匹维溴铵磷脂复合物的制备及其理化性质研究

Preparation and Physicochemical Properties of Pinaverium Bromide Phospholipid Complex

采用单因素试验考察了反应溶剂、投料比、浓度、反应温度和反应时间对匹维溴铵磷脂复合物形成的影响。所得优化制备工艺条件为:以无水乙醇为反应溶剂,匹维溴铵浓度为5 mg/ml,匹维溴铵-大豆磷脂投料比为1:5,60℃反应2 h。对制得的复合物进行紫外扫描、差示扫描量热及X-射线衍射分析,并考察了其溶解性能。结果表明,复合物中药物以无定形形态存在,且该复合物提高了匹维溴铵的表观油水分配系数。

The effects of several influence factors such as solvent, ratio of pinaverium bromide and soybean lecithin, drug concentration, reaction temperature and time on the formation of the pinaverium bromide phospholipid complex were investigated with single factor experiment. The optimized conditions were as follows： pinaverium bromide （5 mg/ml） and soybean lecithin with the ratio of 1 ： 5, reacted in anhydrous ethanol at 60 ℃ for 2 h. The physicochemical properties of the complex were determined by UV spectrum, differential scanning calorimetry and X-ray diffraction. The solubility was also investigated. The results showed that pinaverium bromide dispersed in the complex was in an amorphous form due to the effect of phospholipid. The apparent oil/water partition coefficient of the prepared complex was imoroved.