目的:考察20(S)-原人参二醇(20(S)-PPD)磷脂复合物的羟基磷灰石(HAP)组装体的制备方法。方法:以药物载体HAP对20(S)-PPD磷脂复合物进行组装,考察HAP种类、磷脂复合物浓度、HAP与组装药液比例对组装量的影响,确定20(S)-PPD磷脂复合物HAP组装体的制备工艺。结果:按确定组装工艺制备的20(S)-PPD磷脂复合物HAP组装体中组装的磷脂复合物平均质量为136.26 mg/g,平均组装率为5.3%;FT-IR图谱显示HAP组装体已吸附20(S)-PPD磷脂复合物,氢键效应是HAP组装体吸附20(S)-PPD磷脂复合物组装药物的主要机制;组装体在p H为7.4的磷酸缓冲液中的累积释放率也表明HAP组装体具有缓释效果。结论:该磷脂复合物组装体制备工艺简单,具有明显的缓释作用,可为20(S)-PPD缓释制剂的研究开发提供初步研究基础。
Objective: To study the preparation of 20(S)-protopanaxadiol-phospholipid(20(S)-PPD) complex HAP assemblies.Methods: 20(S)-PPD phospholipid complex was assembled with the drug carriers of HAP. Effects of technological factors on the assembled amount were investigated,including HAP species,phospholipid complex concentration,ratio of HAP and assembled liquid,and then the preparation technology of 20(S)-PPD phospholipid complex HAP assemblies was determined. Results: The average quality of phospholipid complex assembled was 136. 26 mg/g,the average assembled rate was 5. 3% for 20(S)-PPD phospholipid complex HAP assemblies prepared by the determined assembly process. FT-IR showed that 20(S)-PPD phospholipid complex was absorbed in the HAP assemblies,and the hydrogen-bonding effect was the main mechanism of HAP assemblies to assemble and adsorb phospholipid complex. The cumulative release rate in p H 7. 4 phosphate buffer of the HAP assemblies indicated that the assemblies had the effect of sustained release. Conclusion: The phospholipid complex HAP assembles have the advantages of simple preparation process,and sustaining release effect,which can provide preliminary research foundation for research and development of 20(S)-PPD sustained-release preparations.