利他唑酮(LT-01)磷脂复合物制备工艺及其理化性质研究

Study on the preparation technology and physicochemical properties of the litazolid-phospholipid complex

目的确定利他唑酮形成磷脂复合物的最佳制备工艺,并对该磷脂复合物进行理化性质研究。方法以药脂比、反应溶剂、反应浓度、反应温度及反应时间等影响因素为考察项,以复合率为评价指标,对磷脂复合物的制备工艺进行考察,最终确定利他唑酮磷脂复合物最优的制备方法,并对所制备的磷脂复合物进行溶解性考察,采用紫外、红外光谱扫描进行验证。结果该工艺制备磷脂复合物简单易行且质量可控,制备利他唑酮磷脂复合物的复合率大于96%。形成复合物后,利他唑酮在水、油相中的溶解性增加了50~100倍,同时UV扫描和IR光谱结果显示利他唑酮磷脂复合物的生成过程中并没有新的化合物产生。结论该制备工艺能够简单方便的制备出复合率高的利他唑酮磷脂复合物,且所制备的磷脂复合物能够有效的提高药物的溶解性。

Objective To research the best preparation technology and the physical and chemical properties of the LT-phospholipid complex. Methods The preparation technology for the LT-phospholipid complex was optimized. The molar ratio of LT-01 to the phospholipid, solvents, concentrations, temperatures and time during reaction process were considered as key factors. The complex ratio of LT-01 to the phospholipid was used as the index to determine the best preparation technology of the LT-phospholipid complex. The dissolubility of the complex was determined and the physicochemical properties of the complex were validated by UV and IR. Results The process for preparing the phospholipid complex was simple and its quality was controllable. The complex ratio of LT-phospholipid complex remained above 96%. In addition the solubility of the complex in water and oil phase is increased by 50-100 times, while the UV and IR spectrum showed that during the process of producing the LT- phospholipid complex, there did not produce new compounds. Conclusion The preparation process can be simple and easy to prepare an LT-phospholipid complex with high complex ratio, and the prepared phospholipid complex can effectively improve the solubility of the drug.