiles of the domestic erythromycin ethylsuccinate bulk material and preparation, and provide data for the monograph of erythromycin ethylsuccinate in the Chinese PharmacopoEia 2005. Method The ingredient and the related substances of totally 16 batches of erythromycin ethylsuccinate bulk material and preparation of 6 manufacturers were determined using the HPLC method of USP 30, and the erythromycin free base were determined using the method of EP 5.0. Results The major ingredient of domestic erythromycin was erythromycin A and there were minor amount of erythromycin B, C and E. The main related substances was anhydroerythromycin A and the content of other impurities were relatively small. The major related substances of erythromycin ethylsuccinate synthesized by using erythromycin as starting material was erythromycin free base. Conclusion To ensure better quality control for the products, it is recommended that the TLC method involved in the Chinese PharmacopoEIa 2005 to determine the related substances of erythromycin ethylsuccinate to be replaced by the HPLC method. KEY WORDS Erythromycin ethylsuccinate; HPLC; Related substances; Erythromycin free base 琥乙红霉素是以红霉素为原料合成的琥珀酸乙酯衍生物，其组分和有关物质与红霉素原料中的组分和有关物质及厂家的生产工艺密切相关。琥乙红霉素质量标准在中国药典2005版［1］、美国药典30版［2］和欧洲药典5.0版［3］均有收载，中国药典2005版系采用薄层色谱法测定有关物质，对琥乙红霉素各组分及有关物质的定性和定量结果均比较差。USP30版和欧洲药典5.0版则采用HPLC法进行定量测定。USP30版采用杂质对照品对已知杂质进行定量，控制红霉素A烯醇醚不得超过3.0%，N去甲基红霉素A不得超过3.0%，任意单个杂质不得超过3.0%；欧洲药典则采用相对保留时间确定各组分及已知杂质，控制任意单个杂质不得超过3.0%，总杂质不得超过5.0%，并对合成工艺和贮藏条件下产生的游离红霉素进行了限度要求。目前国内对琥乙红霉素有关物质的研究较多［4～6］，但大多仅限于对单个游离红霉素的测