摘要
目的:研究鲑鱼降钙素磷脂复合物(s CT-PC)的制备工艺并对其进行质量评价。方法:以s CTPC的复合率为评价指标,并用单因素试验和正交设计试验[L16(4)5]进行处方优化;研究s CT-PC的油水分配系数、红外特征、晶体特征及相变特性等理化特性。结果:s CT-PC的最佳制备条件为鲑鱼降钙素(s CT)与磷脂(PC)的质量比为1∶15,反应溶剂为二氯甲烷-乙醚(V/V=6∶4),反应时间与温度分别为25℃和4 h;s CT-PC在正辛醇中的溶解度及油水分配系数较s CT或s CT与PC的物理混合物均明显提高;红外分光光度法(IR)、X-射线衍射法(XRD)、差示扫描热量法(DSC)均验证该复合物的形成。结论:s CT-PC的形成受反应溶剂、反应时间及药脂比影响较大;s CT-PC的亲脂性较s CT明显增强,为进一步制备鲑鱼降钙素磷脂复合物的纳米粒奠定基础。
Objective： To study the preparation technics of salmon calcitonin phospholipid complex（ s CT-PC）and its physicochemical properties. Methods： Using composite rate as evaluation criterion,single-factor test and orthogonal experimental design [L16（4）^5] was adopted to optimize the main influential factors. The oil-water partition coefficient, infrared signature, crystal phase transition characteristics and other physicochemical characteristics of s CT-PC were determined. Results： The optimal preparation conditions of s CT-PC were： the ratio of s CT to PC was 1 ∶ 15,the reaction solvent,temperation and time were dichloromethane-ether（ V/V = 6 ∶ 4）,25 ℃ and 4 h,respectively. The solubility and partition coefficients in n-octanol of s CT-PC had been significantly improved than s CT or the mixtures. Infrared spectrophotometry（ IR）,X-ray diffraction（ XRD）,differential scanning calorimetry（ DSC） were used to verify the formation of s CT-PC. Conclusion： The formation of s CT-PC was greatly affected by the reaction solvent,reaction time and the ratio of drug to lipid. The lipophilic of s CT-PCsignificantly enhanced compared with s CT,which layed foundation for the further researching on its nanoparticles preparation.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2017年第21期2602-2608,共7页
Chinese Journal of New Drugs
基金
成都市企业自主创新项目(11GGYB529SW289)
关键词
鲑鱼降钙素
磷脂复合物
正交实验设计
复合率
理化性质
salmon calcitonin
phospholipid complex
orthogonal design
composite rate
physicochemical properties
