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目的优化双氢青蒿素(dihydroartemisinin,DHA)与磷脂形成复合物的制备工艺。方法以DHA磷脂复合物的复合率为评估标准,采用单因素和正交设计试验考察各因素对复合率的影响;并用高效液相色谱法测定DHA磷脂复合物中DHA的含量。结果 DHA磷脂复合物的最优制备条件为55℃制备温度下,以氯仿为反应溶剂,DHA与磷脂的投料比为1∶3,药物浓度为5%,反应时间为3 h。结论在55℃制备温度下DHA磷脂复合物的形成受溶剂、反应物投料比、药物浓度及反应时间的影响较大。
Objective To optimize the preparation of dihydroartemisinin (DHA) complex with phospholipid. Methods The compound rate of DHA phospholipid complex was taken as the evaluation standard. The influence of various factors on the compounding rate was investigated by single factor and orthogonal design experiments. The content of DHA in DHA phospholipid complex was determined by HPLC. Results The optimum preparation conditions of DHA phospholipid complex were prepared at 55 ℃, using chloroform as reaction solvent, the ratio of DHA to phospholipid was 1: 3, the concentration of drug was 5% and the reaction time was 3 h. Conclusion The formation of DHA phospholipid complex under the temperature of 55 ℃ is greatly affected by the solvent, reactant feed ratio, drug concentration and reaction time.