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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。
Objective: To screen the process of preparation of phloroglucinol complex and study the physicochemical properties of phospholipid complex. Methods: The molar ratio of phloroglucinol to phospholipid (A), reaction temperature (B) and reaction time (C) were used as indexes and the compounding ratio of phloroglucinol and phospholipid was used as an index. Triphenylphenol phospholipid complex preparation process, the detection of complex solubility in different solvents and oil-water partition coefficient and compared with the bulk drugs, the use of UV-Vis spectroscopy to verify the physical and chemical properties of the complex. Results: The optimal process conditions A was 1: 2, B was 60 ℃, C was 2h, the recombination rates were above 98%. Compared with the raw materials of phloroglucinol, the solubility of phospholipid complex in water and chloroform and the oil-water partition coefficient all increased. Ultraviolet and infrared spectroscopy confirmed that the drug did not form a new compound with phospholipids. Conclusion: The compound prepared by the optimized process can significantly improve the drug solubility and lipophilicity.