依托泊苷长循环亚微乳的制备和理化性质研究.pdfVIP

• 164 • 现代药物与临床 Drugs Clinic 第 28 卷 第 2 期 2013 年 3 月 依托泊苷长循环亚微乳的制备和理化性质研究 1 2 2 李华龙 ，尹东东 ，王杏林 1. 天津市药品检验所，天津 300070 2. 天津药物研究院 释药技术与药代动力学国家重点实验室，天津 300193 摘 要：目的 制备依托泊苷长循环亚微乳，并对其进行理化性质研究。方法 在依托泊苷亚微乳处方的基础上，通过考察 乳粒表面固有水化层厚度与聚乙二醇 2000 –二硬脂酰磷脂酰乙醇胺（PEG 2000-DSPE ）用量的关系，确定PEG 2000-DSPE 用量，从而确定了依托泊苷长循环亚微乳的处方和制备工艺，并进行了理化性质研究。结果 依托泊苷长循环亚微乳的浓度 为 0.8 mg/mL，平均粒径为（185.4±5.7 ）nm ，Zeta 电位为（−51.6 ±0.8 ）mV ，药物包封率为 97.52% 。结论 得到了包封率 在 95% 以上的依托泊苷浓度为0.8 mg/mL 的依托泊苷长循环亚微乳的处方和制备工艺。 关键词：依托泊苷长循环亚微乳；依托泊苷；长循环亚微乳；聚乙二醇 2000 –二硬脂酰磷脂酰乙醇胺（PEG 2000-DSPE ） 中图分类号：R944 文献标志码：A 文章编号：1674 - 5515(2013)02 - 0164 - 06 DOI: 10.7501/j.issn.1674-5515.2013.02.015 Preparation and physico-chemical properties of etoposide long circulating submicroemulsion 1 2 2 LI Hua-long , YIN Dong-dong , WANG Xing-lin 1. Tianjin Institute for Drug Control, Tianjin 300070, China 2. State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China Abstract: Objective To prepare etoposide long circulating submicroemulsion (ELCSE) and to study its physico-chemical properties. Methods Based on the formulation of etoposide submicroemulsion, the quantity of PEG 2000-DSPE was decided by studying the relationship between the fixed aqueous layer thickness (FALT) of emulsion drop surface and the quantity of PEG 2000-DSPE. Then the ELCSE formulation and the preparing technique were decided, and the physico-chemical properties were studied. Results The concentration of etoposide was 0.8 mg/mL. The mean particle size, Zeta potential, and encapsulation efficiency of ELCSE were (185.4 ± 5.7) nm, (−51.6 ± 0.8) mV, and 97.52%, respectively. Conclusion The ELCSE formulation and preparing technique with etoposide concentration of 0.8 mg/mL and encapsulation