间苯三酚磷脂复合物的制备工艺筛选及其理化性质研究

目的:筛选制备间苯三酚磷脂复合物的工艺并考察其磷脂复合物的理化性质。方法:以间苯三酚与磷脂的摩尔比(A)、反应温度(B)及反应时间(C)为因素,间苯三酚与磷脂的复合率为指标,通过正交试验法优化间苯三酚磷脂复合物的制备工艺,检测复合物在不同溶剂中的溶解度及油水分配系数并与原料药比较,采用紫外、红外光谱扫描验证复合物的理化性质。结果:优选工艺条件A为1∶2、B为60℃、C为2h,复合率均为98%以上。与间苯三酚原料药相比,磷脂复合物在水、氯仿中溶解度以及油水分配系数均有增大。紫外、红外光谱证实药物与磷脂未形成新的化合物。结论:优选工艺后所制复合物可显著提高药物的溶解度和亲脂性。

Preparation and Physicochemical Properties of Phloroglucinol Phospholipids Complex

OBJECTIVE： To optimize the preparation technology of phloroglucinol phospholipids complex and study its physicochemical properties. METHODS： The preparation technology for phloroglucinol phospholipids complex was optimized taking the molar ratio of phloroglucinol to phospholipids （A）, reaction temperature （B） and reaction time （C） as factors and complex ratio of phloroglucinol and phospholipid as index. The dissolubility and oil/water partition coefficient of the complex in different solvents were determined and compared with crude drug, and the new complex＇ s physicochemical properties were validated by UV and IR （infrared spectra）. RESULTS： The optimized preparation conditions for phloroglucinol phospholipids complex were obtained as follows： A was i ： 2; B was 60 ℃ and C was 2 h. The complex ratio remained at above 98%. Compared with phloroglucinol crude drug, the phloroglucinol phospholipids complex in water or chloroform showed increase in both dissolubility and oil/ water partition coefficient. UV and IR confirmed that no new complex had been formed from phloroglucinol and phospholipids. CONCLUSION： The optimized technology greatly enhanced the dissolubility and lipotropy of the phlol-oglucinol phospholipids complex.