两种增加阿托伐他汀钙在大豆油中溶解度的方法的比较  

Comparison of Two Methods for Increasing Solubility of Atorvastatin Calcium in Soybean Oil

作　　者：牛亚伟[1] 董晓婷[1] 秦凌浩[1] 

机构地区：[1]广东药科大学药学院,广东广州510006

出　　处：《广东化工》2017年第4期24-25,6,共3页Guangdong Chemical Industry

基　　金：广东省自然科学基金(编号2014A030310362)

摘　　要：目的:比较两种增加阿托伐他汀钙(ATC)在大豆油中溶解性的方法。方法:采用高效液相色谱法比较ATC经过两种方法增溶后溶解在大豆油中的稳定性,比较不同增溶剂,不用时间,不同温度下的两种方法的稳定性,色谱条件为反向C18色谱柱(250 mm×4.6 mm,5μm),以醋酸铵缓冲液(pH=4.5)-乙腈(62∶38)为流动相,流速为1.0 m L/min,检测波长为244 nm,柱温40℃,进样量20μL。结果:该色谱条件下,药物浓度在5~300μg/m L范围内的线性相关良好(r=0.9999);回收率实验平均回收率为99.33%,RSD值为0.22%;样品在12 h内稳定性良好,RSD值为1.22%;精密度良好,RSD值为0.51%(n=6)。阿托伐他汀钙的在不同的脂肪酸均有不同程度的降解,并呈现一定的相关性;形成磷脂复合物之后能够达到增加其在大豆油中的溶解性,并且稳定性较好。结论:阿托伐他汀钙不适合使用酸性较强的脂肪酸来增加其大豆油中的溶解性,可以通过复合磷脂的方式来增加其在大豆油中的溶解性。Objective To compare two methods for increasing solubility of atorvastatin calcium（ATC） in soybean oil. Methods Using HPLC to compare the ATC’s stability in soybean oil which is solubilized by two methods. And their stability in different solvents, at different times and temperatures were investigated. Spolar C18 column（5 μm, 250 mm×4.6 mm） was used in the HPLC system. The mobile phase was the mixture of ammonium acetate buffer（pH=4.5）-acetonitrile（62∶38）. The detection wavelength was 244 nm. The flow rate was 1.0 m L/min, and the injection volume was 20 μL. Results The calibration curve had a good linearity in the range of 5-300 μg/m L（r=0.9999）. The recovery of atorvastatin calcium was 99.33 %（RSD=0.22 %）. The precision was also good with RSD of 0.51 %（n=6）, and the sample was stable in 12 hours with RSD of 1.22 %. Atorvastatin calcium in different fatty acids has different degrees of degradation, and showed a certain correlation. The phospholipid complex can be formed to increase atorvastatin calcium solubility in soybean oil, and the stability is better. Conclusion Atorvastatin calcium is not suitable for increasing its solubility in soybean oil by using more acidic fatty acids, but it is effective to increase its solubility in soybean oil by complexing the phospholipid.

关 键 词：阿托伐他汀钙 稳定性 高效液相色谱法 溶解性 

分 类 号：O645.12[理学—物理化学]