长春瑞滨磷脂复合物的制备及其性质研究.PDFVIP

• 570 • 现代药物与临床 Drugs Clinic 第 27 卷 第 6 期 2012 年 11 月 长春瑞滨磷脂复合物的制备及其性质研究 李艳贞，阎 卉，刘 欢，靳文仙，王成港 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 制备长春瑞滨磷脂复合物，提高药物的脂溶性，以期进一步制备长春瑞滨微粒载药系统。方法 采用溶剂挥 发法制备长春瑞滨磷脂复合物，以复合率为评价指标进行单因素优化试验。采用差示扫描量热法、X 射线衍射法、紫外分光 光度法对复合物进行鉴别，并考察复合物的体外溶解性质变化。结果 优化条件下制备的磷脂复合物复合率为 89.3%～ 93.7% ；差示扫描量热法、X 射线衍射法、紫外分光光度法验证了复合物的形成；形成磷脂复合物后，长春瑞滨的脂溶性显 著提高。结论 制备的长春瑞滨磷脂复合物能显著增加药物的脂溶性，为进一步制备长春瑞滨微粒载药系统奠定基础。 关键词：长春瑞滨磷脂复合物；长春瑞滨；复合率；差示扫描量热法；X 射线衍射法；紫外分光光度法 中图分类号：R944.2 文献标志码：A 文章编号：1674 - 5515(2012)06 - 0570 - 05 Preparation of vinorelbine-phospholipid complex and its characterization LI Yan-zhen, YAN Hui, LIU Huan, JIN Wen-xian, WANG Cheng-gang State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China Abstract: Objective To prepare vinorelbine-phospholipid complex (VPC) for enhancing the liposolubility of vinorelbine. Methods The complex was prepared using solvent evaporation method. The preparation technology was optimized by single factor design, using the combining ratio as the assessment index. Differential scanning calorimetry (DSC), X-ray diffraction (XRD) spectrum, and UV spectrophotometry were carried out to investigate its characterization. The in vitro solubility change of the complex was also determined. Results The combining ratio of the complex prepared under the optimized conditions was between 89.3% and 93.7%; UV spectrum, DSC and XRD spectra confirmed the formation of the complex. After phospholipid complex being made, the liposolubility of vinorelbine was remarkably enhanced. Conclusions Prepared vinorelbine-phospholipid complex could effectively enhance the liposolubility of vinorelbine and provide the reference for preparation of vinorelbine microsomal drug-loaded system. Key wor