何海冰,殷春阳,徐丽双,唐星
HE Hai-bing,YIN Chun-yang,XU Li-shuang,TANG Xing

• 1:沈阳药科大学药学院
• 2:沈阳东陵药业股份有限公司

摘要(Abstract)：

目的研究丁酸氯维地平亚微乳注射液的制备并考察其理化性质。方法通过高压均质法制备乳剂,以制剂的外观、粒径、粒度分布及含量等为考察指标,采用单因素考察法对丁酸氯维地平亚微乳注射液处方中的磷脂种类和其用量、油酸用量、初乳p H值及制备过程中初乳温度、高压均质压力、次数和灭菌条件等因素进行了优化,确定最优处方及制备工艺。同时对制备的3批样品进行了理化性质研究。结果采用单因素考察法优化丁酸氯维地平亚微乳注射液的处方及制备工艺,在最优处方下制得的丁酸氯维地平亚微乳注射液样品外观均为白色或类白色均匀乳状液体,粒径为(225.3±55.5)nm,Zeta电位为-26.89 m V,p H值为7.01,包封率为98.1%,含量为99.2%。结论制备的丁酸氯维地平亚微乳注射液灭菌稳定性良好,有望开发成为临床用药的新制剂。
Objective To prepare clevidipine butyrate submicron emulsion for intravenous injection( CLVSE)and investigate its physicochemical properties. Methods High pressure homogenization was used to prepare CLVSE. Physical appearance,particle size distribution( PSD),Zeta-potential and content of CLVSE were taken as indexes and the single factor method was employed to investigate the formulation and preparation process of CLVSE. The kinds of lecithin,content of lecithin and oleic acid,p H adjustment of primary emulsion,temperature of preparation,pressure and cycles of high pressure homogenization and sterilization condition were optimized. The basic physicochemical properties of prepared three batches CLVSE were investigated. Results the prepared CLVSE was white and off-white uniform emulsion. The particle size distribution was( 225. 3 ± 55. 5) nm and Zeta-potential was- 26. 89 m V. The p H was 7. 01. The entrapment efficiency( EE) and drug content were 98. 1% and 99. 2%,respectively. Conclusions The prepared CLVSE with good physicochemical characteristics and sterilization stability is expected to be developed as a newpreparation for clinical application.

关键词(KeyWords)： 丁酸氯维地平;亚微乳;高压均质
clevidipine butyrate;submicron emulsion;high pressure homogenization

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 何海冰,殷春阳,徐丽双,唐星
HE Hai-bing,YIN Chun-yang,XU Li-shuang,TANG Xing

DOI: 10.14066/j.cnki.cn21-1349/r.2015.10.003

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